Metabolites Of Paecilomyces Lilacinus ZBY-1from Deep-sea Water And Their Antitumor Activity

Abstract:Marine natural products has become to be an important resource of drug lead compounds, and the products of fungus, especially fungus from deep sea water or sedment is taking increasing concern. In this study,16fungal strains isolated from various sea area were screened for their antitumor and antifungal activities. Concequently,5of the16fungal strains had the inhibition rates over50%on K562cell at100μg/ml of fermentation product.The antitumor-active strain Paecilomyces lilacinus ZBY-1was chosen as the objective strain for antitumor products from its large scale fermentation, and by various means of chromatography and recrystallization,21compounds were isolated thereby. The chemical structures of the21metabolites were conducted with modern spectroscopic and chemical methods, and identified to be five steroids (1～5), one sphingosine analog (6) and its artificial hydrochlorate (7), four cerebrosides (8～11), two DGTSs (12and13), four fatty acids (14～17), and another four compounds (18～21). The antitumor activities of compounds1～21were assyed by MTT method using four human cancer cell lines. Compound1～3showed moderate inhibitory activities to K562, HL-60, MCF-7and BGC-823cells, with the IC50ranging from9.5～59.6μg/ml; compound6and7displayed significant cytotoxic activities on the four cancer cell lines, with the IC5o ranging from0.39～10μg/ml; while the other compounds showed weak or no antitumor activity.In summary,16fungal strains from deap sea were screened for their antitumor activity, and5of them showed positive result. The Paecilomyces lilacinus ZBY-1, one of the active strains, was studied for its antitumor products, and eventually the main active compound paecilaminol (6) was clarified, and steroids1～3also played a role in the antitumor activity of ZBY-1. The metabolite of Paecilomyces lilacinus isolated from deap sea was studied for the first time in this paper. Compounds1～21were isolated from the metabolites of Paecilomyces lilacinus,1,3,12,13and18～21were isolated from the genus Paecilomyces, and3further from the fungi, all for the first time, respectively. These results will provide solid foundation for utilizing Paecilomyces lilacinus.16Figures,8Tables,103References...