Inhibitory Activities of Thai Medicinal Plants with Promising Activities Against Malaria and Cholangiocarcinoma on Human Cytochrome P450

作者: Wiriyaporn Sumsakul , Wiratchanee Mahavorasirikul , Kesara Na-Bangchang

DOI: 10.1002/PTR.5485

关键词:

摘要: Malaria and cholangiocarcinoma remain important public health problems in tropical countries including Southeast Asian nations. Newly developed chemotherapeutic plant-derived drugs are urgently required for the control of both diseases. The aim present study was to investigate propensity inhibit cytochrome P450-mediated hepatic metabolism (CYP1A2, CYP2C19, CYP2D6 CYP3A4) crude ethanolic extract eight Thai medicinal plants with promising activities against malaria cholangiocarcinoma, using human liver microsomes vitro. Piper chaba Linn. (PC) Atractylodes lancea (thung.) DC. (AL) exhibited most potent inhibitory on CYP1A2-mediated phenacetin O-deethylation mean IC50 0.04 0.36 µg/mL, respectively. Plumbago indica (PI) Dioscorea membranacea Pierre. (DM) potently inhibited CYP2C19-mediated omeprazole 5-hydroxylation (mean 4.71 6.92 respectively). DM, Dracaena loureiri Gagnep. (DL) PI showed highest dextromethorphan O-demethylation 2.93-9.57 µg/mL). PC, DL CYP3A4-mediated nifedipine oxidation 1.54-6.43 Clinical relevance potential PC is concern further development these treatment and/or cholangiocarcinoma.

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