米卡诺内酯及其衍生物的抗菌活性。
The antibacterial activities of mikanolide and its derivatives.
作者信息
Facey P C, Peart P C, Porter R B R
机构信息
Department of Chemistry, The University of the West Indies, Kingston 7, Jamaica, West Indies.
出版信息
West Indian Med J. 2010 Jun;59(3):249-52.
OBJECTIVE
The sesquiterpene, mikanolide, was found to possess antibacterial activity. As a result, a structure-activity relationship study was carried out on mikanolide and eleven of its derivatives.
METHODS
Mikanolide and two of its derivatives were isolated from organic extract of Mikania micrantha using chromatographic methods. Nine additional derivatives were synthesized and all were investigated for their antibacterial activity against the Gram positive pathogen Staphylococcus aureus and beta haemolytic Streptococcus group A (BHSA) as well as the Gram negative Escherichia coli using the disk diffusion assay.
RESULTS
The investigation revealed that only four of the derivatives displayed antibacterial activity and only pathogens Staphylococcus aureus and beta haemolytic Streptococcus group A were susceptible at a concentration of 100 microg per disk. However there was an increase in activity for three of the derivatives in comparison to mikanolide.
CONCLUSION
This study underscores the potential for phytochemicals from locally available plants to be further investigated and developed as antibacterial agents.
目的
发现倍半萜米卡诺内酯具有抗菌活性。因此，对米卡诺内酯及其十一种衍生物进行了构效关系研究。
方法
采用色谱法从薇甘菊的有机提取物中分离出米卡诺内酯及其两种衍生物。另外合成了九种衍生物，并使用纸片扩散法研究了它们对革兰氏阳性病原体金黄色葡萄球菌和A组β溶血性链球菌（BHSA）以及革兰氏阴性大肠杆菌的抗菌活性。
结果
研究表明，只有四种衍生物具有抗菌活性，且仅在每片含100微克的浓度下，病原体金黄色葡萄球菌和A组β溶血性链球菌敏感。然而，与米卡诺内酯相比，其中三种衍生物的活性有所增强。
结论
本研究强调了对当地可得植物中的植物化学物质作为抗菌剂进行进一步研究和开发的潜力。
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