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水龙骨素通过一种宿主靶向策略作用于细胞内。

Equisetin Targets Intracellular through a Host Acting Strategy.

机构信息

National Center for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, No. 2 Yuanmingyuan West Road, Beijing 100193, China.

Guangdong Laboratory for Lingnan Modern Agriculture, Guangzhou 510642, China.

出版信息

Mar Drugs. 2022 Oct 22;20(11):656. doi: 10.3390/md20110656.

DOI:10.3390/md20110656
PMID:36354979
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9694014/
Abstract

Mammalian cells act as reservoirs of internalized bacteria to circumvent extracellular antibacterial compounds, resulting in relapse and reinfection diseases. The intracellular persistence of renders most traditional antibiotics useless, due to their inadequate subcellular accumulation. To replenish our antibiotic arsenal, we found that a marine-derived compound, equisetin, efficiently eliminates intracellular by potentiating the host autophagy and inducing mitochondrial-mediated ROS generation to clear the invading . The remarkable anti-infection activity of equisetin was validated in a peritonitis-infected mouse model. The marine product equisetin utilizes a unique dual mechanism to modulate the host-pathogen interaction in the clearance of intracellular bacteria. Thus, equisetin is an inspiring host-acting candidate for overcoming intracellular pathogens.

摘要

哺乳动物细胞充当内化细菌的储库,以规避细胞外抗菌化合物,从而导致疾病复发和再感染。由于大多数传统抗生素在细胞内的积累不足,因此 的细胞内持续存在使它们变得无效。为了补充我们的抗生素库,我们发现一种海洋衍生的化合物,问荆亭,通过增强宿主自噬并诱导线粒体介导的 ROS 生成来清除入侵的 ,有效地消除了细胞内的 。问荆亭在腹膜炎感染的小鼠模型中验证了其显著的抗感染活性。海洋产物问荆亭利用独特的双重机制来调节宿主-病原体相互作用,以清除细胞内细菌。因此,问荆亭是克服细胞内病原体的一种有前途的宿主作用候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/f2ce153f6e36/marinedrugs-20-00656-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/bc7c73d08240/marinedrugs-20-00656-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/937a07daf85f/marinedrugs-20-00656-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/0380bc5e7d68/marinedrugs-20-00656-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/f2ce153f6e36/marinedrugs-20-00656-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/bc7c73d08240/marinedrugs-20-00656-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/937a07daf85f/marinedrugs-20-00656-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/0380bc5e7d68/marinedrugs-20-00656-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6af/9694014/f2ce153f6e36/marinedrugs-20-00656-g004.jpg

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β-Lactams from the Ocean.海洋来源的β-内酰胺类抗生素。
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