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Urease Inhibitory Activities of β-boswellic Acid Derivatives

Urease Inhibitory Activities of β-boswellic Acid Derivatives

Sanaz Golbabaei, Roya Bazl, Sahand Golestanian, Farzaneh Nabati, Zinat Bahrampour Omrany, Behnam Yousefi, Reza Hajiaghaee, Shamsali Rezazadeh, Massoud Amanlou

Daru. 2013 Jan 2;21(1):2.

PMID: 23351363

Abstract:

Background and the purpose of the study:
Boswellia carterii have been used in traditional medicine for many years for management different gastrointestinal disorders. In this study, we wish to report urease inhibitory activity of four isolated compound of boswellic acid derivative.
Methods:
4 pentacyclic triterpenoid acids were isolated from Boswellia carterii and identified by NMR and Mass spectroscopic analysis (compounds 1, 3-O-acetyl-9,11-dehydro-β-boswellic acid; 2, 3-O-acetyl-11-hydroxy-β-boswellic acid; 3. 3-O- acetyl-11-keto-β-boswellic acid and 4, 11-keto-β-boswellic acid. Their inhibitory activity on Jack bean urease were evaluated. Docking and pharmacophore analysis using AutoDock 4.2 and Ligandscout 3.03 programs were also performed to explain possible mechanism of interaction between isolated compounds and urease enzyme.
Results:
It was found that compound 1 has the strongest inhibitory activity against Jack bean urease (IC50 = 6.27 ± 0.03 μM), compared with thiourea as a standard inhibitor (IC50 = 21.1 ± 0.3 μM).
Conclusion:
The inhibition potency is probably due to the formation of appropriate hydrogen bonds and hydrophobic interactions between the investigated compounds and urease enzyme active site and confirms its traditional usage.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP67416619	3-O-Acetyl-11-keto-β-boswellic acid		67416-61-9	Price

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