Department of Pharmaceutical Sciences , Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand.
Phytomedicine. 2010 Jun;17(7):506-12. doi: 10.1016/j.phymed.2009.09.004. Epub 2009 Oct 30.
The effects of Curcuma longa (khamin chan) and Curcuma sp. "khamin-oi" (khamin-oi), as well as isolated major curcuminoids on intestinal P-gp functions were evaluated in vitro. The accumulation of R123 in Caco-2 cells was increased and the R123 efflux ratios were significantly decreased by both Curcuma longa and Curcuma sp. "khamin-oi" extracts, indicating their roles on efflux transporters. The a-b transport of daunorubicin was increased by curcumin, demethoxycurcumin and bisdemethoxycurcumin while the b-a transport was significantly decreased by curcumin and demethoxycurcumin. However, calcein-AM uptake into the human P-gp overexpression cell line, LLC-GA5-COL300, was increased by curcumin and demethoxycurcumin in a concentration-dependent manner but not affected by bisdemethoxycurcumin. These results show that curcumin and demethoxycurcumin could inhibit P-gp but bisdemethoxycurcumin may modulate the function of other efflux transporters such as MRP. Taken together, the information may indicate the impact of Curcuma longa and Curcuma sp. "khamin-oi" on pharmacokinetics of orally administered drugs that are P-gp substrates.
研究了姜黄（khamin chan）和姜黄“khamin-oi”（khamin-oi）以及分离的主要姜黄素类化合物对肠道 P-糖蛋白（P-gp）功能的影响。姜黄和姜黄“khamin-oi”提取物均能增加 R123 在 Caco-2 细胞中的积累，显著降低 R123 外排率，表明它们对外排转运蛋白有作用。姜黄素、脱甲氧基姜黄素和双脱甲氧基姜黄素增加柔红霉素的 a-b 转运，而姜黄素和脱甲氧基姜黄素显著降低柔红霉素的 b-a 转运。然而，姜黄素和脱甲氧基姜黄素呈浓度依赖性地增加人 P-糖蛋白过表达细胞系 LLC-GA5-COL300 中钙黄绿素-AM 的摄取，但双脱甲氧基姜黄素没有影响。这些结果表明，姜黄素和脱甲氧基姜黄素可抑制 P-gp，但双脱甲氧基姜黄素可能调节其他外排转运蛋白（如 MRP）的功能。总之，这些信息可能表明姜黄和姜黄“khamin-oi”对口服 P-gp 底物药物的药代动力学的影响。
