scholarly journals Antihyperglycemic Effects of Annona diversifolia Safford and Its Acyclic Terpenoids: α-Glucosidase and Selective SGLT1 Inhibitiors

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3361
Author(s):  
Miguel Valdés ◽  
Fernando Calzada ◽  
Jessica Elena Mendieta-Wejebe ◽  
Verenice Merlín-Lucas ◽  
Claudia Velázquez ◽  
...  
Keyword(s):  
Ethanolic Extract ◽  
Glucose Absorption ◽  
Oral Glucose ◽  
Significant Activity ◽  
Sucrose Hydrolysis ◽  
Antihyperglycemic Activity ◽  
Glucosidase Inhibitors ◽  
Urinary Glucose ◽  
Intestinal Glucose Absorption ◽  
Glucose Excretion

Annona diversifolia Safford and two acyclic terpenoids were evaluated to determine their antihyperglycemic activity as potential α-glucosidase and selective SGLT-1 inhibitiors. Ethanolic extract (EEAd), chloroformic (CHCl3Fr), ethyl acetate (EtOAcFr), aqueous residual (AcRFr), secondary 5 (Fr5) fractions, farnesal (1), and farnesol (2) were evaluated on normoglycemic and streptozocin-induced diabetic mice. EEAd, CHCl3Fr, Fr5, (1) and (2) showed antihyperglycemic activity. The potential as α-glucosidase inhibitors of products was evaluated with oral sucrose and lactose tolerance (OSTT and OLTT, respectively) and intestinal sucrose hydrolysis (ISH) tests; the potential as SGLT-1 inhibitors was evaluated using oral glucose tolerance (OGTT), intestinal glucose absorption (IGA), and urinary glucose excretion (UGE) tests. In OSTT and OLTT, all treatments showed significant activity at two and four hours. In ISH, half maximal effective concentrations (CE50) of 565, 662 and 590 μg/mL, 682 and 802 μM were calculated, respectively. In OGTT, all treatments showed significant activity at two hours. In IGA, CE50 values of 1059, 783 and 539 μg/mL, 1211 and 327 μM were calculated, respectively. In UGE Fr5, (1) and (2) showed significant reduction of the glucose excreted compared with canagliflozin. These results suggest that the antihyperglycemic activity is mediated by α-glucosidase and selective SGLT-1 inhibition.

scholarly journals Inhibition of α-Glucosidase, Intestinal Glucose Absorption, and Antidiabetic Properties by Caralluma europaea

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Hayat Ouassou ◽  
Touda Zahidi ◽  
Saliha Bouknana ◽  
Mohamed Bouhrim ◽  
Hassane Mekhfi ◽  
...  
Keyword(s):  
Ethyl Acetate Fraction ◽  
Inhibitory Effect ◽  
Tolerance Test ◽  
Glucose Absorption ◽  
Significant Inhibition ◽  
Oral Glucose ◽  
Glucosidase Activity ◽  
Intestinal Glucose Absorption

Many medicinal plants around the world are used for therapeutic purposes against several diseases, including diabetes mellitus. Due to their composition of natural substances that are effective and do not represent side effects for users, unlike synthetic drugs, in this study, we investigated the inhibitory effect of Caralluma europaea (CE) on α-glucosidase activity in vitro; then the kinetics of the enzyme were studied with increasing concentrations of sucrose in order to determine the inhibition type of the enzyme. In addition, this effect of Caralluma europaea (CE) was confirmed in vivo using rats as an experimental animal model. Among the five fractions of CE, only the ethyl acetate fraction of C. europaea (EACe) induced a significant inhibition of α-glucosidase and its inhibition mode was competitive. The in vivo studies were conducted on mice and rats using glucose and sucrose as a substrate, respectively, to determine the oral glucose tolerance test (OGTT). The results obtained showed that the EACe and the aqueous extract of C. europaea (AECe) have significantly reduced the postprandial hyperglycemia after sucrose and glucose loading in normal and diabetic rats. AECe, also, significantly decreased intestinal glucose absorption, in situ. The results obtained showed that Caralluma europaea has a significant antihyperglycemic activity, which could be due to the inhibition of α-glucosidase activity and enteric absorption of glucose.

Antihyperglycemic Effects of Tragia plukenetii Ethanolic Extract

2014 ◽  
Vol 7 (2) ◽  
pp. 2436-2440
Author(s):  
Venkatesh Sama ◽  
Rajini T ◽  
Humera Afrooz ◽  
Balaraju P ◽  
B. Madhava Reddy ◽  
...  
Keyword(s):  
Oral Dose ◽  
Ethanolic Extract ◽  
Tolerance Test ◽  
Diabetic Rats ◽  
Antidiabetic Activity ◽  
Oral Glucose ◽  
Alcoholic Extract ◽  
Antihyperglycemic Activity ◽  
Treatment Of Diabetes

Plants represent a major potential source of drugs for treating diabetes. The study of plants having antidiabetic activity may give a new approach in the treatment of diabetes mellitus. Tragia plukenetii is traditionally claimed to be useful in the treatment of diabetes. The present study was intended to evaluate the antihyperglycemic activity of aqueous ethanolic extract on normal fasted, glucose loaded and alloxan induced diabetic rats, at an oral dose of 75, 150 and 300 mg/kg in male Wistar rats. The alcoholic extract has not produced any hypoglycemia in normal fasted rats. The ethanolic extract has displayed a significant dose dependent antihyperglycemic activity in oral glucose tolerance test and in alloxan induced diabetic rats at an oral dose of 150 and 300 mg/kg. The ethanolic extract has effectively scavenged the stable free DPPH radical in-vitro. It is concluded that Tragia plukenetii aerial parts alcoholic extract is effective in controlling blood glucose levels in diabetic rats.

scholarly journals Effect of a Chronic Intake of the Natural Sweeteners Xylitol and Erythritol on Glucose Absorption in Humans with Obesity

Nutrients ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 3950
Author(s):  
Valentine Bordier ◽  
Fabienne Teysseire ◽  
Götz Schlotterbeck ◽  
Frank Senner ◽  
Christoph Beglinger ◽  
...  
Keyword(s):  
Glucose Tolerance Test ◽  
Area Under The Curve ◽  
Tolerance Test ◽  
Glucose Absorption ◽  
Control Group ◽  
Oral Glucose ◽  
Post Intervention ◽  
Before And After ◽  
Acute Ingestion ◽  
Intestinal Glucose Absorption

In patients with obesity, accelerated nutrients absorption is observed. Xylitol and erythritol are of interest as alternative sweeteners, and it has been shown in rodent models that their acute ingestion reduces intestinal glucose absorption. This study aims to investigate whether a chronic intake of xylitol and erythritol impacts glucose absorption in humans with obesity. Forty-six participants were randomized to take either 8 g of xylitol or 12 g of erythritol three times a day for five to seven weeks, or to be part of the control group (no substance). Before and after the intervention, intestinal glucose absorption was assessed during an oral glucose tolerance test with 3-Ortho-methyl-glucose (3-OMG). The effect of xylitol or erythritol intake on the area under the curve for 3-OMG concentration was not significant. Neither the time (pre or post intervention), nor the group (control, xylitol, or erythritol), nor the time-by-group interaction effects were significant (p = 0.829, p = 0.821, and p = 0.572, respectively). Therefore, our results show that a chronic intake of the natural sweeteners xylitol and erythritol does not affect intestinal glucose absorption in humans with obesity.

scholarly journals ANTIHYPERGLYCEMIC ACTIVITY OF IMPERATA CYLINDRICA ROOT METHANOL EXTRACT IN RATS

2020 ◽  
pp. 140-143
Author(s):  
RUSLIN ◽  
VICA ASPADIAH ◽  
DIAH DHIANAWATY
Keyword(s):  
Inhibitory Activity ◽  
Methanol Extract ◽  
Glucose Absorption ◽  
Imperata Cylindrica ◽  
Antihypertensive Activity ◽  
Significant Activity ◽  
Control Solution ◽  
Antihyperglycemic Activity ◽  
Wistar Strain ◽  
Absorption Level

Objective: This study aims to evaluate the inhibitory activity of Imperatacylindrica root methanol extract on glucose absorption level in intestine of male Wistar strain rats at a dose of 90 mg/kg-bw, which is a dose having antihypertensive activity. Methods: Extract inhibitory activity on the glucose absorption level in the intestine of the rats followed Soedigdo-Marsongkohadi method. Glucose absorption level was measured from a mixture of 30 mmol glucose in 0.9 % sodium chloride solution as the control solution and a mixture of the extract at the dose of 90 mg/kg-bw in another control solution as the tested solution Results: The result showed that the extract at the dose of 90 mg/kg-bw had significant activity (p<0.05) to decrease the glucose absorption level in the intestine of the rats. Conclusion: I. cylindrica root methanol extract at the dose of 90 mg/kg-bw had a significant activity to inhibit the glucose absorption level in the intestine of the rats. Thereby, the extract at the dose of 90 mg/kg-bw had antihyperglycemic activity.

scholarly journals Annona muricata L. extract decreases intestinal glucose absorption and improves glucose tolerance in normal and diabetic rats

2021 ◽  
Vol 10 (3) ◽  
pp. 359-366
Author(s):  
Ana María Guevara-Vásquez ◽  
Julio Víctor Campos-Florián ◽  
Jesús Haydee Dávila-Castillo
Keyword(s):  
Aqueous Extract ◽  
Leaf Extract ◽  
Glucose Absorption ◽  
Diabetic Rats ◽  
Annona Muricata ◽  
Antihyperglycemic Activity ◽  
Aqueous Leaf Extract ◽  
Intestinal Glucose Absorption

Introduction: Poorly controlled hyperglycemia causes numerous health complications. Postprandial hyperglycemia is an important indicator of diabetic status. The aim of this research was to evaluate the effect of Annona muricata L. extract on the in vitro intestinal glucose absorption in diabetic rats and in vivo antihyperglycemic activity in both normal and diabetic rats. Methods: Phytochemical screening of the aqueous extract from the leaves of A. muricata was carried out. Albino rats were randomly assigned into normal and diabetic groups. Each group was divided into three subgroups: control (vehicle), experimental (A. muricata), and standard (Metformin) groups, to determine antihyperglycemic activity at different times after glucose overload. The everted intestinal sac technique was used to study intestinal glucose absorption in diabetic rats. Results: Aqueous leaf extract of Peruvian A. muricata exhibited statistically significant (P < 0.05) in vivo antihyperglycemic activity in both normal and diabetic rats when compared to the control group. The magnitude of the effect was similar to metformin treatment. Moreover, the aqueous leaf extract of A. muricata significantly diminished in vitro intestinal glucose absorption, with a magnitude similar to metformin treatment. Phytochemical analysis of the aqueous extract revealed the presence of tannins, flavonoids, alkaloids, and leucoanthocyanidins, among others. Conclusion: This study reveals that A. muricata aqueous extract is able to reduce in vitro intestinal glucose absorption and improve oral glucose tolerance in rats.

scholarly journals Flavonoids as Human Intestinal α-Glucosidase Inhibitors

Foods ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 1939
Author(s):  
Elizabeth Barber ◽  
Michael J. Houghton ◽  
Gary Williamson
Keyword(s):  
Glucose Absorption ◽  
Inhibitory Effects ◽  
Antidiabetic Drug ◽  
Glucosidase Inhibitors ◽  
Acarbose Treatment ◽  
Ic50 Values ◽  
Intestinal Glucose Absorption ◽  
Inhibition Pattern ◽  
Carbohydrate Digestion ◽  
Enzyme Source

Certain flavonoids can influence glucose metabolism by inhibiting enzymes involved in carbohydrate digestion and suppressing intestinal glucose absorption. In this study, four structurally-related flavonols (quercetin, kaempferol, quercetagetin and galangin) were evaluated individually for their ability to inhibit human α-glucosidases (sucrase, maltase and isomaltase), and were compared with the antidiabetic drug acarbose and the flavan-3-ol(−)-epigallocatechin-3-gallate (EGCG). Cell-free extracts from human intestinal Caco-2/TC7 cells were used as the enzyme source and products were quantified chromatographically with high accuracy, precision and sensitivity. Acarbose inhibited sucrase, maltase and isomaltase with IC50 values of 1.65, 13.9 and 39.1 µM, respectively. A similar inhibition pattern, but with comparatively higher values, was observed with EGCG. Of the flavonols, quercetagetin was the strongest inhibitor of α-glucosidases, with inhibition constants approaching those of acarbose, followed by galangin and kaempferol, while the weakest were quercetin and EGCG. The varied inhibitory effects of flavonols against human α-glucosidases depend on their structures, the enzyme source and substrates employed. The flavonols were more effective than EGCG, but less so than acarbose, and so may be useful in regulating sugar digestion and postprandial glycaemia without the side effects associated with acarbose treatment.

scholarly journals Sotagliflozin Decreases Postprandial Glucose and Insulin Concentrations by Delaying Intestinal Glucose Absorption

2019 ◽  
Vol 105 (4) ◽  
pp. e1235-e1249 ◽  
Author(s):  
David R Powell ◽  
Brian Zambrowicz ◽  
Linda Morrow ◽  
Carine Beysen ◽  
Marcus Hompesch ◽  
...  
Keyword(s):  
Area Under The Curve ◽  
Postprandial Glucose ◽  
Glucose Absorption ◽  
Oral Glucose ◽  
Double Blind ◽  
Local Inhibition ◽  
Clinical Research Organization ◽  
Sodium Glucose Cotransporter ◽  
Intestinal Glucose Absorption ◽  
Oral Doses

Abstract Context The effect of sotagliflozin (a dual sodium–glucose cotransporter [SGLT] 2 and SGLT1 inhibitor) on intestinal glucose absorption has not been investigated in humans. Objective To measure rate of appearance of oral glucose (RaO) using a dual glucose tracer method following standardized mixed meals taken after single sotagliflozin or canagliflozin doses. Setting Clinical research organization Design and participants In a double-blind, 3-period crossover study (NCT01916863), 24 healthy participants were randomized to 2 cohorts of 12 participants. Within each cohort, participants were randomly assigned single oral doses of either sotagliflozin 400 mg, canagliflozin 300 mg, or placebo on each of test days 1, 8, and 15. On test days, Cohort 1 had breakfast containing [6,6-2H2] glucose 0.25 hours postdose and lunch containing [1-2H1] glucose 5.25 hours postdose; Cohort 2 had breakfast containing no labeled glucose 0.25 hours postdose and lunch containing [6,6-2H2] glucose 4.25 hours postdose. All participants received a 10- to 15-hour continuous [U-13C6] glucose infusion starting 5 hours before their first [6,6-2H2] glucose-containing meal. Main Outcome RaO, postprandial glucose (PPG), and postprandial insulin. Results Sotagliflozin and canagliflozin decreased area under the curve (AUC)0–1 hour and/or AUC0–2 hours for RaO, PPG, and insulin after breakfast and/or the 4.25-hour postdose lunch (P &lt; .05 versus placebo). After the 5.25-hour postdose lunch, sotagliflozin lowered RaO AUC0–1 hour and PPG AUC0–5 hours versus both placebo and canagliflozin (P &lt; .05). Conclusions Sotagliflozin delayed and blunted intestinal glucose absorption after meals, resulting in lower PPG and insulin levels, likely due to prolonged local inhibition of intestinal SGLT1 that persisted for ≥5 hours after dosing.

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