Rodrigues Daniel, Alves Celso, Horta André, Pinteus Susete, Silva Joana, Culioli Gérald, Thomas Olivier P, Pedrosa Rui
Marine Resources Research Group (GIRM), ESTM, Polytechnic Institute of Leiria, 2520-641 Peniche, Portugal.
Nice Institute of Chemistry-PCRE, UMR 7272 CNRS, University de Nice-Sophia Antipolis, Parc Valrose, 06108 Nice, France.
Mar Drugs. 2015 Jan 26;13(2):713-26. doi: 10.3390/md13020713.
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).
癌症和传染病仍然是主要的公共卫生问题，因此新药必不可少。由于众所周知海洋生物能提供各种各样的原始化合物，本研究的目的是调查全球分布的红藻冠叶球藻主要成分的生物活性。通过广泛的光谱分析并与文献数据比较，确定了几种溴代二萜的结构。分离并鉴定了五个分子，其中包括一种属于罕见指状二萜烷家族的新溴代二萜，命名为球指二萜醇（1），以及四种已知的球烷溴代二萜（2 - 5）。通过对人肝癌细胞系（HepG - 2细胞）的体外模型进行细胞毒性和抗增殖试验来评估抗肿瘤活性。针对四种致病微生物评估抗菌活性：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对金黄色葡萄球菌表现出最高的抗菌活性（IC50 6.35 μM），化合物5对HepG - 2细胞表现出最高的抗增殖活性（IC50 42.9 μM）。新的二萜球指二萜醇（1）对HepG - 2细胞诱导细胞增殖抑制（IC50 280 μM）和细胞毒性（IC50 720 μM），并对金黄色葡萄球菌表现出抗菌活性（IC50 96.3 μM）。
