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Antitumor and Antimicrobial Potential of Bromoditerpenes Isolated from the Red Alga, Sphaerococcus coronopifolius

机译:从红藻中分离出的溴二苯醚的抗肿瘤和抗菌潜力Coronopifolius

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Cancer and infectious diseases continue to be a major public health problem, and new drugs are necessary. As marine organisms are well known to provide a wide range of original compounds, the aim of this study was to investigate the bioactivity of the main constituents of the cosmopolitan red alga, Sphaerococcus coronopifolius. The structure of several bromoditerpenes was determined by extensive spectroscopic analysis and comparison with literature data. Five molecules were isolated and characterized which include a new brominated diterpene belonging to the rare dactylomelane family and named sphaerodactylomelol (1), along with four already known sphaerane bromoditerpenes (2–5). Antitumor activity was assessed by cytotoxicity and anti-proliferative assays on an in vitro model of human hepatocellular carcinoma (HepG-2 cells). Antimicrobial activity was evaluated against four pathogenic microorganisms: Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Candida albicans. Compound 4 exhibited the highest antimicrobial activity against S. aureus (IC50 6.35 µM) and compound 5 the highest anti-proliferative activity on HepG-2 cells (IC50 42.9 µM). The new diterpene, sphaerodactylomelol (1), induced inhibition of cell proliferation (IC50 280 µM) and cytotoxicity (IC50 720 µM) on HepG-2 cells and showed antimicrobial activity against S. aureus (IC50 96.3 µM).
机译:癌症和传染病仍然是主要的公共卫生问题,因此必须使用新药。众所周知,海洋生物可提供多种原始化合物,因此,本研究的目的是调查世界性红藻藻球菌(Sphaerococcus coronopifolius)的主要成分的生物活性。通过广泛的光谱分析并与文献数据进行比较,确定了几种溴二苯并三萜的结构。分离并鉴定了五个分子,其中包括一个新的溴化二萜,该溴化二萜属于稀有的actetomelane家族,被命名为sphaerodactylomelol(1),以及四个已知的四氢呋喃溴代二萜(2-5)。在人肝细胞癌(HepG-2细胞)的体外模型中,通过细胞毒性和抗增殖试验评估了抗肿瘤活性。评估了对四种病原微生物的抗菌活性:大肠杆菌,铜绿假单胞菌,金黄色葡萄球菌和白色念珠菌。化合物4对金黄色葡萄球菌具有最高的抗菌活性(IC 50 6.35 µM),化合物5对HepG-2细胞具有最高的抗增殖活性(IC 50 42.9 µM )。新的二萜-间苯三酚(1)诱导对HepG-2细胞的细胞增殖(IC 50 280 µM)和细胞毒性(IC 50 720 µM)抑制,并显示出抗菌作用金黄色葡萄球菌的活性(IC 50 96.3 µM)。

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