RESUMO
NIPRISAN(®) is a phytomedicine developed from herbal products used in folkloric practice for the management of sickle cell disease (SCD). The effect of NIPRISAN(®) was tested on human cytochrome P4503A4 drug metabolising enzyme to generate clinically significant data for its safe and efficacious use. Inhibitory activity on CYP3A4 was measured with and without the addition of NIPRISAN(®), by testing different concentrations of the product at 37 °C in reactive mixtures with ketoconazole (2.5 µM) as the positive control. Results showed a low IC(50) value of 0.06 mg/ml, indicating that metabolic processes of NIPRISAN(®) are likely to inhibit CYP3A4. The result suggests possible herb-drug interaction may occur, with potential implication on common medications that are CYP3A4 substrates. It is, therefore, advocated that concomitant administration of NIPRISAN(®) along with medications that are CYP3A4 substrates should be done with caution so as not to compromise NIPRISAN(®')s established beneficial effect in the management of SCD.
Assuntos
Inibidores do Citocromo P-450 CYP3A/farmacologia , Citocromo P-450 CYP3A/metabolismo , Interações Ervas-Drogas , Microssomos Hepáticos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Humanos , Microssomos Hepáticos/enzimologia , Medição de Risco , Especificidade por SubstratoRESUMO
OBJECTIVE: To evaluate the effect of NIPRD-AM1 on CYP3A4 in order to generate clinically significant data for its safe and efficacious use. MATERIALS AND METHODS: NIPRD-AM1 is a phytomedicine developed from aqueous root extracts of Nauclea latifolia Smith (Rubiaceae) for the treatment of uncomplicated malaria. The effect of NIPRD-AM1 on CYP3A4 was measured with and without the addition of NIPRD-AM1, by testing different concentrations of the product at 37 °C in reactive mixtures with ketoconazole (2.5 µM) as the positive control. RESULTS: RESULTS showed a very low IC50 value of 0.01 mg/ml similar to that of ketoconazole (0.016 mg/ml). CONCLUSION: Metabolic processes of NIPRD-AM1 are likely to inhibit CYP3A4, with potential implication on drugs that are CYP3A4 substrates. This is a promising approach for guidance towards the safe and efficacious use of NIPRD-AM1.
