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罗斯托宁B通过直接靶向NLRP3减轻炎症性疾病。

Rosthornin B alleviates inflammatory diseases via directly targeting NLRP3.

作者信息

Yang Yanqing, Liu Didi, Cao Hairuo, Lu Li, Zhang Wei, Liu Chenfei, Zeng Yao, Shang Feifei, Tao Ye, Zhao Bao, Wang Fengchao, Tang Tiantian, Deng Mengmeng

机构信息

Department of Clinical Laboratory, The First Affiliated Hospital of Bengbu Medical University, Bengbu, Anhui, China.

Anhui Provincial Key Laboratory of Immunology in Chronic Disease, Bengbu Medical University, Bengbu, Anhui, China.

出版信息

FASEB J. 2024 Dec 13;38(24):e70248. doi: 10.1096/fj.202401198R.

DOI:10.1096/fj.202401198R
PMID:39673686
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11646051/
Abstract

Aberrant activation of the NLRP3 inflammasome contributes to the evolution of diverse inflammatory diseases. Inhibition of the NLRP3 inflammasome has been proven to be an effective treatment strategy for NLRP3-driven diseases. This study revealed that multiple natural diterpenes from Isodon plants can inhibit the NLRP3 inflammasome, among which Rosthornin B (Ros B) exhibited the best inhibitory effect, with an IC of 0.39 μM. Further study revealed that Ros B directly interacts with NLRP3, thereby restraining NEK7-NLRP3 interaction and inhibiting NLRP3 inflammasome assembly and activation. Remarkably, Ros B had a significant therapeutic benefit in mouse models of NLRP3-driven septic shock, peritonitis, and colitis. Our study has identified a series of natural diterpenes that target the NLRP3 inflammasome. These natural diterpenes, especially those with low IC values, may lead to the development of new drugs and potential clinical therapies for diseases driven by NLRP3 inflammasome activation.

摘要

NLRP3炎性小体的异常激活促进了多种炎症性疾病的发展。抑制NLRP3炎性小体已被证明是治疗由NLRP3驱动的疾病的有效策略。本研究表明，来自香茶菜属植物的多种天然二萜类化合物可抑制NLRP3炎性小体，其中迷迭香二萜B（Ros B）表现出最佳抑制效果，IC50为0.39 μM。进一步研究表明，Ros B直接与NLRP3相互作用，从而抑制NEK7-NLRP3相互作用，并抑制NLRP3炎性小体的组装和激活。值得注意的是，Ros B在NLRP3驱动的脓毒症休克、腹膜炎和结肠炎小鼠模型中具有显著的治疗益处。我们的研究鉴定了一系列靶向NLRP3炎性小体的天然二萜类化合物。这些天然二萜类化合物，尤其是那些IC值较低的化合物，可能会推动针对由NLRP3炎性小体激活驱动的疾病的新药研发和潜在临床治疗方法的发展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/010010299024/FSB2-38-e70248-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/b8a7880305f7/FSB2-38-e70248-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/d5df0c99b7c5/FSB2-38-e70248-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/102a8f0b9e4b/FSB2-38-e70248-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/98dccb30c845/FSB2-38-e70248-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/f6e5983cea29/FSB2-38-e70248-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/010010299024/FSB2-38-e70248-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/b8a7880305f7/FSB2-38-e70248-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/d5df0c99b7c5/FSB2-38-e70248-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/102a8f0b9e4b/FSB2-38-e70248-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/98dccb30c845/FSB2-38-e70248-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/f6e5983cea29/FSB2-38-e70248-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a028/11646051/010010299024/FSB2-38-e70248-g003.jpg

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Trends Biochem Sci. 2023 Apr;48(4):331-344. doi: 10.1016/j.tibs.2022.10.002. Epub 2022 Nov 4.
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