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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >A comparative study of proapoptotic potential of cyano analogues of boswellic acid and 11-keto-boswellic acid.
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A comparative study of proapoptotic potential of cyano analogues of boswellic acid and 11-keto-boswellic acid.

机译:乳香酸和 11-酮乳香酸的氰基类似物促凋亡潜力的比较研究。

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摘要

Semi-synthetic analogues of beta-boswellic acid (BA) and 11-keto-beta-boswellic acid (KBA) were comparatively evaluated for in vitro cytotoxicity against human myeloid leukaemia (HL-60) and human cervical carcinoma (HeLa) cells. 2-Cyano analogues of both the triterpenes were observed to have significant cytotoxicity against both the cells, displaying cytotoxicity in HL-60 cells at low concentrations. Further investigations suggested the proapoptotic potential associated with the two molecules to induce cytotoxicity in HL-60 cells, where one of them showed early proapoptotic effect as evidenced by several biological end-points of the apoptosis such as annexinV binding, DNA fragmentation and increase in sub-G0 DNA fraction and apoptotic bodies formation (Hoechst 33258 staining and SEM studies).
机译:比较评估了β-乳香酸(BA)和11-酮-β-乳香酸(KBA)的半合成类似物对人髓系白血病(HL-60)和人宫颈癌(HeLa)细胞的体外细胞毒性。观察到两种三萜的 2-氰基类似物对两种细胞都具有显着的细胞毒性,在低浓度下对 HL-60 细胞表现出细胞毒性。进一步的研究表明,与这两种分子相关的促凋亡潜力可诱导 HL-60 细胞的细胞毒性,其中一种细胞显示出早期的促凋亡作用,如细胞凋亡的几个生物学终点,如膜联蛋白 V 结合、DNA 片段化和 sub-G0 DNA 组分的增加和凋亡体形成(Hoechst 33258 染色和 SEM 研究)。

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