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从苍耳中鉴定出潜在的炎症抑制剂。

Identification of potential inflammatory inhibitors from Aster tataricus.

机构信息

College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.

Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology, 30 Cheongju, Chungbuk 28116, Republic of Korea.

出版信息

Bioorg Chem. 2019 Nov;92:103208. doi: 10.1016/j.bioorg.2019.103208. Epub 2019 Aug 19.

Abstract

Aster tataricus L.f. is a traditional Eastern Asian herbal medicine used for the relief of cough-related illnesses. In this study, 32 known compounds and two novel monoterpene glycosides were isolated from the roots of A. tataricus. With the aid of reported data, elucidation of the root-extract components was carried out using a multitude of spectroscopic techniques. All isolates were investigated for their ability to inhibit nitric oxide (NO) secretion in lipopolysaccharide-activated RAW264.7 cells. Compound 7 remarkably suppressed NO production with an IC value of 8.5 µM. In addition, compound 7 exhibited significant inhibitory activity against the production of inflammatory cytokines (prostaglandin E, interleukin-6, and interleukin-1 beta) and the expression of inflammatory enzymes (inducible nitric oxide synthase and cyclooxygenase-2) via inhibition of nuclear factor-kappa B activation. Moreover, compound 7 effectively prevented the downstream activation of the mitogen-activated protein kinase signaling pathway by inhibiting phosphorylation of c-Jun N-terminal kinases, extracellular signal-regulated kinases, and p38. These results outline compound 7 as a potential inhibitor for the broad treatment of inflammatory diseases, such as atopic dermatitis, asthma, and various allergies.

摘要

苍术是一种传统的东亚草药,用于缓解与咳嗽相关的疾病。在这项研究中,从苍术的根部分离出 32 种已知化合物和两种新型单萜糖苷。借助报道的数据,采用多种光谱技术对根提取物的成分进行了阐明。所有分离出的化合物都被检测了抑制脂多糖激活的 RAW264.7 细胞中一氧化氮(NO)分泌的能力。化合物 7 对 NO 产生的抑制作用显著,IC 值为 8.5µM。此外,化合物 7 通过抑制核因子-κB 的激活,对炎症细胞因子(前列腺素 E、白细胞介素-6 和白细胞介素-1β)的产生和炎症酶(诱导型一氧化氮合酶和环氧化酶-2)的表达表现出显著的抑制活性。此外,化合物 7 通过抑制 c-Jun N-末端激酶、细胞外信号调节激酶和 p38 的磷酸化,有效阻止丝裂原活化蛋白激酶信号通路的下游激活。这些结果表明化合物 7 可能是一种治疗炎症性疾病的潜在抑制剂,如特应性皮炎、哮喘和各种过敏。

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