IN VITRO SOLUBLE EPOXIDE HYDROLASE ENZYME INHIBITORY ACTIVITY OF SOME NOVEL CHALCONE DERIVATIVES

Authors

  • Kuppusamy Asokkumar
  • Lokeswari Prathyusha Tangella College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
  • Muthusamy Umamaheshwari College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
  • Thirumalaisamy Shivashanmugam College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
  • Varadharajan Subhadradevi College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
  • Puliyath Jagannath College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
  • Arumugam Madeswaran College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,

DOI:

https://doi.org/10.7439/ijpp.v2i4.705

Keywords:

Pattern reversal, Visual evoked potentials

Abstract

Objective Soluble epoxide hydrolase ( sEH) belongs to the ?/? -hydrolase superfamily, a subclass of ?/? proteins. Chalcones are chemical compounds that show hopeful obliging efficacy in controlling numerous diseases. The main objective of the study is to evaluate the sEH inhibitory activity of some synthesized chalcone derivatives and identification of its mode of inhibition. Methods Four different chalcone derivatives (PC-1 to PC-4) were selected for synthesis by Claisen-Schmidt method. The in vitro sEH inhibitory activity was performed for the synthesized compounds by fluorimetric assay. The percentage of sEH activity and IC50 values were calculated for the synthesized compounds. Dissociation constant were determined by following the method described by Lineweaver-Burks plot. Results and Conclusions The IC50 value obtained for PC-1, PC-2, PC-3, and PC-4 were found to be 0.8213 g/mL, 2.64 g/mL, 0.2490 g/mL and 0.5238 g/mL respectively. The order of potency (IC50) of the chalcone and chalcone oxide in sEH inhibition assay was PC-3 > PC-4 > PC-1 >PC-2. All the compounds (PC-1, PC-2, PC-3) showed mixed type of inhibition except PC-4 which showed non-competitive type of inhibition. Further in vivo studies are to be carried out for these compounds to confirm their activity and explore the mechanism by which these compounds act and rationalize their use.

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Author Biographies

  • Kuppusamy Asokkumar
    Professor,Department of Pharmacology,
  • Lokeswari Prathyusha Tangella, College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
    Department of Pharmacology,
  • Thirumalaisamy Shivashanmugam, College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
    Lecturer,Department of Pharmacology,
  • Varadharajan Subhadradevi, College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
    Lecturer,Department of Pharmacology,
  • Puliyath Jagannath, College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
    Lecturer,Department of Pharmacology,
  • Arumugam Madeswaran, College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences,
    Lecturer,Department of Pharmacology,

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Published

2012-09-01

Issue

Section

Research Articles

How to Cite

1.
IN VITRO SOLUBLE EPOXIDE HYDROLASE ENZYME INHIBITORY ACTIVITY OF SOME NOVEL CHALCONE DERIVATIVES. Int J of Phytopharm [Internet]. 2012 Sep. 1 [cited 2025 Mar. 14];2(4):116-21. Available from: https://ssjournals.co.in/index.php/ijpp/article/view/1147