In vitro anti-HIV-1 activity of salicylidene acylhydrazide compounds

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Forthal, Donald N (författare)

In vitro anti-HIV-1 activity of salicylidene acylhydrazide compounds

Artikel/kapitelEngelska2012

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Elsevier BV,2012
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Nummerbeteckningar

LIBRIS-ID:oai:DiVA.org:umu-57955
https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-57955URI
https://doi.org/10.1016/j.ijantimicag.2012.05.023DOI

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Språk:engelska
Sammanfattning på:engelska

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Ämneskategori:ref swepub-contenttype
Ämneskategori:art swepub-publicationtype

Anmärkningar

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.

Ämnesord och genrebeteckningar

NATURVETENSKAP Kemi hsv//swe
NATURAL SCIENCES Chemical Sciences hsv//eng
Salicylidene acylhydrazides
HIV
Microbicide
Iron chelation

Biuppslag (personer, institutioner, konferenser, titlar ...)

Phan, Tran B (författare)
Slepenkin, Anatoly V (författare)
Landucci, Gary (författare)
Chu, Hencelyn (författare)
Elofsson, MikaelUmeå universitet,Kemiska institutionen(Swepub:umu)miel0001 (författare)
Peterson, Ellena (författare)
Umeå universitetKemiska institutionen (creator_code:org_t)

Sammanhörande titlar

Ingår i:International Journal of Antimicrobial Agents: Elsevier BV40:4, s. 354-3600924-85791872-7913

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Av författaren/redakt...: Forthal, Donald ...; Phan, Tran B; Slepenkin, Anato ...; Landucci, Gary; Chu, Hencelyn; Elofsson, Mikael; visa fler...; Peterson, Ellena; visa färre...

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NATURVETENSKAP: NATURVETENSKAP; och Kemi

Artiklar i publikationen: International Jo ...

Av lärosätet: Umeå universitet

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