Scytonemin extracted from Lyngbya aestuarii exhibits anti-cancer activity: involvement of c-Myc pathway inhibition.

IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED
Animesh Sen, Arpan Dey Bhowmik, Sikha Mandal, Paritosh Mondal, Ansuman Chattopadhyay, Jnanendra Rath
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Abstract

The increasing incidence of cancer-related morbidity and mortality underscores the urgent need for novel, less toxic therapeutic options. In this study, we isolated scytonemin from the marine cyanobacterium Lyngbya aestuarii. Its identification was confirmed through an absorption peak at 384 nm and MALDI-TOF MS analysis showing a [M + H]+ ion at m/z 545.838, consistent with its oxidised form (C36H20N2O4). Scytonemin demonstrated significant cytotoxicity against breast cancer cell lines MDA-MB-231 and MCF-7, with IC50 values of 8 μM and 4 μM, respectively, while remaining non-toxic to human peripheral blood lymphocytes (HPBLs). The compound rapidly induced caspase-dependent intrinsic apoptosis within 2 h, with apoptotic effects magnifying at 24 and 48 h. Molecular docking and reporter gene assays revealed that scytonemin inhibits two critical proteins associated with cancer progression c-Myc and Polo-like kinase 1 (PLK1). These results suggest that scytonemin holds promise as a lead compound for the development of targeted anti-cancer therapies.

从山茱萸中提取的细胞收缩素具有抗癌活性:参与c-Myc通路抑制。
随着癌症相关发病率和死亡率的增加,迫切需要新的、毒性更小的治疗方案。在这项研究中,我们从海洋蓝藻蓝藻蓝藻中分离出了丝胞肽。通过384 nm处的吸收峰和MALDI-TOF MS分析证实了它的鉴定,在M /z 545.838处发现了一个[M + H]+离子,与它的氧化形式(C36H20N2O4)一致。丝胞胺对乳腺癌细胞株MDA-MB-231和MCF-7具有显著的细胞毒性,IC50值分别为8 μM和4 μM,而对人外周血淋巴细胞(hbls)无毒。该化合物可在2 h内快速诱导caspase依赖的内在凋亡,在24和48 h时凋亡效应放大。分子对接和报告基因分析显示,scytonemin抑制两种与癌症进展相关的关键蛋白c-Myc和polo样激酶1 (PLK1)。这些结果表明,细胞张力蛋白有望成为开发靶向抗癌疗法的先导化合物。
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来源期刊
Natural Product Research
Natural Product Research 化学-医药化学
CiteScore
5.10
自引率
9.10%
发文量
605
审稿时长
2.1 months
期刊介绍: The aim of Natural Product Research is to publish important contributions in the field of natural product chemistry. The journal covers all aspects of research in the chemistry and biochemistry of naturally occurring compounds. The communications include coverage of work on natural substances of land and sea and of plants, microbes and animals. Discussions of structure elucidation, synthesis and experimental biosynthesis of natural products as well as developments of methods in these areas are welcomed in the journal. Finally, research papers in fields on the chemistry-biology boundary, eg. fermentation chemistry, plant tissue culture investigations etc., are accepted into the journal. Natural Product Research issues will be subtitled either ""Part A - Synthesis and Structure"" or ""Part B - Bioactive Natural Products"". for details on this , see the forthcoming articles section. All manuscript submissions are subject to initial appraisal by the Editor, and, if found suitable for further consideration, to peer review by independent, anonymous expert referees. All peer review is single blind and submission is online via ScholarOne Manuscripts.
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