Harzianoic acids A and B, new natural scaffolds with inhibitory effects against hepatitis C virus

April 9, 2019

Title

Harzianoic acids A and B, new natural scaffolds with inhibitory effects against hepatitis C virus

Author

Bo Li, Li Li, Zonggen Peng, Dong Liu, Longlong Si, Jing Wang, Bochuan Yuan, Jian Huang, Peter Proksch, Wenhan Lin

Year

2018

Journal

Bioorganic & Medicinal Chemistry

Abstract

Two new sesquiterpene-based analogues, namely harzianoic acids A (1) and B (2), were isolated from a sponge-associated fungus Trichoderma harzianum. Their structures were determined on the basis of the extensive spectroscopic analyses in association with the ECD data for the configurational assignment. Harzianoic acids A and B were structurally characterized as a sesquiterpene and a norsesquiterpene with a cyclobutane nucleus, which is uncommonly found from nature. Both compounds exhibited the inhibitory activity to reduce the HCV RNA levels with low cytotoxicity. The preliminary investigation of the mode of action revealed that the compounds blocked the entry step in the HCV life cycle, while the viral E1/E2 and the host cell CD81 were the potential target proteins.

Instrument

J-815

Keywords

Circular dichroism, Absolute configuration, Natural products, Medicinal, Pharmaceutical