Please use this identifier to cite or link to this item: http://hdl.handle.net/1843/56503
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dc.creatorSara Batistado Nascimentopt_BR
dc.creatorWhocely Victor de Castropt_BR
dc.creatorMariana de Lima Nascimentopt_BR
dc.creatorLaís Lobato de Araújopt_BR
dc.creatorFlávio Martins de Oliveirapt_BR
dc.creatorMaria do Carmo Vieirapt_BR
dc.creatorJoaquim Maurício Duarte-almeidapt_BR
dc.creatorJoão Máximo Siqueirapt_BR
dc.creatorIsabela da Costa Césarpt_BR
dc.creatorHartmut Derendorfpt_BR
dc.date.accessioned2023-07-17T20:28:33Z-
dc.date.available2023-07-17T20:28:33Z-
dc.date.issued2020-
dc.citation.volume21pt_BR
dc.citation.issue4pt_BR
dc.citation.spage281pt_BR
dc.citation.epage290pt_BR
dc.identifier.doihttp://doi.org/10.2174/1389200221666200512112718pt_BR
dc.identifier.issn1389-2002pt_BR
dc.identifier.urihttp://hdl.handle.net/1843/56503-
dc.description.resumoAbstract: Background: Maytenus ilicifolia is a Brazilian popular medicine commonly used to treat ulcer and gastritis. Despite the absence of toxicity regarding its consumption, possible interactions when co-administrated with conventional drugs, are unknown. Objective: This study aimed to evaluate the effects of M. ilicifolia extracts on Cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp) activities. Methods: The extracts were obtained by infusion (MI) or turbo-extraction using hydro-acetonic solvent (MT70). The content of polyphenols in each extract was determined. To assess the modulation of M. ilicifolia on P-gp activity, the uptake of fexofenadine (FEX) by Caco-2 cells was investigated in the absence or presence of MI or MT70. The effect on CYP3A activity was evaluated by the co-administration of midazolam (MDZ) with each extract in male Wistar rats. The pharmacokinetic parameters of the drug were determined and compared with those from the control group. The content of total phenolic compounds, tannins, and flavonoids on MT70 extract was about double of that found in MI. Results: In the presence of the extracts, the uptake of the P-gp marker (FEX) by Caco-2 cells increased from 1.7 ± 0.4 ng.mg-1 protein (control) to 3.5 ± 0.2 ng.mg-1 protein (MI) and 4.4 ± 0.5 ng.mg-1 protein (MT70), respectively. When orally co-administrated with MDZ (substrate of CYP3A), the extracts augmented the AUC(0-∞) (Control: 911.7 ± 215.7 ng.h.mL-1; MI: 1947 ± 554.3 ng.h.mL-1; MT70: 2219.0 ± 506.3 ng.h.mL-1) and the Cmax (Control: 407.7 ± 90.4 ng.mL-1; MI: 1770.5 ± 764.5 ng.mL-1; MT70: 1987.2 ± 544.9 ng.mL-1) of the drug in rats indicating a 50% reduction of the oral Cl. No effect was observed when midazolam was given intravenously. Conclusion: The results suggest that M. ilicifolia can inhibit the intestinal metabolism and transport of drugs mediated by CYP3A and P-gp, respectively, however, the involvement of other transporters and the clinical relevance of such interaction still need to be clarified.pt_BR
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Geraispt_BR
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superiorpt_BR
dc.format.mimetypepdfpt_BR
dc.languageengpt_BR
dc.publisherUniversidade Federal de Minas Geraispt_BR
dc.publisher.countryBrasilpt_BR
dc.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOSpt_BR
dc.publisher.departmentFARMACIA - FACULDADE DE FARMACIApt_BR
dc.publisher.initialsUFMGpt_BR
dc.relation.ispartofCurrent Drug Metabolismpt_BR
dc.rightsAcesso Restritopt_BR
dc.subjectMaytenus ilicifoliapt_BR
dc.subjectP-glycoproteinpt_BR
dc.subjectCytochrome P4503Apt_BR
dc.subjectHerbal-drug interactionpt_BR
dc.subjectCaco-2pt_BR
dc.subjectMidazolampt_BR
dc.subject.otherFarmáciapt_BR
dc.subject.otherBiofarmáciapt_BR
dc.titleEvaluation of the effects of maytenus ilicifolia on the activities of cytochrome p450 3a and p-glycoproteinpt_BR
dc.typeArtigo de Periódicopt_BR
dc.url.externahttps://www.eurekaselect.com/article/106564pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0003-1349-9413pt_BR
Appears in Collections:Artigo de Periódico

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