Urease inhibitory activities of β-boswellic acid derivatives

Abstract

Background and the purpose of the studyBoswellia 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.Methods4 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.ResultsIt 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).ConclusionThe 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.

Effectiveness of Liquid-Liquid Extraction, Solid Phase Extraction, and Headspace Technique for Determination of Some Volatile Water-Soluble Compounds of Rose Aromatic Water

“…Due to its fragrance, rose aromatic water is used in cosmetic industry, food flavoring, soaps, and toiletry. It is also used in traditional medicine as antiseptic facial tonic, fever reducer, cooling assist, pain killer, astringent, mild laxative, and antibacterial and in treatment of sore throat, enlarged tonsils, cardiac troubles, eye diseases, gall stones, and gut troubles [ 3 , 5 – 9 ].…”

Synthesis, evaluation, and molecular docking studies of aryl urea‐triazole‐based derivatives as anti‐urease agents

“…Urease inhibitory assays of the synthesized compounds were evaluated at the concentration of 0–10 mg/mL, using the modified Berthelot spectrophotometric method at 625 nm. The obtained results were compared with the standard compounds, hydroxyurea and thiourea …”

Sorokiniol: a new enzymes inhibitory metabolite from fungal endophyte Bipolaris sorokiniana LK12

“…The method of Golbabaei et al [ 19 ] was used to assess the urease enzyme (EC 3.5.1.5) inhibition activities. Briefly, a 0.055 ml urea (100 mM) in phosphate buffer (0.01 M LiCl 2 , 1.0 mM EDTA, 0.01 M K 2 HPO 4 .3H 2 O, pH 8.2), 0.025 ml Jack bean Urease (2 units/mL; Sigma, Germany), and various concentrations of the chemical compounds (10–100 μg/mL) were combined in the reaction mixture with incubation for 15 min in a 96-well plate at 37 °C.…”