Igoli John Ogbaji, Gray Alexander Irvine, Clements Carol Jean, Kantheti Poorna, Singla Rajeev Kumar
Division of Biotechnology, Netaji Subhas Institute of Technology, Azad Hind Fauz Marg, Sector-3, Dwarka-110078 New Delhi-78, India.
Curr Top Med Chem. 2014;14(8):1014-21. doi: 10.2174/1568026614666140324122323.
Chemical investigation of the lichen Cetraria islandica has led to the isolation of four compounds identified as protolichesterinic acid, lichesterinic acid, protocetraric acid and fumarprotocetraric acid. Their structures were characterized using their physical and spectroscopic data. Using an Alamarblue™ 96 well microplate assay, these compounds were tested to evaluate their trypanocidal activity against Trypanosoma brucei brucei. Protolichesterinic acid (MIC = 6.30 µM) and lichesterinic acid (MIC = 12.5 µM) showed very significant activity against the test organism. Docking studies (GRIP technique) of these molecules revealed their strong affinity towards possible targets of Trypanosoma brucei such as riboflavin kinase, sterol-14α-demethylase (CYP51), rohedsain and glutathione synthetase. Hydrophobicity played a significant role in their antitrypanosomal activity.
对地衣冰岛衣进行化学研究，已分离出四种化合物，分别鉴定为原地衣硬脂酸、地衣硬脂酸、原冰岛衣酸和富马原冰岛衣酸。利用其物理和光谱数据对它们的结构进行了表征。使用Alamarblue™ 96孔微孔板测定法，对这些化合物进行测试，以评估它们对布氏布氏锥虫的杀锥虫活性。原地衣硬脂酸（MIC = 6.30 µM）和地衣硬脂酸（MIC = 12.5 µM）对受试生物体显示出非常显著的活性。对这些分子的对接研究（GRIP技术）揭示了它们对布氏锥虫可能的靶点如核黄素激酶、甾醇-14α-脱甲基酶（CYP51）、罗赫德辛和谷胱甘肽合成酶具有很强的亲和力。疏水性在它们的抗锥虫活性中起重要作用。
