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题名: Characterization of Proapoptotic Compounds from the Bark of Garcinia oblongifolia
作者: Feng, Chao1; null(黄胜雄)2; Gao, Xue-Mei3, 4; Xu, Hong-Xi5, 6; Luo, Kathy Qian7
刊名: JOURNAL OF NATURAL PRODUCTS
关键词: ANTICANCER DRUG SCREEN ; INHIBITS TUMOR-GROWTH ; HELA-CELLS ; APOPTOSIS ; ACTIVATION ; DEATH ; RESISTANCE ; DYNAMICS ; LINES ; HER2
英文摘要: Twenty compounds from Garcinia oblongifolia were screened for proapoptotic activity using FRET-based HeLa-C3 sensor cells. Among them, oblongifolins F and G (1 and 2), 1,3,5-trihydroxy-13,13-dimethyl-2H-pyran[7,6-b]xanthone (3), nigrolineaxanthone T (4), and garcicowin B (5) showed significant proapoptotic activity at a concentration of 10 mu M. Bioassessments were then performed to evaluate the potential of these compounds for therapeutic application. All five compounds showed significant cytotoxicity and caspase-3-activating ability in cervical cancer He La cells, with compounds 1 and 2 having the highest potencies. All five compounds specifically induced caspase-dependent apoptosis, which could be prevented by the pan-caspase inhibitor zVAD-fmk. In particular, 3 induced apoptosis through mitotic arrest. Compounds 1-5 displayed similar IC50 values (3.9-16.5 mu M) against the three cancer cell lines He La, MDA-MB-435, and HepG2. In addition, compounds 1, 2, and 4 exhibited similar and potent IC50 values (2.4-5.1 mu M) against several breast and colon cancer cell lines, including those overexpressing either HER2 or P-glycoprotein. HER2 and P-glycoprotein are known factors that confer resistance to anticancer drugs in cancer cells. This is the first study on the cytotoxicity, caspase-3-activing ability, and specificity of proapoptotic compounds isolated from G. oblongifolia in He La cells. The potential application of these compounds against HER2- or P-glycoprotein-overexpressing cancer cells was investigated.
出版日期: 2014-05-01
卷号: 77, 期号:5, 页码:1111-1116
语种: 英语
收录类别: SCI
学科分类: Plant Sciences ; Chemistry, Medicinal ; Pharmacology & Pharmacy
ISSN号: 0163-3864
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/18184
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Hong Kong Univ Sci & Technol, Dept Chem & Biomol Engn, Clear Water Bay, Hong Kong, Peoples R China
2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Yunnan, Peoples R China
3.Yunnan Univ Nationalities, State Ethn Affairs Commiss, Key Lab Chem Ethn Med Resources, Kunming 650031, Yunnan, Peoples R China
4.Yunnan Univ Nationalities, Minist Educ, Kunming 650031, Yunnan, Peoples R China
5.Shanghai Univ Tradit Chinese Med, Sch Pharm, Shanghai 201203, Peoples R China
6.Shanghai Coll TCM New Drug Discovery, Engn Res Ctr, Shanghai 201203, Peoples R China
7.Nanyang Technol Univ, Sch Chem & Biomed Engn, Div Bioengn, Singapore 637457, Singapore

Recommended Citation:
Feng,Chao;Huang,Sheng-Xiong;Gao,Xue-Mei;Xu,Hong-Xi;Luo,Kathy Qian.Characterization of Proapoptotic Compounds from the Bark of Garcinia oblongifolia,JOURNAL OF NATURAL PRODUCTS,2014,77(5):1111-1116
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