Metabolites of endophytic fungus Xylaria sp. with biological activities / 中国药学杂志

ABSTRACT

OB JECTIVE: 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 performance 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 MTT method, and anti-HIV activities were measured by using a firefly luciferase assay system. RESULTS: Six compounds were isolated and identified as TV-acetyltyra-mine(1), schizostatin(2), piliformic acid(3), stigmast-5,22-dien-3-ol(4), dankasterone(5) and demethylincisterol(6) on the basis 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 IC50 values of 0.4 and 0.9 μg · mL, respectively. 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.