摘要
目的对1株西沙群岛永兴岛海域来源短指软珊瑚Sinulariasp.共附生真菌Penicillium sclerotiorum中的azaphilones类化合物及其生物活性进行研究。方法利用硅胶柱层析、薄层色谱、Sephadex LH-20凝胶柱层析、中压制备液相色谱法(MPLC)、高效液相色谱法(HPLC)等分离手段对菌株发酵提取物进行分离和纯化;运用核磁共振(NMR)、质量光谱测定法(MS)等现代波谱学方法,并结合相关文献数据比对,鉴定化合物的结构;通过细胞毒活性模型评价化合物抗肿瘤活性。结果从真菌Penicillium sclerotiorum的代谢产物中获得了9个azaphilones类合物,分别为(+)-Sclerotiorin(1)、Isochromophilone Ia(2)、Isochromophilone Ib(3)、IsochromophiloneⅢ(4)、Epi-isochromophiloneⅢ(5)、IsochromophiloneⅣ(6)、DechloroisochromophiloneⅣ(7)、IsochromophiloneⅤⅢ(8)、TL-1-monoAc(9),其中化合物8对HL-60细胞显示一定的抑制活性,IC50值为11.81μmol·L^-1。
Objective To study the azaphilones compounds of the epiphytic fungus Penicillium sclerotiorumfrom the Xisha Islands soft coral Sinulariasp..Methods The fermentation extracts of the strains were separated and purified by silica gel column chromatography,thin layer chromatography,Sephadex LH-20 gel column chromatography,MPLC and HPLC.The spectroscopy methods such as NMR and MS were used.The literature data was aligned to identify the structures of the compounds.The antitumor activities of the compounds were evaluated by a cytotoxicity experiments.Results Nine azaphilones were isolated from the fungus Penicillium sclerotiorum,namely(+)-Sclerotiorin(1),Isochromophilone Ia(2),Isochromophilone Ib(3),Isochromophilone Ⅲ(4),Epi-isochromophilone Ⅲ(5),Isochromophilone Ⅳ(6),Dechloroisochromophilone Ⅳ(7),Isochromophilone ⅤⅢ(8),TL-1-monoAc(9).Compound 8 showed certain inhibitory activity on HL-60 cells.The IC50 value was 11.81μmol·L^-1.
作者
董尧
王晓梅
唐旭利
李平林
李国强
DONG Yao;WANG Xiao-mei;TANG Xu-li;LI Ping-lin;LI Guo-qiang(Key Laboratory of Marine Drugs,Ministry of Education,School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China;College of Chemistry and Chemical Engineering,Ocean University of China,Qingdao 266100,China)
出处
《中国海洋药物》
CAS
CSCD
2019年第6期15-20,共6页
Chinese Journal of Marine Drugs
基金
国家自然科学基金面上项目(41876161)资助