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花椒属植物中苯丙素类化合物的神经营养和抗神经炎症作用(Rutaceae)。

The neurotrophic and antineuroinflammatory effects of phenylpropanoids from Zanthoxylum nitidum var. tomentosum (Rutaceae).

机构信息

State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, People's Republic of China.

Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering and Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, Southeast University, Nanjing 211189, China.

出版信息

Fitoterapia. 2021 Sep;153:104990. doi: 10.1016/j.fitote.2021.104990. Epub 2021 Jul 9.

Abstract

Three novel lignans (1, 5 and 6) and two novel quinic acids (16 and 17) along with 15 known phenylpropanoids were obtained from the ethanol extract of Zanthoxylum nitidum var. tomentosum (Rutaceae). Their structures were confirmed by comprehensive spectroscopic data (NMR and HRESIMS), and the absolute configurations of all novel compounds were elucidated based on electronic circular dichroism (ECD) spectroscopic data. The production of nitric oxide (NO) in BV-2 microglial cells induced through lipopolysaccharide (LPS) was used to evaluate in vitro anti-neuroinflammatory activity of compounds 1-20. Compound 2, 3, 7 and 16 showed excellent inhibition of LPS-induced NO production. The structure-activity relationships of the isolates were investigated. In addition, the mechanism of action of 2 was elucidated by RT-PCR and Western blotting analysis, which indicated that it reduced neuroinflammatory mainly through NLRP3/caspase1 signaling pathways in LPS-induced BV2 microglial cells.

摘要

从花椒(Rutaceae)的乙醇提取物中分离得到了 3 种新的木脂素(1、5 和 6)和 2 种新的奎尼酸(16 和 17)以及 15 种已知的苯丙素。通过综合光谱数据(NMR 和 HRESIMS)确定了它们的结构,并根据电子圆二色谱(ECD)光谱数据阐明了所有新化合物的绝对构型。使用脂多糖(LPS)诱导的 BV-2 小胶质细胞中产生的一氧化氮(NO)来评估化合物 1-20 的体外抗神经炎症活性。化合物 2、3、7 和 16 对 LPS 诱导的 NO 产生具有出色的抑制作用。对分离物的结构-活性关系进行了研究。此外,通过 RT-PCR 和 Western blot 分析阐明了 2 的作用机制,表明它主要通过 LPS 诱导的 BV2 小胶质细胞中的 NLRP3/caspase1 信号通路来减轻神经炎症。

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