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In vitro anti-HIV-1...
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Forthal, Donald N
(author)
In vitro anti-HIV-1 activity of salicylidene acylhydrazide compounds
- Article/chapterEnglish2012
Publisher, publication year, extent ...
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Elsevier BV,2012
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printrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:umu-57955
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https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-57955URI
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https://doi.org/10.1016/j.ijantimicag.2012.05.023DOI
Supplementary language notes
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Language:English
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Summary in:English
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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Salicylidene acylhydrazide compounds have been shown to inhibit bacterial pathogens, including Chlamydia and Neisseria gonorrhoeae. If such compounds could also target HIV-1, their potential use as topical microbicides to prevent sexually transmitted infections would be considerable. In this study, the in vitro anti-HIV-1 activity, cytotoxicity and mechanism of action of several salicylidene acylhydrazides were determined. Inhibitory activity was assessed using TZM-bl cells and primary peripheral blood mononuclear cells (PBMCs) as targets for HIV-1 infection. Antiviral activity was measured against cell-free and cell-associated virus and in vaginal fluid and semen simulants. Since the antibacterial activity of salicylidene acylhydrazides is reversible by Fe(2+), the ability of Fe(2+) and other cations to reverse the anti-HIV-1 activity of the compounds was determined. Real-time PCR was also employed to determine the stage affected in the HIV-1 replication cycle. Four compounds with 50% inhibitory concentrations against HIV-1 of 1-7μM were identified. In vitro toxicity varied but was generally limited. Activity was similar against three R5 clade B primary isolates and whether the target for virus replication was TZM-bl cells or PBMCs. Compounds inhibited cell-free and cell-associated virus and were active in vaginal fluid and semen simulants. Fe(2+), but not other cations, reversed the anti-HIV-1 effect. Finally, the inhibitory effect of the compounds occurred at a post-integration step. In conclusion, salicylidene acylhydrazides were identified with in vitro anti-HIV-1 activity in the micromolar range. The activity of these compounds against other sexually transmitted pathogens makes them potential candidates to formulate for use as a broad-spectrum topical genital microbicide.
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Added entries (persons, corporate bodies, meetings, titles ...)
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Phan, Tran B
(author)
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Slepenkin, Anatoly V
(author)
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Landucci, Gary
(author)
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Chu, Hencelyn
(author)
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Elofsson, MikaelUmeå universitet,Kemiska institutionen(Swepub:umu)miel0001
(author)
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Peterson, Ellena
(author)
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Umeå universitetKemiska institutionen
(creator_code:org_t)
Related titles
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In:International Journal of Antimicrobial Agents: Elsevier BV40:4, s. 354-3600924-85791872-7913
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