1. Antidiabetic potential of phytochemicals isolated from the stem bark of Myristica fatua Houtt. var. magnifica (Bedd.) Sinclair.
- Author
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Prabha B, Neethu S, Krishnan SL, Sherin DR, Madhukrishnan M, Ananthakrishnan R, Rameshkumar KB, Manojkumar TK, Jayamurthy P, and Radhakrishnan KV
- Subjects
- Binding Sites, Cell Line, Cell Survival drug effects, Diabetes Mellitus, Type 2 drug therapy, Diabetes Mellitus, Type 2 pathology, Glycoside Hydrolase Inhibitors metabolism, Glycoside Hydrolase Inhibitors pharmacology, Humans, Hypoglycemic Agents metabolism, Hypoglycemic Agents pharmacology, Hypoglycemic Agents therapeutic use, Molecular Dynamics Simulation, Muscle Cells cytology, Muscle Cells drug effects, Muscle Cells metabolism, Myristicaceae metabolism, Phytochemicals metabolism, Phytochemicals pharmacology, Plant Bark chemistry, Plant Bark metabolism, Plant Extracts chemistry, Plant Stems chemistry, Plant Stems metabolism, Protein Structure, Tertiary, Resorcinols chemistry, Resorcinols metabolism, Resorcinols pharmacology, alpha-Glucosidases chemistry, alpha-Glucosidases metabolism, Glycoside Hydrolase Inhibitors chemistry, Hypoglycemic Agents chemistry, Myristicaceae chemistry, Phytochemicals chemistry
- Abstract
Phytochemical investigation of the stem bark of Myristica fatua Houtt. led to the isolation of a new compound 1 (3-tridecanoylbenzoic acid), along with six known acylphenols (2-7). All the compounds displayed moderate inhibitory activity on α-amylase and significant activity on α-glucosidase; however malabaricone B (6) and C (7) were identified as potent α-glucosidase inhibitors with IC
50 values of 63.70 ± 0.546, and 43.61 ± 0.620 µM respectively. Acylphenols (compounds 3-7) also showed significant antiglycation property. The molecular docking and dynamics simulation studies confirmed the efficient binding of malabaricone C with C-terminus of human maltase-glucoamylase (2QMJ). Malabaricone B also enhanced the 2-NBDG [2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxy glucose] uptake in L6 myotubes. These findings demonstrate that acylphenols isolated from Myristica fatua Houtt. can be considered as a lead scaffold for the treatment of type II diabetes mellitus., (Copyright © 2018 Elsevier Ltd. All rights reserved.)- Published
- 2018
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