Effects of Curcuma spp. on P-glycoprotein function

被引:36
作者
Ampasavate, Chadarat [2 ]
Sotanaphun, Uthai [3 ]
Phattanawasin, Panadda [4 ]
Piyapolrungroj, Nusara [1 ]
机构
[1] Silpakorn Univ, Dept Biopharm, Fac Pharm, Nakhon Pathom, Thailand
[2] Chiang Mai Univ, Dept Pharmaceut Sci, Fac Pharm, Chiang Mai 50000, Thailand
[3] Silpakorn Univ, Dept Pharmacognosy, Nakhon Pathom, Thailand
[4] Silpakorn Univ, Dept Pharmaceut Chem, Nakhon Pathom, Thailand
关键词
Curcuma longa; Curcuma sp "Khamin-oi; Curcuminoids; P-glycoprotein; MEDIATED TRANSPORT; CACO-2; CELLS; EXPRESSION; MODULATION; EFFLUX; GP; FLAVONOIDS; DIGOXIN;
D O I
10.1016/j.phymed.2009.09.004
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
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. (C) 2009 Elsevier GmbH. All rights reserved.
引用
收藏
页码:506 / 512
页数:7
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