| The unique and diverse marine microorganisms is the ideal resources of new material, medicine, energy. The microbial species according to the statistics, the marine environment contains is very rich, including the eukaryotic microorganism, bacteria, archaebacteria and virus, about 2-10 billion. In recent years, a growing number of scientists devoted to the study of marine microorganism resources. In order to get unique marine microorganisms, we will look to the high salt, high pressure, oligotrophic, low temperature extreme environment and deep or far sea area. We collected nine sponges, and coral,6 mud sample, a lichen, a coral, two water samples. 4 deep sea mud. a total of 23 samples from the xisha islands, the South Pole, the Indian Ocean, the south Atlantic far sea area. Through the processing of these samples and microorganism separation,124 strains of microorganisms were separated, including 95 strains of fungi.29 strains of actinomycetes. By adopting the combination of the biological activity and chemical laboratory screening method,4 genius strains were selected, one fungi strains OUCMDZ-3839 was identified as Penicillium sclerotiorum. The optimal fermentation conditions were determined through the regulation of the salinity and culture.Four new azaphilones,1-4, along with other 12 known azaphilones, were isolated from the sponge-derived fungus Penicillhim sclerotiorum OUCMDZ-3839 by silica gel column chromatography, gel column chromatography HPLC and so on means. The structures of these compounds were determined using NMR, MS, optical, IR, UV, CD, X-ray and chemical method, they were all belong to azaphilones class.For this kind of compounds, a wide range of biological activity were evaluated, including antimicrobial activity, antiviral activity, antitumor activity, antidiabetic activity. Results show that these compounds had no antimicrobial activity; compounds 5,7,10,12,13,14 and 16 had similar anti-H1N1 activity with positive drug Ribavirin; according to the results of antitumor evaluation, these compounds showed weak inhibitory activity on MCF-7, K562, A549, HCT-116 and hela:11 and 14 performed significant resistance to a-glycosidase, far higher than the positive control acarbose.Azaphilone compounds have various biological activity, but its resistance against H1N1 activity and a-glycosidase activity were found for the first. The separation of these 16 azaphilone compounds rich the chemical and biological diversity. |