Evaluation of the effects of maytenus ilicifolia on the activities of cytochrome p450 3a and p-glycoprotein

Página do item simplificado
dc.creatorSara Batistado Nascimento
dc.creatorWhocely Victor de Castro
dc.creatorMariana de Lima Nascimento
dc.creatorLaís Lobato de Araújo
dc.creatorFlávio Martins de Oliveira
dc.creatorMaria do Carmo Vieira
dc.creatorJoaquim Maurício Duarte-almeida
dc.creatorJoão Máximo Siqueira
dc.creatorIsabela da Costa César
dc.creatorHartmut Derendorf
dc.date.accessioned2023-07-17T20:28:33Z
dc.date.accessioned2025-09-08T23:53:12Z
dc.date.available2023-07-17T20:28:33Z
dc.date.issued2020
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.format.mimetypepdf
dc.identifier.doihttp://doi.org/10.2174/1389200221666200512112718
dc.identifier.issn1389-2002
dc.identifier.urihttps://hdl.handle.net/1843/56503
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofCurrent Drug Metabolism
dc.rightsAcesso Restrito
dc.subjectFarmácia
dc.subjectBiofarmácia
dc.subject.otherMaytenus ilicifolia
dc.subject.otherP-glycoprotein
dc.subject.otherCytochrome P4503A
dc.subject.otherHerbal-drug interaction
dc.subject.otherCaco-2
dc.subject.otherMidazolam
dc.titleEvaluation of the effects of maytenus ilicifolia on the activities of cytochrome p450 3a and p-glycoprotein
dc.typeArtigo de periódico
local.citation.epage290
local.citation.issue4
local.citation.spage281
local.citation.volume21
local.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.
local.identifier.orcidhttps://orcid.org/0000-0003-1349-9413
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS
local.publisher.departmentFARMACIA - FACULDADE DE FARMACIA
local.publisher.initialsUFMG
local.url.externahttps://www.eurekaselect.com/article/106564

Arquivos

Licença do pacote

Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
License.txt
Tamanho:
1.99 KB
Formato:
Plain Text
Descrição:
Baixar

Coleções

Artigo de Periódico

Logo UFMG