title: Synthesis and evaluation of asiatic acid derivatives as anti-fibrotic agents: structure/activity studies.
abstract: Fibrotic diseases are characterized by the over-accumulation of fibrous components in the extracellular matrix and the liver, which can lead to liver cirrhosis. Current treatment options cannot reverse or halt liver fibrosis, motivating a search for newer treatment options. Previously, we showed that asiaticoside, a bioactive triterpene glycoside from Centella asiatica, has anti-fibrotic properties. Here, the aglycone asiatic acid was chemically modified, and these derivatives were evaluated for their potential as anti-fibrotic agents. The data obtained from in vivo testing of these compounds in a rodent CCl4-induced liver injury model are discussed. The information obtained from these studies may be useful in the design of novel anti-fibrotic agents.
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Li
authors.affiliation: Sichuan Tourism University, 459 Hongling Road, Longquan District, Chengdu 610100, Sichuan Province, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Yang
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Mingxing
authors.initials: M
authors.lastname: Yuan
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Lijuan
authors.initials: L
authors.lastname: Jiang
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Li
authors.initials: L
authors.lastname: Yuan
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Zhang
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Li
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Lin
authors.initials: L
authors.lastname: Dong
authors.affiliation: School of Pharmacy, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China.
authors.forename: Xu
authors.initials: X
authors.lastname: Bao
authors.affiliation: School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China. Electronic address: chuandayouji217@163.com.
authors.forename: Shufan
authors.initials: S
authors.lastname: Yin
mesh_terms: D000818:Animals; D060326:Chemistry Techniques, Synthetic; D005260:Female; D008103:Liver Cirrhosis / Q000188:drug therapy*; D053978:Pentacyclic Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D053978:Pentacyclic Triterpenes; C017032:asiatic acid
keywords: Anti-fibrotic; Asiatic acid derivatives; Fibrotic diseases; Synthesis