Evaluation of free radical scavenging capacity of methoxy containing-hybrids of thiosemicarbazone-triazole and their influence on glucose transport

Abstract

BackgroundDiabetes mellitus is a metabolic disease in which the body is unable to produce insulin or respond to insulin production, consequently leading to abnormal metabolism of carbohydrates, lipids and proteins causing elevation of glucose in the blood. Oxidative stress, an imbalance between the production of free radicals and body antioxidant system has been implicated in the pathogenesis of diabetes. Free radicals attack important macromolecules leading to cell damage. Antioxidants are intimately involved in the prevention of damage caused by free radicals.MethodsThe anti-diabetic effects of hybrid compounds (2a-h) of thiosemicarbazone and triazole containing methoxy groups at C (4) positions were tested against genes involved in glucose metabolism (Glut-4, Mef2a and Nrf-1) using quantitative real time PCR (qPCR). Free radical scavenging capacity (FRAP, TEAC, DPPH and ORAC) of the hybrids was also carried out by using established antioxidant capacity assays.ResultsFrom the results, hybrid compounds 2b and 2h showed more pronounced effects in up-regulating diabetes associated genes which are important in the up-regulation of glucose uptake. All the hybrid compounds also showed free radical scavenging abilities.ConclusionIn conclusion, hybrid compounds (2b and 2h) can be useful as potential drugs for the management of diabetes mellitus.

Metabolome modulatory effects of Kigelia africana (Lam.) Benth. fruit extracts on oxidative stress, hyperlipidaemic biomarkers in STZ-induced diabetic rats and antidiabetic effects in 3T3 L1 adipocytes

“…To our surprise, hexane fraction exhibited an up-regulation glucose uptake relative to standard reference drugs (metformin and glibenclamide). This could be justified by the activation of key transcription factors such as PPARɣ and protein kinase via the inhibition of glycerophosphate dehydrogenase which is also in consonant with what was observed by Ayeleso et al [47] The metabolites responsible may mimic or perform better than metformin widely recognized as the treatment baseline proposed by Rena et al [19] From the results of the chemical profiling of the hexane fraction of the fruit of this study, some important metabolites were detected, identified and confirmed. These compounds are azulene, trans-'a-bergamotene, and 2,4-di-tert-butylphenol which were identified in previous studies as bacterial metabolites, antioxidants and pharmaceuticals [71][72][73] .…”

“…In vitro glucose uptake in 3T3 L1 adipocytes 3T3 L1 cells derived from mouse 3T3 cells were fully differentiated after cell culture in glucose-free Dulbecco's modified Eagles medium (DMEM) as confluent monolayers into adipocytes and were exposed to the hexane fraction of Kigelia africana fruit extracts at lower concentrations of 0.05, 0.5, 5 and 50 µg/ml as described by Ayeleso et al [47] Glibenclamide (1 µM) was added as positive control as well as metformin (1 µM) as a reference drug control. The plates were mixed together, sonicated and incubated for 3 h. After the incubation period, glucose uptake in 3T3 L1 adipocytes was determined using pulse labelling with [3H]-2-deoxyglucose (3H-2-DOG) in glucose-free DMEM containing the extract and fractions for 15 min.…”

Assessment of In Vitro Antioxidant and Anti-Inflammatory Activities of Pumpkin (Cucurbita pepo) Natural Plant

“…In contrast, DPPH, a stable nitrogen-centered free radical, is commonly used to measure a compound's ability to either scavenge free radicals or donate hydrogen. 58 H 2 O 2 is freely diffusible, and hence, readily permeates the membrane and damages proteins, nucleic acids, carbohydrates, and lipids. It can give rise to singlet oxygen by reacting with superoxide anion or with HOCl or chloramines.…”

Effect of Methanolic Extract of Phoenix dactylifera L. Seeds (PDS) on Blood Glucose levels of Normoglycemic and Dexamethasone induced Diabetic Rabbits

“…Diabetes mellitus is a multietiological condition characterized by chronic symptoms, 8 due to insu cient insulin hormone production or cells that do not respond to the hormones produced 9 . It is a condition in which the body produces insu cient insulin, stops producing insulin, or becomes increasingly resistant to its activity 10 . In patients with the polygenic condition, effective glucose control is the key to preventing diabetic complications and improving quality of life.…”