摘要
对来源于南海红树林底泥的海洋链霉菌H41-59发酵物中的次级代谢产物进行了分离纯化、结构鉴定及抗肿瘤细胞毒活性评价研究。经硅胶柱层析、Sephadex LH-20分子排阻层析和高效液相色谱等分离手段,从中分离得到了10个甾醇类化合物。通过核磁、质谱等方法,并结合与文献数据比对,鉴定分离得到的化合物分别为:麦角甾-7,22-二烯-3β,5α,6β-三醇(1)、麦角甾-7,22-二烯-3β,5α,6α-三醇(2)、麦角甾-7,22-二烯-3β,5α,6β,9α-四醇(3)、麦角甾-7,22-二烯-3β,5α,6β,25-四醇(4)、5α,6α-环氧麦角甾-8(9),22-二烯-3β,7α-二醇(5)、5α,6α-环氧麦角甾-8(14),22-二烯-3β,7α-二醇(6)、麦角甾-8(9),22-二烯-3β,5α,6β,7α-四醇(7)、麦角甾-8(14),22-二烯-3β,5α,6β,7α-四醇(8)、5α,6α-环氧麦角甾-8(14),22-二烯-3β,7β-二醇(9)、麦角甾-5,7,22-三烯-3β-醇(10),化合物1~10均为首次从海洋来源链霉菌中分离得到。采用MTT法对这10个化合物进行体外抗肿瘤细胞活性的筛选,发现均具有一定的细胞毒活性。其中,化合物5、7和8表现出较好的抑制活性,其IC50值均小于50μg/m L。
To study the bioactive constituents of Streptomyces sp. strain H41-59 isolated from the sea bed mud at the mangrove district of South China Sea. By using silica gel, Sephadex LH-20 column chromatography and preparative HPLC methods,ten ergosterols were isolated from its ethyl acetate extract. Based on the analysis of NMR and ESI-MS spectral data,the structures of these compounds were identified as ergasta-7,22-diene-3β,5α,6β-triol(1) ,ergosta-7,22- diene-3β, 5 a, 6α-triol ( 2 ), ergosta-7,22 -diene-3β, 5α, 6β, 9α-tetraol ( 3 ), ergosta-7,22 -diene-3β, 5α, 6β,25 -tetraol ( 4 ), 5α,6α-epoxy-ergosta-8 (9),22-diene-3β, 7α-dlo/(5), 5or, 6cr-epoxy-ergosta-8 (14), 22-diene-3β, 7α-diol (6), ergosta-8 (9), 22-diene-3β, 5α, 6β,7α-tetraol ( 7 ), ergosta-8 (14), 22-diene-3β,5α, 6β,7α-tetraol ( 8 ), 5α, 6α-epoxy-ergosta-8 (14) ,22-diene-3β,4β-diol(9) ,ergosta-5,7,22-tfiene-3β-ol(10). Compound 1-10 were isolated from Streptomyces species for the first time. Cytotoxicities of these sterols against three cancer cell lines were evaluated in vitro by MTT method. All of them showed cytotoxic activity to some extent. Among them, compound 5,7 and 8 displayed moderate eytotoxicity,with IC50 values lower than 50μg/mL.
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2016年第5期690-695,760,共7页
Natural Product Research and Development
基金
国家自然科学基金面上项目(81373320)
广东省自然基金团队项目(2015A030312002)
暨南大学教育部研究基金(21612114)