Study On Secondary Metabolites And Biological Activity Of Two Endogenous Fungi

Two strains of fungi, one of which is Pestalotiopsis podocarpi, the other is Isaria farinosa, are studied in this paper for their metabolites chemical constituents and bioactivity. a variety of separation and purification technology(Silica gel column chromatography preparative thin layer chromatography, gel chromatography, and liquid chromatography) was used, Nineteen compounds were separated and identified in all, in which there are four novel compounds. The new compounds were tested for the biological activity.Pestalotiopsis podocarpi is endophytic fungus from Podocarpus macrophyllus. Thirteen compounds were separated from this strain after liquid fermentation:four alkaloids, induing two new alkaloid, Podocarpiamide (1*) and compound (2*), four sterols Derivatives, three benzene rings and two other types of compounds. Four alkaloid compounds was tested by antitumor activity.The result shows that:Only compound (4) have significant antitumor activity to U25、Hela、A549、MCF-7、HepG2, IC50values were4.4,3.9,10.9,20.9,3.9. The IC50value of compound (4) was not reduce with the growth of time, probably related to the pharmacokinetic.Isaria farinosa is entomogenous fungi from Isaria tenuipes. Six compounds were separated from this strain after liquid fermentation:four series unsaturated ketones compounds, Penostatin L (5*), Penostatin C(6), Penostatin B(7), Penostatin D(8), induing a new compound Penostatin L (5*), a new coumarin compounds (9*), a benzene ring derivatives. Compound (5*-9*) was tested by coagulation target Factore Xa activity anti-Alzheimer ACHE activity, anti-diabetic activity, Obesity target PTP1B protein tyrosine phosphatase inhibitory activity. The result shows that:five compounds display a certain anti-diabetic, obese targets PTP1B protein tyrosine phosphatase inhibitory activity, ICso(ug/ml) values were:4.3,0.12,10-15,5.5,10-15. Compound (6)have a certain anti-diabetes, obesity targets LAR protein tyrosine phosphatase inhibitory activity, IC50(ug/ml) value was15-20. From the result we can known that compound (6) can be potential medicine which have anti-diabetes, obesity targets of PTP1B protein tyrosine phosphatase inhibitory activity.