植物内生真菌炭角菌属HCCB03890代谢产物及生物活性的研究  

Metabolites of Endophytic Fungus Xylaria sp. with Biological Activities

作　　者：金一平[1] 杨志钧[2,3] 罗敏玉[2] 

机构地区：[1]浙江医药股份有限公司,浙江绍兴312366 [2]上海来益生物药物研究开发中心,上海200240 [3]上海交通大学药学院,上海200040

出　　处：《中国药学杂志》2015年第21期1853-1856,共4页Chinese Pharmaceutical Journal

摘　　要：目的为了研究炭角菌属真菌HCCB03890大米发酵产物,对其进行了化学研究和活性分析。方法利用硅胶和制备色谱技术进行分离纯化,化合物采用质谱和核磁光谱进行结构鉴定;抗菌活性采用平板打孔法,肿瘤细胞抑制活性采用MTT法,抗HIV活性采用抑制假型病毒携带报告基因荧光素酶活性来表征。结果从其乙酸乙酯浸提部分分离得到6个化合物。经波谱数据分析,鉴定为N-acetyltyramine（1）、schizostatin（2）、piliformic acid（3）、油菜甾醇（4）、dankasterone（5）和demethylincisterol（6）。化合物3有一定的抑制革兰氏阳性菌活性;化合物4~6具有细胞毒性和HIV抑制活性,其中化合物5和6具有很强的HIV-1抑制活性,IC50分别为0.4和0.9μg·m L-1。结论化合物2、4和5均为首次从该属真菌中分离得到,而且化合物4和5首次从陆生微生物中分离得到。OBJECTIVE To investigate the chemical constituents from the fermented rice substrate of endophytic fungus Xylaria sp. HCCB03890. METHODS The compounds were isolated with silica gel column chromatography and reversed-phase high perform- ance liquid chromatography. The structures of these compounds were elucidated through MS and NMR spectroscopic analysis. The anti- microbes activities were evaluated by disk diffusion method, cytotoxic activities were determined by MTI＂ method, and anti-HIV activi- ties were measured by using a firefly luciferase assay system. RESULTS Six compounds were isolated and identified as N-acetyhyra- mine （ 1 ）, schizostatin （ 2 ）, piliformic acid （ 3 ）, stigmast-5,22 -dien-3-ol （4）, dankasterone （ 5 ） and demethylincisterol （ 6 ） on the ba- sis of spectroscopic data analyses. Compound 3 showed moderate anti-microbial activity. Compounds 4 - 6 exhibited cytotoxic and anti- HIV activities, especially, and compund 5 and 6 showed significant anti-HIV activities with ICs0 values of 0. 4 and 0. 9μg· mL- 1, re- spectively. CONCLUSION Compounds 2, 5 and 6 were for the first time isolated from Xylaria sp. , moreover, 5 and 6 are for the first time found in terrestrial microbes.

关 键 词：炭角菌属HCCB03890 细胞毒性 HIV抑制活性 

分 类 号：R284[医药卫生—中药学]