抗菌性黄类药物:在质中,能够有效地向大肠杆菌的DNA旋转酶
Harshal Shivaji Patil1,2, Jaysing M Dinore3, Ali Alrabie4
1Department of Chemistry, Moreshwar Art's, Science and Commerce College, Bhokarda, India.
Natural product research
|January 8, 2024
概括
莱乌卡斯阿斯佩拉产生了强大的抗微生物化合物,贝卡莱因和贝卡莱因-7-O-β-D-葡萄化物,对细菌有效. 这些化合物显示出开发新抗菌剂的前景.
科学领域:
- 植物化学 植物化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- Leucas aspera是一种具有传统药用历史的植物.
- 研究其化学成分可以揭示新的治疗化合物.
研究的目的:
- 为了隔离和识别来自Leucas aspera的植物化学物质.
- 评估分离化合物的抗菌活性.
- 探索活性化合物的分子机制和药理动力学特性.
主要方法:
- 使用光谱方法进行植物化学分离和表征.
- 在体外抗微生物测定以确定最小抑制度 (MIC).
- 对细菌DNA旋转酶进行分子对接研究.
- 在 silico ADME 配置文件.
主要成果:
- 隔离了黄素 (拜卡莱因,拜卡莱因-7-O-β-D-葡萄糖化物),类固醇 (β-西托斯特醇,斯蒂格马斯特醇) 和三类固醇 (lup-20(29) -ene-3α,23-diol).
- 拜卡莱因和拜卡莱因-7-O-β-D-葡萄化物对黄金葡萄球菌,色菌和大肠杆菌具有显著的抗菌活性.
- 拜卡莱因-7-O-β-D-葡萄化物对大肠杆菌DNA旋转酶 (-5.78 kcal/mol) 具有强烈的结合亲和力,并且在中具有有利的ADME特性.
结论:
- 草是具有显著抗菌潜力的生物活性化合物的来源.
- 拜卡莱因-7-O-β-D-葡萄化物是新型抗菌药物开发的有希望的候选者,因为它的疗效,作用机制和良好的药理学特征.
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