瑞香素：一种新型抗剂。
Daphnetin: A Novel Anti- Agent.
机构信息
Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Los Angeles Biomedical Research Institute, Harbor-UCLA Medical Center, Torrance, CA 90502, USA.
出版信息
Int J Mol Sci. 2019 Feb 15;20(4):850. doi: 10.3390/ijms20040850.
BACKGROUND
Antibiotic-resistant was increasingly found in infected individuals, which resulted in treatment failure and required alternative therapeutic strategies. Daphnetin, a coumarin-derivative compound, has multiple pharmacological activities.
METHODS
The mechanism of daphnetin on was investigated focusing on its effect on cell morphologies, transcription of genes related to virulence, adhesion, and cytotoxicity to human gastric epithelial (GES-1) cell line.
RESULTS
Daphnetin showed good activities against multidrug resistant (MDR) clinical isolates, with minimal inhibitory concentration (MIC) values ranging from 25 to 100 μg/mL. In addition, daphnetin exposure resulted in morphological changes. Moreover, daphnetin caused increased translocation of phosphatidylserine (PS), DNA damage, and expression, and RecA protein production vs. control group. Of great importance, daphnetin significantly decreased adhesion to GES-1 cell line vs. control group, which may be related to the reduced expression of colonization related genes (e.g., and ).
CONCLUSIONS
These results suggested that daphnetin has good activity against MDR The mechanism(s) of daphnetin against were related to change of membrane structure, increase of DNA damage and PS translocation, and decrease of attachment to GES-1 cells.
背景
越来越多的感染个体中发现了对抗生素耐药的 ，这导致了治疗失败，需要替代的治疗策略。香豆素衍生物瑞香素具有多种药理活性。
方法
本研究聚焦于瑞香素对细胞形态、与毒力、黏附相关基因转录以及对人胃上皮（GES-1）细胞系细胞毒性的影响，探讨了瑞香素对 的作用机制。
结果
瑞香素对多重耐药（MDR）临床分离株表现出良好的活性，最小抑菌浓度（MIC）值范围为 25-100μg/ml。此外，瑞香素暴露导致 形态发生变化。此外，与对照组相比，瑞香素引起了磷脂酰丝氨酸（PS）、DNA 损伤和 表达以及 RecA 蛋白产生的增加。非常重要的是，与对照组相比，瑞香素显著降低了 对 GES-1 细胞系的黏附，这可能与定植相关基因（如 和 ）表达降低有关。
结论
这些结果表明，瑞香素对 MDR 具有良好的活性。瑞香素对 的作用机制与膜结构的改变、DNA 损伤和 PS 易位的增加以及 与 GES-1 细胞的黏附减少有关。
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