Characterization of Proapoptotic Compounds from the Bark of Garcinia oblongifolia
Feng, Chao1; Huang, Sheng-Xiong2; Gao, Xue-Mei3,4; Xu, Hong-Xi5,6; Luo, Kathy Qian7; Xu,HX (reprint author),Shanghai Univ Tradit Chinese Med,Sch Pharm,Shanghai 201203,Peoples R China.; xuhongxi88@gmail.com; kluo@ntu.edu.sg
2014-05-01
发表期刊JOURNAL OF NATURAL PRODUCTS
ISSN0163-3864
卷号77期号:5页码:1111-1116
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.
关键词Anticancer Drug Screen Inhibits Tumor-growth Hela-cells Apoptosis Activation Death Resistance Dynamics Lines Her2
资助信息National Research Foundation of Singapore [NRF-CRP8-2011-05, M4092018.0S4];Ministry of Education of Singapore AcRF Tier 1 [M4010891.120];National Natural Science Foundation of China [21002085, 21362044]
学科领域Plant Sciences ; Chemistry, Medicinal ; Pharmacology & Pharmacy
DOI10.1021/np4007316
收录类别SCI
语种英语
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy
WOS类目Plant Sciences ; Chemistry, Medicinal ; Pharmacology & Pharmacy
WOS记录号WOS:000336510700003
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/18184
专题植物化学与西部植物资源持续利用国家重点实验室
通讯作者Xu,HX (reprint author),Shanghai Univ Tradit Chinese Med,Sch Pharm,Shanghai 201203,Peoples R China.; xuhongxi88@gmail.com; kluo@ntu.edu.sg
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
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GB/T 7714
Feng, Chao,Huang, Sheng-Xiong,Gao, Xue-Mei,et al. Characterization of Proapoptotic Compounds from the Bark of Garcinia oblongifolia[J]. JOURNAL OF NATURAL PRODUCTS,2014,77(5):1111-1116.
APA Feng, Chao.,Huang, Sheng-Xiong.,Gao, Xue-Mei.,Xu, Hong-Xi.,Luo, Kathy Qian.,...&kluo@ntu.edu.sg.(2014).Characterization of Proapoptotic Compounds from the Bark of Garcinia oblongifolia.JOURNAL OF NATURAL PRODUCTS,77(5),1111-1116.
MLA Feng, Chao,et al."Characterization of Proapoptotic Compounds from the Bark of Garcinia oblongifolia".JOURNAL OF NATURAL PRODUCTS 77.5(2014):1111-1116.
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