Khan Inamullah, Nisar Muhammad, Ebad Farooq, Nadeem Said, Saeed Muhammad, Khan Haroon, Khuda Fazli, Karim Nasiara, Ahmad Zia
Department of Pharmacy, University of Peshawar, Peshawar 25120, Pakistan.
J Ethnopharmacol. 2009 Jan 12;121(1):175-7. doi: 10.1016/j.jep.2008.10.009. Epub 2008 Oct 21.
Smilax china Linn. is extensively used in traditional Chinese medicine (TCM) as well as in Pakistan for several medicinal purposes including their use in inflammatory disorders.
The aims of the current study were to validate and assess the folk use of Smilax china Linn. on pharmacological grounds using the isolated compound at molecular, in vivo and computational levels.
Seiboldogenin was isolated from ethyl acetate fraction of the plant crude extract. In vitro lipoxygenase and in vivo carrageenan-induced hind paw oedema models were used in experimental studies while molecular docking technique was used to conduct computational study.
Sieboldogenin showed significant lipoxygenase inhibition (IC50: 38 microM). It also exhibited significant inhibition (p<0.05) of carrageenan-induced hind paw oedema at the doses of 10 and 50mg/kg. Computational molecular docking showed its molecular interaction with important amino acid residues in the catalytic site of lipoxygenase, revealing its potential binding mode at molecular level.
Sieboldogenin seems to be a potential new anti-inflammatory compound responsible for anti-inflammatory activities of Smilax china Linn. Its in vitro and in vivo inflammatory activities are in good agreement with the folk medicinal use of Smilax china Linn. in inflammatory disorders.
菝葜在中国传统医学以及巴基斯坦被广泛用于多种药用目的,包括用于炎症性疾病。
本研究的目的是在分子、体内和计算机模拟水平上,基于药理学依据,利用分离得到的化合物验证和评估菝葜的民间药用价值。
从植物粗提取物的乙酸乙酯部分分离出白藜芦醇苷元。实验研究采用体外脂氧合酶和体内角叉菜胶诱导的后爪水肿模型,同时使用分子对接技术进行计算机模拟研究。
白藜芦醇苷元显示出显著的脂氧合酶抑制作用(IC50:38微摩尔)。在10和50毫克/千克剂量下,它对角叉菜胶诱导的后爪水肿也表现出显著抑制作用(p<0.05)。计算机模拟分子对接显示其与脂氧合酶催化位点的重要氨基酸残基存在分子相互作用,揭示了其在分子水平上的潜在结合模式。
白藜芦醇苷元似乎是一种潜在的新型抗炎化合物,它导致了菝葜的抗炎活性。其体外和体内的炎症活性与菝葜在炎症性疾病中的民间药用价值高度一致。