Abstract |
In Gordts et al. (2015), we have shown that lignosulfonic acid, a commercially available lignin derivative, possesses broad antiviral activity against human immunodeficiency virus (HIV) and Herpes simplex virus (HSV) by preventing viral entry into susceptible target cells. Because of the interesting safety profile as potential microbicide, we now determined the antiviral activity of a series of lignosulfonates in order to understand better which molecular features can contribute to their antiviral activity. Here, 24 structurally different lignosulfonates were evaluated for their capacity to inhibit HIV and HSV transmission and replication in various cellular assays. These derivatives differ in origin (hardwood or softwood), counter-ion used during sulphite processing (Na+, Ca2+, or NH4+), sulphur content, carboxylic acid percentage, and molecular weight fraction, which allowed to determine structure-activity relationships. We demonstrate that the broad antiviral activity of lignosulfonates is mainly dependent on their molecular weight and that their mechanism of action is based on interactions with the viral envelope glycoproteins. This makes the lignosulfonates a potential low-cost microbicide that protects women from sexual HIV and HSV transmission and thus prevents life-long infection.
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Authors | Merel Oeyen, Sam Noppen, Emiel Vanhulle, Sandra Claes, Bernt O Myrvold, Kurt Vermeire, Dominique Schols |
Journal | Virus research
(Virus Res)
Vol. 274
Pg. 197760
(12 2019)
ISSN: 1872-7492 [Electronic] Netherlands |
PMID | 31618614
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2019 Elsevier B.V. All rights reserved. |
Chemical References |
- Antiviral Agents
- Viral Envelope Proteins
- lignosulfuric acid
- Lignin
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Topics |
- Animals
- Antiviral Agents
(chemistry, pharmacology)
- Cell Line
- HIV
(drug effects)
- HIV Infections
(prevention & control, transmission)
- Herpes Simplex
(prevention & control, transmission)
- Herpesvirus 2, Human
(drug effects)
- Humans
- Inhibitory Concentration 50
- Lignin
(analogs & derivatives, chemistry, pharmacology)
- Membrane Fusion
(drug effects)
- Molecular Structure
- Molecular Weight
- Viral Envelope Proteins
(chemistry)
- Virus Internalization
(drug effects)
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