The New Star Of Staurosporine From Jiaozhou Bay Marine Actinomycetes Found Seven New Structure Compounds

In our group, since 1999, cultural condition optimization, bioactivity screening and chemical tracking were applied into the secondary metabolite research of marine actinomycetes from Jiaozhou Bay. Some bioactive compounds were isolated, including several novel compounds.In this dissertation, 423 marine strains, including 287 actinomycetes, 116 bacteria and 20 fungi, have been isolated from Jiaozhou bay. The activities screening of the actinomycetes showed that the ratio of moderate active strains toward at least 1out of 8 test microbes applied in our experiment was 50%. The chemical screening of the all the actinomycetes indicated us to decide the best strains for further chemical research.38 compounds were isolated from 3 marine stranis, including 7 new structures. I.e. 21 compounds were isolated from marine streptomycetes sp. M518, including 3 new compounds, N-Foramidostaurosporine, 5,7-Dihydroxy-5,6,7,8-tetrahydro-1H-azocin-2-one and Selina-4(14),7(11)-diene-8,9-diol, and one new rearrangemental derivative, Trimer 3. 5,7-Dihydroxy-5,6,7,8-tetrahydro-1H-azocin-2-one was a new skeleton natural compound. From analysis of this compound and its rearrangemental products, a possible rearrangmental course of this kind of compound was suggested. 10 compounds were isolated from marine streptomyces sp. M491, including 3 new sesquiterpenes, 10α,11-dihydroxyamorph-4-ene, 10α-14-dihydroxyamorph-4-en-3-one and 5α,10α,11-Triydroxyamorphan-3-one, and 1 known sesquiterpene, 10-Hydroxyamorph-4-en-3-one was first isolated from microorganisms. From marine actinomycetes M311, 7 known compounds were identified.The new compound, N-Formamidostaurosporine, had extraordinary activities toward 37 human cancer cell lines, with the average IC50, IC70, IC90 respectively 0.016, 0.171, and 2.352μg/ml. It showed an antitumor selective rate 27%. Furthermore, staurosporine and its derivatives were found to have anti micro-algae activities for the first time.Based on the morphological, physiological characters and 16S rDNA analysis, the taxonomies of the new compounds producer M518 and M491, were investigated. Phylogenetic analysis showed that M518 and M491 were homologous with streptomyces roseoflavus and streptomyces thermolineatus respectively.