Author/Authors :
Golbabaei, Sanaz tehran university of medical sciences tums - Faculty of Pharmacy and Medicinal Plants Research Center - Department of Medicinal Chemistry, تهران, ايران , Bazl, Roya tehran university of medical sciences tums - Faculty of Pharmacy and Medicinal Plants Research Center - Department of Medicinal Chemistry, تهران, ايران , Golestanian, Sahand tehran university of medical sciences tums - Faculty of Pharmacy and Medicinal Plants Research Center - Department of Medicinal Chemistry, تهران, ايران , Nabati, Farzaneh tehran university of medical sciences tums - Faculty of Pharmacy and Medicinal Plants Research Center - Department of Medicinal Chemistry, تهران, ايران , Bahrampour Omrany, Zinat tehran university of medical sciences tums - Faculty of Pharmacy and Medicinal Plants Research Center - Department of Medicinal Chemistry, تهران, ايران , Yousefi, Behnam tehran university of medical sciences tums - School of Advanced Medical Technologies, تهران, ايران , Hajiaghaee, Reza Academic Center for Education, Culture and Research( ACECR) - Medicinal Plants Research Center, Institute of Medicinal Plants - Pharmacognosy Pharmaceutics Department, ايران , Rezazadeh, Shamsali Academic Center for Education, Culture and Research( ACECR) - Medicinal Plants Research Center, Institute of Medicinal Plants - Pharmacognosy Pharmaceutics Department, ايران , Amanlou, Massoud tehran university of medical sciences tums - Faculty of Pharmacy and Medicinal Plants Research Center - Department of Medicinal Chemistry, تهران, ايران
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.
Keywords :
Keywords: Boswellia carterii , Urease inhibitor , Boswellic acid , Docking , Autodock
