Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation

Context: Bauhinia L. species, including Bauhinia holophylla (Bong.) Steud. (Fabaceae), have traditionally been used to treat diabetes. Bauhinia is a complex botanical genus, and the indiscriminate use of the diverse Bauhinia species is reflected in the experimental divergence of their medicinal pote...

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Autores principales:	Nathalia Ap. De Paula Camaforte, Luiz Leonardo Saldanha, Priscilla Maria Ponce Vareda, João M. Rezende-Neto, Mario R. Senger, Aislan Q. Delgado, Henrique J. N. Morgan, Natalia Moretti Violato, Laís Goyos Pieroni, Anne Lígia Dokkedal, Floriano P. Silva-Júnior, José Roberto Bosqueiro
Formato:	article
Lenguaje:	EN
Publicado:	Taylor & Francis Group 2019
Materias:	antidiabetic fabaceae flavonoid-o-glycosides liver plasma lipids Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/c92011cc897643339a978a5d7ca2b0dd
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spelling	oai:doaj.org-article:c92011cc897643339a978a5d7ca2b0dd2021-11-17T14:21:56ZHypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation1388-02091744-511610.1080/13880209.2019.1599962https://doaj.org/article/c92011cc897643339a978a5d7ca2b0dd2019-01-01T00:00:00Zhttp://dx.doi.org/10.1080/13880209.2019.1599962https://doaj.org/toc/1388-0209https://doaj.org/toc/1744-5116Context: Bauhinia L. species, including Bauhinia holophylla (Bong.) Steud. (Fabaceae), have traditionally been used to treat diabetes. Bauhinia is a complex botanical genus, and the indiscriminate use of the diverse Bauhinia species is reflected in the experimental divergence of their medicinal potential. Objective: The hypoglycaemic and hypolipidaemic effects, molecular mechanism of action and phytochemical properties of an authentic extract of B. holophylla leaves were evaluated. Materials and methods: A phytochemical study of a 70% EtOH extract was performed using FIA-ESI-IT-MS/MSn and HPLC-PAD-ESI-IT-MS. The extract (200 or 400 mg/kg b.w.) was administered for 14 days to streptozotocin-induced diabetic Swiss mice. Glucose tolerance and insulin sensitivity, blood parameters, gene and protein expression, and the in vivo and in vitro inhibition of intestinal glucosidases were assessed. Results: HPLC-PAD-ESI-IT-MS analysis identified flavonoid derivatives of quercetin, myricetin, luteolin and kaempferol. Treatment with 400 mg/kg of the extract reduced blood glucose (269.0 ± 32.4 mg/dL vs. 468.0 ± 32.2 mg/dL for diabetic animals), improved glucose tolerance, decreased cholesterol and triglyceride levels, and increased the mRNA expression of proteins involved in glucogenesis in the liver and muscle, such as PI3-K/Akt, GS, GSK3-β (ser-9), AMPK and Glut4. The activity of intestinal maltase was inhibited in vitro (IC50: 43.0 µg/mL for the extract compared to 516.4 µg/mL for acarbose) and in vivo. Discussion and conclusions: Treatment with B. holophylla was associated with a marked hypoglycaemic effect through the stimulation of glycogenesis and inhibition of gluconeogenesis and intestinal glucose absorption, without increasing basal insulinaemia.Nathalia Ap. De Paula CamaforteLuiz Leonardo SaldanhaPriscilla Maria Ponce VaredaJoão M. Rezende-NetoMario R. SengerAislan Q. DelgadoHenrique J. N. MorganNatalia Moretti ViolatoLaís Goyos PieroniAnne Lígia DokkedalFloriano P. Silva-JúniorJosé Roberto BosqueiroTaylor & Francis Grouparticleantidiabeticfabaceaeflavonoid-o-glycosidesliverplasma lipidsTherapeutics. PharmacologyRM1-950ENPharmaceutical Biology, Vol 57, Iss 1, Pp 269-279 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	antidiabetic fabaceae flavonoid-o-glycosides liver plasma lipids Therapeutics. Pharmacology RM1-950
spellingShingle	antidiabetic fabaceae flavonoid-o-glycosides liver plasma lipids Therapeutics. Pharmacology RM1-950 Nathalia Ap. De Paula Camaforte Luiz Leonardo Saldanha Priscilla Maria Ponce Vareda João M. Rezende-Neto Mario R. Senger Aislan Q. Delgado Henrique J. N. Morgan Natalia Moretti Violato Laís Goyos Pieroni Anne Lígia Dokkedal Floriano P. Silva-Júnior José Roberto Bosqueiro Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation
description	Context: Bauhinia L. species, including Bauhinia holophylla (Bong.) Steud. (Fabaceae), have traditionally been used to treat diabetes. Bauhinia is a complex botanical genus, and the indiscriminate use of the diverse Bauhinia species is reflected in the experimental divergence of their medicinal potential. Objective: The hypoglycaemic and hypolipidaemic effects, molecular mechanism of action and phytochemical properties of an authentic extract of B. holophylla leaves were evaluated. Materials and methods: A phytochemical study of a 70% EtOH extract was performed using FIA-ESI-IT-MS/MSn and HPLC-PAD-ESI-IT-MS. The extract (200 or 400 mg/kg b.w.) was administered for 14 days to streptozotocin-induced diabetic Swiss mice. Glucose tolerance and insulin sensitivity, blood parameters, gene and protein expression, and the in vivo and in vitro inhibition of intestinal glucosidases were assessed. Results: HPLC-PAD-ESI-IT-MS analysis identified flavonoid derivatives of quercetin, myricetin, luteolin and kaempferol. Treatment with 400 mg/kg of the extract reduced blood glucose (269.0 ± 32.4 mg/dL vs. 468.0 ± 32.2 mg/dL for diabetic animals), improved glucose tolerance, decreased cholesterol and triglyceride levels, and increased the mRNA expression of proteins involved in glucogenesis in the liver and muscle, such as PI3-K/Akt, GS, GSK3-β (ser-9), AMPK and Glut4. The activity of intestinal maltase was inhibited in vitro (IC50: 43.0 µg/mL for the extract compared to 516.4 µg/mL for acarbose) and in vivo. Discussion and conclusions: Treatment with B. holophylla was associated with a marked hypoglycaemic effect through the stimulation of glycogenesis and inhibition of gluconeogenesis and intestinal glucose absorption, without increasing basal insulinaemia.
format	article
author	Nathalia Ap. De Paula Camaforte Luiz Leonardo Saldanha Priscilla Maria Ponce Vareda João M. Rezende-Neto Mario R. Senger Aislan Q. Delgado Henrique J. N. Morgan Natalia Moretti Violato Laís Goyos Pieroni Anne Lígia Dokkedal Floriano P. Silva-Júnior José Roberto Bosqueiro
author_facet	Nathalia Ap. De Paula Camaforte Luiz Leonardo Saldanha Priscilla Maria Ponce Vareda João M. Rezende-Neto Mario R. Senger Aislan Q. Delgado Henrique J. N. Morgan Natalia Moretti Violato Laís Goyos Pieroni Anne Lígia Dokkedal Floriano P. Silva-Júnior José Roberto Bosqueiro
author_sort	Nathalia Ap. De Paula Camaforte
title	Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation
title_short	Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation
title_full	Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation
title_fullStr	Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation
title_full_unstemmed	Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation
title_sort	hypoglycaemic activity of bauhinia holophylla through gsk3-β inhibition and glycogenesis activation
publisher	Taylor & Francis Group
publishDate	2019
url	https://doaj.org/article/c92011cc897643339a978a5d7ca2b0dd
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Hypoglycaemic activity of Bauhinia holophylla through GSK3-β inhibition and glycogenesis activation

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