染料木素在乳腺癌MCF-7细胞内的代谢研究  

Metabolism study of genistein in breast cancer MCF-7 cells

作　　者：万英凤[1] 王玲兰[1] 许佑君[2] 林禄清[2] 袁波[1] 徐海燕[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2010年第10期813-820,共8页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(30801420)

摘　　要：目的研究染料木素在乳腺癌细胞中的代谢行为。方法将10μmol.L-1染料木素与乳腺癌MCF-7细胞在37℃下孵化一定时间后终止反应。采用UPLC-MS-MS法测定孵化液中染料木素及II相代谢产物的浓度。结果染料木素在乳腺癌MCF-7细胞中可迅速代谢为7或4′-葡萄糖醛酸结合物以及7或4′-硫酸结合物。孵化24、48和72 h后,每100μg孵化样品蛋白中,7-葡萄糖醛酸结合物的生成率分别为2.9、5.2和8.9μg.h-1,4′-葡萄糖醛酸结合物的生成率分别为1.1、1.9和3.0μg.h-1,7-硫酸结合物的生成率分别为20.3、32.9和47.3μg.h-1,4′-硫酸结合物的生成率分别为1.7、3.1和4.5μg.h-1。结论染料木素在乳腺癌MCF-7细胞中的主要代谢产物是7-硫酸结合物。Objective To study the metabolism of genistein in breast cancer cells. Methods Genistein （ 10μmol.L^-1 ） was incubated with MCF-7 cells at 37 ℃ and the amount of metabolites formed in the incu- bation solution was quantified by UPLC-MS/MS. Results Genistein was metabolized to 7-glucuronide, 4＇- glucuronide,7-sulfate and 4＇-sulfate in incubation solution. After incubated with MCF-7 cells at 37 ℃ for 24,48, and 72 h, genistein was metabolized to 7-glucuronide at the rate of 2. 9,5.2 and 8.9μg.h^-1 per 100 μg incubation protein,to 4＇-glucuronide at 1.1,1.9 and 3.0 μg.h^-1 per 100 μg incubation protein,to 7-sulfate at 20. 3,32. 9 and 47.3 μg.h^-1 per 100 μg incubation protein,and to 4＇-sulfate at 1.7,3.1 and 4.5 μg.h^-1 per 100 μg incubation protein, respectively. Conclusions The major metabolite of genistein in MCF-7 cells is 7-sulfate.

关 键 词：染料木素 药物代谢 液-质联用技术 乳腺肿瘤细胞 

分 类 号：R917[医药卫生—药物分析学]