Flavonoid-Drug Interactions: Effects of Flavonoids on ABC ...

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SAR and QSAR Study Objective: To identify structural elements required for potent BCRP inhibition; To derive a QSAR equation for the prediction <strong>of</strong> flavonoid-BCRP interaction activity.
Conclusions <strong>Flavonoid</strong>s can inhibit human BCRP with flavonoids such as chrysin, biochanin A, apigenin and benz<strong>of</strong>lavone having IC50 values in the sub- or low µM range Multiple flavonoids result in additive inhibition <strong>of</strong> BCRP The diversity <strong>of</strong> flavonoids allow the determination <strong>of</strong> SAR and QSAR for these compounds. SAR studies indicated the importance <strong>of</strong> lipophilicity, the placement <strong>of</strong> hydroxyl groups and the 2,3 double bond.
Page 1 and 2: Flavonoid-
Page 3 and 4: Flavonoids ‣ Epi
Page 5 and 6: Flavonoid Products
Page 7 and 8: Flavonoid Products
Page 9 and 10: Hepatocyte OCT1 SMALL ORGANIC CATIO
Page 11 and 12: ABC Transporter Expression in the L
Page 13 and 14: General Study Design ‣ In vitro s
Page 15 and 16: Increase of 3 H-DN
Page 17 and 18: Flavonoid-P-gp <st
Page 19 and 20: Flavonoid-
Page 21 and 22: Multidrug Resistance-Associated Pro
Page 23 and 24: Flavonoids increas
Page 25 and 26: Inhibitory constants for 3 H-LTC4 t
Page 27 and 28: Breast Cancer Resistance Protein (B
Page 29 and 30: BCRP Clinical Implications • Appa
Page 31 and 32: Investigated Flavonoid</str
Page 33 and 34: Correlation Between MX Accumulation
Page 35 and 36: Combined Effects <
Page 37 and 38: Dose-Response Prof
Page 39: Berenbaum’s Interaction Index Met
Page 43 and 44: Effect of GF120918
Page 45 and 46: Effect of Chrysin
Page 47 and 48: Effect of 7,8-benz
Page 49 and 50: Effect of
Page 51 and 52: Effect of
Page 53: Flavonoid

Flavonoid-Drug Interactions: Effects of Flavonoids on ABC ...

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