کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1397587 | 1501178 | 2011 | 11 صفحه PDF | دانلود رایگان |
Semi-synthetic analogues of β-boswellic acid (BA) and 11-keto-β-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).
A series of semi-synthetic analogues of BAs were comparatively evaluated for in vitro cytotoxicity against human cancer cell lines and their apoptotic potential.Figure optionsDownload as PowerPoint slideResearch highlights
► Synthesis of cyanoenone analogues of boswellic acids.
► Evaluation of cytotoxicity against human myeloid leukemia (HL-60) and human cervical carcinoma (HeLa) cells.
► Identification of two leads displaying about 50-100 fold higher cytotoxicity than their parent molecules.
► The lead molecules were able to induce apoptosis evidenced by several biological endpoints.
► Further, one of the two leads induced strong and early apoptotsis.
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 4, April 2011, Pages 1356–1366