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Despite the absence of toxicity regarding its consumption, possible interactions when co-administrated with\nconventional drugs, are unknown.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Objective:<\/jats:title>\n<jats:p>This study aimed to evaluate the effects of M. ilicifolia extracts on Cytochrome P450 3A (CYP3A) and\nP-glycoprotein (P-gp) activities.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Method:<\/jats:title>\n<jats:p>The extracts were obtained by infusion (MI) or turbo-extraction using hydro-acetonic solvent (MT70). The\ncontent of polyphenols in each extract was determined. To assess the modulation of M. ilicifolia on P-gp activity, the\nuptake of fexofenadine (FEX) by Caco-2 cells was investigated in the absence or presence of MI or MT70. The effect\non CYP3A activity was evaluated by the co-administration of midazolam (MDZ) with each extract in male Wistar\nrats. The pharmacokinetic parameters of the drug were determined and compared with those from the control group.\nThe content of total phenolic compounds, tannins, and flavonoids on MT70 extract was about double of that found in\nMI.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p> In the presence of the extracts, the uptake of the P-gp marker (FEX) by Caco-2 cells increased from\n1.7 \u00b1 0.4 ng.mg-1 protein (control) to 3.5 \u00b1 0.2 ng.mg-1 protein (MI) and 4.4 \u00b1 0.5 ng.mg-1 protein (MT70),\nrespectively. When orally co-administrated with MDZ (substrate of CYP3A), the extracts augmented the AUC(0-\u221e)\n(Control: 911.7 \u00b1 215.7 ng.h.mL-1; MI: 1947 \u00b1 554.3 ng.h.mL-1; MT70: 2219.0 \u00b1 506.3 ng.h.mL-1) and the\nCmax (Control: 407.7 \u00b1 90.4 ng.mL-1; MI: 1770.5 \u00b1 764.5 ng.mL-1; MT70: 1987.2 \u00b1 544.9 ng.mL-1) of the drug in rats\nindicating a 50% reduction of the oral Cl. No effect was observed when midazolam was given intravenously.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Conclusion:<\/jats:title>\n<jats:p> The results suggest that M. ilicifolia can inhibit the intestinal metabolism and transport of drugs\nmediated by CYP3A and P-gp, respectively, however, the involvement of other transporters and the clinical\nrelevance of such interaction still need to be clarified.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1389200221666200512112718","type":"journal-article","created":{"date-parts":[[2020,5,12]],"date-time":"2020-05-12T12:28:03Z","timestamp":1589286483000},"page":"281-290","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["Evaluation of the Effects of Maytenus ilicifolia on the Activities of Cytochrome P450 3A and P-glycoprotein"],"prefix":"10.2174","volume":"21","author":[{"given":"Sara Batista","family":"do Nascimento","sequence":"first","affiliation":[{"name":"Federal University of Sao Joao del-Rei, Av. 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