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Betulinic Acid and its Derivatives as Potential Antitumor Agents
Author(s) -
Zhang DongMei,
Xu HongGui,
Wang Lei,
Li YingJie,
Sun PingHua,
Wu XiaoMing,
Wang GuangJi,
Chen WeiMin,
Ye WenCai
Publication year - 2015
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.21353
Subject(s) - betulinic acid , betulin , derivatization , chemistry , cytotoxicity , triterpene , stereochemistry , terpene , combinatorial chemistry , quantitative structure–activity relationship , pharmacology , computational biology , biochemistry , biology , in vitro , organic chemistry , medicine , genetics , high performance liquid chromatography , alternative medicine , pathology
Betulinic acid (BA) is a lupane‐type pentacyclic triterpene, distributed ubiquitously throughout the plant kingdom. BA and its derivatives demonstrate multiple bioactivities, particularly an antitumor effect. This review critically describes the recent research on isolation, synthesis, and derivatization of BA and its natural analogs betulin and 23‐hydroxybetulinic acid. The subsequent part of the review focuses on the current knowledge of antitumor properties, combination treatments, and pharmacological mechanisms of these compounds. A 3D‐QSAR analysis of 62 BA derivatives against human ovarian cancer A2780 is also included to provide information concerning the structure–cytotoxicity relationships of these compounds.