Effects of dietary chemopreventive phytochemicals on P-glycoprotein function

Effects of Spice Constituents on P-Glycoprotein-Mediated Transport and CYP3A4-Mediated Metabolism in Vitro

“…1 indicates similarities in their chemical structures, specifically a 4-hydroxy-3-methoxyphenyl ring and a keto group on the third carbon of the side chain. Both spices were concentration-dependent P-gp inhibitors, which is in agreement with previously published data showing that curcumin and 6-gingerol inhibited the P-gp-mediated cellular accumulation of rhodamine 123 (Anuchapreeda et al, 2002;Nabekura et al, 2005). P app values in Tables 1 and 2 suggest that curcumin is the more efficient P-gp inhibitor on a concentration basis compared with 6-gingerol, although curcumin at the highest applied concentration of 60 M was also incapable of completely abolishing the vectorial transport of [ 3 H]digoxin.…”

Efficacy of traditional Chinese medicine in treating cancer

“…They increased the intracellular concentration of P-gp substrates by inhibiting this anticancer drug efflux transporter. MDR carcinoma KB-C2 cells were more susceptible to the cytotoxicity of vinblastine, as compared with vinblastine alone, when simultaneously treated with 50 µM capsaicin or gingerol (31). Therefore, capsaicin and gingerol can partially reverse MDR in cells that express P-gp.…”

Modulation of nuclear factor E2-related factor 2–mediated gene expression in mice liver and small intestine by cancer chemopreventive agent curcumin

“…The transport function-related genes were the major group of genes being regulated by curcumin in a Nrf2-dependent manner in both liver and small intestine. Although the interaction between curcumin and transporters, such as MDR1 and MDR-associated protein 1, has been investigated in vitro (27), the effects of curcumin on other transporters, especially their expression, have never been examined in vivo. Solute carrier family transporter genes were the major ones to be selectively regulated in liver and small intestine.…”