Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Anti-HIV-1 activity of calanolides used in combination with other mechanistically diverse inhibitors of HIV-1 replication
Autore:
Buckheit, RW; Russell, JD; Xu, ZQ; Flavin, M;
Indirizzi:
So Res Inst, Infect Dis Res Dept, Frederick, MD 21701 USA So Res Inst Frederick MD USA 21701 Dis Res Dept, Frederick, MD 21701 USA Sarawak MediChem Pharmaceut, Lemont, IL USA Sarawak MediChem Pharmaceut Lemont IL USA hem Pharmaceut, Lemont, IL USA
Titolo Testata:
ANTIVIRAL CHEMISTRY & CHEMOTHERAPY
fascicolo: 5, volume: 11, anno: 2000,
pagine: 321 - 327
SICI:
0956-3202(200009)11:5<321:AAOCUI>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
IMMUNODEFICIENCY-VIRUS TYPE-1; REVERSE-TRANSCRIPTASE INHIBITORS; INFECTION; PLASMA; MODEL;
Keywords:
HIV-1; antivirals; NNRTIs;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Buckheit, RW So Res Inst, Infect Dis Res Dept, 431 Aviat Way, Frederick, MD 21701 USA So Res Inst 431 Aviat Way Frederick MD USA 21701 MD 21701 USA
Citazione:
R.W. Buckheit et al., "Anti-HIV-1 activity of calanolides used in combination with other mechanistically diverse inhibitors of HIV-1 replication", ANTIVIR CHE, 11(5), 2000, pp. 321-327

Abstract

The natural product (+)-calanolide A, a unique nonnucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 replication, is currently being evaluated in clinical trials in the USA. (+)-Calanolide A, the congeners costatolide and dihydrocostatolide, and (+)-2-oxo(+)-calanolide A, were evaluated incombination with a variety of mechanically diverse inhibitors of HIV replication to define the efficacy and cellular toxicity of potential clinical drug combinations. These assays should be useful in prioritizing the use of different combination drug strategies in a clinical setting. The calanolides exhibited synergistic antiviral interactions with other nucleoside and non-nucleoside reverse transcriptase inhibitors and protease inhibitors. Additive interactions were also observed when the calanolides were used with representative compounds from each of these classes of inhibitors. No evidence of either combination toxicity or antagonistic antiviral activity was detected with any of the tested compounds. The combination antiviral efficacy of three-drug combinations involving the calanolides, and the efficacy of two- and three-drug combinations using a (+)-calanolide A-resistant challenge virus (bearing the T1391 amino acid change in the reverse transcriptase),was also evaluated in vitro. These assays suggest that the best combination of agents based on in vitro anti-HIV assay results would include the calanolides in combination with lamivudine and nelfinavir, since this was the only three-drug combination exhibiting a significant level of synergy. Combination assays with the (+)-calanolide A-resistant strain yielded identical results as seen with the wild-type virus, although the concentration of thecalanolides had to be increased.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/09/20 alle ore 08:14:53