Broad-Spectrum Antiviral Natural Products from the Marine-Derived Penicillium sp. IMB17-046.

Jiao Li,Jia Jia,Xiaomeng Hao,Yujia Wang,Hongkai Bi,Shan Cen,Chunling Xiao,Zonggen Peng,Maoluo Gan,Shasha Li,Yan Guan

doi:10.3390/molecules24152821

Abstract

A new pyrazine derivative, trypilepyrazinol (1), a new α-pyrone polyketide, (+)-neocitreoviridin (2), and a new ergostane analogue, 3β-hydroxyergosta-8,14,24(28)-trien-7-one (3), were isolated and characterized along with five known compounds from the marine-derived fungus Penicillium sp. IMB17-046. The structures of these new compounds were determined using spectroscopic data analyses (HRESIMS, 1D- and 2D-NMR), X-ray crystallography analysis, and TDDFT ECD calculation. Compounds 1 and 3 exhibited broad-spectrum antiviral activities against different types of viruses, including human immunodeficiency virus (HIV), hepatitis C virus (HCV), and influenza A virus (IAV), with IC50 values ranging from 0.5 to 7.7 μM. Compounds 1 and 2 showed antibacterial activities against Helicobacter pylori, a causative pathogen of various gastric diseases, with minimum inhibitory concentration (MIC) values of 1–16 μg/mL.

Highlights

Viruses such as the human immunodeficiency virus (HIV), influenza virus, and hepatitis B andC viruses (HBV and hepatitis C virus (HCV)) are great global threats to public health
Health Organization (WHO) reports, 36.7 million people were living with HIV in 2015, among which approximately 2.7 million and 2.3 million had a chronic HBV and HCV coinfection, respectively [1,2]
It is estimated that hepatitis viruses caused 1.34 million deaths in 2015 while influenza viruses are responsible for 250,000 to 500,000 death globally every year

Summary

Introduction

Viruses such as the human immunodeficiency virus (HIV), influenza virus, and hepatitis B and. C viruses (HBV and HCV) are great global threats to public health. Health Organization (WHO) reports, 36.7 million people were living with HIV in 2015, among which approximately 2.7 million and 2.3 million had a chronic HBV and HCV coinfection, respectively [1,2]. It is estimated that hepatitis viruses caused 1.34 million deaths in 2015 while influenza viruses are responsible for 250,000 to 500,000 death globally every year. Despite the great achievements made in antiviral drug discovery during the past 50 years, there is still no effective antiviral drug for over 200 infectious diseases [2]. Broad-spectrum antiviral drugs are needed to combat multiple viral infectious diseases since most of the current antiviral drugs are effective to only certain viral strains [2]

Methods

Results

Conclusion