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Gymnema sylvestre, a plant typical of India, has long been known for its hypoglycemic effects. The objective of this study was to evaluate the effect of G. sylvestre administration on glycemic cont...

Glechomae Herba is a Chinese herb, which has been used in China for thousands of years, mainly for the treatment of nephrolithiasis. This paper summarizes the modern research progress on Glechomae Herba from the aspects of botany, traditional medicinal use, phytochemistry, pharmacology, pharmacokinetics, analytical methods and quality control. In addition, it also points out the deficiencies of current research on this herb and provides possible directions for its development. So far, more than 190 chemical components have been isolated and identified from Glechomae Herba, including organic acids and their esters, volatile oils, flavonoids and their glycosides, terpenes and other chemical components. Its extracts and compounds have a wide range of pharmacological effects, including anti-stone, anti-inflammatory, bacteriostatic, cholagogic and diuretic, effect on ileum smooth muscle, anti-tumor effect on tumor and hypoglycemic effects. However, future studies should focus on drug metabolism, clarify its pharmacodynamic mechanism, and establish a reasonable quality control standards for Glechomae Herba.

Background: Diabetes mellitus (DM) is among the diseases with high morbidity and mortality The pathogenesis of DM involves pancreatic s-cell damage or insulin sensitivity disorder that result in hyperglycemia. Tapak liman (Elephantopus scaber L) is known to have high flavonoid content. Flavonoids are antioxidants that play a role in reducing pancreatic s-cell damage or damage to other tissues, which potentially reduce blood glucose levels. Objective: To determine the hypoglycemic effects of tapak liman using the DM rat models. Methods: Twenty-eight Wistar albino rats (Rattus novergicus) were divided into four groups: the normal control group (KKn), not induced by streptozotocin-nicotinamide (STZ-NA) intraperitoneal; negative control group (KK-), induced by STZ-NA; treatment group 1 (KP1), induced by STZ-NA and 150 mg/kg body weight of tapak liman plant extract; and the treatment group 2 (KP2), induced by STZ-NA and 300 mg/kg body weight of tapak liman. Blood glucose levels were measured on the 7th day after STZ-NA induction and the 28th day after the administration of tapak liman plant extract. The results were analyzed for statistical significance. Results: There was a significant decrease in blood glucose levels in KP1 and KP2 (p= 0.05). The decrease in blood glucose in KP1 had not reached normal levels compared to KP2. Conclusion: Administration of tapak liman plant extract at a dose of 300 mg/kg body weight in DM rat models reduced blood glucose levels to normal.

Background: Ammodaucus leucotrichus (Apiaceae) is a medicinal plant widely used by the Moroccan population to treat various diseases including diabetes. Aims: The aim of this study was to evaluate the antidiabetic effect of the aqueous extract prepared from the fruits of this medicinal plant. Normal and streptozotocin-induced diabetic rats were treated orally by the extract of Ammodaucus leucotrichus (A. leucotrichus) at a dose of 10 mg/kg. Methods: The blood glucose levels were determined during 6 hours and 15 days during this treatment. In addition the oral glucose tolerance test as well as the analysis of histopathological changes of liver was performed. The antioxidant activity of aqueous A. Leucotrichus extract was also valuated by the method of trapping of free radical 2,2-diphenyl-1 picrylhydrazyl (DPPH). Results: A. Leucotrichus fruit aqueous extract (ALFAE) reduced the blood glucose levels in both normal and diabetic rats. In addition, a remarkable influence on glucose tolerance was also noticed after ALFAE treatment. Moreover, ALFAE was able to exhibit a beneficial effect on histologlogical structure of liver. Finally a potential antioxidant effect has been shown in vitro. Conclusion: In conclusion, this study demonstrates the antihyperglycemic and hypoglycemic effects of A. Leucotrichus in rats supporting then its traditional use for the management of diabetes.

Pomegranate juice (PJ) has gained popularity attributed to its phenolic compounds and their medicinal properties. Its potential hypoglycemic effect has been related to enzymatic inhibition, insulin release, and the protection of pancreatic tissue. These effects depend on several aspects, such as the content and composition of phenols in pomegranate and characteristics of the organism that consumes the juice. The objective of this study was to systematically review scientific evidence investigating the hypoglycemic effect of PJ; the factors that affect bioactive compounds; and the mechanisms of action attributed to this effect. Human and rodent in vivo and in vitro studies were retrieved from PubMed, Scopus, and ScienceDirect databases. After reviewing the articles, it was identified that the methodologies and results among the scientific evidence were quite heterogeneous. Despite these limitations, many of the in vivo and in vitro studies found important hypoglycemic effects from PJ, as well as an increase in the function of β-cell, insulin secretion, a significantly lower activity of α-amylase enzyme, an inhibition of the enzyme α-glucosidase and dipeptidyl peptidase-4 (DPP-4), and the protection against DNA damage. Determining the potential health benefits of polyphenols contained in the pomegranate is limited for multiple factors that could affect the efficacy of PJ. Overall, the results of this review suggest the need for further experimentation, using controlled variable factors and testing the effect of PJ under similar experimental conditions.

Antidesma bunius (L.) Spreng and Mollugo oppositifolia L., also known as “bignay” and “malagoso” respectively, are commonly used medicinal plants in the Philippines to treat diabetes. However, the hypoglycemic effect of A. bunius (L.) Spreng and M. oppositifolia L. has not been reported to date. Therefore, this study was undertaken to investigate the hypoglycemic effects of the fresh and ethanolic extracts of the plants in db/db diabetic male mice. Fresh and ethanolic extracts (12.5 ml/kg and 250 mg/kg, respectively) were administered by gavage in db/db mouse, an animal model of diabetes. Blood from the tail snip was used to measure blood sugar levels on days 1 (D1), 8 (D8), 15 (D15), 22 (D22) and 29 (D29). Fresh extract of M. oppositifolia L. caused a significant reduction of blood glucose levels on D22 compared to untreated db/db mice (P < 0.05). On D29, fresh extract of A. bunius (L.) Spreng (P < 0.01), and fresh (P < 0.01) and ethanolic leaf extracts (P < 0.05) of M. oppossitifolia L. caused a significant reduction of blood glucose compared to untreated db/db mice. Fresh and ethanolic extracts of A. bunius (L.) Spreng and M. oppositifolia L. exhibited a significant hypoglycemic activity in db/db mice. Key words: Antidesma bunius L, Spreng, Mollugo oppositifolia L., diabetes, mouse, hypoglycemic.

This present study was to evaluate the protein tyrosine phosphatase 1B (PTP1B) inhibitory activity of nine diterpenes isolated from seeds of Phalaris canariensis, as well as their effect on strepto...

Dietary intervention in type 2 diabetes mellitus (T2DM) is a hotspot in international research because of potential threats to human health. Phellinus baumii, a wild fungus traditionally used as a food and medicine source, is now cultivated in certain East Asian countries, and is rich in polyphenols, which are effective anti-inflammatory ingredients useful in treatment of T2DM, with fewer side effects than drugs. To examine the hypoglycaemic effects of Phellinus baumii phenolics (PPE), the metabolite profiles of T2DM mice induced by streptozotocin after PPE intervention were systematically analyzed. Here, 10 normal mice were given normal saline as control group, and 50 model mice were randomly assigned to five groups and daily intragastric administrated with saline, metformin (100 mg/kg), and PPE (50, 100, 150 mg/kg of body weight), for 60 days. The pro-inflammatory factor contents of lipopolysaccharide stimulation of RAW 264.7 cells were decreased in a dose-dependent manner after PPE treatment, we propose that PPE could exert anti-inflammatory properties. PPE could also effectively reduce blood glucose levels, increased insulin sensitivity, and improved other glucolipid metabolism. Q-PCR results suggested that the hypoglycemic effects of PPE might be through activating IRS1/PI3K/AKT pathway in diabetic mice. These results suggest that PPE has strong potential as dietary components in the prevention or management of T2DM.

The rhizome of Polygonatum kingianum has been used as a traditional medicine in China. In this study, a novel polysaccharides (PKPs-1) was isolated from P. kingianum and characterized by its molecular weight, primary structure. The hypoglycemic activity of PKPs-1was investigated by in vitro assay with the HepG2 cell line and in vivo test using STZ-induced diabetic mice. Results showed that the average molecular weight of PKPs-1 was 14.05 kDa and is composed mainly of glucose and mannose. Methylation analysis indicated that this polysaccharides fraction consisted mainly of β1,2-link glucose. Besides, PKPs-1 exhibited significant anti-hyperglycemic activity on STZ-induced mice, improved insulin tolerance, and affected the metabolism of serum lipids. Results of real-time quantitative PCR (RT-PCR) showed that PKPs-1 significantly increased the expression of insulin receptor substrate-1 (IRS-1), phosphoinositide 3-kinase (PI3K) and protein kinase B (AKT), indicating that PKPs-1 regulates glucose metabolism by activating the PI3K/AKT signaling pathway. This study provides new insights for investigating the hypoglycemic effects of PKPs-1 and suggests that PKPs-1 could be a promising functional food or medicine for treating T2DM.

The present investigation was undertaken to assess the hypoglycemic potential of Caesalpinia bonducella (C.bonducella) and Myristica fragrans (M.fragrans), employing various in vitro techniques. The extracts of seeds of C. bonducella and M. fragrans were studied for their effects on glucose adsorption capacity, in vitro glucose diffusion, in vitro amylolysis kinetics and glucose transport across the yeast cells. It was observed that the plant extracts under study adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. The results of amylolysis kinetic experimental model revealed that the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both the plant extracts demonstrated significant inhibitory effects on movement of glucose into external solution across dialysis membrane as compared to control. Also, the plant extracts promoted glucose uptake by the yeast cells. It was observed that the enhancement of glucose uptake was dependent on both the sample and glucose concentration. C. bonducella extract exhibited significantly higher (p≤0.05) activity than the extract of M. fragrans at all concentrations. The results of the study verified the hypoglycemic activity of the extracts of C. bonducella and M. fragrans. However, the observed effects exhibited by the extracts of seeds of C. bonducella and M. fragrans need to be confirmed by using different in vivo models and clinical trials for their effective utilization as therapeutic agents in better management of diabetes mellitus.

To improve the oral efficiency of exenatide, we prepared polyethylene glycol-poly(lactic-co-glycolic acid) (PEG-PLGA) NPs modified with Fc (NPs-Fc) for exenatide oral delivery. Exenatide was encapsulated into the NPs by the w/o/w emulsion-solvent evaporation method. The particle size of the NPs-Fc was approximately 30 nm larger than that of the unmodified NPs with polydispersity indices in a narrow range (PDIs; PDI in vivo imaging in live mice. Therefore, Fc-targeted nano-delivery systems show great promise for oral peptide/protein drug delivery.

Thiazolo[2, 3-f]purine derivatives and their analogs – dihydrothiazolo[2, 3-f]purine, 7-(thietan-3-yl)purine, and 8-(2-hydroxypropylthio)purine derivatives – were synthesized. The compounds synthesized here had no effects on protein glycation reactions using glucose; they gave weak inhibition of glycogen phosphorylase; they had no hemorheological activity. Substances with hypotensive activity greater than that of Dibazol were found. A number of substances had hypoglycemic effects greater than those of chlorpropamide and Adebit. Two compounds inhibited dipeptidylpeptidase-4, but were less active than reference agent vildagliptin.

Graphical abstract, The recent discoveries in the fields of pathogenesis and management of diabetic nephropathy have revolutionized the knowledge about this disease. Little was added to the management of diabetic nephropathy after the introduction of renin angiotensin system blockers. The ineffective role of the renin- angiotensin system blockers in primary prevention of diabetic nephropathy in type 1 diabetes mellitus necessitated the search for other early therapeutic interventions that target alternative pathogenic mechanisms. Among the different classes of oral hypoglycemic agents, recent studies highlighted the distinguished mechanisms of sodium glucose transporter 2 blockers and dipeptidyl peptidase-4 inhibitors that settle their renoprotective actions beyond the hypoglycemic effects. The introduction of antioxidant and anti-inflammatory agents to this field had also added wealth of knowledge. However, many of these agents are still waiting well-designed clinical studies in order to prove their beneficial therapeutic role. The aim of this review of literature is to highlight the recent advances in understanding the pathogenesis, diagnosis, the established and the potential renoprotective therapeutic agents that would prevent the development or the progression of diabetic nephropathy.

Background: Cardiovascular complications account for the majority of deaths caused by diabetes mellitus. Platelet hyperactivity has been shown to increase the risk of thrombotic events and is a therapeutic target for their prevention in diabetes. Modulation of platelet function by diabetes agents in addition to their hypoglycemic effects would contribute to cardiovascular protection. Newly introduced antidiabetic drugs of sodium-glucose cotransporter 2 inhibitors (SGLT2i), glucagon like peptide-1 receptor agonists (GLP-1RA) and dipeptidyl peptidase-4 inhibitors may have anti-platelet effects, and in the case of SGLT2i and GLP-1RA may contribute to their proven cardiovascular benefit that has been shown clinically. Objective: Here, we reviewed the potential effects of these agents on platelet function in diabetes. Results and Conclusion: GLP-1RA and DPP-4i drugs have antiplatelet properties beyond their primary hypoglycemic effects. Whilst we have little direct evidence for the antiplatelet effects of SGLT2 inhibitors, some studies have shown that these agents may inhibit platelet aggregation and reduce the risk of thrombotic events in diabetes.

Background: Diabetes mellitus is a metabolic disorder in which there is increased blood sugar level, glycosuria, dyslipidemia and sometimes ketonemia occurs. Increased blood sugar level leads to characteristic symptoms such as polydipsia, polyurea, blurring of vision, polyphagia and weight loss.Methods: Healthy male Wister rats weighing between 150-250 gm were taken. Total 2 groups A and B were prepared and each group contains 6 animals. Group A was administered voglibose as 0.6 mg/70 kg body weight. Group B was administered vildagliptin as 100 mg/70 kg body weight. Diabetes was induced in group A and B by administration of 120 mg/kg body weight of nicotinamide and 60 mg/kg body weight of streptozocin intraperitoneally. Streptozocin was administered after 15-20 minutes of administration of nicotinamide. After 72 hours of streptozotocin injection, fasting blood glucose level was determined and induction of diabetes was confirmed. The fasting blood samples were collected from all the groups on further days 7, 14, 21 and 28 day to determine the glucose level by glucometer. Results: The decline in fasting blood sugar level by voglibose was 36.4% on day 7, 40.2% on day 14, 43.94% on day 21 and 46.4% on day 28. The reduction in Fasting blood sugar level by vildagliptin was 49% on day 7, 52.25% on day 14 and 54% on day 21 and 28. Thus in group B rats, decline was maximal on day 7 and little fall was recorded on subsequent days. It suggests good efficacy as vildagliptin normalized the blood glucose level effectively. Conclusions: Vildagliptin was found significantly more effective in lowering fasting blood glucose level than voglibose.

Background: Our study aims at exploring the hypoglycemic effect, efficacy, and possible mode of action of ethanol extract of Alpinia nigra (EEAN) as an antidiabetic agent in an animal model. Methods: Oral glucose tolerance test (OGTT) was used to identify primary hypoglycemic effect in mice. Three tests (glucose absorption, sucrose absorption, and disaccharidase activity) were carried out by gut perfusion and six segments studies to assess carbohydrate absorption and glucose utilization. Results: In OGTT, at 400 mg/kg and 800 mg/kg dose of EEAN extract significantly improved oral glucose tolerance among normal mice at 60 min and 90 min with compared to control. Both doses of extract significantly (P < 0.01) reduced blood glucose level and showed the hypoglycemic effect by retarding 11.43% and 20.82% of blood glucose level after 2 h of administration in glucose-induced mice, respectively. In situ perfused rat intestinal model demonstrated reduced glucose absorption at a 500 mg/kg dose. Inhibition of intestinal disaccharidase was also found by the extract. This was confirmed, yet again, via the six segment study. Throughout the length of the gastrointestinal tract, sucrose digestion was found to be inhibited which is also evident in the six segment study. Conclusions: This study suggests that the EEAN has hypoglycemic effects in a dose-dependent manner by inhibiting intestinal glucose absorption, and these may be effective in the treatment of diabetes. Further study is required to explicate the effect this extract or the active compounds have on the individual glucose transporters and the precise mechanism.

Xylaria nigripes (XN) is a medicinal fungus with a high-economic value. The aim of this study was to explore the hypoglycemic effects and mechanisms of the XN aqueous extract in steroid-induced insulin-resistant (SIIR) rats. Significant hypoglycemic effects were observed 60 min after administration of XN aqueous extract. In normal Wistar, hypoglycemic effects were 21% (the plasma glucose level decreased from 128.6 ± 12.5 to 100.9 ± 10.7 mg/dL). In SIIR, hypoglycemic effects were 26% (the plasma glucose level decreased from 177.6 ± 12.5 to 133.3 ± 29.7 mg/dL) rats refer to their baseline. The signaling proteins for insulin-receptor substrate-1 and glucose transporter-4 increased 0.51-fold and 1.12-fold, respectively, as determined by Western blotting; the increase in the proteins was 13% and 9%, respectively, as determined by immunohistochemistry. The serotonin antagonist, α-p-chlorophenylalanine, effectively blocked the hypoglycemic effects and increased the signaling protein levels. After XN administration, none of the animals showed significant changes in plasma-free fatty acids in 60 min. In summary, the XN extract may have hypoglycemic effects in normal Wistar and SIIR rats that may have a serotonin-related hypoglycemic effect and enhance insulin sensitivity in the SIIR rats. Copyright © 2015 John Wiley & Sons, Ltd.

With numerous pharmacological and biological functions bio-flavonoids gain appreciable attention in diabetes and other therapeutic research. Among several beneficial flavonoids quercetin exhibits impressive hypoglycemic effects, with significant improvement, stabilization of long sustaining insulin secretion and regeneration of human islets in the pancreas without producing serious health hazards. However, in oral delivery poor solubility, stability in biological milieu, low permeation, short biological half-life, and insignificant bioavailability limit its wide application in anti diabetic research. Over the last few decades polymeric carrier systems have been widely studied for improvement of quercetin bioavailability. Natural polymers are more preferred in this regard as they possess several favourable properties like biocompatibility, biodegradability, mucoadhesiveness, non-immunogenicity and non-toxicity. This review focuses on quercetin in anti-diabetic research and the progress in the synthesis of polymer-based formulations for efficient quercetin delivery, with an emphasis on producing an improved biological efficacy of the flavonoid. Diabetic complications, probable mechanisms of quercetin absorption, regulation and anti diabetic effects, obstacles to produce desired bio-efficacy and possible remedies are also brought into focus. To overcome these barriers encapsulation of quercetin within various safe polymeric vehicles are discussed. Further, this review sheds light on enhancing the efficacy of quercetin in novel ways for successful diabetes treatment and others.

Efficacy and safety of a drug and its plasma concentration are closely correlated, and plasma concentrations are used as an index of the drug’s effects. Therefore, it is important to understand the relationship between the drug’s plasma concentration and its effects. Plasma glucose control of diabetics retards its progression and glimepiride is widely used for its treatment. In the present study, pharmacokinetic-pharmacodynamic analysis of glimepiride was performed in Wistar rats, with normal plasma glucose levels (Normal), and streptozotocin-induced type 1 diabetes rats (Type 1) and type 2 diabetes GK rats (Type 2). The PK-PD model was structured to investigate time-dependent plasma glucose changes in relation to the plasma concentration, and the PK and PD characteristics of glimepiride were investigated. PK analysis of glimepiride in the three groups showed no significant differences in total body Clearance (CL) and half-life of the β phase. Plasma concentration profiles at a 0.5 mg/kg dose increased in the following order; Type 1, Normal, and Type 2 groups. The area under the plasma concentration-time curves for glimepiride was dosedependent in Normal and Type 2 groups. The CL decreased in the Type 2 group compared to the other groups at a 0.5 mg/kg dose. The maximum decrease in the plasma glucose level was increased in the following order; Normal, Type 2, and Type 1. From the estimated PK-PD analysis, the plasma glimepiride concentration necessary to produce hypoglycemic effects was higher, and the responsiveness of the drug at a drug concentration at the half-maximum effect was quicker, in the Type 2 group compared to the other groups. These effects of glimepiride were considered to improve the pathological condition. This study of the PK-PD characteristics of glimepiride is useful for prediction of the influence of drug-drug interactions and the change in clinical conditions of patients.

A surface extract of the aerial parts of Salvia chamaedryoides afforded 13 diterpenes (1-13), with seven compounds (1, 3, 4, 7-9, 12) described for the first time. The structures of the new compounds were established using 1D and 2D NMR spectroscopic methods, HRESIMS, and ECD data. The potential hypoglycemic effects of the crude extract, fractions, and pure compounds from S. chamaedryoides were investigated by inhibition of α-glucosidase and α-amylase enzymes. The extract and its fractions showed a moderate dose-dependent inhibition; the pure compounds exhibited differential inhibitory activity against these two enzymes. Molecular modeling studies were also performed to suggest the interaction mode of compound 3 in the α-glucosidase enzyme active site. The antimicrobial activity of the purified compounds was investigated against 26 clinical pathogens. No activity was detected for the Gram-negative species tested nor on Candida albicans and C. glabrata, while variable susceptibilities were observed using Gram-positive staphylococcal and enterococcal species.

Artemisia sieberi a member of Compositae family is an endemic species in Iran and commonly named “desert worm wood” or “dermaneh”. It has some pharmacological activities such as antimicrobial, antinociceptive, insecticidal and hypoglycemic effects as its traditional uses and used for treatment of malaria and coccidiosis.

A series of amides of 2,3-dihydroimidazo- and 2,3,4,10-tetrahydropyrimido[1,2-a]benzimidazolyl-N-acetic acids were synthesized. Their pharmacological activity was studied. It was established that the synthesized substances possessed antiaggregant properties and antiarrhythmic activity. Some of these amides exhibited antioxidant and hypoglycemic effects in addition to antagonist activity with respect to serotonin 5-HT2 and purine P2Y1 receptors.

Ethnopharmacological relevance Type 2 diabetes is the most common type of diabetes and its prevalence is rapidly increasing throughout the world. Modifications of lifestyle such as suitable diet and exercise programs along with pharmacotherapy and education of patients are beneficial therapies for patients with type 2 diabetes. The ethnopharmacological use of herbal medicines, many of them part of our diet as spices, vegetables and fruits, has been developed for the treatment of diabetes due to inexpensiveness, easy availability and few side effects. Aim of the study Our aim is to present a review for researchers who are interested in the biologically active dietary plants traditionally utilized in the treatment of diabetes. Materials and methods Information was obtained from a literature search of electronic databases such as Google Scholar, Pubmed, Sci Finder and Cochrane. Common and scientific name of the fruits, vegetables, beverages, oils and spices and the words ‘antidiabetic’, ‘hypoglycemic’, ‘anti-hyperglycemic’, ‘type 2 diabetes’ were used as keywords for search. Results Certain fruits and vegetables are functional foods and their consumption reduces the incidence of type 2 diabetes. Hypoglycemic effects of fruits and vegetables may be due to their inducing nature on pancreatic β-cells for insulin secretion, or bioactive compounds such as flavonoids, alkaloids and anthocyanins, which act as insulin-like molecules or insulin secretagogues. Conclusion This write-up covers hypoglycemic, anti-hyperglycemic and anti-diabetic activities of some dietary fruits, vegetables, beverages, oils and spices and their active hypoglycemic constituents. Including such plant species in the diet might improve management of type 2 diabetes.

Background Diabetes mellitus is a metabolic disorder of multiple aetiology characterised by hyperglycemia resulting from defects in insulin secretion, insulin action or both. It is a global epidemic ravaging both developed and developing countries. The situation will worsen if nothing is done urgently. In fact, the need to identify natural products with antidiabetic potentials is of great importance as supported by several research efforts all over the world, in search of antidiabetic plant based products that are safe and efficacious. Available literatures show that several phytochemicals with antidiabetic properties have been identified in certain plants amongst which include Uvaria chamae. The potentials of Uvaria chamae as an antidiabetic and hypolipidemic drug-candidate are thus tested. Methods Diabetes mellitus was experimentally induced after the rats were fasted overnight by administering intraperitoneally, 60 mg/kg streptozotocin. After 72 h, the rats with plasma glucose levels >200 mg/dl were classified as diabetic. A total of six groups containing five rats per group were used. One group of diabetic rats was untreated. Three diabetic groups, each were treated orally with 100, 250 and 400 mg/kg body weight of the extract. Another diabetic group was treated with insulin (0.5 IU/kg) subcutaneously. The control received 0.5 ml (2% solution) of acacia orally. The treatment was for 8 days. The effects of the extract on weight, plasma glucose and other biochemical parameters were evaluated using standard procedures. Results The diabetic rats treated with the extract showed significant reductions (p

Objectives: The 4-Aminoquinoline, Chloroquine is still indicated for treatment of malaria fever due to sensitive Plasmodium species. The hypoglycemic effects of Chloroquine have been sparsely reported in human and animal models of type 2 diabetes and a widely held perception among health caregivers in this part of the world is that administering intramuscularly Chloroquine to fasting malaria patients could be complicated by syncope directly caused by hypoglycemia. This study investigated the effects of a single adult human intramuscular bolus of Chloroquine on the blood glucose level in fasting normoglycemic Wistar rats. Methods: Fifteen acclimatized adult male rats were randomly divided into three groups of 5 per group. Group I and II rats were fasted overnight and received 4.17 mg/kg of intramuscular Chloroquine in the morning. Group III rats were also fasted but received 1ml of sterile water injection. Fasting blood sugar level was determined immediately after injection and at 2 hour and 4 hour intervals using Accucheck glucometer. Results: The results were recorded as Mean ± SEM. The mean sugar levels of the groups were compared with each other within a given time point as well between the different time intervals within a given group using Student’s t test of significance. There were no observable statistical significant differences between the Mean blood glucose levels of the groups. Conclusion: The results of this study suggest that intramuscular Chloroquine injection in fasted normoglycemic rats did not lower significantly lower their blood glucose level and syncope in fasting adult humans immediately following treatment by this route was likely the result of a cardiovascular complication rather than from a Chloroquine-induced hypoglycemic effect.

Two-layered dissolving microneedles (DMs) containing intermediate-acting insulin, protamine sulfate insulin (PSI), were prepared. Then a pharmacodynamic study was performed to evaluate the prolonged hypoglycemic effects in rats. The DMs were approximately 497±5 μm long, with 303±3 μm diameter at their base. The length of the insulin loaded space was 182±4 μm. PSI contents in DMs were 0.51±0.02 IU. A three-month stability study showed that 99.9±1.4% of PSI was recovered at 4 °C. As the temperature increased to 40 °C, recovery decreased to 97.5±2.0%. PSI was released within 5 min from DMs. Hypoglycemic effects of PSI DMs were evaluated in rats where subcutaneous injection preparations were used as references. Total area above the plasma glucose level (% of the pre-dose level) vs. time curve as an index of hypoglycemic effect was 144.0±16.0% h and 243.3±8.5% h for PSI DMs at 1.46 and 3.28 IU/kg. The relative pharmacologic availability of PSI from DMs were 100.2±9.8% and 91.4±4.1%. No significant difference of hypoglycemic curves was found between DMs and injection solutions, which suggests the usefulness of two-layered DMs of PSI for the displacement therapy of sc injection preparation.

For the purpose of investigating the in vitro antidiabetic activity of a medicinal herb mixture prepared through traditional antidiabetic prescription, the study analyzed the existence of insulin-similar components and examined -amylase and -glucosidase inhibition activity. As a result of arranging the medicinal herb mixture extracts over the 3T3-L1 fibroblast in the concentration of , which confirmed that it included much of insulin sensitizer components as 151.7% in the differentiation of 3T3-L1 fibroblast. The inhibition activity against -amylase of the medicinal herb mixture extracts as hypoglycemic agent were 38.4, 31.5 and 16.6% in the concentration of 10.0, 1.0 and 0.1 mg/mL, respectively. The inhibition activity against -glucosidase of the medicinal herb mixture extracts were 81.3, 35.8 and 26.7% in the concentration of 10.0, 1.0 and 0.1 mg/mL, respectively. The inhibition activity against -glucosidase in the ethyl acetate fractions of the water and 80% ethanol extracts were 66.9% and 55.1%, respectively, the highest levels in the various solvent extracts.

Banaba (Lagerstroemia speciosaL.) extracts have been used for many years in folk medicine to treat diabetes, with the first published research study being reported in 1940. This review summarizes the current literature regarding banaba and its constituents. The hypoglycemic effects of banaba have be

5 Abstract: The evaluation of the acute and subchronc toxicities of a Nigerian polyherbal tea remedy, prepared with Anthocleista vogelii, Ficus exasperata leaves and Viscum album (mistletoe), was carried out in Swiss albino mice and Wistar rats of both sexes. The lyophilized extract in the dose ranges of 1.0 g to 20.0 g/kg body weight was administered orally to the mice and observed continuously for the first 4 h and hourly for the next 12 h, then 6 hourly for 56 h (72 h, acute toxicity). Wistar rats were also fed with different doses of the lyophilized formulation for 30 days and the effects on some tissues - heart, liver and testes - wer e histologically evaluated. Also the effects on the biochemical and haematological parameters were evaluated (subchronic toxicity model). The median acute toxicity value (LD50) of the polyherbal tea was determined to be 8.970 g/kg body weight. The tea significantly reduced (p

As a percutaneous sustained-release preparation, insulin micropiles (MPs) were prepared with biodegradable polymers poly(lactic acid) (PLA), poly(ϵ-caprolactone) (PCL) and poly(lactic-co-glycolic acid) (PLGA) as the base. The obtained PLA, PCL, and PLGA MPs of which the insulin:polymer ratio was 1:2 were administered to rat skin at 40 IU/kg and hypoglycemic effects measured for 6 days. The order of the hypoglycemic effect was PLAPCLPLGA. PLA MP showed the strongest hypoglycemic effect (2 days). The hypoglycemic effect of insulin PLA MP was dependent on the formulation; the order was insulin:PLA (2:1)insulin:PLA (1:1)insulin:PLA (1:2). As the ratio of insulin to the polymer base increased, the hypoglycemic effect increased. The area above the plasma glucose levels vs. time curves for 6 days from insulin:PLA (2:1) MPs, 10, 20, 30, and 40 IU/ kg, were 249 ± 108, 2003 ± 379, 3960 ± 794, and 6311 ± 726%·h. A dose-dependent hypoglycemic effect was obtained at 10-40 IU/kg and pharmacological availabilities were 11.1%, 44.5%, 58.6%, and 70%, respectively. Insulin:PLA (2:1) MP showed high plasma insulin level, 86.9-134.7 IU/mL, for 3 days. There was no damage to rat skin. These results suggest the usefulness of insulin:PLA (2:1) MP as a sustained-release percutaneous delivery system for insulin.

Sesquiterpene glycoside, nerolidol-3-O-alpha-l-rhamnopyranosyl(1-->4)-alpha-l-rhamnopyranosyl(1-->2)-[alpha-l-rhamnopyranosyl(1-->6)]-beta-d-glucopyranoside was isolated from dried leaves of loquat [Eriobotrya japonica (Thunb.) Lindl., Rosaceae]. Hypoglycemic effects of this natural product were assessed in normal and alloxan-diabetic mice model. Animals received orally administration of the sesquiterpene glycoside in dose of 25 and 75 mg/kg. The anti-hyperglycemic effect was compared with gliclazide's. The dose of 25 and 75 mg/kg both exerted a significant (p

The methanolic extract from the whole plant of Sinocrassula indica (Crassulaceae) was found to inhibit the increase in serum glucose levels in oral administration of sucrose and glucose in rats at a dose of 250 mg/kg (p.o.). However, the extract did not inhibit the increase in serum glucose levels after intraperitoneal administration of glucose in these animals but did partly inhibit the gastric emptying. On the other hand, this extract significantly inhibited the increase in serum glucose levels after administration for 2 weeks in KK-Ay mice, a genetically type II diabetic mice, at a dose of 250 mg/kg/d (p.o.) without significant changes of the weights of body, liver, and visceral fat. From the extract, four new acylated flavonol glycosides, sinocrassosides A1, A2, B1, and B2, were isolated together with 11 flavonoids and 2 megastigmanes. The absolute stereostructures of the four new compounds were elucidated on the basis of chemical and physicochemical evidence.

The novel gluconeogenesis inhibitor FR225654, isolated from the culture broth of Phoma sp. No. 00144, has an unique structure that consists of a highly oxygenated trans-decalin ring and a beta-keto-enol, with a characteristic side chain. This compound selectively inhibited gluconeogenesis of rat primary hepatocytes and had hypoglycemic effects in several in vivo mouse models.

A recent randomized and double-blind placebo-controlled clinical study has indicated that Ganoderma lucidum polysaccharides (GLP) decrease blood glucose in patients with type II diabetes. The aim of this study was to investigate the effect of the GLP extract in alloxan-induced diabetic rats. Oral administration of GLP at 0.25, 0.5 and 1.0 g/kg for 4 weeks resulted in a reduction of blood glucose levels by 12.5, 18.7 and 33.7% respectively, while glibenclamide treatment brought the hyperglycemic value down to normal. The hypoglycemic effect was supported by a significant decrease in glycosylated haemoglobin and increased plasma insulin levels (p＜0.01) in a dose- and time-dependent manner. This study showed that GLP has similar hypoglycemic effects as glibenclamide in alloxan-induced diabetic rats.

Objective Research has determined differences in the pharmacokinetics and therapeutic actions of glyburide and glipizide. The goal of this study was to evaluate the hypoglycemic effects of glyburide/glipizide combination therapy in the management of patients with diabetes not adequately controlled on either agent alone. Methods Nine patients (3 men, mean age 50.6 ± 11 y) who were hyperglycemic on either glyburide or glipizide monotherapy continued their previous regimen with doses titrated up to maximum daily doses and dietary therapy for 4 weeks, and then they were placed on morning glipizide/evening glyburide combination therapy for 12 weeks. Results Combination therapy had no significant effect on glycemic control; no differences in glycosylated hemoglobin (HbAIC) were observed (baseline, 15.3% ± 3.6%; monotherapy, 14.8% ± 3.3%; combination, 13.4% ± 3.5%). However, during combined glyburide/glipizide therapy, fasting plasma glucose was significantly reduced by 53.4 ± 20.0 mg/dL in young (age AIC was reduced by 3.8% ± 4.0% in young and increased by 1.7% ± 1.3% in older subjects. No significant changes in blood pressure, body weight, or lipid parameters occurred. Conclusions Our preliminary data indicate the limited usefulness of combined glyburide/glipizide therapy. The modest reduction in hyperglycemia observed in patients younger than 50 years of age warrant future studying.

Bombyx batryticatus (B. batryticatus), a well-known traditional animal Chinese medicine, has been commonly used in China for thousands of years. The present paper reviewed advances in traditional uses, origin, chemical constituents, pharmacology and toxicity studies of B. batryticatus. The aim of the paper is to provide more comprehensive references for modern B. batryticatus study and application. In Traditional Chinese Medicine (TCM) culture, drugs containing B. batryticatus have been used to treat convulsions, headaches, skin prurigo, scrofula, tonsillitis and fever. Many studies indicate B. batryticatus contains various compounds, including protein and peptides, fatty acids, flavonoids, nucleosides, steroids, coumarin, polysaccharide and others. Numerous investigations also have shown that extracts and compounds from B. batryticatus exert a wide spectrum of pharmacological effects both in vivo and in vitro, including effects on the nervous system, anticoagulant effects, antitumor effects, antibacterial and antifungal effects, antioxidant effects, hypoglycemic effects, as well as other effects. However, further studies should be undertaken to investigate bioactive compounds (especially proteins and peptides), toxic constituents, using forms and the quality evaluation and control of B. batryticatus. Furthermore, it will be interesting to study the mechanism of biological activities and structure-function relationships of bioactive constituents in B. batryticatus.

Background: The Philippines is one of the countries with high prevalence of diabetes mellitus. Although there are several drugs marketed to control it, there are unwanted side effects. Knowing this, alternative options have been sought for to control the disease. Aims and Objectives: To evaluate the effects of aqueous extracts of Cycas riuminiana on the blood glucose and cholesterol levels of alloxan-induced diabetic mice. Materials and Methods: Aqueous crude leaf extract from C. riuminiana was administered to 6 and 30 ICR mice (Mus musculus) to determine whether there are toxic effects and effects on the blood glucose and cholesterol levels, respectively. The 30 mice were divided into six groups and were either treated with double distilled water, glimepiride, or the C. riuminiana aqueous extract. Results: After performing the acute oral toxicity, there were no deaths signifying that the extracts may be safe to administer in mice. After 28 days of treatment, statistical analyses indicated that the treatment groups had anti-hyperglycemic effects on the diabetic mice. The high-dose group had the lowest mean blood glucose values, which surpassed the hypoglycemic effects of the positive control group, which was treated with glimepiride. Furthermore, there was no difference between the control and the treatment groups. On the other hand, blood cholesterol values of the treatment and control groups were within the normal range after the 28 days study. Conclusion: The results of the study shows that C. riuminiana leaves have antidiabetic properties by lowering glucose and cholesterol levels at doses between 250 and 1000 mg/kg body weight.

Background: Diabetes mellitus is a metabolic disease that is usually associated with abnormalities in the metabolism of different substrates leading to high blood glucose levels (BGL). Aims and Objectives: Aims and objectives are to evaluate the effects of ethanolic extracts of Cajanus cajan (CCEE) leaves on its antihyperglycemic effects on BGL of normoglycemic mice. Materials and Methods: 45, 5-week-old female, mice were divided into five groups and were administered with either double distilled water, glimepiride, or CCEE. Results: Baseline BGLs were measured before the induction of hyperglycemia by glucose loading. 30 min after, the BGLs were measured again and ranged between 167.667 and 185.778 mg/dL. Immediately after the hyperglycemic BGLs were measured, the corresponding treatments were administered. Subsequently, three blood collections were done spanning 3 h with 1 h interval. The treatment doses were observed to have a faster onset than the positive control supported by the fact that the treatment groups had significant differences (P < 0.05) with their respective hyperglycemic BGLs on the 1st h, while the positive control group exhibited significant difference with its hyperglycemic BGL on the 2nd h. The hypoglycemic effect of the positive control peaked at the 3rd h with 67.33 mg/dL and surpassed the hypoglycemic effect of the medium- and high-dose groups with 83.778 and 98.556 mg/dL, respectively. The low-dose group did not have significant difference with the negative control group past the 1st h suggesting that this dosage has a weak hypoglycemic effect. Conclusion: These results indicate that the CCEE leaves were able to produce hypoglycemic effects at doses between 400 and 800 mg/kg bodyweight.

The positive influence of Aloe vera, a tropical cactus, on the healing of full-thickness wounds in diabetic rats is reported. Full-thickness excision/incision wounds were created on the back of rats, and treated either by topical application on the wound surface or by oral administration of the Aloe vera gel to the rat. Wound granulation tissues were removed on various days and the collagen, hexosamine, total protein and DNA contents were determined, in addition to the rates of wound contraction and period of epithelialization. Measurements of tensile strength were made on treated/untreated incision wounds. The results indicated that Aloe vera treatment of wounds in diabetic rats may enhance the process of wound healing by influencing phases such as inflammation, fibroplasia, collagen synthesis and maturation, and wound contraction. These effects may be due to the reported hypoglycemic effects of the aloe gel.

Introduction alkaloids are a group of naturally occurring chemical compounds that contain mostly basic nitrogen atoms. In particular berberine is a quaternary ammonium salt from the protoberberine group of isoquinoline alkaloids with anti-lipogenic and hypoglycemic effects. On the other hand, mate plant has reported to have high antioxidant potential, including an inhibitory ability against plasma and LDL oxidation. Areas covered Most of the studies reported in literature about alkaloids are pre-clinical trials, and we have already discussed them in a previous review we conducted. This time we want to focus our attention on clinical studies about berberine, and mate plant, so the aim of this review is to evaluate berberine and mate plant efficacy and safety in humans. Conclusion Berberine is a potent oral hypoglycemic agent with a good effect on lipid metabolism. It is safe and the cost of treatment is very low. Also mate plant seems to have antioxidant and hypolipidemic actions, even if further studies are necessary.