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

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

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: radhu2005@gmail.com.
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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