Betulinic Acid and its Derivatives as Potential Antitumor Agents

被引：171

作者：

Zhang, Dong-Mei ^{[1
]}

Xu, Hong-Gui ^{[2
]}

Wang, Lei ^{[1
]}

Li, Ying-Jie ^{[1
]}

Sun, Ping-Hua ^{[2
]}

Wu, Xiao-Ming ^{[3
]}

Wang, Guang-Ji ^{[3
]}

Chen, Wei-Min ^{[2
]}

Ye, Wen-Cai ^{[1
]}

机构：

[1] Jinan Univ, Coll Pharm, Guangdong Prov Key Lab Pharmacodynam Constituents, Guangzhou 510632, Guangdong, Peoples R China

[2] Jinan Univ, Coll Pharm, Dept Med Chem, Guangzhou 510632, Guangdong, Peoples R China

[3] China Pharmaceut Univ, Coll Pharm, Pharmaceut Res Inst, Nanjing 210009, Jiangsu, Peoples R China

来源：

MEDICINAL RESEARCH REVIEWS | 2015年 / 35卷 / 06期

基金：

美国国家科学基金会;

关键词：

betulinic acid; derivatives; antitumor effect; structure-cytotoxicity relationship; CYTOCHROME-C RELEASE; SP TRANSCRIPTION FACTORS; MULTIPLE-MYELOMA CELLS; HUMAN-MELANOMA CELLS; HUMAN CANCER-CELLS; NF-KAPPA-B; IN-VITRO; 23-HYDROXYBETULINIC ACID; LUPANE TRITERPENOIDS; CYTOTOXIC ACTIVITY;

D O I：

10.1002/med.21353

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2015 Wiley Periodicals, Inc.

引用

页码：1127 / 1155

页数：29

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