ABSTRACT
In this study, bioactive compounds were isolated and characterized from the leaves and root-barks extracts of S.latifolius, with subsequent in vitro experimental investigations for antihyperglycemic potentials on α-amylase and α-glucosidase enzymes. Thirteen bioactive compounds were identified, including 10-Hydroxystrictosamide (2) and Quinovic acid-3-O-α-L-rhamnosyl-28-O-ß-d-glucopyranosyl ester (8), using chromatographic, nuclear magnetic resonance spectroscopy (NMR), and mass spectrometry (MS) techniques. Experimental assays revealed that compounds 1-4 exhibited potent inhibition of α-amylase and α-glucosidase, with compound 2 demonstrating the most potent α-amylase inhibition (IC50 value of 0.52 ± 0.003 µg/mL). Compound 8 showed a lower IC50 value (0.098 ± 0.016 µg/mL) against α-glucosidase compared to compound 2 and acarbose. Synergistic effects among the compounds could enhance their inhibitory actions on the enzymes, positioning them as potential anti-hyperglycemia agents. Compound 2 displayed the highest binding affinity (-7.970 kcal/mol) when docked against α-amylase (PDB ID: 2QV4), comparable to acarbose (-8.515 kcal/mol). It also ranked among the top ligands against α-glucosidase (PDB ID 3TOP), although compound 13 and acarbose had higher docking scores. All compounds exhibited ideal ADMET properties, suggesting good bioavailability and low toxicity. In conclusion, the isolated compounds exhibit promising antihyperglycemic potential and favourable safety profiles for further exploration.
Subject(s)
Glycoside Hydrolase Inhibitors , Hypoglycemic Agents , Molecular Docking Simulation , Phytochemicals , Plant Leaves , Plant Roots , alpha-Amylases , Phytochemicals/pharmacology , Phytochemicals/isolation & purification , Plant Leaves/chemistry , alpha-Amylases/antagonists & inhibitors , Glycoside Hydrolase Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/isolation & purification , Plant Roots/chemistry , Molecular Structure , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , alpha-Glucosidases/metabolism , Plant Extracts/pharmacology , Plant Extracts/chemistry , Computer SimulationABSTRACT
Mn(OAc)3-mediated tandem phosphonyl radical addition to ß-nitrostyrenes followed by denitration to form (E)-2-alkenyl phosphonates in good yield is described.
ABSTRACT
Direct radical acetoxyphosphorylation of styrenes mediated by Mn(OAc)3 with diphenylphosphine oxide and dialkyl phosphites was described, and a new type of difunctionalization of alkenes was achieved.
Subject(s)
Alkenes/chemistry , Manganese/chemistry , Organophosphorus Compounds/chemistry , Phosphites/chemistry , Styrenes/chemistry , Molecular Structure , PhosphorylationABSTRACT
Mn(OAc)3-mediated direct Csp2-H radical trifluoromethylation of coumarins with CF3SO2Na (Langlois reagent) to afford selective 3-trifluoromethyl coumarins in moderate to good yields is described. This methodology can also be applied to the trifluoromethylation of quinolinones and pyrimidinones.
Subject(s)
Coumarins/chemistry , Hydrocarbons, Fluorinated/chemistry , Manganese/chemistry , Mesylates/chemistryABSTRACT
A novel CuO-catalyzed coupling reaction of arylhydrazines with trialkyl phosphites to afford arylphosphonates is described. The reaction proceeded at 80 °C in air without external reductants, oxidants, and ligands.
