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(科:)植物成分的多靶点抗炎特性报告

A Report on Multi-Target Anti-Inflammatory Properties of Phytoconstituents from (Family: ).

机构信息

Research Center of Bioactive Materials, Department of Bioactive Material Sciences, Division of Life Sciences (Molecular Biology Major), Jeonbuk National University, Jeonju 54896, Korea.

Department of Biochemistry and Molecular Biology, National University, Gazipur 1704, Bangladesh.

出版信息

Molecules. 2021 Dec 6;26(23):7397. doi: 10.3390/molecules26237397.

Abstract

This study aims to investigate the potential analgesic properties of the crude extract of leaves using in vivo experiments and in silico analysis. The extract, in a dose-dependent manner, exhibited a moderate analgesic property (~54% pain inhibition in acetic acid-induced writhing test), which is significant (** < 0.001) as compared to the control group. The complex inflammatory mechanism involves diverse pathways and they are inter-connected. Therefore, multiple inflammatory modulator proteins were selected as the target for in silico analysis. Computational analysis suggests that all the selected targets had different degrees of interaction with the phytochemicals from the extract. Rutin (RU), protocatechuic acid (PA), vanillic acid (VA), and ferulic acid (FA) could regulate multiple targets with a robust efficiency. None of the compounds showed selectivity to Cyclooxygenase-2 (COX-2). However, regulation of COX and lipoxygenase (LOX) cascade by PA can reduce non-steroidal analgesic drugs (NSAIDs)-related side effects, including asthma. RU showed robust regulation of cytokine-mediated pathways like RAS/MAPK and PI3K/NF-kB by inhibition of EGFR and IKBα (IKK), which may prevent multi-organ failure due to cytokine storm in several microbial infections, for example, SARS-CoV-2. Further investigation, using in vivo and in vitro experiments, can be conducted to develop multi-target anti-inflammatory drugs using the isolated compounds from the extract.

摘要

本研究旨在通过体内实验和计算分析来探究 叶粗提物的潜在镇痛特性。该提取物具有中度的镇痛特性(在醋酸诱导的扭体试验中,约有 54%的疼痛抑制作用),与对照组相比具有显著差异(** < 0.001)。复杂的炎症机制涉及多种途径,它们是相互关联的。因此,选择了多种炎症调节剂蛋白作为计算分析的靶标。计算分析表明,所选的所有靶标都与提取物中的植物化学物质具有不同程度的相互作用。芦丁(RU)、原儿茶酸(PA)、香草酸(VA)和阿魏酸(FA)可以以强大的效率调节多种靶标。没有一种化合物对环氧化酶-2(COX-2)表现出选择性。然而,PA 对 COX 和脂氧合酶(LOX)级联的调节可以减少非甾体类镇痛药(NSAIDs)相关的副作用,包括哮喘。RU 通过抑制 EGFR 和 IKBα(IKK),对细胞因子介导的途径(如 RAS/MAPK 和 PI3K/NF-kB)表现出强大的调节作用,这可能防止由于 SARS-CoV-2 等几种微生物感染引起的细胞因子风暴导致的多器官衰竭。可以进行进一步的体内和体外实验研究,以利用提取物中分离的化合物开发多靶标抗炎药物。

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