Significant Blood Glucose Lowering Effect Research Articles

Effects of light-intensity physical activity on cardiometabolic parameters in young adults with overweight and obesity: The SED-ACT randomized controlled crossover trial.

To investigate how a change in body position with light-intensity physical activity (PA) 'snacks' (LIPAS, alternate sitting and standing, walking or standing continuously) compared with uninterrupted prolonged sitting affects glucose metabolism and heart rate variability (HRV) parameters in young adults with overweight and obesity. We conducted a four-arm randomized controlled crossover trial. The following conditions were tested during an 8-h simulated workday: uninterrupted prolonged sitting (SIT), alternate sitting and standing (SIT-STAND; 2.5 h total), continuous standing (STAND), and continuous walking (1.0 mph; WALK). The primary outcome was to investigate how a change in body position (alternate sitting and standing, walking or standing continuously) compared with uninterrupted sitting affects mean 8-h glucose metabolism. Secondary outcomes included the effects on 2-h postprandial glucose concentrations, as well as on 8-h/24-h heart rate and HRV parameters, in the respective study arms. Capillary blood samples were drawn from an hyperemised earlobe in the fasted state and once every hour during each trial intervention by puncturing the earlobe with a lancet and collecting 20 μL of blood (Biosen S-Line Lab+; EKF diagnostics, Barleben, Germany). HRV was assessed for 24 h including the 8-h intervention phase, and a home phase by means of a Holter electrocardiogram. All participants received the same standardized non-relativised breakfast and lunch during the four trial visits. Seventeen individuals (eight women, mean age 23.4 ± 3.3 years, body mass index 29.7 ± 3.8 kg/m2, glycated haemoglobin level 34.8 ± 3.1 mmol/mol [5.4 ± 0.3%], body fat 31.8 ± 8.2%) completed all four trial arms. Compared with SIT (89.4 ± 6.8 mg/dL), 8-h mean glucose was lower in all other conditions (p < 0.05) and this was statistically significant compared with WALK (86.3 ± 5.2 mg/dL; p = 0.034). Two-hour postprandial glucose after breakfast was approximately 7% lower for WALK compared with SIT (p = 0.002). Furthermore, significant time × condition effects on HRV parameters favouring light-intensity walking were observed (p < 0.001). Replacement and interruption of prolonged sitting with light-intensity walking showed a significant blood glucose-lowering effect and improved HRV during an 8-h work environment in young adults with overweight and obesity.

Screening of Manilkara zapota (L) P. Royen stem bark ethanolic extract for in vitro \u03b1-glucosidase inhibition, preliminary antidiabetic effects, and improvement of diabetes and its complications in alloxan-induced diabetes in Wistar rats

BackgroundA perusal of the literature suggested that Manilkara zapota (L.) P. Royen stem bark (MZSB) is enriched with several bioactive phytoconstituents but had not been yet screened for its in vitro and in vivo antidiabetic potentials. Thus, the present study aimed to investigate the effects of 70% ethanolic extract of Manilkara zapota (L) P. Royen stem bark (EMZSB) in DPPH- and H2O2-scavenging assay, in vitro α-glucosidase inhibition assay, ameliorating diabetes and its complications in alloxan-induced diabetes in Wistar rats.ResultsWith a maximum extractive yield of 9.16% w/w, EMZSB has shown the presence of various phytochemicals like flavonoids, phenolic compounds, tannins, anthraquinone glycosides, steroids, terpenoids, and alkaloids. EMZSB has elucidated a considerable in vitro free radical scavenging potential by DPPH and H2O2 assays when compared with absolute ethanolic extract of Manilkara zapota (L) P. Royen stem bark (AEMZSB), while ascorbic acid was taken as the standard. Further, EMZSB demonstrated high in vitro α-glucosidase enzyme inhibition potential (IC50 = 119.79 ± 1.52 µg/mL) than AEMZSB (IC50 = 129.92 ± 2.29 µg/mL) with a significant difference (p < 0.01), when acarbose was taken as reference inhibitor (IC50 = 86.43 ± 1.26 µg/mL). During acute toxicity studies EMZSB was safe up to 2000 mg kg−1 doses while, found causing moribund status followed by mortality in mice at 3000 mg kg−1 and above doses. A preliminary antidiabetic study with EMZSB-250 mg kg−1 in normal rats showed no sign of hypoglycemia; however, a dose-dependent antihyperglycemic effects were observed in oral glucose tolerance test in glucose-loaded rats. In vivo assessment with EMZSB-250 mg kg−1 in alloxan-induced rats demonstrated significant blood glucose-lowering effects with perfection in serum lipid profile, body weight enhancement, cardiovascular risk indices, nephroprotective effects, augmentation in liver glycogen content, and histopathological evidence of normal architecture of kidneys with no marks for nephritis.ConclusionsEMZSB-250 showed significant antidiabetic effects and ameliorated diabetic complications by improving glycemic control and accompanying biochemical alteration.

Insulinotropic Potential of Moxifloxacin and Gemifloxacin: An In Vivo Rabbits Model Study Followed by Randomized Phase I Clinical Trial.

Fluoroquinolones (FQs) have been reported to cause dysglycemia in both diabetic and non-diabetic patients. However, diabetic patients are usually on polypharmacy, so we cannot attribute the dysglycemia specifically to FQs. To answer the question as to whether Moxifloxacin and Gemifloxacin influence blood glucose levels and serum insulin levels or otherwise, rabbits were used as experimental animals in an in vivo model followed by a phase I randomized clinical trial in euglycemic healthy volunteers. The effects on the serum insulin and blood glucose levels in the Moxifloxacin and Gemifloxacin treated groups were, respectively, determined on the fifth day in both the in-vivo rabbits model and in the test subjects of the phase I clinical trial. The effects of these drugs were also checked on the histomorphology of the pancreas in the rabbits. The findings of our study suggest that Moxifloxacin and Gemifloxacin significantly (p < 0.05) reduced the blood glucose levels via a subsequent significant shift in the serum insulin levels both in the in vivo animal model and in the test subjects of the phase I clinical trial. No prominent effects on the beta cells histomorphology were noted in this study. Moxifloxacin showed a more significant effect than Gemifloxacin. The insulinotropic effect was comparable to the effect of Glibenclamide. It is concluded that Moxifloxacin and Gemifloxacin have a significant blood glucose lowering effect mediated through insulinotropic action. (Clinical Trials.gov identifier: NCT04692623).

Chemical Profiling and Antihyperglycaemic Study on Butanol Fraction of Chlorophytum alismifolium Baker (Liliaceae)

Purpose: Diabetes mellitus is a disorder associated with debilitating complications. This study was aimed at evaluating the chemical profile and antihyperglycaemic effect of butanol fraction of Chlorophytum alismifolium. Methodology: The powdered plant was extracted sequentially using soxhlet apparatus with solvents of varying polarities until butanol fraction was obtained. GC-MS analysis, phytochemical screening and acute toxicity studies were carried out. Antihyperglycaemic study was carried out using alloxan-induced hyperglycaemia in rats. Male Wistar rats were injected with 120 mg/kg of alloxan intraperitoneally, the rats with fasting blood glucose levels between 200 and 350 mg/dL were considered hyperglycaemic. Experimental groups were set up using normal rats in group I and hyperglycaemic rats in five groups of six rats each. Group II was the hyperglycaemic control while groups III, IV and V received the butanol fraction of C. alismifolium at 250, 500 and 1000 mg/kg respectively. Group VI received glimepiride 1 mg/kg. Blood glucose levels were monitored before treatment at 0 hour and 1, 2, 3 and 5 hours after treatment. Findings: Phytochemical screening revealed the presence of alkaloids, saponins, flavonoids, glycosides and triterpenes while GC-MS analysis revealed the presence of thirteen compounds some of which include; isoxazolidine, isothiazole and acetamide. Oral median lethal dose of the extract in rats was estimated to be >5,000 mg/kg. The butanol fraction of C. alismifolium at all the doses tested showed significant (p<0.05) blood glucose lowering effect when compared over time. Conclusion: The findings from this research showed that butanol fraction of Chlorophytum alismifolium possesses important compounds with antihyperglycaemic activity. Keywords: Chlorophytum alismifolium, Hyperglycaemia, Gas chromatography-mass spectrometry

Therapeutic Efficacy of Ficus Glomerata Leaves in Alloxan Monohydrate Induced Type-1 Diabetes in Albino Rats

Present study was aimed to evaluate the anti-diabetic efficacy of Ficus glomerata in Alloxan monohydrate induced albino rats. Oral administration of fresh Ficus glomerataleaves (2 - 4 g/day) for 60 days shows significant blood glucose lowering effect in experimental alloxan induced diabetic rats. These diabetic rats blood glucose level became normal when fed with Ficus glomerata leaves. It is amply revealed that fresh Ficus glomerata indica leaves possessed anti-diabetic properties. The results suggest that statistically significant anti-diabetic potential in alloxan monohydrate induced diabetic rats. The Ficus glomerata leaves to be almost similar effect like insulin treatment in alloxan monohydrate administered animal model. From the present investigation it appeared that Ficus glomerata leaves might have some ingredients to increase the output of insulin by binding to the receptors of the Beta cells of the Langerhans located in the pancreas. Once they bind to the Sulphonyl urea receptors, the K+ -ATP channels are probably closed and therefore the membrane is depolarized and insulin production is stimulated.

Antidiabetic effect of bio-enhanced preparation of turmeric in streptozotocin-nicotinamide induced type 2 diabetic Wistar rats

BackgroundPoor oral bioavailability of curcumin, the active ingredient in turmeric, has limited its therapeutic use in various diseases including diabetes mellitus (DM). Objective(s)The present study was aimed at evaluating and comparing the antidiabetic activity as well as pharmacokinetic profile of two turmeric extracts. Materials and methodsRats were divided into seven groups (n = 6) including Normal control (NC), Diabetic control (DC), two standard control groups- Glibenclamide (GLIB) 5 mg/kg and Metformin (MET) 500 mg/kg, two bio-enhanced turmeric extract (BTE) treated groups (BTE-30 (30 mg/kg), BTE-60 (60 mg/kg)) and one regular turmeric extract treated (RTE) group RTE-30 (30 mg/kg). Treatment was given orally for 30 days. Streptozotocin (60 mg/kg) and Nicotinamide (110 mg/kg) were administered intraperitoneally to induce diabetes. Fasting blood glucose (FBG), oral glucose tolerance test at 60 min and 120 min (OG1 and OG2) were analysed at baseline and at the end of study on Day 29. FBG, fasting serum insulin, and concentration of curcumin and its derivatives present in pancreas were analysed at the end of study on Day 30. ResultsTurmeric extract treated groups showed significant (p < 0.05) blood glucose lowering effect, when compared with DC group. FBG, OG1 and OG2 readings were found significantly (p < 0.05) higher in RTE-30 treated group when compared with BTE-30 treated groups. Turmeric extracts showed improved beta-cell function, insulin sensitivity and decreased insulin resistance. BTE-30 had more pancreatic bioavailability of curcumin than RTE-30. ConclusionTurmeric extracts demonstrated an antidiabetic effect in streptozotocin-nicotinamide induced type 2 diabetic Wistar rats. BTE extract was found to be an effective agent as compared to RTE in controlling hyperglycemia.

Effect of Aglycon and Glycoside Flavonoid-Enriched Extracts Obtained from Buxus sempervirens L. on Glucose and Lipid Metabolism in Diabetic Rats.

Buxus sempervirens L. is a medicinal plant with several beneficial effects on health and is widely used in Moroccan folklore as an antidiabetic plant. The aim of this study was to evaluate the antidiabetic effect of both aglycone and glycoside flavonoid enriched extracts of this plant in the experimental diabetic state. In the current work, the effect of aglycone and glycoside flavonoid-enriched extracts from the leaves of Buxus sempervirens L. (AFBS and GFBS) (10 mg/kg) on blood glucose levels has been evaluated in normal and streptozotocin (STZ) diabetic rats. Moreover, the histopathological changes in the liver and pancreas have been assessed in STZ diabetic rats. The ability of AFBS and GFBS to improve glucose tolerance in normal rats was also evaluated. In normal rats, both a single and repeated administration of AFBS and GFBS (10 mg/kg) showed no significant effects on blood glucose levels. However, both single and repeated oral administration of the two fractions showed a significant blood glucose lowering effect (p<0.0001) in STZ rats. In addition, histopathological analysis has demonstrated the beneficial impact of AFBS and GFBS on the pancreas and liver. Whereas, the oral glucose tolerance test demonstrated no significant ability of these extracts to improve the increase in blood glucose levels in normal and diabetic treated rats. In the current study, no significant changes in body weight in normal and STZ rats have been shown. In addition, the antioxidant activity of both AFBS and GFBS revealed the antioxidant effect of both extracts. Furthermore, both flavonoid-enriched fractions had no significant effect on blood lipid levels. In conclusion, AFBS and GFBS exhibited an interesting antidiabetic effect on streptozotocin rats and GFBS which seems to be more effective than AFBS.

Evaluation of in vitro and in vivo Anti-Diabetic, Anti-Hyperlipidemic and Anti-Oxidant Activity of Flower Crude Extract and Solvent Fractions of Hagenia Abyssinica (Rosaceae).

BackgroundThe flower of Hagenia abyssinica (Rosaceae) has been used in traditional health systems to treat diabetes mellitus in Ethiopia and Tanzania. However, the antidiabetic activity of this medicinal plant is not scientifically validated and authenticated. The present study aimed to investigate the in vitro and in vivo anti-diabetic activity of flower crude extract and solvent fractions of Hagenia abyssinica.MethodsThe in vitro α–amylase inhibition and antioxidant activity of the crude extract and solvent fractions of Hagenia abyssinica were evaluated by using 3,5-dinitrosalicylic acid (DNSA) and diphenyl-2-picrylhydrazyl (DPPH) assay model, respectively. Blood glucose lowering activity of 80% methanolic flower crude extract and solvent fraction was studied in four animal models: normoglycemic mice model, oral glucose loaded mice model, single dose-treated streptozotocin-induced diabetic mice model, and repeated dose-treated streptozotocin-induced diabetic mice model. The effect of the crude extract and solvent fraction of Hagenia abyssinica on diabetic lipid profile and body weight was also studied.ResultsThe acute toxicity study of Hagenia abyssinica flower extract did not show mortality in the animals at the limit dose of 2g/kg during the observation period. The result of α–amylase enzyme inhibition activity was found in a dose-dependent manner, the strongest activity was shown by ethyl acetate fraction (54.23% inhibition at 800 μg/mL) compared to the standard acarbose having 91.87% inhibition at 800 μg/mL. Among these extracts, the crude extract had the highest antioxidant activity (58.38% inhibition at 500 μg/mL). The crude extract of H. abyssinica showed significant blood glucose-lowering effect on normoglycemic mice and oral glucose loaded mice. In streptozotocin-induced diabetic mice model, the crude extract and ethyl acetate fraction significantly decreased the fasting blood glucose level after 14 days of treatment. There were significant reductions in serum total cholesterol, serum triglycerides, very low-density lipoprotein, and low-density lipoprotein. However, there were significant increments in body weight and high-density lipoprotein as compared to untreated diabetic mice.ConclusionThe result demonstrated the beneficial biochemical effects of Hagenia abyssinica extract by inhibiting α–amylase, scavenging diphenyl-2-picrylhydrazyl (DPPH) and improving serum lipid profile levels. The flower crude extract and solvent fractions of Hagenia abyssinica are effective in lowering blood glucose levels in diabetic and normoglycemic mice. The claimed traditional use as antidiabetic has scientific ground.

The first assessment on antioxidant and antidiabetic activities of leaves and stems of Vaccinium secundiflorum Hook. (Ericaceae), an endemic plant of Madagascar

Vaccinium secundiflorum Hook. (Ericaceae family) is an endemic shrub of the Tapia forests of Madagascar widely used by local Malagasy population to treat diabetes mellitus. This study aims to preliminarily determine the antioxidant activity and anti-diabetic properties of this plant. Plant leaf and stem powders were macerated in methanol 95%. The methanol extract (MVS) was used for (i) phytochemical fingerprint by High Performance Liquid Chromatography (HPLC), (ii) total phenolic content (TPC) evaluation by the Folin–Ciocalteu colourimetric method, (iii) 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenger spectrophotometric assay, (iv) antioxidant capacity by Ferric Reducing Antioxidant Power (FRAP) assay, and (v) antidiabetic activity evaluation by oral glucose tolerance test and acute toxicity in mice. Leaves and stems of V. secundiflorum presented a high rate of TPC (4151.02 ± 745.21mgGAE/100 g of dry weight). The HPLC fingerprint analysis showed the presence of several secondary metabolite classes including organic acids (55.31%), phenolic compounds (29.66%), carotenoids (10.90%), vitamin C (3.96%), and monoterpenes (0.10%). The DPPH free radical scavenger spectrometric assay showed a MVS high potential scavenging activity (IC50 = 76.06 ± 1.08 µg/mL). This potential antioxidant capacity was confirmed by the FRAP assay results (69.31 ± 3.31 mmol Fe2+/Kg of dry weight). The oral glucose tolerance test in mice showed a highly significant blood glucose-lowering effect. The acute toxicity in mice revealed that the MVS did not show toxicity at the dose of 2000 mg/kg. Leaves and stems of V. secundiflorum showed significant antioxidant and antidiabetic properties supporting the plant traditional use, even if further studies on bioactive compounds and their action mechanisms should be carried out to confirm these preliminary results.

Standardized Extract from Enicostemma littorale Ameliorates Post-prandial Hyperglycaemia in Normal and Diabetic Rats

Enicostemma littorale Blume (Gentianaceae) is traditionally used medicinal plant. It is locally known as Chota Chirata. It is used for the treatment of various ailments including diabetes in Indian subcontinent. Its main constituent is a secoiridoid glycoside namely swertiamarin. The aim of current study was to evaluate swertiamarin-rich fraction of E. littorale in controlling post prandial hyperglycemia through the inhibition of carbohydrate metabolizing enzymes in in-vitro and in-vivo studies. Standardized extract of E. littorale (SEL) was prepared by ultrasound assisted extraction (UAE) and its swertiamarin content was estimated by HPTLC. The content of swertiamarin was found to be 13.62 ± 1.46 (% w/w) in SEL on dry weight basis. The effect on α-amylase and α-glucosidase was evaluated in-vitro. It was followed by antihyperglycemic studies in carbohydrate challenged normal and STZ-induced diabetic rats. SEL was found to inhibit α-amylase and α-glucosidase with IC50 values of 12.29 ± 0.31 mg/ml and 9.42 ± 0.61 mg/ml, respectively. In-vivo studies with normal and diabetic rats revealed that the treatment with SEL (200 mg/kg b.w.), twenty minutes prior to carbohydrate challenge produced significant (p < 0.01) blood glucose lowering effect in both the models. The present study clearly indicates the beneficial effects of swertiamarin-rich fraction of E. littorale in controlling post prandial hyperglycemia.

Evaluation of In Vivo Antidiabetic, In Vitro α-Amylase Inhibitory, and In Vitro Antioxidant Activity of Leaves Crude Extract and Solvent Fractions of Bersama abyssinica Fresen (Melianthaceae).

Background.The leaves of Bersama abyssinica are used for the treatment of diabetes mellitus in folk medicine system of Ethiopia. The present study was done based on the traditional claim of B abyssinica for the treatment of diabetes mellitus.Methods.The α-amylase inhibition and antioxidant activities of B abyssinica extracts were evaluated by using 3,5-dinitrosalicylic acid method and diphenyl-2-picrylhydrazyl assay model, respectively. Blood glucose lowering activity of the extracts was studied in 4 animal models; normoglycemic, oral glucose loaded, and streptozotocin-induced diabetic mice models.Results.Among the extracts, the crude extract showed the highest α-amylase enzyme inhibition activity with an IC50 of 6.57 μg/mL. The water fraction showed the strongest antioxidant activity with an IC50 of 3.43 μg/mL. The crude extract at doses of 200, and 400 mg/kg showed significant (P < .05) hypoglycemic activity in normoglycemic mice. All doses of the crude extract significantly (P < .05) reduced blood glucose levels of oral glucose-loaded mice. In streptozotocin-induced diabetic mice models, both the crude and solvent fractions showed a significant (P < .05) blood glucose lowering effect as compared with the negative control group post 8 hour treatment.Conclusion.The results demonstrated the beneficial biochemical effects of B abyssinica extract by inhibiting α-amylase and scavenging the free radicals. The crude extract and solvent fractions of B abyssinica had significant blood glucose lowering effect in all animal models.

Therapeutic Potential of Aegle marmelos (Linn.) Leaves in Alloxan Monohydrate Induced Type-1 Diabetes in Experimental Rats

Present study was aimed to evaluate the anti-diabetic activity of Aegle marmelos in Alloxan monohydrate induced albino rats. Oral administration of fresh Aegle marmelos leaves (2 - 4 g/day) for 28 days shows significant blood glucose lowering effect in experimental alloxan induced diabetic rats. These diabetic rats blood glucose level became normal when fed with Aegle marmelos leaves. It is amply revealed that Aegle marmelos leaves possessed anti-diabetic and beta cells restoration properties. The results suggest that statistically significant anti-diabetic potential in alloxan monohydrate induced diabetic rats. The Aegle marmelos leaves to be almost similar effect like insulin treatment in alloxan monohydrate administered experimental animal model. From the present study it appeared that Aegle marmelos might have some key ingredients to increase the output of insulin by binding to the receptors of the Beta cells of the Langerhans located in the pancreas. Once they bind to the Sulphonyl urea receptors, the K+ -ATP channels are probably closed and therefore the membrane is depolarized and insulin production is stimulated. During the course of study, Aegle marmelos leaves fed experimental animals were normal blood glucose levels compared to insulin treated animals.

Discovery of novel pyridazine derivatives as glucose transporter type 4 (GLUT4) translocation activators.

We report herein the synthesis and structure-activity relationships (SAR) of a series of pyridazine derivatives with the activation of glucose transporter type 4 (GLUT4) translocation. Through a cell-based phenotype screening in L6-GLUT4-myc myoblasts and functional glucose uptake assays, lead compound 1a was identified as a functional small molecule. After further derivatization, the thienopyridazine scaffold as the central ring (B-part) was revealed to have potent GLUT4 translocation activities. Consequently, we obtained promising compound 26b, which showed a significant blood glucose lowering effect in the severe diabetic mice model (10-week aged db/db mice) after oral dosing even at 10 mg/kg, implying that our pyridazine derivatives have potential to become novel therapeutic agents for diabetes mellitus.

Thrombolytic, Membrane Stabilizing and Hypoglycemic Activities of Anethum sowa Linn.

The hexane (HE), dichloromethane (DCME), ethyl acetate (EAE) and methanol (ME) extracts of seed and stem of Anethum sowa were subjected to screenings for thrombolytic, membrane stabilizing and hypoglycemic activities. Ethyl acetate extract of stem showed highest thrombolytic activity. In addition, the dichloromethane, ethyl acetate and methanol extract of seed revealed higher percentage (%) of inhibition in hypotonic solution induced hemolysis. In hypoglycemic activity, the dichloromethane and ethyl acetate extracts of stem and seed displayed significant blood glucose lowering effect.&#x0D; Dhaka Univ. J. Pharm. Sci. 17(2): 237-241, 2018 (December)

Antidiabetic Effect of Spearmint in Streptozotocin-Induced Diabetic Rats.

Mentha spicata is a medicinal plant with several beneficial effects on health. The objective of this study was to evaluate the antidiabetic effect of this plant in the experimental diabetic state. In this work, the effect of Mentha spicata (L.) (M. spicata) aerial part aqueous extract (A.P.A.E) at a dose of 20 mg/kg body weight on blood glucose levels has been demonstrated in normal and streptozotocin (STZ) diabetic rats. Additionally, a preliminary phytochemical screening for various bioactive constituents was realized and a dosage of polyphenols and flavonoid has been done. Moreover, the histopathological changes in liver and pancreas have been evaluated both in normal and STZ diabetic rats. The effect of M. spicata aqueous extract to improve glucose tolerance in normal rats was also evaluated. In normal rats, both a single and repeated administration of the A.P.A.E (20 mg/kg) had not shown a significant reduction in blood glucose levels. However, repeated oral administration of M. spicata aqueous extract showed a significant blood glucose lowering effect (p<0.0001) in STZ diabetic rats. The blood glucose lowering activity of A.P.A.E was comparable to glibenclamide treatment at the dose used. Also, a histopathological study has showed the better act of M. spicata in pancreas and liver. Moreover, the oral glucose tolerance test demonstrated the ability of the aqueous extract (20 mg/kg) to improve the increase in blood glucose levels in normal treated rats. In the current study, no significant changes in body weight in normal and STZ rats have been shown. In addition, the preliminary phytochemical screening of M. spicata A.P.A.E. showed the presence of several beneficial compounds including polyphenols, flavonoids, anthraquinones, tannins, saponins, sterol, glucides, glycosides, terpenoids and reducing sugars. Furthermore, the result of dosage of some bioactive compounds present in this plant showed an important value of polyphenol (424.37±43.93 mg EAG) and showed also a non-negligible content of flavonoid. (9.74 ±0.39 mg EQ/g of extract). In conclusion, aqueous M. spicata extract exhibits an interesting antidiabetic effect in streptozotocin rats.

Synthesis, docking, in vitro and in vivo antidiabetic activity of pyrazole-based 2,4-thiazolidinedione derivatives as PPAR-γ modulators.

The design, synthesis, structure-activity relationship, and biological activity of 2,4-thiazolidinedione derivatives as peroxisome proliferator-activated receptor-γ (PPAR-γ) modulators for antidiabetic activity are reported. Fifteen 2,4-thiazolidinedione derivatives clubbed with pyrazole moiety were docked into the ligand binding domain of PPAR-γ by the Glide XP module of Schrodinger. Eight derivatives (5a, 5b, 5d, 5f, 5i, 5l, 5n, 5o) having Glide XP scores > -8 as compared to the standard drug, rosiglitazone (Glide XP score = -9.165), showed almost similar interaction with the amino acids such as HIS 449, TYR 473, TYR 327, HIS 323, and SER 289 in the molecular docking studies. These eight derivatives were further screened for PPAR-γ transactivation and in vivo blood glucose lowering activity in the streptozotocin-induced diabetic rat model. Compounds 5o, 5n, 5a, 5i, and 5b showed 52.06, 51.30, 48.65, 43.13, and 40.36% PPAR-γ transactivation as compared to the reference drugs rosiglitazone and pioglitazone with 85.30 and 65.22% transactivation, respectively. The data analysis showed significant blood glucose lowering effects (hypoglycemia) of compounds 5o, 5n, and 5a (140.1 ± 4.36, 141.4 ± 6.15, and 150.7 ± 4.15, respectively), along with reference drugs pioglitazone (135.2 ± 4.91) and rosiglitazone (141.1 ± 5.88) as compared to the diabetic control. Furthermore, the most potent compound 5o also elevated the PPAR-γ gene expression by 2.35-fold as compared to rosiglitazone (1.27-fold) and pioglitazone (1.6-fold). It also significantly lowered the AST, ALT, and ALP levels and caused no damage to the liver.

Anti-hyperglycaemic activity of tuber extract of Chlorophytum alismifolium Baker in streptozotocin-induced hyperglycaemic rats

The tubers of Chlorophytum alismifolium (Liliaceae) are widely used in Nigerian Herbal Medicine to treat diabetes mellitus and their efficacy is widely acclaimed among the rural communities of Northern Nigeria. This study was aimed at investigating the antihyperglycaemic potential of the tuber extract of Chlorophytum alismifolium (CAE) in streptozotocin-induced hyperglycaemic rats. Phytochemical screening and oral median lethal dose (LD50) estimation of CAE in rats were carried out. Antihyperglycaemic screening of the extract (at oral doses of 150, 300 and 600 mg/kg) was performed using normal and streptozotocin-induced hyperglycaemic rats for 28 days. Fasting blood glucose levels were measured and serum lipids were analyzed. Liver, kidney, heart and pancreatic tissues were examined for histopathological damages using standard histological processing. Phytochemical screening revealed the presence alkaloids, saponins, flavonoids, triterpenes and glycosides. Oral LD50 was estimated to be >5000 mg/kg body weight in rats. C. alismifolium extract at all the doses tested showed blood glucose lowering effect. Statistical significant (p < .01) blood glucose lowering effect at 150 mg/kg on day 21, at 300 mg/kg on days 21 and 28 (p < .001 and p < .01 respectively) and 600 mg/kg on days 7, 14, 21 and 28 (p < .05, p < .01, p < .001 and p < .01 respectively) was produced by the extract. The extract also reduced the levels of total cholesterol, triglycerides and low density lipoprotein. Histopathological examination of the pancreas showed restoration of pancreatic islet cells at the doses of 300 and 600 mg/kg of the extract. In conclusion, the results obtained suggest the tuber extract of Chlorophytum alismifolium possesses antihyperglycaemic activity.

English

The leaves of Ajuga remota benth have been utilized traditionally for the treatment of patients with diabetes mellitus. However, its use has not been scientifically validated. The present study was therefore, aimed to assess the antihyperglycemic and antihyperlipidemic activities of ethanol extract of A. remota leaves in streptozotocin (STZ) induced diabetic rats. Antihyperglycemic and antihyperlipidemic activities of ethanol extract of A. remota leaves (AREt) were studied in streptozotocin induced diabetic rats. The effect of extract on fasting blood glucose, body weight, lipid profile, serum, alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, urea, creatinine and total protein were analyzed. Glibenclamide was used as standard drug. Ethanol extract of A. remota leaves has showed significant blood glucose lowering effect as compared to the diabetic control group. After diabetic rats were treated with 200 and 400 mg/kg ethanol extract of A. remota leaves for 28 days, there were a significant decrease in fasting blood glucose, total cholesterol, triacylglycerol, low density lipoprotein cholesterol, serum alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase, and significant increase in body weight, serum total protein, high density lipoprotein cholesterol levels as compared to untreated control diabetic rats. The results of the present study showed that ethanol extract of A. remota leaves might be useful for management of diabetes mellitus and other associated abnormalities. The present study might support the traditional use of A. remota for diabetes mellitus treatment. Key words: Ajuga remota benth, diabetes mellitus, streptozotocin.

Phytochemical Screening and Hypoglycaemic Effect of Methanol Extract of Solanum anomalum Thonn. Fruits in Alloxan induced Hyperglycaemic and Normal Wistar Rats

The study investigated the hypoglycaemic effect of methanol extract of Solanum anomalum fruit. Extraction of the powdered fruit was done with 90% methanol. Rats were divided into five groups of five rats per group. Hyperglycaemia was induced using alloxan at a dose of 150 mg/kg in groups two to five. Groups one to five received distilled water 2 ml/kg (normal control), distilled water 2 ml/kg (diabetic control), S. anomalum extract 500 mg/kg, S. anomalum extract 1,000 mg/kg and glibenclamide 10 mg/kg respectively. The treatment was continued for 14 days during which blood glucose levels were monitored. Phytochemical screening revealed the presence carbohydrate, cardiac glycosides, saponins, tannins, flavonoids and alkaloids. The oral LD50 was found to be above 5,000 mg/kg. The methanol extract of S. anomalum fruit at 1,000 mg/kg showed a statistically significant blood glucose lowering effect (p<0.05) between the blood glucose level at zero hour (337.8 ± 29.4 mg/dL) and blood glucose level after 24 h (317.4 ± 21.5 mg/dL) for the groups being administered with the extract. The groups receiving 500 mg/kg and 1,000 mg/kg of the extract showed a statistical significant blood glucose lowering (p<0.05) between the blood glucose level at day zero (329 ± 34 and 337 ± 29 mg/dL) was compared to the blood glucose at day 15 (237 ± 32 and 143 ± 15 mg/dL). In conclusion, methanol extract of S. anomalum fruit contains one or more active agents that has anti-hyperglycaemic and hypoglcaemic activity in alloxan induced hyperglcaemic and normoglycaemic rats.

Efficacy of the Hydroalcoholic Extract of Tribulus terrestris on the Serum Glucose and Lipid Profile of Women With Diabetes Mellitus: A Double-Blind Randomized Placebo-Controlled Clinical Trial.

Considering traditional use of Tribulus terrestris in diabetes and proven antihyperglycemic and antihyperlipidemic effects of T terrestris in animal studies, we aimed to evaluate the efficacy of the hydroalcoholic extract of T terrestris on the serum glucose and lipid profile of women with non-insulin-dependent diabetes mellitus. Ninety-eight women with diabetes mellitus type 2 were randomly allocated to receive the T terrestris (1000 mg/d) or placebo for 3 months. The patients were evaluated in terms of the fasting blood glucose, 2-hour postprandial glucose, glycosylated hemoglobin, and lipid profile. Tribulus terrestris showed a significant blood glucose-lowering effect in diabetic women compared to placebo (P < .05). Also, the total cholesterol and low-density lipoprotein of T terrestris group was significantly reduced compared with placebo, while no significant effect was observed in the triglyceride and high-density lipoprotein levels. The study showed preliminary promising hypoglycemic effect of T terrestris in women with diabetes mellitus type 2.