Work

Marmin of Aegle Marmelos Correa Antagonizes AChM3 Receptors: In Silico and In Vitro Studies on Isolated-Guinea Pig Illeum Smooth Muscle

Year: 2014

Type: article

Abstract: A previous study has shown that ethanolic extract of leaves of A. marmelos Correa on isolated ileum had an antagonistic effect on the contraction induced by histamine.Apart from H 1 receptors, muscarinic acetylcholine (AChM) receptors are also involved in the mechanism of ileum contraction.Marmin is predicted to antagonize the AChM 3 receptors.This study was aimed at determining the effect of marmin on smooth muscle contraction of isolated guinea pig ileum induced by metacholine, an AChM 3 agonist.The methods used were in vitro (isolated organ) and in silico (docking PLANTS) studies.In the in vitro study, marmin exhibited a competitive antagonistic effect at a concentration of 100 μM (pA 2 = 1,728) on the AChM 3 receptors.A reversibility assay of the AChM 3 receptors showed that by washing the ileum with Tyrode's buffer every 6 minutes for 30 minutes, the bond of marmin to the receptors was still not completely detached.In the in silico study, marmin was observed to be bound to the AchM 3 receptors (docking score: -102.086).The marmin bond was weaker than that of the native ligand of the AChM 3 receptors (tiotropium, docking score: -115.107),but stronger than that of the AChM3 receptor agonist and antagonist.Based on the results, we conclude that marmin has competitive antagonist activity on AChM 3 receptors.

Source: Journal of Mathematical and Fundamental Sciences

DOI: 10.5614/j.math.fund.sci.2014.46.3.6

Authors: Puguh Noviarsito, Sugeng Riyanto, Agung Endro Nugroho

Institutions: Universitas Gadjah Mada, Muhammadiyah University of Yogyakarta

Language: English

Topic: Phytochemicals and Medicinal Plants

Subfield: Complementary and alternative medicine

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $150