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2.
Antiviral Res ; 61(1): 57-62, 2004 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-14670594

RESUMEN

We investigated whether crude hop extracts and purified hop components representing every major chemical class of hop compound have antiviral activity. These hop constituents were tested for antiviral activity against bovine viral diarrhea virus (BVDV) as a surrogate model of hepatitis C virus (HCV), human immunodeficiency virus (HIV), influenza A virus (FLU-A), influenza B virus (FLU-B), rhinovirus (Rhino), respiratory syncytial virus (RSV), yellow fever virus (YFV), cytomegalovirus (CMV), hepatitis B virus (HBV), and herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2). The extracts all failed to prevent the replication of HIV, FLU-A, FLU-B, RSV and YFV. A xanthohumol-enriched hop extract displayed a weak to moderate antiviral activity against BVDV (therapeutic index (TI)=6.0), HSV-2 (TI=>5.3), Rhino (TI=4.0) and HSV-1 (TI=>1.9) with IC(50) values in the low microg/ml range. Pure iso-alpha-acids demonstrated low to moderate antiviral activity against both BVDV (TI=9.1) and CMV (TI=4.2) with IC(50) values in the low microg/ml range. No antiviral activity was detected using beta-acids or a hop oil extract. Ultra-pure preparations (>99% pure) were used to show that xanthohumol accounted for the antiviral activity observed in the xanthohumol-enriched hop extract against BVDV, HSV-1 and HSV-2. Xanthohumol was found to be a more potent antiviral agent against these viruses than the isomer iso-xanthohumol. With Rhino, the opposite trend was observed with iso-xanthohumol showing superior antiviral activity to that observed with xanthohumol. Xanthohumol also showed antiviral activity against CMV, suggesting that it might have a generalized anti-herpesvirus antiviral activity. Again, superior antiviral activity was observed with the xanthohumol isomer against CMV. In summary, iso-alpha-acids and xanthohumol were shown to have a low-to-moderate antiviral activity against several viruses. These hop constituents might serve as interesting lead compounds from which more active anti-HCV, anti-Rhino and anti-herpesvirus antiviral agents could be synthesized.


Asunto(s)
Antivirales/farmacología , Virus ADN/efectos de los fármacos , Humulus/química , Extractos Vegetales/farmacología , Propiofenonas/farmacología , Virus ARN/efectos de los fármacos , Animales , Línea Celular , Citomegalovirus/efectos de los fármacos , Citomegalovirus/crecimiento & desarrollo , Virus ADN/crecimiento & desarrollo , Virus de la Diarrea Viral Bovina/efectos de los fármacos , Virus de la Diarrea Viral Bovina/crecimiento & desarrollo , Flavonoides , Herpesvirus Humano 1/efectos de los fármacos , Herpesvirus Humano 1/crecimiento & desarrollo , Herpesvirus Humano 2/efectos de los fármacos , Herpesvirus Humano 2/crecimiento & desarrollo , Humanos , Virus ARN/crecimiento & desarrollo , Replicación Viral/efectos de los fármacos
3.
Antimicrob Agents Chemother ; 47(9): 2810-6, 2003 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-12936978

RESUMEN

Shikonin is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities, including inhibition of human immunodeficiency virus (HIV) type 1 (HIV-1). G protein-coupled chemokine receptors are used by HIV-1 as coreceptors to enter the host cells. In this study, we assessed the effects of shikonin on chemokine receptor function and HIV-1 replication. The results showed that, at nanomolar concentrations, shikonin inhibited monocyte chemotaxis and calcium flux in response to a variety of CC chemokines (CCL2 [monocyte chemoattractant protein 1], CCL3 [macrophage inflammatory protein 1alpha], and CCL5 [regulated upon activation, normal T-cell expressed and secreted protein]), the CXC chemokine (CXCL12 [stromal cell-derived factor 1alpha]), and classic chemoattractants (formylmethionyl-leucine-phenylalanine and complement fraction C5a). Shikonin down-regulated surface expression of CCR5, a primary HIV-1 coreceptor, on macrophages to a greater degree than the other receptors (CCR1, CCR2, CXCR4, and the formyl peptide receptor) did. CCR5 mRNA expression was also down-regulated by the compound. Additionally, shikonin inhibited the replication of a multidrug-resistant strain and pediatric clinical isolates of HIV in human peripheral blood mononuclear cells, with 50% inhibitory concentrations (IC(50)s) ranging from 96 to 366 nM. Shikonin also effectively inhibited the replication of the HIV Ba-L isolate in monocytes/macrophages, with an IC(50) of 470 nM. Our results suggest that the anti-HIV and anti-inflammatory activities of shikonin may be related to its interference with chemokine receptor expression and function. Therefore, shikonin, as a naturally occurring, low-molecular-weight pan-chemokine receptor inhibitor, constitutes a basis for the development of novel anti-HIV therapeutic agents.


Asunto(s)
Fármacos Anti-VIH/farmacología , Antiinflamatorios/farmacología , Medicamentos Herbarios Chinos/farmacología , Naftoquinonas/farmacología , Receptores de Quimiocina/antagonistas & inhibidores , Señalización del Calcio/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Quimiotaxis de Leucocito/efectos de los fármacos , Regulación hacia Abajo/efectos de los fármacos , Citometría de Flujo , Humanos , ARN Viral/biosíntesis , ARN Viral/genética , Receptores CCR5/biosíntesis , Reacción en Cadena de la Polimerasa de Transcriptasa Inversa , Transducción de Señal/efectos de los fármacos , Replicación Viral/efectos de los fármacos
4.
Expert Opin Investig Drugs ; 11(8): 1077-97, 2002 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-12150703

RESUMEN

The increased incidence of HIV/AIDS disease in women aged 15 - 49 years has identified the urgent need for a female-controlled, efficacious and safe vaginal topical microbicide. To meet this challenge, new topical microbicide candidates consisting of molecules or formulations that modify the genital environment (BufferGel, engineered Lactobacillus, over-the-counter lubricants), surfactants (C31D/Savvy, sodium dodecyl sulfate, sodium lauryl sulfate), polyanionic polymers (PRO 2000, beta-cyclodextrin, Carraguard, CAP, D2S, SPL-7013), proteins (cyanovirin-N, monoclonal antibodies, thromspondin-1 peptides, Pokeweed antiviral protein and others), reverse transcription inhibitors (PMPA [Tenofovir ]), UC-781, SJ-3366, DABO and thiourea) and other molecules (NCp7-specific virucides, chemokine receptor agonists/antagonists, WHI-05 and WHI-07) are currently being investigated for activity, safety and efficacy. This review will assess the development of these molecules in the context of cervicovaginal defences and the clinical failure of nonoxynol-9.


Asunto(s)
Infecciones por VIH/prevención & control , VIH-1/efectos de los fármacos , Enfermedades Virales de Transmisión Sexual/prevención & control , Espermicidas/uso terapéutico , Animales , Ensayos Clínicos como Asunto , Evaluación Preclínica de Medicamentos , Femenino , Infecciones por VIH/transmisión , Infecciones por VIH/virología , Humanos , Masculino , Nonoxinol/farmacología , Nonoxinol/uso terapéutico , Enfermedades Virales de Transmisión Sexual/transmisión , Enfermedades Virales de Transmisión Sexual/virología , Espermicidas/farmacología , Insuficiencia del Tratamiento
5.
Bioorg Med Chem ; 10(2): 283-90, 2002 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-11741777

RESUMEN

The existing methods for the synthesis of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors proceed from symmetrical benzophenones and therefore result in products with identical aromatic rings. New methods have therefore been devised for the preparation of stereochemically defined ADAMs with non-identical aromatic rings. The new routes rely on palladium-catalyzed reactions, including Sonogashira, Suzuki, Stille, and hydroarylation methodology. Several of the new ADAMs inhibited the cytopathic effect of HIV-1 in cell culture and HIV-1 reverse transcriptase at submicromolar concentrations.


Asunto(s)
Bioquímica/métodos , Transcriptasa Inversa del VIH/antagonistas & inhibidores , Inhibidores de la Transcriptasa Inversa/química , Inhibidores de la Transcriptasa Inversa/farmacología , Células Cultivadas , Evaluación Preclínica de Medicamentos/métodos , Humanos , Hidrocarburos Aromáticos/química , Concentración 50 Inhibidora , Relación Estructura-Actividad
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