title: Reversing P-glycoprotein-mediated multidrug resistance in vitro by α-asarone and β-asarone, bioactive cis-trans isomers from Acorus tatarinowii.
abstract: P-Glycoprotein (P-gp), an ATP-binding cassette transporter, plays an important role in multidrug resistance (MDR). α-Asarone and β-asarone, bioactive cis-trans isomers found in Acorus tatarinowii Schott, were tested for their potential ability to modulate the expression and function of P-gp in Caco-2 cells. MTT assays revealed that both α-asarone and β-asarone significantly enhanced the vincristine-induced cytotoxicity to cells. β-Asarone was the most potent. Flow cytometry showed that α- and β-asarone increased Rhodamine 123 (Rh123) uptake and inhibited Rh123 efflux in Caco-2 cells in a concentration-dependent manner. Furthermore, P-gp expression and P-gp mRNA in cells were decreased by exposure to α- and β-asarone. In addition, β-asarone increased the inhibition of P-gp activity in cells more than α-asarone. Thus, α- and β-asarone effectively reversed MDR by inhibiting P-gp function and expression.
authors: College of Life Sciences, Northwest University, No. 229, Taibai Northern Road, Mail Box 195#, Xi'an, 710069, China.
authors: Xue
authors: X
authors: Meng
authors: Sha
authors: S
authors: Liao
authors: Xueyan
authors: X
authors: Wang
authors: Shixiang
authors: S
authors: Wang
authors: Xinfeng
authors: X
authors: Zhao
authors: Pu
authors: P
authors: Jia
authors: Weijing
authors: W
authors: Pei
authors: Xiaopu
authors: X
authors: Zheng
authors: Xiaohui
authors: X
authors: Zheng
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D029023:Acorus / Q000737:chemistry*; D000081248:Allylbenzene Derivatives; D000840:Anisoles / Q000302:isolation & purification / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000494:pharmacology*; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D004847:Epithelial Cells / Q000187:drug effects*; D006801:Humans; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D020112:Rhodamine 123 / Q000378:metabolism; D013194:Staining and Labeling; D013778:Tetrazolium Salts / Q000378:metabolism; D013844:Thiazoles / Q000378:metabolism
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000081248:Allylbenzene Derivatives; D000840:Anisoles; D000970:Antineoplastic Agents; D010936:Plant Extracts; D013778:Tetrazolium Salts; D013844:Thiazoles; C012195:asarone; D020112:Rhodamine 123; C022616:thiazolyl blue