白头翁中抗肿瘤物质的筛选及其作用机制研究

Screening of Antitumor Compounds from Radix Pulsatillae and Researching on Their Mechanism

从白头翁中筛选出具有抗肿瘤活性的物质,并进一步研究其作用机制,为开发新的抗肿瘤药物奠定基础。以人肝癌SNU-387细胞为研究对象,用MTT法检测各白头翁提取物的抗肿瘤活性,获得活性较高的物质。运用Annexin V-FITC/PI双染法,通过流式细胞仪检测BTW10和BTW11对SNU-387细胞凋亡的影响;采用Elisa法,检测它们对Bax与Bcl-2蛋白表达的影响。白头翁皂苷(BTW)类物质多数有抑瘤活性。其中BTW10和BTW11活性较高,IC_(50)分别为1.633μg/m L与3.104μg/m L;均能促进SNU-387细胞凋亡,促进Bax和抑制Bcl-2的表达。BTW10和BTW11具有明显的抑瘤作用,其抑瘤机制与其促进Bax和抑制Bcl-2的表达,破坏线粒体通透性,导致细胞凋亡有关。

The aim of this study was to screen out antitumor compounds from Radix Pulsatillae and to further research their mechanism, so as to lay a foundation for the development of new antitumor drugs. The inhibition effect of Radix Pul- satillae extract （BTWs） on SNU-387 cell were detected by MTT methoed. Apoptosis induced by BTW10 and BTW11 with higher inhibition were detected with the Annexin V-FITC/PI double staining flow eytometry. The effects on expres-sions of Bax and Bcl-2 of BTW10 and BTWll were determined with Elisa method. Most of anemosides showed high inhibition on SNU-387. BTW10 and BTW11 of them showed higher inhibition. Their IC50 were 1.633 μg/mL and 3.104 μg/mL, respectively. They can induce apeptosis of SNU-387,premote the expression of Bax ,and inhibit the expression of Bel-2. Hence, it was concluded that BTW10 and BTW11 had higher inhibition on SNU-387. The mechanisms of inhibition were relevant to their promotion of Bax and inhibition of Bcl-2,damaging permeability of mitochondria and inducing apoptosis.