Anti-HCV protease of diketopiperazines produced by the Red Sea sponge-associated fungus Aspergillus versicolor

Eman Ahmed, Mostafa Rateb, L.T. Abou El-Kassem, Usama Hawas

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)
120 Downloads (Pure)

Abstract

Hepatitis C virus (HCV) infection is a global problem due to the difficulties in developing a protective vaccine. In this work, we demonstrated that the ethyl acetate extract of the endophytic fungus Aspergillus versicolor exhibited significant activity against HCV NS3/4A protease with IC50 value of 30 μg/mL. The fungus was isolated from the Red Sea black sponge Spongia officinalis and identified by its morphology and 18S rDNA. Large-scale fermentation of the fungus followed by chromatographic purification with silica gel, Sephadex LH-20 and semipreparative HPLC of the active extract led to isolation of some known metabolites related to cyclodipeptides and the so-called diketopiperazines (DKPs). The DKP, cyclo(L-Tyr-L-Pro), displayed strong effect as HCV protease inhibitor with IC50 value of 8.2 μg/mL. A computational docking study of cyclo(L-Tyr-L-Pro) against HCV protease was used to formulate a hypothetical mechanism for the inhibitory activity of the active compound on the tested enzyme.

Original languageEnglish
Pages (from-to)101-106
JournalApplied Biochemistry and Microbiology
Volume53
Issue number1
DOIs
Publication statusPublished - 1 Jan 2017

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