Activity and mechanism of the action of zeylasterone against Bacillus subtilis
Activity and mechanism of the action of zeylasterone against Bacillus subtilis
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DOI：
10.1111/j.1365-2672.2007.03663.x
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发表时间：
2008-05-01
影响因子：
4
通讯作者：
Moujir, L.
中科院分区：
文献类型：
--
作者：
de Leon, L.;Moujir, L.
目的：研究白眉藤中6-氧酚类三萜对不同微生物的抑菌性能及对枯草芽孢杆菌的作用方式。方法与结果：采用微量稀释法测定zeylasterone和去甲基zeylasterone的活性。Zeylasterone对革兰氏阳性菌（最低抑菌浓度3-20 μ g ml(-1)）和白色念珠菌（10 μ g ml(-1)）均有较高的抑菌活性。杀伤曲线显示，对枯草芽孢杆菌的抑菌作用取决于生长阶段和接种量。Zeylasterone引起枯草芽孢杆菌细胞膜改变，表现为钾渗漏和中粒体样结构的形成。然而，LIVE/DEAD背光试验或细胞内成分外排测量均未发现膜破坏。Zeylasterone对n -乙酰氨基葡萄糖和尿苷掺入的影响较早，对胸苷和亮氨酸掺入的影响较晚。结论：不同的微生物对所研究的化合物表现出敏感性。细胞质膜的通透性变化和大分子合成的非同时停止表明zeylasterone可以作用于枯草芽孢杆菌的多个靶点。研究的意义和影响：对枯草芽孢杆菌的抑菌活性为进一步研究6-氧酚类三萜的防腐和消毒性能提供了有价值的信息。
Aims: To investigate the antimicrobial properties of 6-oxophenolic triterpenoids isolated from Maytenus blepharodes against different micro-organisms and the mode of action on Bacillus subtilis.Methods and Results: The activity of zeylasterone and demethylzeylasterone was evaluated by microdilution method. Zeylasterone showed a higher activity, being active against Gram-positive bacteria (minimum inhibitory concentration 3-20 mu g ml(-1)) and Candida albicans (10 mu g ml(-1)). Killing curves revealed a bacteriostatic effect on B. subtilis that was dependent on the growth phase and inoculum size. Zeylasterone caused cell membrane alterations in B. subtilis, as shown by potassium leakage and formation of mesosome-like structures. However, membrane disruption was not revealed by either LIVE/DEAD Baclight assay or measurement of intracellular constituent efflux. Zeylasterone showed an early effect on N-acetyl-glucosamine and uridine incorporation and later on that of thymidine and leucine.Conclusions: Diverse micro-organisms exhibit sensitivities towards compounds studied. The permeability changes in the cytoplasmic membrane and nonsimultaneous ceasing of macromolecular synthesis suggest that zeylasterone could act on multiple targets on B. subtilis.Significance and Impact of the Study: The activity showed against B. subtilis as a model of spore-forming bacteria would provide valuable information for further studies in the development of 6-oxophenolic triterpenoids as antiseptic and disinfectant properties.