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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。
Aim To study the fermentative product of HCCB03890 rice, and to conduct chemical research and activity analysis. Methods The compounds were separated and purified by silica gel and preparative chromatography. The compounds were identified by mass spectrometry and nuclear magnetic resonance spectroscopy. The antibacterial activity was determined by the plate puncturing method. The MTT assay was used to determine the inhibitory activity of tumor cells. Enzyme activity to characterize. As a result, six compounds were isolated from the ethyl acetate fraction. The results of spectral analysis showed that N-acetyltyramine (1), schizostatin (2), piliformic acid (3), rapeseed sterol (4), dankasterone (5) and demethylincisterol (6). Compound 3 has a certain inhibition of Gram-positive bacteria activity; Compounds 4 to 6 have cytotoxicity and HIV inhibitory activity, of which compounds 5 and 6 have a strong inhibitory activity of HIV-1, IC50 were 0.4 and 0.9μg · m L -1. Conclusion Compounds 2, 4 and 5 were isolated from the fungi for the first time, and compounds 4 and 5 were isolated from terrestrial microorganisms for the first time.