大蒜有机硫化物对药物代谢酶和转运体影响的研究进展  

Research progress in the effect of garlic organosulfur compounds on drug metabolic enzymes and transporters

作　　者：杨园园 王彬 刘燕 徐晓燕 YANG Yuan-yuan;WANG Bin;LIU Yan;XU Xiao-yan(School of Pharmaceutical Sciences,Shandong First Medical University&Shandong Academy of Medical Sciences,Tai’an Shandong 271000;Shandong Tops-pharm Research and Development Company Limited,Tai’an Shandong 271000)

机构地区：[1]山东第一医科大学(山东省医学科学院)药学院,山东泰安271000 [2]山东特谱药物研发有限公司,山东泰安271000

出　　处：《中南药学》2023年第5期1321-1329,共9页Central South Pharmacy

基　　金：山东省自然科学基金项目(No.ZR2020QH366)。

摘　　要：近年来,大蒜有机硫化物(GOSCs)及其活性代谢产物在慢性阻塞性肺疾病(COPD)的治疗中表现出低毒高效的效果,且可减少布地奈德等药物的不良反应,因此GOSCs具有单独开发和与现有药物复方开发的巨大潜力。为发现可能存在的药物相互作用,我们需明确GOSCs及活性代谢产物对药物代谢酶和转运体的影响。通过查阅PubMed、中国知网及万方数据等数据库,检索到GOSCs药理作用相关文献46篇,GOSCs代谢转运和生物转化机制相关文献46篇及COPD相关文献6篇。作者对主要的GOSCs及活性代谢物的药理活性、生物转化机制,对主要的药物Ⅰ相、Ⅱ相代谢酶及药物转运体的调控机制进行综述,并结合目前主流COPD治疗药物的代谢机制,推测了药物联用可能发生的药物相互作用,以期为GOSCs的进一步开发和临床合理用药提供理论基础。In recent years,garlic organosulfur compounds(GOSCs)and their active metabolites have shown low toxicity and high efficiency in the treatment of chronic obstructive pulmonary disease(COPD).They can reduce the side effects of such drugs as budesonide,so GOSCs have great potential to be developed both alone and in combination with other drugs.To identify possible drug interactions,the effects of GOSCs and their active metabolites on drug metabolic enzymes and transporters need to be clarified.By reviewing PubMed,China National Knowledge Infrastructure(CNKI)and Wanfang databases,46 papers related to the pharmacological effects of GOSCs,46 papers related to the metabolic transport and biotransformation mechanisms of GOSCs and 6 papers related to COPD were retrieved.This paper reviewed the pharmacological activities and biotransformation mechanisms of GOSCs and their active metabolites,as well as the regulatory mechanism of drug phaseⅠandⅡmetabolic enzymes and drug transporters.Based on the metabolic characteristics of the current main stream COPD therapeutic drugs,the authors speculated on the possible drug interactions between drugs for COPD and GOSCs in combination,to provide a theoretical basis for the further development and rational clinical use of GOSCs.

关 键 词：大蒜 有机硫化物 细胞色素P450酶 药物代谢酶 药物转运体 药物相互作用 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]