scholarly journals Molecular Docking of Mangostin and Sinensetin Derivatives on SUR1-Pancreatic KATP Channel Target as Antidiabetic

2021 ◽  
Vol 8 (3) ◽  
pp. 271
Author(s):  
Intan Kris Prasetyanti ◽  
Sukardiman Sukardiman ◽  
Suharjono Suharjono
Keyword(s):  
Type 2 Diabetes ◽  
Molecular Docking ◽  
Blood Glucose ◽  
Katp Channel ◽  
The Body ◽  
Discovery Studio ◽  
Reduce Blood Glucose ◽  
Macromolecular Binding ◽  
Complex Chronic Disease

Background: Diabetes Mellitus (DM) is a complex chronic disease characterized by increased blood glucose. The incidence of this disease is rising, especially type 2 diabetes which is caused by insulin resistance in the body. SUR1-Pancreatic KATP Channel is a receptor as an antidiabetic target because its inhibition process can increase insulin production so that it can reduce blood glucose in people with type 2 diabetes. Objective: This study aims to identify the in-silico activity of the SUR1-Pancreatic KATP Channel macromolecules. Methods: Identification of macromolecular binding sites using Protein Plus software, then carried out molecular docking using AutoDock software, where the formed molecular interactions are further identified using the BIOVIA Discovery Studio software. Results: After determining the macromolecular binding site, the RMSD value was 1.253, allowing for further molecular docking. Molecular docking showed that the Ligands of mangostin (α, β, γ-mangostin) and sinensetin derivatives had a good affinity, namely α-mangostin -6,31 kcal/mol; β-mangostin -5.78 kcal/mol; γ-mangostin -6.17 kcal/mol and sinensetin -4.75 kcal/mol. Conclusion: The affinity sequence in the docking process for the SUR1 KATP channel macromolecules is α-mangostin > γ-mangostin > β-mangostin > sinensetin. The highest affinity for the docking process on the macromolecule SUR1 KATP channel was α-mangostin with a value of ΔG -6.31 kcal/mol Ki 23.65 μM.

Inhibition of α-glucosidase by trilobatin and its mechanism: kinetics, interaction mechanism and molecular docking

2022 ◽  
Author(s):  
Ming He ◽  
Yuhan Zhai ◽  
Yuqing Zhang ◽  
Shuo Xu ◽  
Shaoxuan Yu ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Molecular Docking ◽  
Blood Glucose ◽  
Interaction Mechanism ◽  
Postprandial Blood Glucose

α-Glucosidase is related to the increase of postprandial blood glucose in vivo. Inhibition of α-glucosidase is supposed to be an effective approach to treat type 2 diabetes mellitus (T2DM). Trilobatin,...

scholarly journals Herbal constituent sequoyitol improves hyperglycemia and glucose intolerance by targeting hepatocytes, adipocytes, and β-cells

2012 ◽  
Vol 302 (8) ◽  
pp. E932-E940 ◽  
Author(s):  
Hong Shen ◽  
Mengle Shao ◽  
Kae Won Cho ◽  
Suqing Wang ◽  
Zheng Chen ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Blood Glucose ◽  
Glucose Intolerance ◽  
Insulin Signaling ◽  
Glucose Production ◽  
Water Soluble ◽  
Β Cells ◽  
Β Cell ◽  
Reduce Blood Glucose

The prevalence of insulin resistance and type 2 diabetes increases rapidly; however, treatments are limited. Various herbal extracts have been reported to reduce blood glucose in animals with either genetic or dietary type 2 diabetes; however, plant extracts are extremely complex, and leading compounds remain largely unknown. Here we show that 5- O-methyl- myo-inositol (also called sequoyitol), a herbal constituent, exerts antidiabetic effects in mice. Sequoyitol was chronically administrated into ob/ob mice either orally or subcutaneously. Both oral and subcutaneous administrations of sequoyitol decreased blood glucose, improved glucose intolerance, and enhanced insulin signaling in ob/ob mice. Sequoyitol directly enhanced insulin signaling, including phosphorylation of insulin receptor substrate-1 and Akt, in both HepG2 cells (derived from human hepatocytes) and 3T3-L1 adipocytes. In agreement, sequoyitol increased the ability of insulin to suppress glucose production in primary hepatocytes and to stimulate glucose uptake into primary adipocytes. Furthermore, sequoyitol improved insulin signaling in INS-1 cells (a rat β-cell line) and protected INS-1 cells from streptozotocin- or H2O2-induced injury. In mice with streptozotocin-induced β-cell deficiency, sequoyitol treatments increased plasma insulin levels and decreased hyperglycemia and glucose intolerance. These results indicate that sequoyitol, a natural, water-soluble small molecule, ameliorates hyperglycemia and glucose intolerance by increasing both insulin sensitivity and insulin secretion. Sequoyitol appears to directly target hepatocytes, adipocytes, and β-cells. Therefore, sequoyitol may serve as a new oral diabetes medication.

scholarly journals TCM Formula Xiaoyaosan Decoction Improves Depressive-Like Behaviors in Rats with Type 2 Diabetes

2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Na Li ◽  
Qun Liu ◽  
Xiao-Juan Li ◽  
Xiao-Hui Bai ◽  
Yue-Yun Liu ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Blood Glucose ◽  
High Fat Diet ◽  
Hippocampal Formation ◽  
Morphological Changes ◽  
Fasting Blood Glucose ◽  
The Body ◽  
High Fat ◽  
Body Weights

The mechanism of depression with type 2 diabetes remains elusive, requiring further study.Objective. To evaluate the effect of TCM formula Xiaoyaosan on depressive-like behaviors in rats with type 2 diabetes.Methods. Rats were divided into 5 groups and drugs were administered during the model period of 21 days. The model of depressive-like behaviors in rats with type 2 diabetes was induced by a high fat diet, low doses of STZ injection, and chronic restraint stress for 21 days. The body weight, fasting blood glucose, ITT, OGTT, 5-HT, DA, depression behaviors, and morphological changes of formation were measured and observed.Results. After modeling, marked changes were found in model rats; behavioral analyses of rats indicated that this modeling method negatively impacts locomotor function. In the H&E staining, changes were found predominately in the CA1 and DG subregions of the hippocampus. After 21 days of treatment by fluoxetine and Xiaoyaosan, rats’ body weights, behaviors and fasting blood glucose, and hippocampal formation were modified.Conclusions. A new model of depressive-like behaviors in rats with type 2 diabetes was successfully created. Xiaoyaosan and fluoxetine in this study independently contribute to exacerbate the disease progression.

scholarly journals Experience of the use of liraglutide (Victoza) in women with type 2 diabetes mellitus and obesity

2011 ◽  
Vol 14 (2) ◽  
pp. 91-93
Author(s):  
Vladimir Ivanovich Kudinov ◽  
Natalya Vladimirovna Zolotareva ◽  
Maria Sergeeva Nichitenko
Keyword(s):  
Type 2 Diabetes ◽  
Blood Glucose ◽  
Total Duration ◽  
Hdl Cholesterol ◽  
The Body ◽  
C Peptide ◽  
Target Values ◽  
Before And After ◽  
Total Fat

Aim. To study efficacy of treatment with liraglutide in women with type 2 diabetes (T2D) and obesity. Materials and methods. A group of 12 women aged 52-58 yr with T2D duration of 3-5 years, BMI 32-35 kg/m2, abnormally high C-peptide level,and НbА1с 7.5-8.5% were treated with 1500-2000 mg metformin/day and sulfonylureas at 50% of the maximum dose. Liraglutide was given insteadof sulfonylureas by a standard method (0.6 U/day for 1 week subcutaneously and 1.2 U/day thereafter). The total duration of therapy was 3 months.We analysed blood glucose level before and 2 hr after meals, НbА1с, lipidogram, C-peptide, HOMA index, BMI, waist circumference, percent of totalfat in the body, frequency of hypoglycemia, and side effects (nausea). Results. All patients achieved target values of НbА1с and a significant decrease in blood glucose before and after meals, body weight, total fat content,BMI, HOMA, systolic blood pressure; HDL cholesterol increased while LDL decreased. No case of hypoglycemia was documented. All the patientshad mild nausea of short duration (2-3 days). Conclusion. The use of liraglutide (Victoza) in women with T2D and obesity improve carbohydrate metabolism and insulin resistance without seriousside effects.

Effect of Capparis spinosa Extract on Metabolic Parameters in Patients with Type-2 Diabetes: A Randomized Controlled Trial

2019 ◽  
Vol 19 (1) ◽  
pp. 100-107 ◽  
Author(s):  
Hamideh Vahid ◽  
Shokoufeh Bonakdaran ◽  
Zahra Mazloum Khorasani ◽  
Lida Jarahi ◽  
Hassan Rakhshandeh ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Metabolic Syndrome ◽  
Blood Glucose ◽  
The Body ◽  
Hypoglycemic Agents ◽  
Diabetic Patients ◽  
Glycemic Status ◽  
Significant Difference ◽  
Capparis Spinosa

Background: Experimental studies have reported beneficial effects of Capparis spinosa L., a perennial shrub from the Capparidaceae family, on the glycemic status and serum lipids in diabetic animals. Objective: The aim of the present randomized triple-blind placebo-controlled clinical trial was to investigate the safety and efficacy of C. spinosa oxymel on blood glucose, lipid profile, and other diagnostic indexes of metabolic syndrome in patients with poorly controlled type 2 diabetes. Method: The C. spinosa oxymel was prepared by adding hydroalcoholic extract of C. spinosa fruit to simple oxymel (a mixture of grape vinegar and lactulose). Thirty diabetic patients with metabolic syndrome whose glycemic status was not controlled despite receiving full doses of oral hypoglycemic agents did not want to start insulin therapy and were randomly allocated to three groups to receive placebo, simple oxymel, or C. spinosa oxymel (10 mL/thrice daily for 3 months). All patients continued conventional therapy with hypolipidemic, antihyperlipidemic, and antihypertensive drugs during the study. Results: C. spinosa oxymel significantly decreased the body weight and body mass index at the end of the study compared to the baseline. While the patients in the placebo and simple oxymel groups displayed further increase in the level of FBG or PPBG, administration of C. spinosa oxymel inhibited the progression of hyperglycemia. Nevertheless, there was not a significant difference between placebo and intervention groups regarding HbA1c at the end of the study. C. spinosa oxymel had no significant effect on the serum cholesterol but inhibited the progression of hypertriglyceridemia during the study. There were no significant changes in creatinine, microalbuminuria, AST, ALT, and ALP values following C. spinosa treatment, suggesting that it had no unwanted effects on kidney and liver function. Conclusion: The results suggest that although C. spinosa oxymel cannot enhance the effects of hypoglycemic and hypolipidemic drugs, it can prevent further increase of blood glucose and triglycerides in patients with poorly controlled diabetes.

scholarly journals Blood sugar level follows perceived time rather than actual time in people with type 2 diabetes

2016 ◽  
Vol 113 (29) ◽  
pp. 8168-8170 ◽  
Author(s):  
Chanmo Park ◽  
Francesco Pagnini ◽  
Andrew Reece ◽  
Deborah Phillips ◽  
Ellen Langer
Keyword(s):  
Type 2 Diabetes ◽  
Blood Glucose ◽  
Blood Glucose Level ◽  
Glucose Level ◽  
The Body ◽  
Glucose Levels ◽  
Actual Time ◽  
Blood Glucose Levels ◽  
Time Changes

The current study investigates whether perceived time has an effect on blood glucose level in people with type 2 diabetes. The hypothesis is that perceived time will have a greater influence over blood glucose level than actual time. Changes in blood glucose levels were measured in 46 participants with diabetes while they completed simple tasks during a 90-min period. Participants’ perception of time was manipulated by having them refer to clocks that were either accurate or altered to run fast or slow. Blood glucose levels changed in accordance with how much time they believed had passed instead of how much time had actually passed. These results are an example of the influence psychological processes can directly exert on the body.

scholarly journals Novel GPR120 Agonists with Improved Pharmacokinetic Profiles for the Treatment of Type 2 Diabetes

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6907
Author(s):  
Guoxia Ji ◽  
Qinghua Guo ◽  
Qidi Xue ◽  
Ruifang Kong ◽  
Shiben Wang ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Blood Glucose ◽  
Pancreatic Beta Cells ◽  
Drug Candidate ◽  
Dependent Manner ◽  
Promising Target ◽  
Reduce Blood Glucose ◽  
Glucagon Like Peptide 1 ◽  
The Stability

GPR120 is a promising target for the treatment of type 2 diabetes (T2DM), which is activated by free fatty acids (FFAs) and stimulates the release of glucagon-like peptide-1(GLP-1). GLP-1, as an incretin, can enhance glucose-dependent secretion of insulin from pancreatic beta cells and reduce blood glucose. In this study, a series of novel GPR120 agonists were designed and synthesized to improve the stability and hydrophilicity of the phenylpropanoic acid GPR120 agonist TUG-891. Compound 11b showed excellent GPR120 agonistic activity and pharmacokinetic properties, and could reduce the blood glucose of normal mice in a dose-dependent manner. In addition, no hypoglycemic side effects were observed even at a dose of 100 mg/kg. Moreover, 11b showed good anti-hyperglycemic effects in diet-induced obese (DIO) mice. Molecular simulation illustrated that compound 11b could enter the active site of GPR120 and interact with ARG99. Taken together, the results indicate that compound 11b might be a promising drug candidate for the treatment of T2DM.

scholarly journals Characterization of Obesity Phenotypes inPsammomys Obesus(Israeli Sand Rats)

2000 ◽  
Vol 1 (3) ◽  
pp. 177-184 ◽  
Author(s):  
Ken R. Walder ◽  
Richard P. Fahey ◽  
Greg J. Morton ◽  
Paul Z. Zimmet ◽  
Greg R. Collier
Keyword(s):  
Type 2 Diabetes ◽  
Animal Model ◽  
Body Weight ◽  
Blood Glucose ◽  
Body Fat ◽  
Plasma Insulin ◽  
Fat Content ◽  
The Body ◽  
Psammomys Obesus

Psammomys obesus(the Israeli sand rat) has been well studied as an animal model of Type 2 diabetes. However, obesity phenotypes in these animals have not been fully characterized. We analyzed phenotypic data including body weight, percentage body fat, blood glucose and plasma insulin concentration for over 600 animals from thePsammomys obesuscolony at Deakin University to investigate the relationships between body fat, body weight and Type 2 diabetes using regression analysis and general linear modelling. The body weight distribution inPsammomys obesusapproximates a normal distribution and closely resembles that observed in human populations. Animals above the 75th percentile for body weight had increased body fat content and a greater risk of developing diabetes. Increased visceral fat content .was also associated with elevated blood glucose and plasma insulin concentrations in these animals. A familial effect was also demonstrated inPsammomys obesus, and accounted for 51% of the variation in body weight, and 23–26% of the variation in blood glucose and plasma insulin concentrations in these animals.Psammomys obesusrepresents an excellent animal model of.obesity and Type 2 diabetes that exhibits a phenotypic pattern closely resembling that observed in human population studies. The obesity described in these animals was familial in nature and was significantly associated with Type 2 diabetes.

scholarly journals A clinical study to evaluate the role of Madhumehari Vati in the management of Madhumeha type 2 diabetes

2021 ◽  
Vol 8 (4) ◽  
pp. 574
Author(s):  
Sachin Kumar Sharma ◽  
Alankruta R. Dave ◽  
Brijbala Vasishth ◽  
Vasundhara Sharma
Keyword(s):  
Type 2 Diabetes ◽  
Blood Glucose ◽  
Antioxidant Activities ◽  
Communicable Disease ◽  
Fasting Blood Glucose ◽  
The Body ◽  
Antidiabetic Activity ◽  
Plain Water ◽  
Excessive Sweating

Background: Type 2 Diabetes is a major, non-communicable disease with increasing prevalence at the global level. Type 2 diabetes is a metabolic disorder which can be correlated with Madhumeha. Madhumeha is Tridoshaj in origin with predominance of Vata and Kapha. Type 2 diabetes results when the body produces insufficient insulin or the body cannot use the insulin it produces. Most of the contents of Madhumehari Vati are having Katu (pungent), Tikta (bitter), Kashaya (astringent) Rasa (taste), Laghu (light), Ruksha (rough) Guna (properties), Katu (pungent) Vipaka (taste after digestion), Ushna (hot) Virya (potency), Deepana, Pachana Kapha-Pitta Shamaka properties and hypoglycaemic,antidiabetic activity,Hepatoprotective, hypolipidemic and antioxidant activities which are essential in the management of Madhumeha (type 2 diabetes). So, this study was taken up to evaluate the effectiveness of Madhumehari Vati in the management of Madhumeha (type 2 Diabetes).  Aim of the study was to evaluate the efficacy of Madhumehari Vati in the management of Madhumeha w.s.r type 2 diabetes.Methods: Total 31 patients were selected from OPD of Kayachikitsa, department, I. T. R. A., Jamnagar. In this study Madhumehari Vati was given in dose of one tablet (1000 mg each) three times in a day with plain water before meal.Results: After the course of therapy for 8 weeks, statistically highly significant improvement was found in subjective parameters like Pindikodwestana (calf muscles cramps), Guru Gatrata  (heaviness of body), Supti (numbness), Karapada Daha (burning sensation in palm and soles), Prabhutamutrata (polyuria), Atipipasa (polydipsia) whereas Shithila Angata (flaccidity of body parts), Swedadhikya (excessive sweating), Kshudha Adhikya (polyphasia) and Nidra Adhikya (excessive sleep) remained statistically significant (p<0.05). In objective parameters statistically highly, significant improvement was found in post prandial blood glucose whereas statistically significant improvement was found fasting blood glucose and HbA1C.Conclusions: Madhumehari Vati is effective in the management of Madhumeha (type 2 diabetes). No ADR (adverse drug reaction) was reported during the study.

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