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从紫檀中分离得到的紫檀芪的体外细胞毒性、抗增殖和抗氧化活性评价。

In vitro evaluation of the cytotoxic, anti-proliferative and anti-oxidant properties of pterostilbene isolated from Pterocarpus marsupium.

机构信息

Molecular Endocrinology Laboratory, Department of Biotechnology, Indian Institute of Technology Roorkee, Roorkee 247 667, Uttarakhand, India.

出版信息

Toxicol In Vitro. 2010 Jun;24(4):1215-28. doi: 10.1016/j.tiv.2010.02.007. Epub 2010 Feb 10.

DOI:10.1016/j.tiv.2010.02.007
PMID:20152895
Abstract

Pterostilbene, a dimethyl ester derivative of resveratrol, may act as an cytotoxic and hence as an anti-cancer agent. The present study was conducted to test the anti-cancer activity of pterostilbene purified from Pterocarpus marsupium on breast (MCF-7) and prostate (PC3) cancer cell lines. The purified pterostilbene was found to cause apoptosis in both the cell lines, which was marked by DNA fragmentation, formation of apoptotic bodies and membrane distortions. Apoptosis probably was due to the production of reactive oxygen species in MCF-7 and nitric oxide over production in PC3 cells. Even the drug detoxifying anti-oxidant enzymes could not nullify the effect of pterostilbene as required by the cancer cells for survival. Pterostilbene was found to inhibit the cell proliferating factors like Akt, Bcl-2 and induced the mitochondrial apoptotic signals like Bax, and the series of caspases. It also inhibited Matrix metalloproteinase 9 (MMP9) and alpha-methylacyl-CoA recemase (AMACR), two very well known metastasis inducers. In conclusion, pterostilbene has multiple target sites to induce apoptosis. Hence, after proper validation it can be used as a potential agent for the cure of breast and prostate cancer.

摘要

紫檀芪是白藜芦醇的二甲酯衍生物,可能具有细胞毒性,从而起到抗癌作用。本研究旨在测试从紫檀中提取的紫檀芪对乳腺癌(MCF-7)和前列腺癌(PC3)细胞系的抗癌活性。纯化的紫檀芪被发现能诱导这两种细胞系发生凋亡,其特征是 DNA 片段化、凋亡小体形成和细胞膜扭曲。凋亡可能是由于 MCF-7 中活性氧的产生和 PC3 细胞中一氧化氮的过度产生。即使是药物解毒抗氧化酶也不能消除紫檀芪对癌细胞生存的需求。紫檀芪能抑制 Akt、Bcl-2 等细胞增殖因子,并诱导 Bax 等线粒体凋亡信号和一系列半胱天冬酶。它还能抑制基质金属蛋白酶 9(MMP9)和α-甲基酰基辅酶 A 受体(AMACR),这两种都是非常著名的转移诱导物。总之,紫檀芪有多个诱导凋亡的靶点。因此,经过适当的验证,它可以作为治疗乳腺癌和前列腺癌的潜在药物。

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