Antidiabetic potential of phytochemicals isolated from the stem bark of Myristica fatua Houtt. var. magnifica (Bedd.) Sinclair

  • Bioorg Med Chem. 2018 Jul 23;26(12):3461-3467. doi: 10.1016/j.bmc.2018.05.020.
B Prabha  1 ,  S Neethu  2 ,  S Lekshmy Krishnan  3 ,  D R Sherin  4 ,  M Madhukrishnan  1 ,  R Ananthakrishnan  5 ,  K B Rameshkumar  5 ,  T K Manojkumar  4 ,  P Jayamurthy  6 ,  K V Radhakrishnan  7
Affiliations
  • 1. Chemical Science and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, India.
  • 2. Chemical Science and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, India; Academy of Scientific and Innovative Research (AcSIR), Thiruvananthapuram 695019, India.
  • 3. Agroprocessing and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, India.
  • 4. Centre for Computational Modeling and Data Engineering, Indian Institute of Information Technology and Management, Thiruvananthapuram 695581, India.
  • 5. Phytochemistry Division, Jawaharlal Nehru Tropical Botanic Garden and Research Institute, Palode, Thiruvananthapuram 695562, India.
  • 6. Academy of Scientific and Innovative Research (AcSIR), Thiruvananthapuram 695019, India; Agroprocessing and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, India.
  • 7. Chemical Science and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, India; Academy of Scientific and Innovative Research (AcSIR), Thiruvananthapuram 695019, India. Electronic address: [email protected].
PMID: 29789207 DOI: 10.1016/j.bmc.2018.05.020
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 IC50 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.

Keywords
Glucose uptake in L6 myotubes; Myristica fatua Houtt; Protein glycation; Simulation studies; α-Amylase; α-Glucosidase.
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