五环三萜类化合物的口服吸收与代谢研究进展  

Advances in Studies on Oral Absorption and Metabolism of Pentacyclic Triterpenoids

作　　者：班玉娟 陈瑞 张宇 张丽 刘婉霞 朱高峰 汤磊 BAN Yu-juan;CHEN Rui;ZHANG Yu;ZHANG Li;LIU Wan-xia;ZHU Gao-feng;TANG Lei(School of Pharmacy,Guizhou Medical University,Guiyang 550004,China;Provincial Engineering Technology Research Center for Chemical Drug R&D,Guizhou Medical University,Guiyang 550004,China)

机构地区：[1]贵州医科大学药学院,贵州贵阳550004 [2]贵州医科大学贵州省化学合成药物研发利用工程技术研究中心,贵州贵阳550004

出　　处：《化学试剂》2021年第7期906-916,共11页Chemical Reagents

基　　金：国家自然科学基金资助项目(82060632);贵州省高层次创新型人才培养项目(黔科合人才(2016)4015)。

摘　　要：五环三萜类化合物在自然界中分布广泛、资源丰富,我国多种传统中草药如甘草、柴胡、远志、人参、三七、白头翁和积雪草等皆含有五环三萜类化合物,且大量研究表明该类化合物是上述中草药的有效成分之一。国内外研究者发现五环三萜类化合物具有多种优良的药理活性,如抗肿瘤、抗糖尿病、抗炎、抗菌和抗病毒等,但由于其口服生物利用度偏低,极大地影响了进一步的开发及在临床上的应用。药物的吸收与代谢对生物利用度和药效的影响很大。因此,就近年来国内外有关五环三萜类化合物的口服吸收特征以及体内外代谢途径研究进行综述,以期对该类化合物的进一步研究及开发利用提供参考。Pentacyclic triterpenoids having abundant resources, are widely distributed in nature.Many traditional Chinese herbal medicines such as Licorice, Bupleurum, Polygala, Ginseng, Notoginseng, Pulsatilla, and Centellaasiatica contain pentacyclic triterpenoids, and a large number of studies have shown that such compounds are the main effective ingredients in these Chinese herbal medicines.Researchers found that these compounds have a variety of excellent pharmacological activities such as anti-tumor, anti-diabetes, anti-inflammatory, antibacterial and anti-viral.However, due to their low oral bio-availability, further clinical applications of this kind of compounds have been greatly restrained.The absorption and metabolism of drugs greatly influence on its bio-availability and efficacy, so this article aims to review the studies on the oral absorption characteristics and metabolic pathways of pentacyclic triterpenoids in vitro and in vivo in recent years, and to give a reference for further research and development of this kind of compounds.

关 键 词：五环三萜 生物利用度 吸收 代谢 细胞色素P450 

分 类 号：R969[医药卫生—药理学]