南极深海来源真菌Penicillium crustosum PRB-2中1个新的二酮哌嗪类化合物  

One new diketopiperazine from Antarctic marine-derived fungus Penicillium crustosum PRB-2

作　　者：刘艳珍 常一民 范程 张国建[1,2] 李德海 车茜[1] 朱天骄 LIU Yan-zhen;CHANG Yi-min;FAN Cheng;ZHANG Guo-jian;LI De-hai;CHE Qian;ZHU Tian-jiao(Key Laboratory of Marine Drugs,Ministry of Education,School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China;Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology,Qingdao 266237,China)

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]青岛海洋科学与技术国家实验室海洋药物与生物制品功能实验室,山东青岛266237

出　　处：《中国海洋药物》2023年第1期7-11,共5页Chinese Journal of Marine Drugs

基　　金：国家重点研发计划项目(2018YFC1406705);新药创制国家科技重大专项(2018ZX09735004)资助。

摘　　要：目的 通过OSMAC策略,研究南极海洋来源真菌Penicillium crustosum PRB-2的次级代谢产物。方法 采用硅胶柱层析、Sephadex LH-20凝胶柱层析、高效液相色谱(HPLC)等分离方法对菌株发酵提取物进行分离纯化;运用NMR、MS等现代波谱学方法,确定化合物结构;通过活性筛选评价化合物活性。结果 从P. crustosum PRB-2中分离到1个新化合物chainstatin(1)和2个已知化合物penilloid A(2)、tryhistatin(3)。化合物1是首次报道C-5位被2-甲基戊-2-醇取代的二酮哌嗪类化合物。化合物1具有较弱的抗氧化活性,IC50值为294μmol/L。Objective To study the metabolites of Antarctic marine-derived fungus Penicillium crustosum PRB-2 by one strain many compounds(OSMAC) strategy. Methods Silica gel column chromatography, Sephadex LH-20 gel column chromatography, HPLC and other separation methods were used to isolate and purify the fermented extracts of the strain. NMR, MS and other modern spectroscopic methods were used to determine the structure of the compounds. The activity of compounds was evaluated by activity screening. Results One new compound, chainstatin(1) and two known compounds, penilloid A(2) and tryhistatin(3) were isolated from the P. crustosum PRB-2. Compound 1 was a novel structure diketopiperazine with the 2-methylpentan-2-ol group at C-5-position, which was naturally occurring for the first time. Compound 1 exhibited weak antioxidant activity with an IC50value of 294 μmol/L.

关 键 词：二酮哌嗪 南极 海洋来源真菌 青霉菌 抗氧化生物活性 

分 类 号：R931.77[医药卫生—生药学]