Synthesis and anti-tumor activity of NO-donating derivatives of gambogic acid

被引：0

作者：

Wang Jin-Xin ^{[1
]}

Zhang Bai-Hong ^{[2
]}

Xu Dan-Dan ^{[1
]}

Miao Guang-Qiang ^{[1
]}

Wang Fan ^{[1
]}

Guo Qing-Long ^{[4
]}

You Qi-Dong ^{[1
,3
]}

机构：

[1] China Pharmaceut Univ, Jiangsu Key Lab Drug Design & Optimizat, Nanjing 210009, Jiangsu, Peoples R China

[2] Gen Hosp Peoples Liberat Army, Dept Oncol, Lanzhou 730050, Peoples R China

[3] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China

[4] China Pharmaceut Univ, Key Lab Carcinogenesis & Intervent Jiangsu Prov, Nanjing 210009, Jiangsu, Peoples R China

来源：

CHINESE JOURNAL OF NATURAL MEDICINES | 2013年 / 11卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Gambogic acid and derivatives; Apoptosis inducer; Nitric oxide; Cytotoxicity; NITRIC-OXIDE; IN-VITRO; BIOLOGICAL EVALUATION; MELANOMA-CELLS; APOPTOSIS; EXPRESSION; PROLIFERATION; GROWTH; CANCER; GENE;

D O I：

10.1016/S1875-5364(13)60015-1

中图分类号：

R [医药、卫生];

学科分类号：

10 ;

摘要：

AIM: To find a potent apoptosis inducer from gambogic acid and its derivatives. METHODS: Eight new NO-donating derivatives of gambogic acid were synthesized as potential anti-tumor lead compounds and their inhibitory activity on the HT-29, Bel-7402, BGC-823, and A549 cell lines were evaluated in vitro by the MTT assay. RESULTS: Among these compounds, 4 with a hydroxyl group at C35 of the gambogic acid moiety was identified as a SKOV3 cell apoptosis inducer through the MTT cell assay, observations of morphological changes, and Annexin-V/PI double staining assay. CONCLUSION: Compound 4 showed significant effects in inducing apoptosis and might serve as a potential lead compound for the discovery of new anticancer drugs.

引用

页码：87 / 96

页数：10

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