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      Flavonoid baicalin inhibits HIV-1 infection at the level of viral entry.

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          Abstract

          Baicalin (BA) is a flavonoid compound purified from medicinal plant Scutellaria baicalensis Georgi and has been shown to possess anti-inflammatory and anti-HIV-1 activities. In an effort to elucidate the mechanism of the anti-inflammatory effect of BA, we recently found that this flavonoid compound was able to form complexes with selected chemokines and attenuated their capacity to bind and activate receptors on the cell surface. These observations prompted us to investigate whether BA could inhibit HIV-1 infection by interfering with viral entry, a process known to involve interaction between HIV-1 envelope proteins and the cellular CD4 and chemokine receptors. We found that BA at the noncytotoxic concentrations, inhibited both T cell tropic (X4) and monocyte tropic (R5) HIV-1 Env protein mediated fusion with cells expressing CD4/CXCR4 or CD4/CCR5. Furthermore, presence of BA at the initial stage of HIV-1 viral adsorption blocked the replication of HIV-1 early strong stop DNA in cells. Since BA did not inhibit binding of HIV-1 gp120 to CD4, we propose that BA may interfere with the interaction of HIV-1 Env with chemokine coreceptors and block HIV-1 entry of target cells. Therefore, BA can be used as a basis for developing novel anti-HIV-1 agents.

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          Author and article information

          Journal
          Biochem Biophys Res Commun
          Biochemical and biophysical research communications
          Elsevier BV
          0006-291X
          0006-291X
          Sep 24 2000
          : 276
          : 2
          Affiliations
          [1 ] Laboratory of Antiviral Drug Mechanism, National Cancer Institute-Frederick Cancer Development Center, Maryland 21702, USA. bqli@mail.ncifcrf.gov
          Article
          S0006-291X(00)93485-5
          10.1006/bbrc.2000.3485
          11027509
          feeb272d-f278-4d02-8b46-86bdfafa06f2
          History

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