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Presentaci n de PowerPoint Grape Seed Ext

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					                                                                                                                                                                                                  Is the bioavailability of water- and fat-soluble
                                                                                                                                                                                                  actives derived from plant extracts influenced
                                                                                                                                                                                                        by a simultaneous administration?
                                                                                                                                                                                                                                    Karin Engelhart1, Roland Wacker1, Inka Pfitzner1, Smail Alaoui2 and Sybille Buchwald-Werner3
                                                                                                                                                                                                                                                          1BioTeSys GmbH, D-73728 Esslingen, Germany
                                                                                                                                                                                                                                              2Cognis Iberia s.l., E-08740 Sant Andreu de la Barca (Barcelona), Spain
                                                                                                                                                                                                                                           3Cognis Deutschland GmbH & Co. KG, D-40789 Monheim am Rhein, Germany



                                                                                                                                                                                                                                                                                                                                        INTRODUCTION
Plant extracts are at present in the focus of anti-aging and health care pro-                                                                                                                                                                                                                                                                                                                     lutein esters. Formula II (=regenerating) contained passionflower in combi-na-
ducts. They are widely used as food additives, food supplements, and as                                                                                                                                                                                                                                                                                                                           tion with grape seed. Both formula are intended to be used as food supple-
cosmetic ingredients. However, it is little known about the influences be-                                                                                                                                                                                                                                                                                                                        ment.
tween different bioactive compounds concerning their bioavailability when                                                                                                                                                                                                                                                                                                                         The extracts were dissolved in an appropriate solvent. The supplementation
administered simultaneously.                                                                                                                                                                                                                                                                                                                                                                      dose was based on the intended amount of active ingredient per food sup-
In the present study we investigated the bioavailability of different plant                                                                                                                                                                                                                                                                                                                       plement daily dosage under consideration of cytotoxicity results. For the
extracts for CaCo-2 cells in vitro when applied as single extract and as                                                                                                                                                                                                                                                                                                                          different formula the relation between the single compounds were kept
formula. CaCo-2 cells were supplemented with grape seed, red clover,                                                                                                                                                                                                                                                                                                                              proportionately as indicated for the food supplement formula. The con-
passionflower (Plantalin Passiflora™), vitamin E (Covitol™), and lutein esters                                                                                                                                                                                                                                                                                                                    centration of each compound was similar for the uptake as single compound
(Xangold™) as single extracts.                                                                                                                                                                                                                                                                                                                                                                    and as formula ingredient.
Formula I (=anti-aging) contained grape seed, red clover, vitamin E and


                                                                                                                                                                                                                                                                                                                        CELLS AND ANALYSIS


                  0,40                                                                                                                                                      280 nm
                                                                                                                                                                                                                                                                                                                                                                                         240,00
                  0,38




                                                                                                                                                                                                                                                                                                                                                                                                                                                                                 TOC - 2,806
                                                                                                                                                                                                                                                                                                                                                                                         220,00                                                                                                                                                 293/325 nm
                  0,36
                                                                                                                                                                                                 Biochanin A - 29,855




                  0,34                                                                                                                                                                                                                                                                                                                                                                   200,00
                  0,32
                                                                                                                                                                                                                                                                                                                                                                                         180,00
                  0,30
                  0,28                                                                                                                                                                                                                                                                                                                                                                   160,00
                  0,26
                                                                                                                                                                                                                                                                                                                                                                                         140,00
                  0,24
                  0,22                                                                                                                                                                                                                                                                                                                                                                   120,00
                                                                                                                                                                                                                                                                                                                                                                          Fluorescence




                  0,20                                                                                                                                                                                                                                                                                                                                                                   100,00
             AU




                  0,18
                                                                                                                                                                                                                                                                                                                                                                                          80,00
                  0,16




                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Formula
                  0,14                                                                                                                                                                                                                                                                                                                                                                    60,00
                                                                    Catechin - 8,523




                                                                                                                                                                                                                                                                                                                                                                                                                                                          IS - 1,880




                  0,12
                                                                                                                                                                                                                                                                                                                                                                                          40,00
                  0,10
                  0,08                                                                                                                                                                                                                                                                                                                                                                    20,00
                  0,06
                                                                                                                                                                                                                                                                                                                                                                                           0,00
                  0,04
                  0,02                                                                                                                                                                                                                                                                                                                                                                   -20,00

                  0,00
                  -0,02
                      0,00           2,00      4,00     6,00      8,00                 10,00                     12,00    14,00   16,00    18,00 20,00
                                                                                                                                          Minutes
                                                                                                                                                            22,00   24,00   26,00    28,00      30,00                   32,00   34,00     36,00
                                                                                                                                                                                                                                                                                                                                                                                         -40,00

                                                                                                                                                                                                                                                                                                                                                                                         -60,00
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Formula I (anti-aging):
                                                                                                                                                                                                                                                                                                                                                                                                                                  1,00                        2,00                         3,00                         4,00             5,00                  6,00                7,00


            Biochanin A and Catechin (Formula I)                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         daily dosage / single supplementation
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                     Minutes




                                                                                                                                                                                                                                                                                                                                                                          α-Tocopherol (Covitol™)
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Red Clover 20% Genins: 175 mg
                                                                                                                                                                                                    BCA - 29, 96




                                                                                                                                                 280 nm
                                                                                                                                                                                                                                                                                                                                                                                         0,0007
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                               IS - 7,043




                  0,18
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                          484 nm


                  0,16


                  0,14
                                                                                                                                                                                                                                                                                    Confluent CaCo-2                                                                                     0,0006
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Covitol 1370:                                                                                         11 mg
                                                                                                                                                                                                                                                                                                                                                                                         0,0005

                  0,12

                                                                                                                                                                                                                                                                                       monolayer                                                                                                                                                                                                                                                                                                                         Xangold 15% OLV:                                                                                      80 mg
                                                                                                                                                                                                                                                                                                                                                                                                                                         LUT - 2,863




                                                                                                                                                                                                                                                                                                                                                                                         0,0004
                  0,10
             AU




                                                                                                                                                                                                                                                                                                                                                                            AU




                  0,08                                                                                                                                                                                                                                                                                                                                                                   0,0003


                  0,06



                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Grape Seed (>15% OPC): 50 mg
                                                                                                                                                                                                                                                                                                                                                                                         0,0002

                  0,04


                  0,02
                                                                                                                                                                                                                                                                                        Supplementation                                                                                  0,0001



                  0,00
                                                                                                                                                                                                                                                                                                                                                                                         0,0000


                                     2,00   4,00       6,00     8,00                   10,00                 12,00       14,00    16,00    18,00 20,00     22,00    24,00   26,00    28,00      30,00                   32,00   34,00   36,00
                                                                                                                                                                                                                                                                                                                                                                                                                                 2,00                   4,00                  6,00                            8,00             10,00            12,00              14,00             16,00
                                                                                                                                          Minutes
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                     Minutes



            Biochanin A (Red Clover )                                                                                                                                                                                                                                        Cell harvest after                                                                           Lutein (Xangold™)                                                                                                                                                                                                                              Formula II (regenerating):
                                                                                                                                                                                                                                                                             1h, 3h, 5h, 7h, 24h
                  0,022                                                                                                                                                              280 nm
                                                                                                                                                                                                                                                                                                                                                                                         0,0065
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Passifora incarnata 2%
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                18, 262




                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                   484 nm
                  0,020

                  0,018


                  0,016
                                                                                                                                                                                                                                                                   determination of
                                                                                                                                                                                                                                                                                                                                                                                         0,0060

                                                                                                                                                                                                                                                                                                                                                                                         0,0055

                                                                                                                                                                                                                                                                                                                                                                                         0,0050
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Vitexin/Isovitexin:                                                                                   119 mg
                                                                                                                                                                                                                                                                 intracellular marker
                                                                                                                                                                                                                                                                                                                                                                                         0,0045
                  0,014




                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         Grape Seed (>15% OPC): 50 mg
                                                                                                                                                                                                                                                                                                                                                                                         0,0040
                  0,012
                                                                                                                                                                                                                                                                                                                                                                                         0,0035
             AU




                                                                                                                                                                                                                                                                                                                                                                           AU




                  0,010



                                                                                                                                                                                                                                                               concentration by HPLC
                                                                                                                                                                                                                                                                                                                                                                                         0,0030
                                                                                       Catechin - 7,171




                  0,008
                                                                                                                                                                                                                                                                                                                                                                                         0,0025

                  0,006                                                                                                                                                                                                                                                                                                                                                                  0,0020

                  0,004                                                                                                                                                                                                                                                                                                                                                                  0,0015

                                                                                                                                                                                                                                                                                                                                                                                         0,0010
                  0,002
                                                                                                                                                                                                                                                                                                                                                                                         0,0005
                  0,000
                                                                                                                                                                                                                                                                                                                                                                                         0,0000
                                        2,00          4,00        6,00                                    8,00       10,00        12,00      14,00        16,00     18,00     20,00           22,00                     24,00     26,00
                                                                                                                                          Minutes                                                                                                                                                                                                                                                            2,00                   4,00               6,00            8,00     10,00                       12,00      14,00     16,00     18,00          20,00       22,00    24,00         26,00
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                    Minutes


            Catechin (Grape Seed)                                                                                                                                                                                                                                                                                                                                         Isovitexin (Passionflower)




                                                                                                                                                                                                                                                                                                                                                           UPTAKE
                                                                    Passionflower in Different Formulations                                                                                                                                                                                                   Red Clover in Different Formulations
                                                                          Uptake Kinetics in CaCo-2                                                                                                                                                                                                               Uptake Kinetics in CaCo-2
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                     Covitol in Different Formulations
                                                                                                                                                                                                                                                                                                                                                             Red Clover
                                      0,25                                                                                                                                                                                                 Passionflow er                                          25                                                                                                                                                                                                                                                                                                                                                                                  Uptake Kinetics in CaCo-2
                                                                                                                                                                                                                                                                                                                                                             Anti-Aging
                                                                                                                                                                                                                                           Formula
                                                                                                                                                                                                                                                                                                   20                                                                                                                                                                                                                                                                                                                                                                    30
                                      0,20
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                Covitol
                                                                                                                                                                                                                                                                                    pmol/µg DNA




                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         25
                                                                                                                                                                                                                                                                 cellular conc.




                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                Anti-Aging
                    pmol/µg DNA
                    cellular conc.




                                                                                                                                                                                                                                                                                                   15
                                      0,15
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         20
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                           pmol/µg DNA
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                    cellular conc.




                                                                                                                                                                                                                                                                                                   10
                                      0,10
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         15
                                                                                                                                                                                                                                                                                                   5
                                      0,05                                                                                                                                                                                                                                                                                                                                                                                                                    Red clover, Vitamin E, Luteinester and Grape seed                                                                                                                                                          10

                                                                                                                                                                                                                                                                                                   0
                                                                                                                                                                                                                                                                                                                                                                                                                                                                          in Anti-Aging Formulation
                                      0,00                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                5
                                                                                                                                                                                                                                                                                                         1h        3h         5h        7h           24h                                                                                                                  Uptake kinetics in CaCo-2
                                                             1h                                                     3h                        5h                       7h                               24h                                                                                                                                                                                                                                                                                                                                                                                                Biochanin A
                                                                                                                                                                                                                                                                                                                                                                                                                                   20,0                                                                                                                                                                                                                                   0
                                                                                                                                                                                                                                                                                                                          Biochanin A                                                                                                                                                                                                                                                                      Tocopherol
                                                                                                                                          Isovitexin                                                                                                                                                                                                                                                                               17,5                                                                                                                                                                                                                                         1h       3h         5h         7h        24h
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                           Lutein
                                                                                                                                                                                                                                                                                                                                                                                                                                   15,0                                                                                                                                                                    Catechin                                                                             a-Tocopherol
                                                                                                                                                                                                                                                                                                                                                                                                                   pmol/µg DNA
                                                                                                                                                                                                                                                                                                                                                                                                  cellular conc.




                                                                                                                                                                                                                                                                                                                                                                                                                                   12,5

                                                                                                                                                                                                                                                                                                                                                                                                                                   10,0

                                                                                                                                                                                                                                                                                                                                                                                                                                    7,5

                                                                                                                                                                                                                                                                                                                                                                                                                                    5,0
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                     Xangold in Different Formulations
                                                                                                                                                                                                                                                                                                                                                                                                                                    2,5
                                                               Grape seed and Passionflower in a Formula                                                                                                                                                                                                      Grape Seed in Different Formulations                                                                                                                                                                                                                                                                                                                                      Uptake Kinetics in CaCo-2
                                                                                                                                                                                                                                                                                                                  Uptake Kinetics in CaCo-2                                                                                         0,0
                                                                       Uptake kinetics in CaCo-2
                                                                                                                                                                                                                                                                                                                                                                                                                                                                       1h                                       3h                          5h                                7h                     24h                                                                 0,03
                                                                                                                                                                                                                                                  Catechin                                         1,6                                                                                                                                                                                                                                                                                                                                                                                                                          Xangold
                                       1,20                                                                                                                                                                                                                                                                                                                 Grape Seed                                                                                                                                                                 Anti-Aging
                                                                                                                                                                                                                                                  Isovitexin                                                                                                                                                                                                                                                                                                                                                                                                             0,02                                                   Anti-Aging
                                                                                                                                                                                                                                                                                                   1,4                                                      Anti-Aging
                                       1,00
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                     pmol/µg DNA




                                                                                                                                                                                                                                                                                                   1,2
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                           cellular conc.




                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         0,02
                    cellular conc.
                    pmol/µg DNA




                                       0,80
                                                                                                                                                                                                                                                                                     pmol/µg DNA
                                                                                                                                                                                                                                                                   cellular conc.




                                                                                                                                                                                                                                                                                                   1,0

                                       0,60                                                                                                                                                                                                                                                        0,8                                                                                                                                                                                                                                                                                                                                                                   0,01

                                                                                                                                                                                                                                                                                                   0,6
                                       0,40
                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                         0,01
                                                                                                                                                                                                                                                                                                   0,4
                                       0,20
                                                                                                                                                                                                                                                                                                   0,2                                                                                                                                                                                                                                                                                                                                                                   0,00
                                       0,00                                                                                                                                                                                                                                                        0,0                                                                                                                                                                                                                                                                                                                                                                          1h        3h         5h        7h        24h
                                                               1h                                                        3h                     5h                          7h                                          24h                                                                              1h        3h         5h        7h           24h                                                                                                                                                                                                                                                                                                                                            Lutein
                                                                                                                                            Formula                                                                                                                                                                        Catechin




                                                                                                                                                                                                                                                                                                                                             CONCLUSION
All plant extracts are well available for CaCo-2 cells. There is a clear                                                                                                                                                                                                                                                                                                                          This reflects the different uptake mechanisms. The simultaneous
difference in the kinetics of water- and fat-soluble active ingredients with                                                                                                                                                                                                                                                                                                                      administration of different flavonoid-rich extracts had no influence on the
water-soluble actives being taken up very rapidly and decreased after few                                                                                                                                                                                                                                                                                                                         bioavailability of these investigated components. Tocopherol and lutein
hours whereas fat-soluble actives were taken up slowly but continuously.                                                                                                                                                                                                                                                                                                                          uptake was also not influenced.



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Description: Presentaci n de PowerPoint Grape Seed Ext