中国中西医结合杂志2024，Vol.44Issue(1)：91-95,5.DOI:10.7661/j.cjim.20230508.131
丹参主要活性成分对瑞格列奈体外代谢性相互作用影响
Effects of Main Active Components of Salvia Miltiorrhiza on Metabolic Interaction of Repaglinide in vitro
摘要
Abstract
Objective Based on the metabolic mechanism of cytochrome P450(CYP450)enzyme,the effects of the main active ingredients of Salvia Miltiorrhiza,tanshinone Ⅰ,cryptotanshinone,and sodium tanshinone ⅡA sulfonate on the metabolism of repaglinide were studied,so as to provide reference for clinically safe and rational drug use.Methods The in vitro incubation systems were established for rat and human liver microsomes,co-incubated in a 37℃ water bath with concentrations ranging 0.25-50 μ mol/L tanshinone Ⅰ,cryptotanshinone,and tanshinone Ⅱ A sodium sulfonate and repaglinide(concentration in rat liver microsomes 44 μ mol/L and human liver microsomes 5.5 μ mol/L),respectively.The residual concentration of repaglinide in liver microsomes was determined by UPLC with atorvastatin as the internal standard.Finally,the effects of three components on the metabolism of repaglinide were observed by reduced amount of repaglinide in liver microsomes.Results When the concentration of tanshinone Ⅰ was 50 μ mol/L,the percentage of residual repaglinide in rat and human liver microsomes was 98.11％and 96.50％respectively.When the concentration of cryptotanshinone was 50 μ mol/L,the percentage of residual repaglinide in rat and human liver microsomes was 102.37％and 84.69％respectively.Tanshinone Ⅱ A Sodium Sulfonate Injection 10 and 50 μ mol/L showed inhibitory effects on rat and human liver microsomes,and its half inhibitory concentration on repaglinide in rat and human liver microsomes incubation system was 0.17 and 0.33 μ mol/L respectively.Conclusions Tanshinone Ⅰ and cryptotanshinone had no obvious effect on the metabolism of repaglinide in rat liver microsomes,while cryptotanshinone had a slight induction effect on the metabolism of repaglinide in human liver microsomes.Tanshinone Ⅱ A sulfonate sodium had a strong inhibitory effect on repaglinide in both rat and human liver microsomes.Therefore,when Tanshinone Ⅱ A Sodium Sulfonate Injection was used in combination with repaglinide,blood glucose should be monitored to avoid hypoglycemic events in patients.关键词
丹参酮Ⅰ/隐丹参酮/丹参酮ⅡA磺酸钠/瑞格列奈/细胞色素P450酶/药物相互作用/超高效液相/中药Key words
tanshinone Ⅰ/cryptotanshinone/sodium tanshinone Ⅱ A sulfonate/Repaglinide/cytochrome P450/drug-drug interaction/ultra-high performance liquid phase/Chinese herbal medicine引用本文复制引用
何文娟,刘秀菊,孙倩,赵晓娟,李敬瑄,王淑梅..丹参主要活性成分对瑞格列奈体外代谢性相互作用影响[J].中国中西医结合杂志,2024,44(1):91-95,5.基金项目
河北省2021年度中医药类科研指令性计划课题(No.2121132) （No.2121132）
