摘要
四环三萜化合物是植物来源中药里具有多种生物活性的一类重要化合物,但研究发现四环三萜类化合物普遍口服生物利用度低,肠吸收不佳,严重影响了该类成分的开发和应用。四环三萜类化合物按照苷元不同大致可以分为达玛烷型、羊毛脂烷型、葫芦素烷型、环阿屯烷型、原帖烷型、楝烷型等几类,总结了不同结构类型的四环三萜化合物单体的肠吸收机制,探讨其肠吸收不佳的原因;综述发现肠吸收多用于研究中药单体、单味中药和中药复方配伍的有效吸收成分及其相互作用规律,并表明中药配伍对有效成分的肠道吸收具有很好的改善作用,以期为改善中药四环三萜类化合物的口服利用度、新剂型的研发设计以及临床的合理用药提供参考。
Tetracyclic triterpenes are a kind of important compounds with a variety of biological activities in traditional Chinese medicine,but it has been found that tetracyclic triterpenes have low oral bioavailability and poor intestinal absorption,which seriously affect the development and application of tetracyclic triterpenes.Intestinal perfusion in vivo and Caco-2 cell model are often used to study the intestinal absorption of drugs.According to the difference of aglycone,tetracyclic triterpenes can be roughly divided into damarane type,lanolin type,cucurbitane type,cycloartenane type,protopane type,neem type and so on.in this paper,the intestinal absorption mechanism of tetracyclic triterpenes with different structures was summarized,and the reasons for their poor intestinal absorption were discussed.It is found that intestinal absorption is mainly used to study the effective absorption components and their interaction of monomer,single traditional Chinese medicine and compound prescription of traditional Chinese medicine,and shows that the compatibility of traditional Chinese medicine can improve the intestinal absorption of effective components.in order to provide reference for improving the oral availability of tetracyclic triterpenes in traditional Chinese medicine,the research and design of new dosage forms and the rational use of drugs in clinic.
作者
王丽
杨冰
牛玉清
徐旭
田成旺
张铁军
陈昆南
WANG Li;YANG Bing;NIU Yuqing;XU Xu;TIAN Chengwang;ZHANG Tiejun;CHEN Kunnan(Graduate School of Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;Tianjin Key Laboratory of Quality Markers of Traditional Chinese Medicine,Tianjin Institute of Materia Medica,Tianjin 300301,China;The State Key Laboratory of Drug Release Technology and Pharmacokinetics of Tianjin Institute of Materia Medica,Tianjin 300301,China;Guangzhou Baiyunshan Mingxing Pharmaceutical Co.,Ltd.,Guangzhou 510250,China)
出处
《药物评价研究》
CAS
2022年第1期162-170,共9页
Drug Evaluation Research
基金
国家重点研发计划资助项目(2019YFC1711300)
广西科技重大专项(桂科AA18118049-3)
中医药国际合作专项(基地类项目)(0610-2140NF020630)。
关键词
四环三萜化合物
中药
吸收转运
肠吸收
生物利用度
中药配伍
tetracyclic triterpenes
traditional Chinese medicine
absorption and transport
intestinal absorption
bioavailability
compatibility of traditional Chinese medicine
