Lignosulfonic acid exhibits broadly anti-HIV-1 activity--potential as a microbicide candidate for the prevention of HIV-1 sexual transmission.

PloS One
Min QiuZhiwei Wu

Abstract

Some secondary metabolites from plants show to have potent inhibitory activities against microbial pathogens, such as human immunodeficiency virus (HIV), herpes simplex virus (HSV), Treponema pallidum, Neisseria gonorrhoeae, etc. Here we report that lignosulfonic acid (LSA), a polymeric lignin derivative, exhibits potent and broad activity against HIV-1 isolates of diverse subtypes including two North America strains and a number of Chinese clinical isolates values ranging from 21.4 to 633 nM. Distinct from other polyanions, LSA functions as an entry inhibitor with multiple targets on viral gp120 as well as on host receptor CD4 and co-receptors CCR5/CXCR4. LSA blocks viral entry as determined by time-of-drug addiction and cell-cell fusion assays. Moreover, LSA inhibits CD4-gp120 interaction by blocking the binding of antibodies specific for CD4-binding sites (CD4bs) and for the V3 loop of gp120. Similarly, LSA interacts with CCR5 and CXCR4 via its inhibition of specific anti-CCR5 and anti-CXCR4 antibodies, respectively. Interestingly, the combination of LSA with AZT and Nevirapine exhibits synergism in viral inhibition. For the purpose of microbicide development, LSA displays low in vitro cytotoxicity to human genital tract epi...Continue Reading

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Citations

Feb 16, 2016·Journal of Nutritional Science and Vitaminology·Yasushi HasegawaSatoshi Kawaminami
May 4, 2015·Biochemical and Biophysical Research Communications·Koji MatsuhisaKiyohito Yagi
Jul 8, 2016·Asian-Australasian Journal of Animal Sciences·Yasushi HasegawaSatoshi Kawaminami
Jun 8, 2017·International Journal of Molecular Sciences·Maria Pilar Vinardell, Montserrat Mitjans
Jun 14, 2018·ChemSusChem·Khatereh Bahrpaima, Pedram Fatehi
Sep 25, 2019·Critical Reviews in Food Science and Nutrition·Jianming TaoGuohua Zhao

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Methods Mentioned

BETA
ELISA
FACS
enzyme-linked immunosorbent assay
PCR

Software Mentioned

CalcuSyn
Modeller
Discovery Studio
Autodock
VMD
ChemOffice Ultra

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