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Métodos Terapéuticos y Terapias MTCI
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1.
J Ethnopharmacol ; 155(3): 1433-40, 2014 Sep 29.
Artículo en Inglés | MEDLINE | ID: mdl-25138353

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: A substantial proportion of the population in Papua New Guinea (PNG) lives with human immunodeficiency virus (HIV). Treatment requires lifelong use of antiretroviral therapy (ART). The majority of people in PNG use traditional medicines (TM) derived from plants for all types of health promotions. Consequently, there is a concern that herb-drug interactions may impact the efficacy of ART. Herb-drug, or drug-drug, interactions occur at the level of metabolism through two major mechanisms: enzyme induction or enzyme inhibition. In this study, extracts of commonly-used medicinal plants from PNG were screened for herb-drug interactions related to cytochrome P450s (CYPs). MATERIALS AND METHODS: Sixty nine methanol extracts of TM plants were screened for their ability to induce CYPs by human aryl hydrocarbon receptor- (hAhR-) and human pregnane X receptor- (hPXR-) dependent mechanisms, utilizing a commercially available cell-based luciferase reporter system. Inhibition of three major CYPs, CYP1A2, CYP3A4, and CYP2D6, was determined using human liver microsomes and enzyme-selective model substrates. RESULTS: Almost one third of the TM plant extracts induced the hAhR-dependent expression of CYP1A2, the hPXR-dependent expression of CYP3A4, or both. Almost two thirds inhibited CYP1A2, CYP3A4, or CYP2D6, or combinations thereof. Many plant extracts exhibited both induction and inhibition properties. CONCLUSIONS: We demonstrated that the potent and selective ability of extracts from PNG medicinal plants to affect drug metabolizing enzymes through induction and/or inhibition is a common phenomenon. Use of traditional medicines concomitantly with ART could dramatically alter the concentrations of antiretroviral drugs in the body; and their efficacy. PNG healthcare providers should counsel HIV patients because of this consequence.


Asunto(s)
Inhibidores Enzimáticos del Citocromo P-450/farmacología , Sistema Enzimático del Citocromo P-450/biosíntesis , Interacciones de Hierba-Droga , Extractos Vegetales/farmacología , Plantas Medicinales , Antirretrovirales , Inducción Enzimática/efectos de los fármacos , Humanos , Microsomas Hepáticos/efectos de los fármacos , Microsomas Hepáticos/metabolismo , Papúa Nueva Guinea , Receptor X de Pregnano , Receptores de Hidrocarburo de Aril/metabolismo , Receptores de Esteroides/metabolismo
2.
Planta Med ; 75(12): 1326-30, 2009 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-19444772

RESUMEN

Lipophilic fractions of stem extracts from Exocarpos latifolius, native to Papua New Guinea, showed significant activity against Mycobacterium tuberculosis H37Ra. Bioactivity-guided fractionation yielded exocarpic acid (E-octadeca-13-ene-9,11-diynoic-acid) as the major active component. Several new exocarpic acid analogs were also shown to be active. Exocarpic acid has previously been reported active against gram-positive, but not gram-negative bacteria. Work presented here demonstrates the selective activity of exocarpic acid against Mycobacterium tuberculosis H37Ra.


Asunto(s)
Antibacterianos/farmacología , Diinos/farmacología , Ácidos Grasos Insaturados/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Santalaceae/química , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Fraccionamiento Químico , Diinos/química , Diinos/aislamiento & purificación , Ácidos Grasos Insaturados/química , Ácidos Grasos Insaturados/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología
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