scholarly journals Hypoglucemic Effect Exerted by an Ethynyl-Phenylamino-Steroid-Pyrazole Derivative against Glucose Levels using a Diabetic Model

2021 ◽  
Vol 10 (4) ◽  
pp. 2887-2897

The research aimed to prepare an ethynyl-phenylamino-steroid-pyrazole derivative to evaluate their hypoglycemic activity in a diabetic model using either metformin or glibenclamide as controls. Besides, a theoretical analysis was carried out to evaluate estrone derivative interaction with either insulin receptor (3iga) or potassium channel (3w12). The results showed that steroid derivatives decrease glucose levels, and this effect was in a similar form to metformin. Besides, other data suggest that the ethynyl-phenylamino-steroid-pyrazole derivative could have a higher interaction with the 3iga protein surface compared with metformin. In conclusion, the hypoglycemic activity exerted by the ethynyl-phenylamino-steroid-pyrazole derivative against glucose levels is interesting. In this way, this compound could be a good candidate for the treatment of diabetes.

2020 ◽  
Vol 11 (2) ◽  
pp. 9553-9565

In this study, three steroid derivatives (compounds 2-4) were prepared from an estrone derivative (compound 1) to evaluate their biological activity on glucose concentration using a diabetic model. Besides, the compounds 1 and 4 were bound to technetium-99m (Tc-99m) via a radioimmunoassay method to evaluate the biodistribution of either compounds 1 and 4 in different organs over time (15, 30, 45, and 60 min). The results showed that both compounds 1 and 4 increase glucose levels compared with either compounds 2 and 3. In addition, other data showed that the biodistribution of the Tc-99m-compound 4 conjugate in all organs was higher compared with Tc-99m- compound 1 complex. In conclusion, compound 4 had greater hypoglycemic effects, and its biodistribution was wider than 1. The data suggest that amino groups may be important to the hypoglycemic activity of compound 4, and this could be related to their higher lipophilicity degree compared with compound 1.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Taofik O. Sunmonu ◽  
Anthony J. Afolayan

Artemisia afraJacq. ex Willd. is a widely used medicinal plant in South Africa for the treatment of diabetes. This study aimed to evaluate the hypoglycemic activity and possible toxicity effect of aqueous leaf extract of the herb administered at different dosages for 15 days in streptozotocin-induced diabetic rats. Administration of the extract at 50, 100, and 200 mg/kg body weight significantly (P<0.05) increased body weight, decreased blood glucose levels, increased glucose tolerance, and improved imbalance in lipid metabolism in diabetic rats. These are indications of antidiabetic property ofA. afrawith 200 mg/kg body weight of the extract showing the best hypoglycemic action by comparing favourably well with glibenclamide, a standard hypoglycemic drug. The extract at all dosages tested also restored liver function indices and haematological parameters to normal control levels in the diabetic rats, whereas the kidney function indices were only normalized in the diabetic animals administered with 50 mg/kg body weight of the extract. This investigation clearly showed that in addition to its hypoglycemic activity,A. aframay also protect the liver and blood against impairment due to diabetes. However, some kidney functions may be compromised at high dosages of the extract.


2021 ◽  
pp. 193229682110675
Author(s):  
Mark C. Matli ◽  
Andrea B. Wilson ◽  
Leah M. Rappsilber ◽  
Farron P. Sheffield ◽  
Miranda L. Farlow ◽  
...  

On March 23, 2020, all insulin products were reclassified as biologics instead of drugs under the Biological Price Competition and Innovation (BPCI) Act of 2009. This allows biosimilar insulin products to be manufactured when the patent expires for the reference biologic, sometimes called the originator or brand name product. A biosimilar product may not be substituted for the reference biologic at the pharmacy counter unless the biosimilar undergoes further switch trials to earn the designation as an interchangeable biosimilar. Insulin glargine-yfgn 100 units/mL is the first biosimilar insulin to attain interchangeable status with the reference insulin glargine. In the INSTRIDE 1 and INSTRIDE 2 trials, insulin glargine-yfgn has proven noninferiority regarding blood glucose reduction and adverse effect profile versus reference insulin glargine; even in the INSTRIDE 3 trial in which treatment of diabetes was switched between insulin glargine-yfgn and reference insulin glargine throughout the trial without statistically significant changes to glucose levels or adverse effects. Insulin glargine-yfgn may be substituted at the pharmacy counter without consultation with the prescriber, in accordance with state laws. In suit with other biosimilars, insulin glargine-yfgn’s list price is significantly lower than other insulin glargine products. This increases market competition leading to decreases in costs of other insulin glargine products. Many patients who could not previously afford insulin therapy may now have significantly improved access to treatment. Providers will need education to increase awareness of these new biosimilars and interchangeable biosimilar insulin products, cost benefits, and substitution allowances.


2017 ◽  
Vol 4 (4) ◽  
pp. 207
Author(s):  
Suresh Chandra ◽  
Mohd. Adil Khan ◽  
Anand Mohan

Objective: The diabetes mellitus is most common diseases. Which are spread all over the world. At they  are change in modified in life style disease  in this study where the prescribe drugs while using in the diagnostic and treatment of diabetes mellitus .the most commonly use drugs Sitagliptin +Metfomin in the community clinic in U.P. In the survey which are found to be the prescription pattern in Jajmau (Kanpur, U.P.) areas the most common drug which are running Sitagliptin + Metformin the survey which are randomly collect the prescription there are many variation in prescribing pattern of diabetes mellitus .the prescribing pattern is most strong tools to role of drug use in the society which are treat the DM during medication follow the proscription pattern of the drugs. There is need for appropriate safe &effective treatment and economical study to find out the pattern of drug therapy among DM.Methods: In this study the method randomized and non randomized study design was conducted in October 2016 – November 2016 community clinic in U.P. this study found to the date which group gender in fasting blood sugar various classes of drugs analyzed them.Results: A total of 200 patients were included in this one month’s study. All the patients had Type 2 diabetes. Metformin is the drug of choice and Sitagliptin is the most preferred combination with Metformin.Conclusions:Insulin was not preferred as mono-therapy. Despite combination therapy, the postprandial glucose levels were not in range–suggesting either poor patient compliance or inadequate dosing/inappropriate therapy. In addition to drugs, the services of a clinical pharmacist might be helpful in these patients. Metformin is the drug of choice and Sitagliptin is the most preferred combination with Metformin. 


Author(s):  
Pratik Choudhary ◽  
Stephanie A. Amiel

Hypoglycaemia (low blood glucose concentration) is the most important acute complication of the pharmacological treatment of diabetes mellitus. Low blood glucose impairs brain (and, potentially, cardiac) function. The brain has minimal endogenous stores of energy, with small amounts of glycogen in astroglial cells. The brain is therefore largely dependent on circulating glucose as the substrate to fuel cerebral metabolism and support cognitive performance. If blood glucose levels fall sufficiently, cognitive dysfunction is inevitable. In health, efficient glucose sensing and counterregulatory mechanisms exist to prevent clinically significant hypoglycaemia. These are impaired by diabetes and by its therapies. Patients with diabetes rank fear of hypoglycaemia as highly as fear of chronic complications such as nephropathy or retinopathy (1). Fear of hypoglycaemia, hypoglycaemia itself and attempts to avoid hypoglycaemia limit the degree to which glycaemic control can be intensified to reduce the risk of chronic complications of diabetes both for type 1 and type 2 diabetes.


2017 ◽  
Vol 1 (12) ◽  
pp. 1435-1439 ◽  
Author(s):  
Lavanya Viswanathan ◽  
Imali Sirisena

Abstract Type B insulin resistance is a rare syndrome characterized by fluctuating glucose levels (ranging from hyperglycemia with extreme insulin resistance to intractable hypoglycemia without exogenous insulin administration), high serum insulin levels, and insulin receptor autoantibodies. Most cases occur in the African American population in association with other underlying autoimmune systemic diseases. Treatments with high-dose steroids, immunosuppressants, and plasmapheresis have been used, with variable outcomes, in patients without spontaneous remission. We report the case of a 60-year-old African American woman with history of systemic lupus erythematosus presenting with extreme fluctuations in glucose levels, ranging from severe hyperglycemia to refractory hypoglycemia, with high serum concentration of insulin in both phases. Her presentation and phenotype were very similar to those seen in known cases of type B insulin resistance associated with insulin receptor antibodies. Treatment in other reported cases used a combination of high-dose steroids and immunosuppressants. We tried high-dose steroids, azathioprine, and intravenous immunoglobulins, which resulted in improvement and barely detectable insulin receptor antibody. We present a case of type B insulin resistance with abnormally low titers of insulin receptor antibodies despite a typical clinical course and response. Future research is needed to improve diagnosis and treatment in this rare disease.


2020 ◽  
Vol 21 (21) ◽  
pp. 7815
Author(s):  
Tomoko Okuyama ◽  
Jun Shirakawa ◽  
Kazuki Tajima ◽  
Yoko Ino ◽  
Heidrun Vethe ◽  
...  

Abnormal hepatic insulin signaling is a cause or consequence of hepatic steatosis. DPP-4 inhibitors might be protective against fatty liver. We previously reported that the systemic inhibition of insulin receptor (IR) and IGF-1 receptor (IGF1R) by the administration of OSI-906 (linsitinib), a dual IR/IGF1R inhibitor, induced glucose intolerance, hepatic steatosis, and lipoatrophy in mice. In the present study, we investigated the effects of a DPP-4 inhibitor, linagliptin, on hepatic steatosis in OSI-906-treated mice. Unlike high-fat diet-induced hepatic steatosis, OSI-906-induced hepatic steatosis is not characterized by elevations in inflammatory responses or oxidative stress levels. Linagliptin improved OSI-906-induced hepatic steatosis via an insulin-signaling-independent pathway, without altering glucose levels, free fatty acid levels, gluconeogenic gene expressions in the liver, or visceral fat atrophy. Hepatic quantitative proteomic and phosphoproteomic analyses revealed that perilipin-2 (PLIN2), major urinary protein 20 (MUP20), cytochrome P450 2b10 (CYP2B10), and nicotinamide N-methyltransferase (NNMT) are possibly involved in the process of the amelioration of hepatic steatosis by linagliptin. Thus, linagliptin improved hepatic steatosis induced by IR and IGF1R inhibition via a previously unknown mechanism that did not involve gluconeogenesis, lipogenesis, or inflammation, suggesting the non-canonical actions of DPP-4 inhibitors in the treatment of hepatic steatosis under insulin-resistant conditions.


2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Elisa Vega-Ávila ◽  
José Luis Cano-Velasco ◽  
Francisco J. Alarcón-Aguilar ◽  
María del Carmen Fajardo Ortíz ◽  
Julio César Almanza-Pérez ◽  
...  

Introduction.Catharanthus roseus(L.) is used in some countries to treat diabetes. The aim of this study was to evaluate the hypoglycemic activity of extracts from the flower, leaf, stem, and root in normal and alloxan-induced diabetic mice.Methods. Roots, leaves, flowers, and stems were separated to obtain organic and aqueous extracts. The blood glucose lowering activity of these extracts was determinate in healthy and alloxan-induced (75 mg/Kg) diabetic mice, after intraperitoneal administration (250 mg/Kg body weight). Blood samples were obtained and blood glucose levels were analyzed employing a glucometer. The data were statistically compared by ANOVA. The most active extract was fractioned. Phytochemical screen and chromatographic studies were also done.Results. The aqueous extracts fromC. roseusreduced the blood glucose of both healthy and diabetic mice. The aqueous stem extract (250 mg/Kg) and its alkaloid-free fraction (300 mg/Kg) significantly () reduced blood glucose in diabetic mice by 52.90 and 51.21%. Their hypoglycemic activity was comparable to tolbutamide (58.1%, ).Conclusions. The best hypoglycemic activity was presented for the aqueous extracts and by alkaloid-free stem aqueous fraction. This fraction is formed by three polyphenols compounds.


2014 ◽  
Vol 5 (1) ◽  
pp. 29-33
Author(s):  
E. V Biryukova

Diabetes mellitus (DM) is a chronic disease associated with the development of micro-and macrovascular complications, prevention of which is an important task of modern medicine. Achieving and maintaining blood glucose levels close to normal, however, is almost impossible without the full participation of the patient in the treatment of diabetes. Self-monitoring of blood glucose (SAG) is the basis of the effectiveness of glucose-lowering therapy and prevention of hypoglycemia. This article discusses the recommended frequency of SCG depending on the type of diabetes. For measuring blood sugar at home now a variety of devices is available. Selection of quality meter is determined by ease of use, ease of operation of the device, ease of preparation and fair presentation of results of the results of measurement.


Author(s):  
Padmaja Shetty K. ◽  
Pushpa V. H.

Background: Diabetes mellitus is a multifactorial metabolic disorder with several microvascular and macrovascular complications. Several plants have been used as dietary adjuvants to conventional drug therapy. Garcinia indica exhibits significant hypolipidemic and hypoglycemic activity. This study was conducted to evaluate the hypoglycemic effects of methanolic extract of seeds of Garcinia indica on blood glucose levels in Streptozotocin induced diabetic albino rats.Methods: Five groups of wistar albino rats (n=6) weighing 150-200g of either sex aged 3-4 months were obtained for the study. After overnight fasting, streptozotocin (50mg/kg) was administered intraperitoneally to induce diabetes. Five groups are: Group-1: Non diabetic control group, Group-2: diabetic control, Group-3: diabetic standard, Group-4: test group, Group-5: half of test + half of standard. Fasting blood sugar was estimated on 1, 3, 7, 14 and 28th day by capillary blood glucose method. The data obtained were subjected to statistical analysis.Results: In this study, following Streptozotocin administration the blood glucose levels increased in all groups on day 0. In group 2, blood glucose level gradually increased to 445.6±1.75mg/dl over a period of 4 weeks. Following glibenclamide administration in Group 3 - there was a gradual reduction in blood glucose levels: 269.8mg/dl - day 7 to 101.8mg/dl - week 4. Group 4 - persistent and significant (p<0.05) fall in blood glucose levels reaching upto 107mg/dl at the end of 4 weeks. Group 5 - 330mg/dl on day 1 which significantly (p<0.05) reduced to 101mg/dl on day 28. There was improvement in weight in group 4 and group 5 diabetic rats.Conclusions: The extract alone and in combination with glibenclamide showed significant hypoglycemic activity in comparison to diabetic control group.


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