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Depsides: lichen metabolites active against hepatitis C virus
Thi Huyen Vu1, Anne-Cécile Le Lamer2, Claudia Lalli1
1CNRS, UMR-6226, Institut des Sciences Chimiques de Rennes (ISCR), Rennes, France; Université de Rennes 1, Rennes, France.
Plos One
|March 21, 2015
Summary
Lichen compounds, including atranorin derivatives, show activity against hepatitis C virus (HCV). Atranorin and synthesized analogs inhibit viral entry and replication, offering potential new antiviral strategies.
Area of Science:
- Phytochemistry
- Virology
- Medicinal Chemistry
Background:
- The lichen Stereocaulon evolutum produces atranorin derivatives.
- Pilot studies indicated atranorin's potential to interfere with hepatitis C virus (HCV) lifecycle.
Purpose of the Study:
- To isolate and characterize atranorin derivatives from S. evolutum.
- To evaluate the antiviral activity of these compounds against HCV.
- To synthesize analogs to explore structure-activity relationships.
Main Methods:
- Phytochemical isolation and structure elucidation of natural products.
- Synthesis of atranorin analogs.
- In vitro antiviral assays against HCV, including viral entry and replication inhibition studies.
Main Results:
- Eight compounds were isolated, including a novel derivative.
- Two synthetic analogs were prepared.
- Most compounds exhibited anti-HCV activity (IC50: 10–70 µM), with depsides being more potent than monoaromatic phenols.
- Atranorin inhibited viral entry, while synthetic analogs interfered with viral replication.
Conclusions:
- Atranorin derivatives from S. evolutum possess significant anti-HCV activity.
- Structural modifications influence the mechanism of action, targeting either viral entry or replication.
- These findings highlight the therapeutic potential of lichen-derived compounds for HCV treatment.
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