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Mar. Drugs 2016, 14(10), 190; doi:10.3390/md14100190

Different Culture Metabolites of the Red Sea Fungus Fusarium equiseti Optimize the Inhibition of Hepatitis C Virus NS3/4A Protease (HCV PR)

1
Marine Chemistry Department, Faculty of Marine sciences, King Abdulaziz University, P.O. Box 80207, Jeddah 21589, Saudi Arabia
2
Pharmacognosy Department, National Research Centre, Dokki 12622, Cairo, Egypt
*
Author to whom correspondence should be addressed.
Academic Editor: Sadanandan E. Velu
Received: 30 August 2016 / Revised: 29 September 2016 / Accepted: 11 October 2016 / Published: 20 October 2016
(This article belongs to the Special Issue Enzyme Inhibitors of Marine Origin)
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Abstract

The endophytic fungus Fusarium equiseti was isolated from the brown alga Padina pavonica, collected from the Red Sea. The fungus was identified by its morphology and 18S rDNA. Cultivation of this fungal strain in biomalt-peptone medium led to isolation of 12 known metabolites of diketopeprazines and anthraquinones. The organic extract and isolated compounds were screened for their inhibition of hepatitis C virus NS3/4A protease (HCV PR). As a result, the fungal metabolites showed inhibition of HCV protease (IC50 from 19 to 77 μM), and the fungus was subjected to culture on Czapek’s (Cz) media, with a yield of nine metabolites with potent HCV protease inhibition ranging from IC50 10 to 37 μM. The Cz culture extract exhibited high-level inhibition of HCV protease (IC50 27.6 μg/mL) compared to the biomalt culture extract (IC50 56 μg/mL), and the most potent HCV PR isolated compound (Griseoxanthone C, IC50 19.8 μM) from the bio-malt culture extract showed less of an inhibitory effect compared to isolated ω-hydroxyemodin (IC50 10.7 μM) from the optimized Cz culture extract. Both HCV PR active inhibitors ω-hydroxyemodin and griseoxanthone C were considered as the lowest selective safe constituents against Trypsin inhibitory effect with IC50 48.5 and 51.3 μM, respectively. View Full-Text
Keywords: brown alga; Padina pavonica; Red Sea; Fusarium equiseti; HCV protease brown alga; Padina pavonica; Red Sea; Fusarium equiseti; HCV protease
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MDPI and ACS Style

Hawas, U.W.; Al-Farawati, R.; Abou El-Kassem, L.T.; Turki, A.J. Different Culture Metabolites of the Red Sea Fungus Fusarium equiseti Optimize the Inhibition of Hepatitis C Virus NS3/4A Protease (HCV PR). Mar. Drugs 2016, 14, 190.

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