Suliman Mohamed Malik, Timan Idriss Mona, Khedr Amgad I M, Abd AlGadir Haidar, Takeshita Satoshi, Shah Mohammad Monir, Ichinose Yoshio, Maki Toshihide
Department of Pharmaceutics, Faculty of Pharmacy, University of Khartoum, 11111 Qasr Street, P.O. Box 1996, Sudan.
Graduate School of Biomedical Sciences, School of Pharmaceutical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki-shi 852-8521, Japan.
Int J Bacteriol. 2014;2014:481686. doi: 10.1155/2014/481686. Epub 2014 Sep 28.
A bioassay-guided fractionation of methanol extract of Aristolochia bracteolata whole plant was carried out in order to evaluate its antimicrobial activity and to identify the active compounds in this extract. Antibacterial and antifungal activities of methanol extract against gram-positive, gram-negative, and fungal strains were investigated by the agar disk diffusion method. Among the strains tested, Moraxella catarrhalis and sea urchin-derived Bacillus sp. showed the highest sensitivity towards the methanol extract and hence they are used as test organisms for the bioassay-guided fractionation. From this extract, aristolochic acid 1 (AA-1) has been isolated and has showed the greatest antibacterial activity against both standard strain and clinical isolates of Moraxella catarrhalis with equal minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 25 and 50 μg/mL. Modification of the AA-1 to AA-1 methyl ester completely abolished the antibacterial activity of the compound and the piperonylic acid moiety of AA-1 which suggested that the coexistence of phenanthrene ring and free carboxylic acid is essential for AA-1 antibacterial activity.
为了评估苞叶马兜铃全草甲醇提取物的抗菌活性并鉴定该提取物中的活性化合物,对其进行了生物测定指导的分级分离。采用琼脂平板扩散法研究了甲醇提取物对革兰氏阳性、革兰氏阴性和真菌菌株的抗菌和抗真菌活性。在所测试的菌株中,卡他莫拉菌和海胆源芽孢杆菌对甲醇提取物表现出最高的敏感性,因此它们被用作生物测定指导分级分离的测试生物。从该提取物中分离出了马兜铃酸1(AA-1),其对卡他莫拉菌的标准菌株和临床分离株均表现出最大的抗菌活性,最小抑菌浓度(MIC)和最小杀菌浓度(MBC)值相等,均为25和50μg/mL。将AA-1修饰为AA-1甲酯完全消除了该化合物的抗菌活性以及AA-1的胡椒酸部分,这表明菲环和游离羧酸的共存对AA-1的抗菌活性至关重要。