乙柏林抑制了Helicobacter pylori,并通过降低尿酶表达的调节来减少宿主亡和炎症损伤
Huimin Wu1, Xinrui Xie2, Qin Tang3
1Engineering Research Center of Coptis Development and Utilization (Ministry of Education), College of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, China; Chongqing Haiwang Biological Engineering Co., Chongqing, 409900, China.
乙柏林 (EPI) 通过抑制尿素酶活性和减少胃炎症,有效地对抗抗生素耐药的Helicobacter pylori (H. pylori). 这种传统中医药化合物为H. pylori感染提供了一个有希望的替代方案.
科学领域:
- 药理学 药理学是指药理学的学科.
- 微生物学 微生物学
- 胃肠病学 胃肠病学
背景情况:
- Helicobacter pylori (H. pylori) 抗生素耐药性的增加需要新的治疗策略.
- 中国传统医药中的Rhizoma Coptidis表现出强大的抗H. pylori作用.
- 作为一个关键的化物,Epiberberine (EPI) 显示出潜力,但它的H. pylori清除和尿酶抑制机制需要阐明.
研究的目的:
- 为了评估Epiberberine (EPI) 对H.pylori的抑制作用.
- 探索EPI对Helicobacter pylori尿酶 (HPU) 的多方面的作用.
主要方法:
- 在体外和体内测试 (MIC,MBC,生长动力学,TEM,动物模型) 评估了EPI的抗H. pylori疗效和耐药性发展.
- 生物化学和分子对接研究研究了EPI与HPU的相互作用.
- 转录组分析和RT-PCR检查了ureB基因表达.
- 通过MTT测定,霍希斯特染色,JC-1,西斑和格里斯测定,评估了EPI对胃上皮细胞的影响.
主要成果:
- EPI在体外表现出显著的抗H. pylori活性,诱导细菌碎片化和无抵抗的亡.
- 在体内研究证实了EPI的H. pylori清除和减少H. pylori诱导的胃炎症.
- EPI表现出三重机制:抑制ureB表达,直接结合并抑制HPU活性,并减轻HPU诱导的亡和炎症.
结论:
- 乙柏林 (EPI) 是一种对抗H. pylori的有效药物,可以作为抗生素的替代品.
- EPI通过向尿酶活性和降低 ureB 表达的调节来减少宿主胃亡和炎症.
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