Department of Medicinal Chemistry, Faculty of Pharmacy and Medicinal Plants Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Daru. 2013 Jan 2;21(1):2. doi: 10.1186/2008-2231-21-2.
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.
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.
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).
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.
乳香属植物在传统医学中已被使用多年，用于治疗多种胃肠道疾病。在这项研究中，我们希望报道 4 种乳香酸衍生物的化合物的脲酶抑制活性。
从乳香属植物中分离出 4 种五环三萜酸，并通过 NMR 和质谱分析（化合物 1、3-O-乙酰基-9,11-去氢-β-乳香酸；2、3-O-乙酰基-11-羟基-β-乳香酸；3、3-O-乙酰基-11-酮-β-乳香酸和 4、11-酮-β-乳香酸）进行鉴定。评估它们对杰克豆脲酶的抑制活性。还使用 AutoDock 4.2 和 Ligandscout 3.03 程序进行对接和药效团分析，以解释分离化合物与脲酶之间相互作用的可能机制。
发现化合物 1 对杰克豆脲酶具有最强的抑制活性（IC50=6.27±0.03 μM），与硫脲作为标准抑制剂（IC50=21.1±0.3 μM）相比。
抑制效力可能是由于研究化合物与脲酶酶活性部位之间形成了适当的氢键和疏水相互作用，这证实了其在传统医学中的应用。
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