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作 者:卜萌萌 胡家淳 蒋建东 王琰 BU Mengmeng;HU Jiachun;JIANG Jiandong;WANG Yan(State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences/Peking Union Medical College,Beijing 100050,China)
机构地区:[1]中国医学科学院药物研究所,天然药物活性物质与功能国家重点实验室,北京100050
出 处:《中国药学杂志》2024年第8期657-663,共7页Chinese Pharmaceutical Journal
基 金:国家自然科学基金项目资助(82173888);北京市重点实验室项目资助(Z141102004414062);中国医学科学院医学与健康科技创新工程项目资助(2021-I2M-1-007,2021-I2M-1-028)。
摘 要:多年来,天然药物如黄酮类、多糖类、环烯醚萜苷类和皂苷类等已被证实对多种疾病具有良好的疗效。一般来说,天然药物口服后在肠道内的生物利用度比较低。而肠道菌群作为调节宿主适应环境的生态系统之一,与宿主所处的内、外在环境之间存在着双向影响作用,通常对天然药物的药效起到关键的调控作用。特别是近年来靶向肠道菌群的新策略研究,为理解难吸收药物的药效作用机制提供了新的思路。肠道菌群与天然药物代谢之间的媒介往往是肠道菌编码的各种酶,通过酶的催化作用肠道菌可将口服类药物代谢并与其疗效及安全性紧密相关,而目前围绕天然药物在肠道菌作用下的代谢转化研究仍然有限。因此,笔者着重讨论肠道菌来源的主要代谢酶的特征以及它们在天然药物代谢转化中的研究进展,以丰富肠道菌作用下天然药物的代谢机制,以期为肠道菌作为参与机体其他器官功能调控轴中的一员提供直接的证据,并为深入理解肠道菌作用下天然药物代谢转化及药理学意义提供科学参考。Natural drugs have been used in clinic for thousands of years in China,with complete and systematic theories,and are the treasure of the Chinese nation.Among them,flavonoids,polysaccharides,iridoid glycosides,saponins and other natural drugs have been proved to have curative effects on many diseases.Generally,the bioavailability of natural drugs absorbed in the intestine after oral administration is relatively low.As one of the ecosystems regulating the host′s adaptation to the environment,the gut microbiota has a two-way effect on the host′s internal and external environment,which is usually closely related to the efficacy of natural drugs.In order to understand the mechanism of the effect of drugs that are difficult to absorb,the exploration of targeting the gut microbiota has become a new strategy in recent years.The metabolism of natural drugs is often achieved through the enzymes produced by the gut microbiota,which is closely related to its efficacy and safety.The research of metabolic transformation by the gut microbiota is still limited.So in this review,we mainly discussed the characteristics of major metabolic enzymes derived from gut microbiota and the research progress in the metabolism and transformation of natural drugs,aiming to enrich the information on the metabolism mechanism of natural drugs under the action of gut microbiota and provide evidence for proving that gut microbiota is part of the regulation axis of other organs.It also provides some scientific reference for deepening the understanding and cognition of the metabolism and transformation of natural drugs under the action of intestinal bacteria.
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