单宁酸
流出
P-糖蛋白
生物化学
化学
罗丹明123
多重耐药
有机化学
抗生素
作者
Shuji Kitagawa,Tomohiro Nabekura,Yutaka Nakamura,Tomoharu Takahashi,Yoshiki Kashiwada
标识
DOI:10.1211/jpp.59.7.0008
摘要
Abstract We studied the effects of tannic acid and 1(β),2,3,4,6-penta-O-galloyl-D-glucose (pentagalloylglucose), one of the components of tannic acid, on the P-glycoprotein (P-gp) function in multidrug-resistant P-gp over-expressing KB-C2 cells. Both tannic acid and pentagalloylglucose markedly elevated the accumulation of P-gp substrates, rhodamine 123 and daunorubicin, by inhibiting their efflux. A 19-fold increase in cellular rhodamine 123 was observed for tannic acid at 60 μM (85 μg mL−1) and a 21-fold increase was observed for pentagalloylglucose at 100 μM (94 μg mL−1). The increasing effects of these compounds in the accumulation were much larger than that of (-)epigallocatechin-3-O-gallate (EGCG), which has been revealed to have a prominent inhibitory effect on P-gp compared with other flavonoids. Analysis of verapamil-stimulated ATPase activity in membrane vesicles expressing human P-gp suggested that inhibition of P-gp function by tannic acid and pentagalloylglucose was at least partly due to ATPase inhibition of P-gp. The findings also suggested that the presence of a large number of galloyl groups in polyphenols strengthens the interaction with regulatory regions in P-gp.
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