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1.
J Pharm Pharm Sci ; 18(4): 484-93, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26626246

RESUMEN

PURPOSE: The Cree of Eeyou Istchee in Northern Quebec identified Sarracenia purpurea L. as an important plant for the treatment of Type 2 diabetes. Traditionally the plant is used as a decoction (boiling water extract) of the leaf, however, in order to study the extract in a laboratory setting, an 80% ethanol extract was used. In this study, the phytochemistry of both extracts of the leaves was compared and quantified. METHODS: Two S. purpurea leaf extracts were prepared, one a traditional hot water extract and the other an 80% ethanol extract. Using UPLC-ESI-MS, the extracts were phytochemically compared for 2 triterpenes, betulinic acid and ursolic acid, using one gradient method and for 10 additional substances, including the actives quercetin-3-O-galactoside and morroniside, using a different method. RESULTS: The concentrations of the nine phenolic substances present, as well as an active principle, the iridoid glycoside morroniside, were very similar between the two extracts, with generally slightly higher concentrations of phenolics in the ethanol extract as expected. However, two triterpenes, betulinic acid and ursolic acid, were 107 and 93 times more concentrated, respectively, in the ethanol extract compared to the water extract. CONCLUSION: The main phytochemical markers and most importantly the antidiabetic active principles, quercetin-3-O-galactoside and morroniside, were present in similar amounts in the two extracts, which predicts similar bioactivity.This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Extractos Vegetales/química , Sarraceniaceae/química , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Etanol/química , Humanos , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Indígenas Norteamericanos , Medicina Tradicional , Hojas de la Planta , Quebec , Espectrometría de Masa por Ionización de Electrospray/métodos , Agua/química
2.
J Pharm Pharm Sci ; 18(4): 562-77, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26626249

RESUMEN

PURPOSE: The purpose of this study was to assess safety of the traditional antidiabetic extracts of either S. purpurea or its lead active principle, morroniside at the transcriptional level. The overarching objective was to profile and validate transcriptional changes in the cytochrome P450 family of genes, in response to treatment with S. purpurea ethanolic extract or its lead active, morroniside. METHODS: Transcriptional activity was profiled using a 19K human cDNA microarray in C2BBe1 cells, clone of Caco-2 intestinal cells, which are a model of first-pass metabolism (1, 2). Cells were treated with S. purpurea extract for 4 and 24 hrs, as well as the pure compound morroniside for 4 hrs, to determine their effects. RESULTS: No evidence of cytochrome P450 transcriptome regulation or of transcriptional activation of other diabetes relevant mRNA was detected after rigorous quantitative-PCR validation of microarray results. CONCLUSION: Our data do not support a transcriptional mechanism of action for either S. purpurea extract or its lead active, morroniside. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.


Asunto(s)
Sistema Enzimático del Citocromo P-450/genética , Glicósidos/toxicidad , Extractos Vegetales/toxicidad , Sarraceniaceae/química , Células CACO-2 , ADN Complementario/genética , Glicósidos/aislamiento & purificación , Humanos , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/toxicidad , Indígenas Norteamericanos , Medicina Tradicional , Análisis de Secuencia por Matrices de Oligonucleótidos/métodos , Extractos Vegetales/aislamiento & purificación , Reacción en Cadena de la Polimerasa , Quebec , ARN Mensajero/metabolismo , Factores de Tiempo
3.
J Ethnopharmacol ; 150(3): 1087-95, 2013 Dec 12.
Artículo en Inglés | MEDLINE | ID: mdl-24184081

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Interactions between conventional drug and traditional medicine therapies may potentially affect drug efficacy and increase the potential for adverse reactions. Cree traditional healing is holistic and patients may use medicinal plants simultaneously with the conventional drugs. However, there is limited information that these medicinal plants may interact with drugs and additional mechanistic information is required. In this study, extracts from traditionally used Cree botanicals were assessed for their potential interaction that could alter the disposition of two blood glucose lowering drugs, gliclazide (Diamicron) and repaglinide (Gluconorm) though inhibition of either metabolism or transport across cell membranes. MATERIALS AND METHODS: The effect of 17 extracts on metabolism was examined in a human liver microsome assay by HPLC and individual cytochrome P450s 2C9, 2C19, 2C8 and 3A4 in a microplate fluorometric assay. Gliclazide, rhaponticin and its aglycone derivative, rhapontigenin were also examined in the fluorometric assay. The effect on transport was examined with 11 extracts using the intestinal epithelial Caco-2 differentiated cell monolayer model at times up to 180 min. RESULTS: Both blood glucose lowering medications, gliclazide and repaglinide traversed the Caco-2 monolayer in a time-dependent manner that was not affected by the Cree plant extracts. Incubation of the Cree plant extracts inhibited CYP2C9, 2C19, 2C8 and 3A4-mediated metabolism, and the formation of four repaglinide metabolites: M4, m/z 451-A, m/z 451-B and the glucuronide of repaglinide in the human liver microsome assay. Gliclazide caused no significant inhibition. Likewise, rhaponticin had little effect on the enzymes causing changes of less than 10% with an exception of 17% inhibition of CYP2C19. By contrast, the aglycone rhapontigenin showed the greatest effects on all CYP-mediated metabolism. Its inhibition ranged from a mean of 58% CYP3A4 inhibition to 89% inhibition of CYP2C9. While rhaponticin and the aglycone did not show significant effects on repaglinide metabolism, they demonstrated inhibition of gliclazide metabolism. The aglycone significantly affected levels of gliclazide and its metabolites. CONCLUSION: These studies demonstrate that the Cree plant extracts examined have the potential in vitro to cause drug interactions through effects on key metabolic enzymes.


Asunto(s)
Carbamatos/farmacología , Gliclazida/farmacología , Hipoglucemiantes/farmacología , Piperidinas/farmacología , Extractos Vegetales/farmacología , Hidrocarburo de Aril Hidroxilasas/antagonistas & inhibidores , Hidrocarburo de Aril Hidroxilasas/metabolismo , Células CACO-2 , Interacciones Farmacológicas , Glucuronosiltransferasa/metabolismo , Humanos , Absorción Intestinal , Medicina Tradicional , Microsomas Hepáticos/metabolismo , Plantas Medicinales , Quebec , Estilbenos/metabolismo
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