Hypoglycaemic activity of Bauhinia holophylla through GSK3-beta inhibition and glycogenesis activation
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Data
2019-01-01
Autores
De Paula Camaforte, Nathalia Ap [UNESP]
Saldanha, Luiz Leonardo [UNESP]
Ponce Vareda, Priscilla Maria [UNESP]
Rezende-Neto, Joao M.
Senger, Mario R.
Delgado, Aislan Q. [UNESP]
Morgan, Henrique J. N. [UNESP]
Violato, Natalia Moretti [UNESP]
Pieroni, Lais Goyos [UNESP]
Dokkedal, Anne Ligia [UNESP]
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Editor
Taylor & Francis Ltd
Resumo
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-beta (ser-9), AMPK and Glut4. The activity of intestinal maltase was inhibited in vitro (IC50: 43.0 mu g/mL for the extract compared to 516.4 mu g/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.
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Palavras-chave
Antidiabetic, Fabaceae, flavonoid-O-glycosides, liver, plasma lipids
Como citar
Pharmaceutical Biology. Abingdon: Taylor & Francis Ltd, v. 57, n. 1, p. 269-279, 2019.