Armeniaspirol A: a novel anti-Helicobacter pylori agent,Microbial Biotechnology

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Armeniaspirol A: a novel anti-Helicobacter pylori agent
Microbial Biotechnology ( IF 4.8 ) Pub Date : 2021-03-29 , DOI: 10.1111/1751-7915.13807
Jia Jia _{1,

2} , Chongwen Zhang ₁ , Yaqi Liu ₃ , Yanqiang Huang ₁ , Yuefan Bai ₁ , Xudong Hang ₁ , Liping Zeng ₁ , Dongqing Zhu ₃ , Hongkai Bi _{1,

2}

Affiliation

Antibiotic resistance in Helicobacter pylori has been growing worldwide with current treatment regimens. Development of new compounds for treatment of H. pylori infections is urgently required to achieve a successful eradication therapy in the future. Armeniaspirols, a novel class of natural products isolated from Streptomyces armeniacus, have been previously identified as antibacterial agents against Gram-positive pathogens. In this study, we found that armeniaspirol A (ARM1) exhibited potent antibacterial activity against H. pylori, including multidrug-resistant strains, with MIC range values of 4–16 μg ml^-1. The underlying mechanism of action of ARM1 against H. pylori involved the disruption of bacterial cell membranes. Also, ARM1 inhibited biofilm formation, eliminated preformed biofilms and killed biofilm-encased H. pylori in a dose-dependent manner. In a mouse model of multidrug-resistant H. pylori infection, dual therapy with ARM1 and omeprazole showed efficient in vivo killing efficacy comparable to the standard triple therapy, and induced negligible toxicity against normal tissues. Moreover, at acidic pH 2.5, ARM1 exhibited a much more potent anti-H. pylori activity than metronidazole. Thus, these findings demonstrated that ARM1 is a novel potent anti-H. pylori agent, which can be developed as a promising drug lead for treatment of H. pylori infections.

中文翻译：

Armeniaspirol A：一种新型抗幽门螺杆菌药物

随着目前的治疗方案，幽门螺杆菌的抗生素耐药性在全球范围内不断增长。未来迫切需要开发治疗幽门螺杆菌感染的新化合物，以实现成功的根除治疗。Armeniaspirols 是从Streptomyces armeniacus中分离出来的一类新型天然产物，之前已被鉴定为抗革兰氏阳性病原体的抗菌剂。在这项研究中，我们发现亚美尼亚螺环醇 A (ARM1) 对幽门螺杆菌（包括多重耐药菌株）表现出有效的抗菌活性，其 MIC 范围值为 4-16 μg ml ^-1。ARM1 对幽门螺杆菌的潜在作用机制涉及细菌细胞膜的破坏。此外，ARM1以剂量依赖性方式抑制生物膜形成、消除预先形成的生物膜并杀死生物膜包裹的幽门螺杆菌。在多重耐药幽门螺杆菌感染的小鼠模型中，ARM1 和奥美拉唑的双重治疗显示出与标准三联疗法相当的有效体内杀伤效果，并且对正常组织的毒性可忽略不计。此外，在酸性 pH 值 2.5 下，ARM1 表现出比甲硝唑更有效的抗幽门螺杆菌活性。因此，这些发现表明 ARM1 是一种新型有效的抗H. pylori药物，可以开发为治疗H. pylori的有前景的药物先导剂。感染。

更新日期：2021-03-29

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