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亚麻木酸-甲硝唑：一种缓解耐药性并抑制幽门螺杆菌的复方药物。

Linolenic Acid-Metronidazole: a Compound Relieving Drug Resistance and Inhibiting Helicobacter pylori.

机构信息

Research Center for the Prevention and Treatment of Drug Resistant Microbial Infecting, Youjiang Medical University for Nationalities, Baise, Guangxi Zhuang Autonomous Region, China.

出版信息

Antimicrob Agents Chemother. 2022 Jul 19;66(7):e0007322. doi: 10.1128/aac.00073-22. Epub 2022 Jun 27.

DOI:10.1128/aac.00073-22
PMID:35758720
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9295599/
Abstract

Metronidazole (Met) is the first choice for treating Helicobacter pylori (). However, is easy to resistant, making Met unable to be widely used. How to overcome 's Met resistance is still an issue. In this study, Met was used as the primary raw material with linolenic acid to prepare a novel compound-linolenic acid-metronidazole (Lla-Met). The MIC, minimum bactericidal concentration (MBC), colonization amount of in gastric mucosa, etc., were evaluated, respectively. Lla-Met was successfully prepared by the detection of nuclear magnetic resonance, etc., and its MIC and MBC to were 24 μg/mL, 816 μg/mL. Moreover, experiments, Lla-Met significantly reduced the colonization of drug-resistant in gastric mucosa. In the toxicity test, Lla-Met inhibited rate to GES-1 and BGC823 cells were 15% at 128 μg/mL; the mice were administered 10 times treatment Lla-Met treatment (240 mg/kg), have no difference significant injuries were found in their stomach, liver, spleen, kidney, and weight. In addition, G27 continued for 18 days with sub-Lla-Met concentration, G27 did not show drug resistance to Lla-Met; Lla-Met did not exert an effect on non- species with 128 μg/mL; Compared with a neutral environment, when the acid concentration is 3.0, Lla-Met is not decomposed and has better stability. Conclusion: Lla-Met, a newly prepared compound, has relatively well antibacterial of Met-resistant and sensitive , with a capability of overcoming the metronidazole resistance of

摘要

甲硝唑（Met）是治疗幽门螺杆菌（）的首选药物。然而，很容易产生耐药性，使得 Met 无法广泛应用。如何克服的 Met 耐药性仍然是一个问题。在这项研究中，以 Met 为主要原料，用亚油酸制备了一种新型化合物-亚油酸-甲硝唑（Lla-Met）。分别评估 MIC、最小杀菌浓度（MBC）、胃黏膜中定植量等。通过核磁共振等检测，成功制备了 Lla-Met，其对的 MIC 和 MBC 分别为 24μg/mL 和 816μg/mL。此外，实验表明，Lla-Met 显著降低了耐药在胃黏膜中的定植。在毒性试验中，Lla-Met 对 GES-1 和 BGC823 细胞的抑制率在 128μg/mL 时为 15%；给予小鼠 10 次 Lla-Met 治疗（240mg/kg），胃、肝、脾、肾无明显损伤，体重无差异。此外，G27 继续用亚 Lla-Met 浓度治疗 18 天，G27 对 Lla-Met 没有表现出耐药性；Lla-Met 对 128μg/mL 浓度下非物种没有作用；与中性环境相比，当酸度为 3.0 时，Lla-Met 不会分解，稳定性更好。结论：新制备的化合物 Lla-Met 对耐药和敏感的具有较好的抗菌作用，具有克服的 Met 耐药性的能力

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/ae4346f567c8/aac.00073-22-f006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/5c09273b1be0/aac.00073-22-f001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/6030d1ca2c76/aac.00073-22-f002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/9e3fcc9f9e68/aac.00073-22-f003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/89010a09bacd/aac.00073-22-f004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/080266f25b10/aac.00073-22-f005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/ae4346f567c8/aac.00073-22-f006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/5c09273b1be0/aac.00073-22-f001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/6030d1ca2c76/aac.00073-22-f002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/9e3fcc9f9e68/aac.00073-22-f003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/89010a09bacd/aac.00073-22-f004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/080266f25b10/aac.00073-22-f005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9b9/9295599/ae4346f567c8/aac.00073-22-f006.jpg

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