Natural Products: Potential Source of DPP-IV Inhibitors

2019 ◽  
Vol 20 (12) ◽  
pp. 1218-1225 ◽  
Author(s):  
Rajeev K. Singla ◽  
Rishabh Kumar ◽  
Sameer Khan ◽  
Mohit ◽  
Kajal Kumari ◽  
...  

Out of multiple therapeutic targets, DPP-IV is the lead target for the treatment of type 2 diabetes. Natural products have always been available for the possible lead generation against various diseases and disorders. In the present review, we have covered various natural sources which have experimentally validated anti-diabetic activity for type 2 diabetic patients with specific focus on the DPP-IV inhibition. Out of all, the most potent DPP-IV inhibitors were found to be resveratrol, luteolin, apigenin and flavone having activity in nanomolar range. Standard drugs like sitagliptin, saxagliptin, and diprotin A have complex structures as compared to these phenolic compounds. Flavonoids and phenolic compounds have their added advantages in being present in a number of functional foods and carry antioxidant properties as well. So, the scientists working on the new chemical entity hunting for the type 2 diabetes treatment can also explore these natural sources for lead generation.

Drug Research ◽  
2017 ◽  
Vol 67 (07) ◽  
pp. 396-403 ◽  
Author(s):  
Kenji Akahane ◽  
Kazuma Ojima ◽  
Ayaka Yokoyama ◽  
Toshihiro Inoue ◽  
Sumiyoshi Kiguchi ◽  
...  

Abstract We compared the individual effects of mitiglinide and glibenclamide administered in combination with the dipeptidyl peptidase-IV (DPP-IV) inhibitor sitagliptin on plasma DPP-IV activity and blood glucose levels in rats with streptozotocin-nicotinamide-induced type 2 diabetes (STZ-NA rats). We examined the inhibitory activity of mitiglinide and glibenclamide as well as their combination with sitagliptin on plasma DPP-IV activity in STZ-NA rats. The oral glucose tolerance test (OGTT) was used to compare effects of mitiglinide, glibenclamide, and their combination with sitagliptin on blood glucose levels in STZ-NA rats. Mitiglinide and glibenclamide did not inhibit rat DPP-IV and did not influence the inhibitory effect of sitagliptin on rat plasma DPP-IV activity. In STZ-NA rats, plasma glucose levels were stronger suppressed by a combination of mitiglinide and sitagliptin than by either drug used alone. However, no clear effect of the combination of glibenclamide and sitagliptin was observed. These results indicate that the combination of mitiglinide and sitagliptin has a lower risk of hypoglycemia in the rats with induced type 2 diabetes compared with the combination of glibenclamide and sitagliptin. The combination of mitiglinide and sitagliptin can be a promising combination for the treatment of diabetic patients.


2010 ◽  
Vol 2 (2) ◽  
pp. 81-85
Author(s):  
Venkatesham Allenki ◽  
Rama Krishna Devarakonda ◽  
Rama Narsimha Reddy Anreddy ◽  
Narayana Pantam ◽  
Narsimha Reddy Yellu

Dipeptidyl peptidase-IV (DPP-IV) could serve as a potential biomarker in monitoring the disease progression and improvement on treatment. To investigate fasting & post prandial response of DPP-IV enzyme as indirect marker of incretin response failure after chronic treatment with metformin in type 2 diabetes. The study included twelve nondiabetic subjects, ten patients with glycosylated hemoglobin values (6-8%) and fifteen patients with glycosylated hemoglobin greater than 8 % of type-2 diabetes patients of either sex with metformin treatment above 3 years were recruited. Fasting and post prandial DPP-IV levels were calculated. HbA1c was used to assess diabetes status. DPP-IV activity (fasting) in type 2 diabetic subjects with HbA1c > 8 % was significantly higher DPP-IV (44.67 ± 2.19 U/l) than in non diabetic subjects (24.39 ± 3.97 U/l). A significant correlation between DPP-IV (fasting / post prandial) and HbA1c (r = 0.821 & r = 0.732, P< 0.01) was observed in both diabetic (HbA1c 6-8, HbA1c < 8) patients. Hyperglycemia induces significant increase in serum DPP-IV activity in fasting condition and might contribute to the reduction in active glucagon like peptide-1(GLP-1) in type 2 diabetic subjects. In normal subjects during post prandial condition, there is sudden increase followed by decrease of GLP-1 due to cleavage of GLP-1 to as substrate of DPP-IV is seen as upsurge of DPP-IV. This response was lacking in diabetic patients with high HbA1c indicates indirectly metformin failure to secrete GLP-1. High fasting level and decreased post prandial of DPP-IV may indicate drug failure in type-2 diabetes mellitus.  Key words: Type 2 diabetes; metformin; DPP-IV; HbA1c; GLP-1.DOI: 10.3329/sjps.v2i2.1698Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 81-85


2015 ◽  
Vol 85 (3-4) ◽  
pp. 145-155 ◽  
Author(s):  
Marjan Ghane Basiri ◽  
Gity Sotoudeh ◽  
Mahmood Djalali ◽  
Mohammad Reza Eshraghian ◽  
Neda Noorshahi ◽  
...  

Abstract. Background: The aim of this study was to identify dietary patterns associated with general and abdominal obesity in type 2 diabetic patients. Methods: We included 728 patients (35 - 65 years) with type 2 diabetes mellitus in this cross-sectional study. The usual dietary intake of individuals over 1 year was collected using a validated semi-quantitative food frequency questionnaire. Weight, height, and waist circumference were measured according to standard protocol. Results: The two major dietary patterns identified by factor analysis were healthy and unhealthy dietary patterns. After adjustment for potential confounders, subjects in the highest quintile of the healthy dietary pattern scores had a lower odds ratio for the general obesity when compared to the lowest quintile (OR = 0.45, 95 % CI = 0.26 - 0.79, P for trend = 0.02), while patients in the highest quintile of the unhealthy dietary pattern scores had greater odds for the general obesity (OR = 3.2, 95 % CI = 1.8 - 5.9, P for trend < 0.001). There were no significant associations between major dietary patterns and abdominal obesity, even after adjusting for confounding factors. Conclusion: This study shows that in patients with type 2 diabetes mellitus, a healthy dietary pattern is inversely associated and an unhealthy dietary pattern is directly associated with general obesity.


Author(s):  
Shah Namrata Vinubhai ◽  
Pardeep Agarwal ◽  
Bushra Fiza ◽  
Ramkishan Jat

Background: Serum ferritin is known as an index for body iron stores also as an inflammatory marker and it is influenced by several disease. We were looking for a correlation between HbA1c and S. Ferritin in type 2 DM. Methodology: The present study a total of 150 participants were enrolled of which 100 were confirmed cases of Type 2 Diabetes Mellitus and rest 50 age and sex matched healthy subjects constituted the control group. All were screened for HbA1c, Fasting blood sugar, Post prandial blood sugar and S.Ferritin. Results: A highly significant variation and positive correlation was observed with respect to S.Ferritin and HbA1c levels. Mean S.Ferritin was high in the subgroup with poor glycemic control. Conclusion: The fasting, post prandial sugar levels, HbA1c and S.Ferritin were significantly higher in the diabetic subjects. This study shows a positive correlation between HbA1c and S. Ferritin levels. So we can conclude that in diabetic patients S. Ferritin may serve as an independent marker of poor glycemic and metabolic control. Keywords: Serum ferritin, Type 2 Diabetes Mellitus, HbA1c.


2019 ◽  
Vol 25 (23) ◽  
pp. 2510-2525 ◽  
Author(s):  
Bashir Usman ◽  
Neha Sharma ◽  
Saurabh Satija ◽  
Meenu Mehta ◽  
Manish Vyas ◽  
...  

The incidence of diabetes has increased globally in recent years and figures of diabetic patients were estimated to rise up to 642 million by 2040. The disorder is accompanied with various complications if not managed at the early stages, and interlinked high mortality rate and morbidity with time. Different classes of drugs are available for the management of type 2 diabetes but were having certain limitations of their safety. Alphaglucosidase is a family of enzyme originated from the pancreas which plays a role in the anabolism of 80-90% of carbohydrate consumed into glucose. This glucose is absorbed into the blood and results in frank postprandial hyperglycemia and worsens the conditions of diabetic patients which precipitate complications. Inhibition of these enzymes helps to prevent postprandial hyperglycemia and the formation of glycated end products. Alphaglucosidase inhibitors are reported to be more important in adequate control of type 2, but marketed drugs have various side effects, such as poor patient compliance and also expensive. This proves the needs for other class of drugs with better efficacy, safety, patient compliance and economic. In this review, we have emphasized the recent advances in the field of new alpha-glucosidase inhibitors with improved safety and pharmacological profile.


2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Ada Krawęcka ◽  
Aldona Sobota ◽  
Emilia Sykut-Domańska

Type 2 diabetes has become one of the major health problems of the modern world. It is assumed that environmental factors have a significant impact on the development of the disease, and great importance is ascribed to the diet, which can be modified accordingly. The diet can exert prophylactic and therapeutic effects; changes in the diet in advanced disease can improve the quality of life of diabetic patients and minimise the risk of complications, which are the direct cause of diabetes-related death. Functional food, which has a potentially health-enhancing effect in addition to its nutritional value, has been increasingly recognised and required. Cereal products are crucial in diabetic nutrition. Their function can additionally be enhanced by fortification with compounds with proven hypoglycaemic effects. Pasta has a low glycaemic index and is a good carrier of fortifying substances; hence, it can be highly recommended in diets for diabetic patients.


2006 ◽  
Vol 290 (1) ◽  
pp. E54-E59 ◽  
Author(s):  
Lucilla D. Monti ◽  
Emanuela Setola ◽  
Gabriele Fragasso ◽  
Riccardo P. Camisasca ◽  
Pietro Lucotti ◽  
...  

The aim of the present study was to evaluate the effect of prolonged inhibition of β-oxidation on glucose and lipid muscle forearm metabolism and cGMP and endothelin-1 forearm release in patients with type 2 diabetes mellitus and ischemic cardiomyopathy. Fifteen patients were randomly allocated in a double-blind cross-over parallel study with trimetazidine (20 mg tid) or placebo lasting 15 days. At the end of each period, all patients underwent euglycemic hyperinsulinemic clamps with forearm indirect calorimetry and endothelial balance of vasodilator and vasoconstricor factors. Compared with placebo, trimetazidine induced 1) an increase in insulin-induced forearm glucose uptake and glucose oxidation accompained by a reduction in forearm lipid oxidation and citrate release and 2) a decrease of endothelin-1 release paralleled by a significant increase in forearm cGMP release. Forearm glucose oxidation significantly correlated with cGMP release ( r = 0.37, P < 0.04), whereas forearm lipid oxidation positively correlated with endothelin-1 release ( r = 0.40, P < 0.03). In conclusion, for the first time, we demonstrated that insulin-induced forearm glucose oxidation and forearm cGMP release were increased whereas forearm endothelin-1 release was decreased during trimetazidine treatment. Muscle's metabolic and vascular effects of trimetazidine add new interest in the use of trimetazidine in type 2 diabetic patients with cardiovascular disease.


Nutrients ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 183
Author(s):  
Anna Izzo ◽  
Elena Massimino ◽  
Gabriele Riccardi ◽  
Giuseppe Della Pepa

Type 2 diabetes mellitus (T2DM) represents a major health burden for the elderly population, affecting approximately 25% of people over the age of 65 years. This percentage is expected to increase dramatically in the next decades in relation to the increased longevity of the population observed in recent years. Beyond microvascular and macrovascular complications, sarcopenia has been described as a new diabetes complication in the elderly population. Increasing attention has been paid by researchers and clinicians to this age-related condition—characterized by loss of skeletal muscle mass together with the loss of muscle power and function—in individuals with T2DM; this is due to the heavy impact that sarcopenia may have on physical and psychosocial health of diabetic patients, thus affecting their quality of life. The aim of this narrative review is to provide an update on: (1) the risk of sarcopenia in individuals with T2DM, and (2) its association with relevant features of patients with T2DM such as age, gender, body mass index, disease duration, glycemic control, presence of microvascular or macrovascular complications, nutritional status, and glucose-lowering drugs. From a clinical point of view, it is necessary to improve the ability of physicians and dietitians to recognize early sarcopenia and its risk factors in patients with T2DM in order to make appropriate therapeutic approaches able to prevent and treat this condition.


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Michael Albosta ◽  
Jesse Bakke

Abstract Background Type 2 Diabetes is a metabolic disorder characterized by hyperglycemia that causes numerous complications with significant long-term morbidity and mortality. The disorder is primarily due to insulin resistance particularly in liver, skeletal muscle, and adipose tissue. In this review, we detail the hormonal mechanisms leading to the development of diabetes and discuss whether intermittent fasting should be considered as an alternative, non-medicinal treatment option for patients with this disorder. Methods We searched PubMed, Ovid MEDLINE, and Google Scholar databases for review articles, clinical trials, and case series related to type 2 diabetes, insulin resistance, and intermittent fasting. Articles were carefully reviewed and included based on relevance to our topic. We excluded abstracts and any non-English articles. Results The majority of the available research demonstrates that intermittent fasting is effective at reducing body weight, decreasing fasting glucose, decreasing fasting insulin, reducing insulin resistance, decreasing levels of leptin, and increasing levels of adiponectin. Some studies found that patients were able to reverse their need for insulin therapy during therapeutic intermittent fasting protocols with supervision by their physician. Conclusion Current evidence suggests that intermittent fasting is an effective non-medicinal treatment option for type 2 diabetes. More research is needed to delineate the effects of intermittent fasting from weight loss. Physicians should consider educating themselves regarding the benefits of intermittent fasting. Diabetic patients should consult their physician prior to beginning an intermittent fasting regimen in order to allow for appropriate oversight and titration of the patients medication regimen during periods of fasting.


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