枇杷叶6种三萜酸的人肠道菌群生物转化及其抑制α-葡萄糖苷酶活性研究  

Biotransformation of six triterpene acids from Eriobotrya japonica leaves by human intestinal bacteria and their relation to in vitroα-glucosidase inhibitory activity

作　　者：陈剑[1] 赵磊[1] 黄晓杰 潘胤安 马丽[1] 刘艳[1] CHEN Jian;ZHAO Lei;HUANG Xiao-jie;PANG Yin-an;MA Li;LIU Yan(Jiangsu Province Service Center for Anti-diabetic Drugs Screening,Institute of Botany,Jiangsu Province and Chinese Academy of Sciences,Nanjing 210014,China)

机构地区：[1]江苏省中国科学院植物研究所(南京中山植物园)江苏省抗糖尿病药物筛选技术服务中心,江苏南京210014

出　　处：《时珍国医国药》2022年第2期270-272,共3页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(81773885,21102058)。

摘　　要：目的探讨人肠道菌群对中药枇杷叶中6种主要活性三萜酸的生物转化,并考察原型化合物和转化产物对α-葡萄糖苷酶抑制活性的变化。方法将6种三萜酸:熊果酸(1)、科罗索酸(2)、蔷薇酸(3)、委陵菜酸(4)、齐墩果酸(5)和马斯里酸(6)在厌氧条件下与人肠道菌群共温孵培养3 d,利用UPLC-Q-TOF-MS技术对转化产物进行鉴定;采用体外活性筛选方法对原型化合物和转化产物的α-葡萄糖苷酶抑制作用进行评价。结果6种三萜酸中熊果酸(1)和齐墩果酸(5)在人肠道菌群培养系统中发生了微弱的生物转化反应,分别生成3-羰基熊果酸(7)和3-羰基齐墩果酸(8)。2种转化产物均具有较好的α-葡萄糖苷酶抑制活性,且转化产物8的抑制活性优于原型化合物。结论6种三萜酸在人肠道菌群培养系统中相对比较稳定,菌群生物转化后可能具有一定的降血糖增效作用。Objective To investigate the microbial transformation of six main and active triterpene acids from Eriobotrya japonica leaves via human intestinal bacteria and their inhibitory activities againstα-glucosidase in vitro.Methods Six triterpene acids including ursolic acid(1),corosolic acid(2),rosolic acid(3),tormentic acid(4),oleanolic acid(5)and maslinic acid(6),were incubated with human intestinal bacteria in an anaerobic condition for 3 days.Their transformed products were identified by UPLC-Q-TOF-MS and their inhibitory activity against yeastα-glucosidase was determined by in vitro inhibition model.Results The biotransformation of 1 produced one metabolite,3-carbonyl ursolic acid(7),while 5 gave the other metabolite,3-carbonyl oleanolic acid(8).However,the other substrates showed no transformation in the whole process.Bioactivity testing showed that both transformed products exhibited good inhibitory activity againstα-glucosidase with 8 more potent than its original compound 5.Conclusion Six triterpene acids are relatively stable in the human intestinal bacteria incubation system.They may have a certain degree of blood sugar lowering and synergistic effects after the biotransformation.

关 键 词：枇杷叶 三萜酸 肠道菌群 生物转化 降血糖作用 

分 类 号：R285[医药卫生—中药学]