Deoxyshikonin: a promising lead drug grass against drug resistance or sensitivity to Helicobacter pylori in an acidic environment.

IF 4.1 2区 医学 Q2 MICROBIOLOGY Antimicrobial Agents and Chemotherapy Pub Date : 2024-10-08 Epub Date: 2024-08-22 DOI:10.1128/aac.00959-24
Jia-Yin Xu, Hui-Hua Dong, Li-Juan Liao, Shi-Xian Yang, Lu-Yao Wang, Hao Chen, Peipei Luo, Liang Huang, Ai-Xing Guan, Yan-Qiang Huang
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Abstract

Helicobacter pylori (H. pylori) is closely associated with the diseases such as gastric sinusitis, peptic ulcers, and gastric adenocarcinoma. Its drug resistance is very severe, and new antibiotics are urgently needed. Nine comfrey compounds were screened by antimicrobial susceptibility testing, among which deoxyshikonin had the best inhibitory effect, with a minimum inhibitory concentration (MIC) of 0.5-1 µg/mL. In addition, deoxyshikonin also has a good antibacterial effect in an acidic environment, it is highly safe, and H. pylori does not readily develop drug resistance. Through in vivo experiments, it was proven that deoxyshikonin (7 mg/kg) had a beneficial therapeutic effect on acute gastritis in mice infected with the multidrug-resistant H. pylori BS001 strain. After treatment with desoxyshikonin, colonization of H. pylori in the gastric mucosa of mice was significantly reduced, gastric mucosal damage was repaired, inflammatory factors were reduced, and the treatment effect was better than that of standard triple therapy. Therefore, deoxyshikonin is a promising lead drug to solve the difficulty of drug resistance in H. pylori, and its antibacterial mechanism may be to destroy the biofilm and cause an oxidation reaction.

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脱氧雪腐镰刀菌素:在酸性环境中对抗幽门螺旋杆菌耐药性或敏感性的前景广阔的先导药物草。
幽门螺杆菌与胃窦炎、消化性溃疡和胃腺癌等疾病密切相关。其耐药性非常严重,迫切需要新的抗生素。通过抗菌药敏试验筛选出了九种紫草化合物,其中去氧紫草素的抑菌效果最好,最低抑菌浓度(MIC)为 0.5-1 µg/mL。此外,脱氧雪腐镰刀菌素在酸性环境中也有很好的抗菌效果,安全性高,幽门螺杆菌不易产生耐药性。通过体内实验证明,脱氧雪腐镰刀菌素(7 毫克/千克)对感染耐多药幽门螺杆菌 BS001 株的小鼠急性胃炎有良好的治疗效果。使用去氧石蒜碱治疗后,小鼠胃黏膜的幽门螺杆菌定植率明显降低,胃黏膜损伤得到修复,炎症因子减少,治疗效果优于标准三联疗法。因此,脱氧雪腐镰刀菌素是一种有望解决幽门螺杆菌耐药性难题的先导药物,其抗菌机制可能是破坏生物膜并引起氧化反应。
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来源期刊
CiteScore
10.00
自引率
8.20%
发文量
762
审稿时长
3 months
期刊介绍: Antimicrobial Agents and Chemotherapy (AAC) features interdisciplinary studies that build our understanding of the underlying mechanisms and therapeutic applications of antimicrobial and antiparasitic agents and chemotherapy.
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