1株海洋来源真菌Nigrospora sp.蒽醌类化合物及其生物活性研究  

Study on anthraquinone derivatives isolated from a marine-derived fungus Nigrosporasp.and their biological activities

作　　者：邢倩[1] 杨凯琳[1] 王毓[1] 杨瑞云[2] 王长云[1] 邵长伦[1] 

机构地区：[1]中国海洋大学海洋药物教育部重点实验室,医药学院,山东青岛266003 [2]广西师范大学药用资源化学与药物分子工程教育部重点实验室,化学化工学院,广西桂林541004

出　　处：《中国海洋药物》2014年第6期8-14,共7页Chinese Journal of Marine Drugs

基　　金：国家自然科学基金项目(41130858;41322037);药用资源化学与药物分子工程教育部重点实验室课题(CMEMR2011-08)资助

摘　　要：目的对1株海洋来源真菌Nigrosporasp.(TA26-9)中的蒽醌类化合物进行结构表征,筛选评价生物活性。方法采用波谱分析方法和单晶衍射技术对化合物进行结构表征,采用微量稀释法测定化合物对10株致病菌的抗菌活性,采用Solis改良法测定化合物的卤虫致死活性。结果结构表征确定了6个蒽醌类化合物(1~6)的结构。对化合物1~6及其乙酰化衍生物3a,4a,5a^5d生物活性评价表明,所有化合物对辣椒炭疽病菌Colletotrichum capsici都有选择性抗菌活性,MIC=0.26~1.22μmol/L;除化合物3外,对玉米大斑病菌Setosphaeria turcica也表现出很好的抗菌活性,MIC=0.27~4.82μmol/L。特别地,化合物3a具有广谱抗菌活性,对8株致病菌的MIC在0.27~4.32μmol/L之间,该化合物还显示卤虫致死活性,在25μg/mL浓度下对卤虫Artemia salina的致死率为78.9%。结论海洋来源真菌Nigrosporasp.(TA26-9)中的蒽醌类化合物具有选择性抗菌活性,具有开发成抗菌剂的潜力。Objective To characterize the structures of anthraquinone derivatives isolated from a marine derived fungus Nigrospora sp. （TA26-9） and evaluate their biological activities. Methods Structural characterization was established by extensive spectroscopic analysis as well as single-crystal X-ray dif- fraction analysis using Cu Ks radiation. Antimicrobial activities of anthraquinone derivatives against ten pathogenic strains were determined by micro-dilution method. Brine shrimp lethality was measured u- sing Solis modified method. Results The structures of six anthraquinone derivatives （1-6） were deter- mined by structural characterization. Compounds 1-6 and their acetylated derivatives 3a, 4a, 5a--5d were evaluated for their biological activities. All compouncts snowea selecuve atnmun gainst Colletotrichum capsici with the minimum inhibitory concentrations （MICs） ranging from 0. 26 to 1.22 μmol/L, and all the tested compounds, except 3, also exhibited antifungal activities against Seto- sphaeria turcica with the MICs of 0. 27N 4. 82 μmol/L. Specifically, 3a displayed broad-spectrum anti- microbial activity against eight pathogenic strains （MIC=0. 27N 4. 32μmol/L）. In addition, 3a showed lethal activity against brine shrimp Artemia salina with a lethality rate of 78.9 % at 25μg/mL. Conclu- sion Anthraquinone derivatives isolated from Nigrospora sp. （TA26-9） possess selective antimicrobial activities with the potential to be developed into antimicrobial agents.

关 键 词：海洋来源真菌Nigrosporasp.蒽醌 抗菌活性 

分 类 号：R931[医药卫生—生药学]