Antihyperglycemic activity of the aqueous extract of Urtica dioica

When administered 30 min before glucose loading, the aqueous extract of Urtica dioica (nettle) (250 mg/kg) showed a strong glucose lowering effect. The decrease of glycemia has reached to 33+/-3.4% of the control value 1 h after glucose loading. This effect was persistent during 3 h. In contrast, nettle did not show hypoglycemic effect in alloxan-induced diabetic rats. The amount of glucose absorbed in a segment jejunum in situ was 8.05+/-0.68 mg in presence of nettle extract vs. 11.11+/-0.75 mg in control rats during 2 h (P<0.05). The results indicate that nettle has a significant antihyperglycemic effect in OGTT model. This effect may be caused in part by the reduction of intestinal glucose absorption. LD(50) is 3.5 g/kg (i.p.).     

Effects of Bauhinia megalandra aqueous leaf extract on intestinal glucose absorption and uptake by enterocyte brush border membrane vesicles

Aqueous extract of Bauhinia megalandra leaves was able to inhibit the intestinal glucose absorption in a concentration-dependent way and additive to phlorizine. Moreover, B. megalandra leaf extract drastically reduced the 14C-glucose uptake by enterocyte brush border membrane vesicles. The B. megalandra leaf extract administrated orally, simultaneously with glucose improved the glucose tolerance with a significant reduction of the 30-min peak. The extract did not have an effect on the glucose tolerance when glucose was administrated subcutaneously.     

Hypoglycemic and hypocholesterolemic activities of the aqueous leaf and seed extract of Phyllanthus amarus in mice

The effect of the aqueous leaf and seed extracts of Phyllanthus amarus at oral dose of 150, 300 and 600 mg/kg was investigated for their antidiabetic and anti-lipidemic potentials. The extract produced a dose-dependent decrease in the fasting plasma glucose and cholesterol, and reduction in weights in treated mice. The results suggest that the extract could be enhancing peripheral utilization of glucose but the mechanisms on how this works remain unclear.     

Hypoglycemic and antidiabetic activities on the stem bark aqueous and ethanol extracts of Musanga cecropioides in normal and alloxan-induced diabetic rats

Daily oral administration of the aqueous and ethanolic extracts of Musanga cecropioides stem bark in normal and diabetic rats at doses of 250, 500 and 1000 mg/kg/day, for 14 days significantly lowered the fasting plasma glucose levels in normal and alloxan-induced diabetic rats in dose-dependent fashion. The ethanol extract induced more significant antidiabetic effect than the aqueous extract.     

Inhibition of glucose intestinal absorption by kaempferol 3-O-α-rhamnoside purified from Bauhinia megalandra leaves

Glucose intestinal absorption (GIA) is one of the factors that increase glycemia. Its reduction could be an important factor in decreasing hyperglycemia in diabetic patients. It has been shown that the aqueous extract of Bauhinia megalandra leaves inhibits GIA. In the present study we identified a compound present in the extract of B. megalandra responsible for the biological effect. The methanol extract of B. megalandra leaves was fractionated using different solvents, and high-speed counter-current chromatography yielding two pure compounds identified by ¹H NMR and ¹³C NMR as kaempferol 3-O-α-rhamnoside and quercetin 3-O-α-rhamnoside. The first one increased the K_M without changes in the V_MAX of GIA. In addition it exerted an additive inhibitory effect, on GIA, when combined with phlorizin. We suggest that kaempferol 3-O-α-rhamnoside is a competitive inhibitor of intestinal SGLT1 cotransporter.     

Improving permeability and oral absorption of mangiferin by phospholipid complexation

Mangiferin is an active ingredient of medicinal plant with poor hydrophilicity and lipophilicity. Many reports focused on improving aqueous solubility, but oral bioavailability of mangiferin was still limited. In this study, we intended to increase not only solubility, but also membrane permeability of mangiferin by a phospholipid complexation technique. The new complex's physicochemical properties were characterized in terms of scanning electron microscopy (SEM), differential scanning calorimetry (DSC), infrared absorption spectroscopy (IR), aqueous solubility, oil–water partition coefficient and in vitro dissolution. The intestinal absorption of the complex was studied by the rat in situ intestinal perfusion model. After oral administration of mangiferin–phospholipid complex and crude mangiferin in rats, the concentrations of mangiferin were determined by a validated RP-HPLC method. Results showed that the solubility of the complex in water and in n-octanol was enhanced and the oil–water partition coefficient was improved by 6.2 times and the intestinal permeability in rats was enhanced significantly. Peak plasma concentration and AUC of mangiferin from the complex (C_max: 377.66 μg/L, AUC: 1039.94 μg/L*h) were higher than crude mangiferin (C_max: 180 μg/L, AUC: 2355.63 μg/L*h). In view of improved solubility and enhanced permeability, phospholipid complexation technique can increase bioavailability of mangiferin by 2.3 times in comparison to the crude mangiferin.     

Hypoglicemic effect of Leandra lacunosa in normal and alloxan-induced diabetic rats

Leandra lacunosa, popularly known as "erva-do-jabuti", is used in Brazilian folkloric medicine for the treatment of diabetes mellitus. Based on this traditional indication, the aim of this work was to evaluate the hypoglycemic activity of the hydroalcoholic extract of L. lacunosa aerial parts (LLH) in normal and alloxan-induced diabetic rats. Chromatographic fractionation of LLH was also carried out by several techniques, affording isolation of the following major compounds: ursolic acid (1), kaempferol (2), luteolin (3), and quercetin (4). The oral administration of LLH (500 mg/kg) in normal rats caused a significant reduction of 24.7% (P<0.05) in the blood glucose levels after 2 h of treatment, while the administration of chlorpropamide (20 mg/kg, p.o.) led to a reduction of 40.2% (P<0.01). After oral administration of glucose (10 g/kg, p.o.), LLH (500 mg/kg, p.o.) significantly inhibited the increase in blood glucose levels compared with the negative control group. The oral treatment with LLH (500 mg/kg) in alloxan-induced diabetic rats significantly reduced the blood glucose levels in 47.8% after 4 h of treatment, while chlorpropamide resulted in a significant reduction of 71.7% in the 4th hour. Our results showed that LLH, displays hypoglycemic activity, which may be related to the effect of the major compounds identified in the crude extract. This study seems to provide biological evidence for the folkloric use of L. lacunosa in the treatment of diabetes mellitus.     

Antidiabetic properties of aqueous barks extract of Parinari excelsa in alloxan-induced diabetic rats

The aqueous extract of the Parinari excelsa barks at doses of 100 and 300 mg/kg/day for 7 days has a significant antihyperglycemic effect on alloxan-induced diabetic rats. At the same dose the acute oral administration of aqueous extract of the P. excelsa barks (100 and 300 mg/kg) induced a significant decrease of blood glucose on glucose-loaded normoglycaemic rats. Our results seem to confirm the rational bases for its use in traditional medicine.     

Relaxant effect of aqueous extract of Cistus ladaniferus on rodent intestinal contractions

The effects of the aqueous extract of Cistus ladaniferus leaves and stems were studied on the rodent isolated jejunum. The extract produced a reversible concentration dose-dependent (0.1-3 mg/ml) inhibition of the spontaneous motility of the rabbit jejunum. The inhibitory effects of the extract were not affected by pretreatment with the inhibitors of the alpha and beta adrenergic receptors yohimbine, prazosin or propranolol. The extract also inhibited K(+)-induced contractions in rabbit and rat jejunum at a similar concentration range. This result suggests that the antispasmodic action of the extract is mediated through calcium channel blockade. The results confirm the traditional use of C. ladaniferus in treating intestinal ache.     

Inhibition of dipeptidyl peptidase activity by flavonol glycosides of guava (Psidium guajava L.): A key to the beneficial effects of guava in type II diabetes mellitus

Based on the traditional use in popular medicine, the effect of extracts from Psidium guajava L. leaves and of the main flavonol-glycoside components on dipeptidyl-peptidase IV (DP-IV), a key enzyme of blood glucose homoeostasis, has been investigated in-vitro. An ethanolic extract was prepared from dried, powdered leaves of guava and was found to contain seven main flavonol-glycosides, which were isolated by semipreparative HPLC and tested individually. The ethanolic guava leave extract was shown to exert a dose-dependent inhibition of DP-IV, with an IC₅₀ of 380 μg/ml test assay solution. Also the individual flavonol-glycosides inhibited DP-IV dose-dependently, with variations of the effects by a factor of 10, and an overall effect accounting for 100% of that observed for the total guava extract. The recovery of individual flavonol-glycosides in CaCo-2 epithelial cells, a model of gastrointestinal tract absorption, amounted to 2.3–5.3% of the amount available for absorption over 60 min at 37 °C.     

Beneficial effect of Embelia ribes ethanolic extract on blood pressure and glycosylated hemoglobin in streptozotocin-induced diabetes in rats

Embelia ribes (common name, Vidanga) is extensively used in traditional system of medicine for treatment of various disorders. It is described in Ayurveda, as a powerful anthelmintic, antifertility and antihyperlipidemic agent. The present study was undertaken to investigate modulatory effect of 6 weeks' chronic oral administration of E. ribes ethanolic extract on diabetes mellitus induced by a diabetogen, streptozotocin (STZ) with special reference to changes in glucose levels, glycated haemoglobin status and cardiac toxicity. STZ treatment (40 mg/kg iv) resulted in significant increase in blood glucose levels, glycated haemoglobin levels, heart rate (HR) and systolic blood pressure (SBP). Oral administration of E. ribes ethanolic extract in dose of 100 mg/kg and 200 mg/kg significantly reduced the levels of blood glucose, glycated haemoglobin, heart rate (HR) and systolic blood pressure (SBP) in animals when compared with diabetic rats.     

Morphological evidences for onion-induced growth inhibition of Trichophyton rubrum and Trichophyton mentagrophytes

The antifungal activity of onion (Allium cepa L.) on two important dermatophytes, Trichophyton rubrum and Trichophyton mentagrophytes, with special reference to morphological aspects was studied. Growth of both fungi was found to be strongly inhibited by aqueous onion extract (AOE) as a dose-dependent manner. The extract showed fungicidal effect for both fungi at concentrations >3.12% (v/v). The fungus T. mentagrophytes was more affected by the onion as compared to T. rubrum at all concentrations used. Morphological effects of onion exposure were examined in correlation with fungal growth. Corresponding to the growth inhibition, light and electron microscopy observations revealed morphological anomalies in hyphal compartments. The results demonstrated that AOE targets the cell membrane of the fungi as breaking down of both inner and outer membranes with consequent extrution of materials into the surrounding medium. Cytoplasmic membranes and other membranous structures of organelles, such as nuclei and mitochondria, were also disrupted. In correlation to the fungal growth, morphological alterations occurred to a less content for T. rubrum compared with T. mentagrophytes. The hyphae of T. rubrum were found to be mainly affected by converting to resistant forms, i.e., chlamidospores as a consequence of phenotype switching response to AOE. Plasmolysis accompanied by an almost complete depletion and disorganization of cytoplasmic structures were found to be the final event which led to cell death. Ultrastructural evidences obtained from this study strongly support that morphological changes of T. rubrum and T. mentagrophytes caused by AOE are associated with its fungistatic and fungicidal activities. With respect to the morphological results and the preliminary data on fungal biochemistry, a mechanism of action by interacting of AOE with thiol (-SH) groups present in essential compartments of the fungal cells was postulated.     

Hypoglycemic effect of Mucuna pruriens seed extract on normal and streptozotocin-diabetic rats

The hypoglycemic effect of the aqueous extract of the seeds of Mucuna pruriens was investigated in normal, glucose load conditions and streptozotocin (STZ)-induced diabetic rats. In normal rats, the aqueous extract of the seeds of Mucuna pririens (100 and 200 mg/kg body weight) significantly (P<0.001) reduced the blood glucose levels after an oral glucose load from 127.5+/-3.2 to 75.6+/-4.8 mg% 2 h after oral administration of seed extract. It also significantly lowered the blood glucose in STZ diabetic rats from 240.5+/-7.2 to 90.6+/-5.6 mg% after 21 days of daily oral administration of the extract (P<0.001). Thus, this study shows that M. pruriens has an anti-hyperglycemic action and it could be a source of hypoglycemic compounds.     

Antihyperglycemic effect of Cucurbita ficifolia fruit extract in streptozotocin-induced diabetic rats

In the present study, the antihyperglycemic effects of Cucurbita ficifolia fruit extract were investigated on streptozotocin-induced experimental diabetes in rats. Oral administration of the extract (300 and 600 mg/kg body weight, day) for 30 days resulted in a significant reduction in blood glucose, glycosylated haemoglobin, and an increase in plasma insulin and total haemoglobin. The effect was compared with 150 mg/kg b.w. tolbutamide.     

Myorelaxant and antispasmodic effects of the aqueous extract of Mitragyna inermis barks on Wistar rat ileum

Mitragyna inermis is used in the Senegal traditional medicine for treating stomach and intestinal disorders. At concentrations of 0.5, 0.75 and 1 mg/ml, the aqueous extract of M. inermis bark (AEMIB) significantly induced a decrease of the ileal basal tonus, respectively, from 37+/-1, 51+/-1 and 75+/-2% (P<0.05; n=5), compared to the baseline values. As well as atropine, AEMIB inhibited submaximal contractions induced by 0.01 mg/ml ACh with IC(50) value of approximately 0.75 mg/ml (n=5). These results show that AEMIB possesses both myorelaxant and antispasmodic actions in the ileum. This may justify the pharmacological basis for the popular use of Mitragyna for the treatment of gastrointestinal disorders.     

Effect of Mitragyna speciosa aqueous extract on ethanol withdrawal symptoms in mice

Administration of the aqueous extract of Mitragyna speciosa at a dose of 300 mg/kg significantly inhibited ethanol withdrawal-induced behaviors that included rearing, displacement and head weaving. The results also showed that at doses of 100, 300 and 500 mg/kg M. speciosa showed antidepressant activity without effect on the spontaneous motor activity.     

Hypoglycaemic activity of Alpinia galanga rhizome and its extracts in rabbits

This investigation was carried out to study effects of Alpinia galanga rhizome on blood glucose levels. In normal rabbits, powdered rhizome and its methanol and aqueous extracts significantly lowered the blood glucose. Gliclazide also produced a significant decrease in blood glucose in the rabbits. In alloxan-diabetic rabbits, A. galanga and its methanol and aqueous extracts did not produce significant reduction in blood glucose. The hypoglycaemic effect of A. galanga in normal rabbits was comparable to gliclazide. The rhizome was found to contain high levels of certain minerals. Acute toxicity and behavioral studies revealed no visible signs of toxicity and any abnormal behavior in rabbits even at high doses. It is concluded that A. galanga produces fall in blood glucose levels in normal rabbits and the principles, both organic and inorganic, are extractable in methanol and water.     

Antidiabetic activity of hydro-ethanolic extract of Cyperus rotundus in alloxan induced diabetes in rats

In light of the traditional claim of Cyperus rotundus in the treatment of diabetes, investigations were carried out to evaluate its effect on alloxan induced hyperglycemia in rats. Oral daily administration of 500 mg/kg of the extract (once a day for seven consecutive days) significantly lowered the blood glucose levels. This antihyperglycemic activity can be attributed to its antioxidant activity as it showed the strong DPPH radical scavenging action in vitro.     

Antihyperglycemic activity of Euphrasia officinale leaves.

The effects of the aqueous extract of the leaf of Euphrasia officinale on blood glucose levels in normal and alloxan-diabetic rats were investigated. The treatment of alloxan-induced diabetic rats brought down the raised glucose levels, while the extract was devoid of hypoglycemic effect in normal rats.     

Compositional analysis and in vivo anti-diabetic activity of wild Algerian Marrubium vulgare L. infusion

Marrubium vulgare (Lamiaceae) is a plant traditionally used for the treatment of diabetes in Algeria. Compositional analysis of the aqueous infusion revealed the presence of fifteen metabolites, all belonging to the class of polyphenols. Particularly, seven flavonoids have been detected, together with 5-caffeoylquinic (chlorogenic) acid in small amounts; the extract is dominated by the presence of a series of complex molecules, characterized as verbascoside (acteoside) derivatives. Concerning the anti-diabetic effectiveness a series of in vivo experiments were carried out on albinos Wistar rats. Diabetes was induced in the animals by intra-peritoneal injection of alloxane; they were treated twice a day with aqueous extract from aerial part infusion (100, 200 and 300 mg/kg body weight) and glibenclamide (5mg/kg body weight) for 15 days. Oral administration of 200 and 300 mg/kg body weight of aqueous extract the Marrubium vulgare induced an significant effect antidiabetic and antihyperlipidemic (dose-dependent effect). A decrease in blood glucose by 50% for the dose 100 mg/kg and more than 60% for doses 200 and 300 mg/kg, as well as a significant lowering of total lipids, triglycerides, and total cholesterol levels in treated animals, compared with diabetic controls group (p<0.001), have been observed. Glibenclamide was used as reference and showed similar effects.