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从内生真菌蜂巢头孢 Cephalotheca faveolata Yaguchi、Nishim. 和 Udagawa 中分离得到的核盘菌素的抗癌活性。

Anticancer activity of sclerotiorin, isolated from an endophytic fungus Cephalotheca faveolata Yaguchi, Nishim. & Udagawa.

作者信息

Giridharan Periyasamy, Verekar Shilpa Amit, Khanna Amit, Mishra P D, Deshmukh Sunil Kumar

机构信息

Piramal Healthcare Ltd, 1, Nirlon Complex, Off Western Express Highway, Near NSE Complex, Goregaon (East), Mumbai 400 063, India.

出版信息

Indian J Exp Biol. 2012 Jul;50(7):464-8.

PMID:22822525
Abstract

Biodiversity provides critical support for drug discovery. A significant proportion of drugs are derived, directly or indirectly, from biological sources. Through high throughput screening (HTS) and bioassay-guided isolation, bioactive compound sclerotiorin has been isolated from an endophytic fungus Cephalotheca faveolata. Sclerotiorin was found to be potent anti-proliferative against different cancer cells. In this study sclerotiorin has been found to induce apoptosis in colon cancer (HCT-116) cells through the activation of BAX, and down-regulation of BCL-2, those further activated cleaved caspase-3 causing apoptosis of cancer cells.

摘要

生物多样性为药物研发提供了关键支持。相当一部分药物直接或间接来源于生物资源。通过高通量筛选(HTS)和生物测定引导的分离方法,从内生真菌蜂窝头孢霉中分离出了具有生物活性的化合物核盘菌素。研究发现核盘菌素对不同癌细胞具有强大的抗增殖作用。在本研究中,已发现核盘菌素通过激活BAX和下调BCL-2诱导结肠癌细胞(HCT-116)凋亡,进而激活裂解的半胱天冬酶-3,导致癌细胞凋亡。

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