Isolation and characterization of three new anti-proliferative Sesquiterpenes from Polygonum barbatum and their mechanism via apoptotic pathway

摘要: The emergence of chemoresistant cancers and toxicity related to existing chemotherapeutic agents, demand the search for new pharmacophore with enhanced anti-cancer activity least toxicity. For this purpose, three sesquiterpenes were isolated from ethyl acetate fraction aerial parts plant Polygonum barbatum evaluated their potential. structural elucidation characterization compounds 1–3 performed using various spectroscopic techniques such as mass, UV, IR, extensive 1D/2D–NMR spectroscopy. Furthermore, subjected screening against different cell lines followed by brief analysis apoptotic anti-angiogenic potentials potent hit non-small lung carcinoma line. All anti-proliferative potential (NCI-H460), breast cancer (MCF-7), cervical (HeLa) normal mouse fibroblast (NIH-3 T3) lines. Among these, compound 3 was found be more cytotoxic NCI-H460 MCF-7 cells (IC50 = 17.86 ± 0.72 11.86 ± 0.46 μM respectively). When compared standard drug cisplatin have (IC50 = 19 ± 1.24 μM) 9.62 ± 0.5 μM). Compound induced apoptosis in a dose dependent manner. It significantly downregulated, expression anti-apoptotic (BCL-2 L1 p53) increased pro-apoptotic (BAK BAX) genes. Besides apoptosis, it also reduced migration downregulated angiogenic genes (i.e. VEGF COX-2), thereby, inhibiting angiogenesis cells. possesses well inhibited cancerous altering gene expression, responsible it.