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

Abstract

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/MS n 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 (IC 50 : 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.

Lupin protein isolate improves insulin sensitivity and steatohepatitis in vivo and modulates the expression of the Fasn, Gys2, and Gsk3b genes

“…Here, we found that LPI treatment increased Gys2 and Gsk3b gene expression in the liver. Similar results were also found in the gene expression and protein levels in diabetic mice treated with Bauhinia holophylla extract, a plant belonging to the Fabaceae family (Camaforte et al, 2019). Furthermore, our results showed that LPI induced a recovery of insulin sensitivity and a subsequent decrease in hyperglycemia, a finding that may have involved the activation of hepatic glycogenesis.…”

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“…In the present study, HPPT (400 mg/kg dose) showed significant inhibition of weight loss in animals. STZ induced diabetes is also associated with liver insulin resistance which reduces the level of glycogen synthase and causes the reduction in liver glycogen content 44 . In the present study, the test drug (HPPT at 400 mg/kg dose) treated group showed a significant increase in liver glycogen content.…”

Vochysia tucanorum Mart. butanol fraction presents antitumoral activity in vivo and prevents the installation of cachexia in solid Ehrlich tumor model

“…The Fr-BuVt concentration was 10 times higher than the most effective treatment (200 mg/kg). The acute toxicity test was performed as described by Camaforte et al [23].…”

“…Tumors of TV200 group (200 mg/kg Fr-BuVt) were collected in extraction buffer and Western blot was performed as described Camaforte et al [23]. Images were acquired by documental system (G:BOX, Syngene) and analyzed using ImageJ software.…”