Synthesis of indole derivatives as diabetics II inhibitors and enzymatic kinetics study of α-glucosidase and α-amylase along with their in-silico study

Investigation of effective natural inhibitors for starch hydrolysing enzymes from Simaroubaceae plants by molecular docking analysis and comparison with in-vitro studies

“…Several natural molecules such as luteolin ( Yan et al., 2014 ), raspberry ketone ( Xiong et al., 2018 ), and kaempferol ( Peng et al., 2016 ) as well as some of the indole derivatives ( Taha et al., 2021 ) and Indazole Schiff bases ( Shamim et al., 2021 ) have stabilized in the active site pocket of YAG through hydrogen bond and hydrophobic interactions in a similar way as picrasidine-X observed in the present docking study. Further, few aromatic residues were involved in the hydrophobic interactions with picrasidine-X and standard AGIs.…”

Synthesis and Evaluation of 1,3,5-Triaryl-2-Pyrazoline Derivatives as Potent Dual Inhibitors of Urease and α-Glucosidase Together with Their Cytotoxic, Molecular Modeling and Drug-Likeness Studies

“…73c 250 mL of acarbose at different concentrations (250−1000 mg/mL) was incubated with 500 mL of 1.0 U/mL of α-glucosidase solution in 100 mM phosphate buffer (pH 6.8) for 20 min at 37 °C. 250 mL of 4nitrophenyl-b-D-glucopyranoside solution and 250 mL of 1% starch 42 dissolved in 100 mM phosphate buffer (pH 6.8), respectively, were then added to the reaction mixture and incubated for 1 h at 37 °C. 20 Then, 1.0 mL of the 3,5dinitrosalicylic acid coloring reagent was added to the reaction mixture and it was boiled for 10 min.…”

“…Diabetes mellitus metabolic disease gives rise to solemn health disorders, for instance cardiovascular disorders, nephropathy, retinopathy, amputations, neuropathy, cancer, and reduced ability of wound healing. The control of glycemia is an illustrious method to cure diabetes mellitus. − α-Glucosidase is a significant enzyme present on the epithelial wall of the small intestine that is involved in carbohydrate metabolism, and the inhibition of this enzyme lowers the glucose level in the blood facilitating the treatment of DM. , Many detrimental effects such as gastrointestinal diseases, flatulence, and diarrhea are associated with typical available clinical drugs such as voglibose, miglitol, and acarbose. , The inhibition of α-glucosidase via these inhibitors lowers the absorption of glucose that is released from the pancreas and salivary glands for the conversion of oligosaccharides into simple sugar via hydrolysis, consequently, lowering the postprandial blood glucose level, which is a beneficial approach to cure diabetes. , …”

Synthesis of γ‐Butyrolactone Derivatives from Dihydrotagetone and Evaluation of Their Antidiabetic Activity

“…[6] These AGIs are associated with gastrointestinal adverse effects like stomach pain, diarrhoea, cramping, enhanced flatulence, and rectal bleeding. [7,8] The adverse effects of these drugs are forcing researchers to search a new, effective, and safer alternate molecules. Current research has focused on finding naturally derived potent compounds that act as AGIs.…”

“…The clinically available oral AGI drugs, acarbose, miglitol, and voglibose are therapeutic approaches to reduce the risk of T2DM [6] . These AGIs are associated with gastrointestinal adverse effects like stomach pain, diarrhoea, cramping, enhanced flatulence, and rectal bleeding [7,8] . The adverse effects of these drugs are forcing researchers to search a new, effective, and safer alternate molecules.…”