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At least 667 records · Page 37Linked to original sources
PubMed1996

What kind of cardiovascular alterations could be influenced positively by oral antidiabetic agents?

Since the first publication of the University Group Diabetes Programme in 1970 the possible deleterious cardiovascular effects of certain hypoglycaemic sulphonylurea products has been well known. In contrast, international knowledge of the advantageous cardiovascular effects of certain sulphonylurea compounds became available recently. Glibenclamide decreases the incidence of fatal myocardial infarction and the development of ventricular fibrillation in patients suffering from acute myocardial infarction. It also lowers the incidence of ventricular ectopic beats in digitalized patients compared with patients treated with other investigated sulphonylurea compounds. The survival of patients treated with glibenclamide, insulin or diet alone is longer after the first attack of angina pectoris or after first acute myocardial infarction compared with those on other investigated sulphonylurea therapy. Glibenclamide decreases arrhythmogenesis during acute myocardial infarction in rats and strophanthin cardiotoxicity in rabbits. Arterial blood pressure and myocardial contractile force are not influenced by glibenclamide whereas these parameters are increased by other investigated sulphonylurea compounds. Consequently, deleterious cardiovascular effects of certain hypoglycaemic sulphonylurea drugs may contribute to the high cardiovascular mortality rate in diabetes mellitus, partly due to the effect on membrane channels and partly due to independent cardiac and extracardiac actions. Finally, recent observations suggest that glimepiride has a more advantageous cardiovascular effect than glibenclamide.

Administration, Oral↗
PubMed1986

Pharmacological evaluation of Dioscorea dumetorum tuber used in traditional antidiabetic therapy.

This study was undertaken to confirm or otherwise disprove the alleged effectiveness of Dioscorea dumetorum tuber in the traditional treatment of clinical diabetes mellitus. Hydroalcoholic extracts of the tuber were fractionated by precipitation or solvent partition and the various extracts or fractions subjected to phytochemical and pharmacological tests. Whereas the alkaloid-containing fraction was hyperglycaemic in fasting normal mice, the whole extract and the fractions containing steroidal derivatives evinced significant hypoglycaemic activities in fasting normal mice or rabbits and in fasting alloxan-diabetic rabbits. The hypoglycaemic action of the glycosidic portion in particular was prompt and potent, in normal as well as in severely alloxan-diabetic rabbits suggesting thereby the possibility of obtaining an agent that could act in conditions of even severe insulin lack.

Animals↗
PubMed1989

A review of natural products and plants as potential antidiabetic drugs.

The present paper reviews the active, natural principles and crude extracts of plants which have been experimentally studied for hypoglycemic activity in the last ten years. Phytoconstituents with known structures have been classified in appropriate chemical groups and the active crude extracts have been listed alphabetically according to genus. Data are reported on their pharmacological activity, mechanism of action, toxicity and other properties.

Animals↗
PubMed1989

Antidiabetic effects of Tinospora crispa in rats.

In Malaysia, an aqueous extract of Tinospora crispa stems is taken orally to treat diabetes mellitus. In the present study, normal and alloxan-diabetic rats were used to evaluate the hypoglycaemic properties of the extract. A hypoglycaemic effect was observed in moderately diabetic rats with concomitant improvement in insulinaemia. After a 2-week treatment with the extract (4 g/l in the drinking water), these rats also showed improvement in glucose tolerance. Moreover, acute intravenous treatment with the extract (50 mg/kg) caused an increase in plasma insulin levels. The data support the traditional belief that T. crispa extract could improve diabetic conditions by virtue of its action on the endocrine pancreas.

Animals↗
PubMed1990

Antidiabetic effect of a leaf extract from Gymnema sylvestre in non-insulin-dependent diabetes mellitus patients.

The effectiveness of GS4, an extract from the leaves of Gymnema sylvestre, in controlling hyperglycaemia was investigated in 22 Type 2 diabetic patients on conventional oral anti-hyperglycaemic agents. GS4 (400 mg/day) was administered for 18-20 months as a supplement to the conventional oral drugs. During GS4 supplementation, the patients showed a significant reduction in blood glucose, glycosylated haemoglobin and glycosylated plasma proteins, and conventional drug dosage could be decreased. Five of the 22 diabetic patients were able to discontinue their conventional drug and maintain their blood glucose homeostasis with GS4 alone. These data suggest that the beta cells may be regenerated/repaired in Type 2 diabetic patients on GS4 supplementation. This is supported by the appearance of raised insulin levels in the serum of patients after GS4 supplementation.

Adult↗
PubMed2004

Comparative effects of GLP-1 and GIP on cAMP production, insulin secretion, and in vivo antidiabetic actions following substitution of Ala8/Ala2 with 2-aminobutyric acid.

The two major incretin hormones, glucagon-like peptide-1 (GLP-1), and glucose-dependent insulinotropic polypeptide (GIP), are currently being considered as prospective drug candidates for treatment of type 2 diabetes. Interest in these gut hormones was initially spurred by their potent insulinotropic activities, but a number of other antihyperglycaemic actions are now established. One of the foremost barriers in progressing GLP-1 and GIP to the clinic concerns their rapid degradation and inactivation by the ubiquitous enzyme, dipeptidyl peptidase IV (DPP IV). Here, we compare the DPP IV resistance and biological properties of Abu8/Abu2 (2-aminobutyric acid) substituted analogues of GLP-1 and GIP engineered to impart DPP IV resistance. Whereas (Abu8)GLP-1 was completely stable to human plasma (half-life >12 h), GLP-1, GIP, and (Abu2)GIP were rapidly degraded (half-lives: 6.2, 6.0, and 7.1 h, respectively). Native GIP, GLP-1, and particularly (Abu8)GLP-1 elicited significant adenylate cyclase and insulinotropic activity, while (Abu2)GIP was less effective. Similarly, in obese diabetic (ob/ob) mice, GIP, GLP-1, and (Abu8)GLP-1 displayed substantial glucose-lowering and insulin-releasing activities, whereas (Abu2)GIP was only weakly active. These studies illustrate divergent effects of penultimate amino acid Ala8/Ala2 substitution with Abu on the biological properties of GLP-1 and GIP, suggesting that (Abu8)GLP-1 represents a potential candidate for future therapeutic development.

Adenylyl Cyclases↗
PubMed2005

Dual PPAR-alpha and -gamma activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential.

2,4-Thiazolidinedione derivatives of 1,3-benzoxazinone were synthesized and evaluated for their PPAR-alpha and -gamma dual activation. DRF-2519, a compound obtained through SAR of TZD derivatives of benzoxazinone, has shown potent dual PPAR activation. In ob/ob mice, it showed better efficacy than the comparator molecules. In fat fed rat model, it showed significant improvement in lipid parameters, which was better than fibrates.

Animals↗
PubMed2006

Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.

A series of novel pyridine-2-propanoic acids was synthesized. A structure-activity relationship study of these compounds led to the identification of potent dual PPARalpha/gamma agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compound (S)-13 was selected for further profiling.

Animals↗
PubMed2006

Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.

A series of novel pyridine-3-propanoic acids was synthesized. A structure-activity relationship study of these compounds led to the identification of potent dual PPARalpha/gamma agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compounds (S)-14 and (S)-19 were selected for further profiling.

Animals↗
PubMed2006

The status of diabetes control and antidiabetic drug therapy in Japan--a cross-sectional survey of 17,000 patients with diabetes mellitus (JDDM 1).

The number of diabetic patients has been increasing in Japan and consequently diabetic complications are the most important target to be prevented through improving glycemic control. In order to describe the glycemic control status and treatment of diabetic patients by specialists in Japan over three years, from 2000 to 2002, we examined HbA1c, other laboratory data and the modality of drug therapy in the study population, 8170 in 2000, 11,831 in 2001, and 16,934 in 2002. Patients were registered at clinics and hospitals that were members of the Japan Diabetes Clinical Data Management Study Group (JDDM). HbA1c levels, other laboratory data, and details of drug therapy were collected and analyzed using SPSS and MS Access. The mean HbA1c levels were essentially unchanged during the study periods, ranging from 7.9% to 7.8%, and from 7.1% to 7.0%, in type 1 and type 2 diabetic patients, respectively. In type 2 diabetes, the frequency of oral hypoglycemic agents (OHA) use increased from 44.9% to 51.4%, while the use of diet-only therapy decreased from 29.9% to 25.4% over the study period. Although the systolic blood pressure was slightly above target, the mean blood pressure and the mean lipid profile were mostly within the treatment goals set by the Japan Diabetes Society. This first report from a large scale study of the daily management of diabetes in Japan revealed that the average HbA1c level was superior to most of the results reported from other countries. Nonetheless, 66% of the patients still had HbA1c levels and half of the patients had other laboratory parameters including blood pressure and lipid profile that were greater than those recommended by the Japan Diabetes Society. The nature of diabetes drug therapy in Japan has gradually changed as new drugs have appeared in the market.

Aged↗
PubMed2004

Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma.

We investigated the biological activity of Dr. Reddy's Research Foundation (DRF) 2519, a benzoxazinone analogue of the thiazolidinedione class of compounds. In the in vitro transactivation assay, DRF 2519 showed interesting dual activation of Peroxisome Proliferator Activated Receptor (PPAR) alpha and gamma. In insulin-resistant ob/ob mouse model, DRF 2519 showed significant alleviation of insulin resistance and dyslipidemia, which is better than rosiglitazone. Fatty Zucker rats treated with DRF 2519 showed better reduction of plasma insulin, triglyceride and free fatty acid levels than those treated with rosiglitazone. In addition, these rats were able to clear plasma lipids better when challenged with exogenous lipid (i.v.). DRF 2519 treatment resulted in improved plasma lipid profiles in high-fat-fed Sprague-Dawley rats. Treated rats showed better plasma lipid clearance and hepatic triglyceride secretion. When compared to DRF 2519, fenofibrate was comparatively less efficacious while rosigltiazone showed no activity in these models. In ex vivo studies, DRF 2519 showed induction of liver acyl CoA oxidase mRNA and increase in lipoprotein lipase (LPL) protein expression and activity in adipose tissue. In the in vitro studies, DRF 2519 inhibited the lipid biosynthesis and secretion of apolipoprotein B from human hepatoma (Hep)G2 cells. It also enhanced insulin-induced relaxation of rat aortic smooth muscle. These results indicate that DRF 2519, a dual activator of PPAR-alpha and gamma, could be an interesting development candidate in the management of metabolic disorders and associated complications.

Animals↗
PubMed2006

Antidiabetic effect of garlic oil but not diallyl disulfide in rats with streptozotocin-induced diabetes.

We investigated the effects of garlic oil and diallyl disulfide (DADS) on glycemic control and renal function in rats with streptozotocin-induced diabetes. Rats received by gavage garlic oil (100 mg/kg body wt) or DADS (40 or 80 mg/kg body wt) every other day until 16 weeks after the induction of diabetes. The control rats were treated with corn oil only. Neither garlic oil nor DADS significantly affected fasting blood glucose concentrations throughout the investigation period. Garlic oil did not affect oral glucose tolerance in diabetes acutely but significantly improved oral glucose tolerance at 4, 8, 12, and 16 weeks and significantly ameliorated proteinuria at the end of 16 weeks. DADS did not significantly affect oral glucose tolerance or renal function. Diabetic rats fed 80 mg DADS/kg body wt had a significantly lower rate of body weight gain and a significantly lower ratio of muscle weight to body weight than did vehicle-treated diabetic rats. In conclusion, long-term treatment of diabetes with garlic oil can improve oral glucose tolerance and renal function in diabetes but not through the action of DADS. High doses of DADS may further complicate the metabolic disturbances in diabetes.

Allyl Compounds↗
PubMed2005

Antidiabetic potential of Butea monosperma in rats.

The antihyperglycemic activity of the ethanolic extract of Butea monosperma (BMEE) was studied in glucose-loaded and alloxan-induced diabetic rats. Single dose treatment of BMEE (200 mg/kg, p.o.) significantly improved glucose tolerance and caused reduction in blood glucose level in alloxan-induced diabetic rats. Repeated oral treatment with BMEE (200 mg/kg/day) for 2 weeks significantly reduced blood glucose, serum cholesterol and improved HDL-cholesterol and albumin as compared to diabetic control group.

Animals↗
PubMed2006

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.

Administration, Oral↗
PubMed2004

Antidiabetic effect of aqueous extract of seed of Tamarindus indica in streptozotocin-induced diabetic rats.

In Indian traditional system of medicine, herbal remedies are prescribed for the treatment of diseases including diabetes mellitus. In recent years, plants are being effectively tried in a variety of pathophysiological states. Tamarindus indica Linn. is one of them. In the present study, aqueous extract of seed of Tamarindus indica Linn. was found to have potent antidiabetogenic activity that reduces blood sugar level in streptozotocin (STZ)-induced diabetic male rat. Supplementation of this aqueous extract by gavage at the dose of 80 mg/0.5 ml distilled water/100 g body weight per day in STZ-induced diabetic rat resulted a significant diminution of fasting blood sugar level after 7 days. Continuous supplementation of this extract for 14 days resulted no significant difference in this parameter from control level. Moreover, this supplementation produced a significant elevation in liver and skeletal muscle glycogen content, activity of liver glucose-6-phosphate dehydrogenase in respect to diabetic group. Activities of liver glucose-6-phosphatase, liver and kidney glutamate oxaloacetate transaminase (GOT) and glutamate pyruvate transaminase (GPT) activities were decreased significantly in the aqueous extract supplemented group in respect to diabetic group. All these parameters were not resettled to the controlled level after 7 days of this extract supplementation but after 14 days of this supplementation, all the above mentioned parameters were restored to the control level.

Administration, Oral↗