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Candidate sulfonated and sulfated topical microbicides: comparison of anti-human immunodeficiency virus activities and mechanisms of action.

Publication ,  Journal Article
Scordi-Bello, IA; Mosoian, A; He, C; Chen, Y; Cheng, Y; Jarvis, GA; Keller, MJ; Hogarty, K; Waller, DP; Profy, AT; Herold, BC; Klotman, ME
Published in: Antimicrob Agents Chemother
September 2005

Poly(styrene 4-sulfonate), cellulose sulfate, polymethylenehydroquinone, and PRO 2000 are sulfated or sulfonated polymers (SPs) under development as topical microbicides. They are presumed to work through similar mechanisms of action, although to date there has been no extensive comparison of their anti-human immunodeficiency virus activities. To determine whether any of these candidate microbicides offers a potential advantage, their in vitro activities, mechanisms of action, stabilities in biological secretions, and toxicities were compared. All four compounds were found to be active against X4, R5, and dualtropic primary isolates and against X4 and R5 laboratory-adapted strains in CD4+ T cells, macrophages, and single-coreceptor cell lines. Our single-cycle experiments using pseudotyped virus suggest that all four SPs function at the binding and entry stages of the viral life cycle but differ in degree of postentry effect. Surface plasmon resonance analyses demonstrate that SPs bind to X4 and R5 monomeric glycoprotein 120 with similar high binding affinities. When mixed with cervicovaginal lavage fluid, SPs maintain inhibitory activity at concentrations achievable in formulations.

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Published In

Antimicrob Agents Chemother

DOI

ISSN

0066-4804

Publication Date

September 2005

Volume

49

Issue

9

Start / End Page

3607 / 3615

Location

United States

Related Subject Headings

  • Vagina
  • Surface Plasmon Resonance
  • Sulfonic Acids
  • Sulfates
  • Polymers
  • Microbiology
  • Macrophages
  • Indicators and Reagents
  • Humans
  • HIV-1
 

Citation

APA
Chicago
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Scordi-Bello, I. A., Mosoian, A., He, C., Chen, Y., Cheng, Y., Jarvis, G. A., … Klotman, M. E. (2005). Candidate sulfonated and sulfated topical microbicides: comparison of anti-human immunodeficiency virus activities and mechanisms of action. Antimicrob Agents Chemother, 49(9), 3607–3615. https://doi.org/10.1128/AAC.49.9.3607-3615.2005
Scordi-Bello, Irini A., Arevik Mosoian, Cejiang He, Yiban Chen, Yang Cheng, Gary A. Jarvis, Marla J. Keller, et al. “Candidate sulfonated and sulfated topical microbicides: comparison of anti-human immunodeficiency virus activities and mechanisms of action.Antimicrob Agents Chemother 49, no. 9 (September 2005): 3607–15. https://doi.org/10.1128/AAC.49.9.3607-3615.2005.
Scordi-Bello IA, Mosoian A, He C, Chen Y, Cheng Y, Jarvis GA, et al. Candidate sulfonated and sulfated topical microbicides: comparison of anti-human immunodeficiency virus activities and mechanisms of action. Antimicrob Agents Chemother. 2005 Sep;49(9):3607–15.
Scordi-Bello, Irini A., et al. “Candidate sulfonated and sulfated topical microbicides: comparison of anti-human immunodeficiency virus activities and mechanisms of action.Antimicrob Agents Chemother, vol. 49, no. 9, Sept. 2005, pp. 3607–15. Pubmed, doi:10.1128/AAC.49.9.3607-3615.2005.
Scordi-Bello IA, Mosoian A, He C, Chen Y, Cheng Y, Jarvis GA, Keller MJ, Hogarty K, Waller DP, Profy AT, Herold BC, Klotman ME. Candidate sulfonated and sulfated topical microbicides: comparison of anti-human immunodeficiency virus activities and mechanisms of action. Antimicrob Agents Chemother. 2005 Sep;49(9):3607–3615.

Published In

Antimicrob Agents Chemother

DOI

ISSN

0066-4804

Publication Date

September 2005

Volume

49

Issue

9

Start / End Page

3607 / 3615

Location

United States

Related Subject Headings

  • Vagina
  • Surface Plasmon Resonance
  • Sulfonic Acids
  • Sulfates
  • Polymers
  • Microbiology
  • Macrophages
  • Indicators and Reagents
  • Humans
  • HIV-1