The Secondary Metabolites From Penicillium Sp.and Aspergillus Versicolor Collected From The Bohai Sea

Marine-derived fungi Penicillium and Aspergillus are very common strains and their secondary metabolites are abundant.Polyketones,alkaloids and anthraquinones are the three major secondary metabolites produced by them.In this paper,three kinds of secondary metabolites as the main research object were isolated from Penicillium sp.XL-01 and Aspergillus versicolor CF-09-9 which were collected from the Bohai Sea.The HPLC of the two fungi were obtained by several small-scale fermentations.It was found that the two fungi were rich in these three kinds of secondary metabolites.Therefore,the two fungi were selected for large-scale fermentation culture.In order to find the three kinds of secondary metabolites with new structure and good biological activity,we study their structure by various modern separation methods and test their biological activities.In this study,31 compounds were isolated and identified from two fungi from the Bohai Sea,1–22 were isolated from Penicillium sp.XL-01 and 23–31 were isolated from Aspergillus versicolor CF-09-9.Among them,1 and 2 are new compounds.All compounds are classified into three categories:1–5 belongs to linear polyketones,24–25 belongs to non-linear polyketones;6–20,26 and 27 belong to alkaloids,which can be subdivided into indole-dione-piperazines,peptides,lactams,etc.21 and 22 belong to mixed terpenoids,28–31belong to sesquiterpenes.Among them,the absolute configuration of 1 was determined by ECD calculation method.The results of antimicrobial activity test of these compounds showed that 10 had strong activity against five kinds of bacteria,in which had strong activity against B.cereus?MIC value was 0.20?g/mL?;20 had moderate activity against P.aeruginosa with MIC value of6.25?g/mL;24 and 25 also had moderate activity against B.cereus with MIC value of 6.25?g/mL.27 had inhibitory effect on E.coli?MIC value was 5.0?g/mL?.The results of antineoplastic activity test showed that 1,3 and 5 had strong inhibitory activity to MGG-803,MDA-MB-231,A-5493,MCF-7 and Hela with IC₅₀ values of 1.84,1.91,2.50,3.80 and 3.91?M,respectively.The IC₅₀ values of new compound 1 on human gastric cancer cell MGC-803only were 0.96?M lower than that of positive control cisplatin.In summary,three kinds of secondary metabolites,polyketones,alkaloids and terpenoids,were isolated from the fungi Penicillium sp.XL-01 and Aspergills versicolor CF-09-9 which were collected from the Bohai Sea.Biological activity tests showed that the new compounds belonging to verrucosidin had good antineoplastic activity,and this finding has great significance for the study of anticarcinogens.