HPLC-characterized phenolics from Acer oblongifolium attenuate inflammation, pain, and CNS-related disturbances: docking, edema, nociception, and behavioural studies.

IF 6.3 2区 医学 Q2 IMMUNOLOGY
Inflammopharmacology Pub Date : 2026-10-01 Epub Date: 2026-09-14 DOI:10.1007/s10787-026-02398-w
Hammad Ismail, Saqib Hussain Hadri, Umer Rashid, Hafiza Aqsa Ashraf, Amna Mahmood, Abdullah Tariq, Ayesha Jannat, Adeena Ansar, Sheeza Masud, Muhammad Rashid, Lyba Sarfraz, Muhammad Zeeshan Bhatti
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引用次数: 0

Abstract

Background: Phenolic compounds of plant origin are promising alternatives, but the potential of Acer oblongifolium and its components has not been studied.

Objective: To evaluate analgesic, anti-inflammatory and anxiolytic effects of Acer oblongifolium extract and four of its major phenolics, catechin, syringic acid, vanillic acid and gentisic acid-with the help of in silico, in vivo and biochemical techniques.

Methods: HPLC was performed to investigate the phenolic content of the plant extract. The binding of known compounds with TNF α, IL-6 and IL-1β was evaluated with the help of molecular docking. In-vivo tests, including the hole board test, open field test, hot plate test, writhing assay, carrageenan induced paw edema and histamine induced edema were used to evaluate the pharmaceutical potential. ELISA was performed to measure serum and tissue IL-6, IL-1β and TNF-α levels.

Results: HPLC validated the presence of four phenolic compounds, including Gentisic acid, vanillic acid, catechin and syringic acid. Gentisic acid exhibited strong hydrogen binding with TNF-α and IL-1β. The most pronounced anxiolytic-like activity was exhibited by vanillic acid which decreased immobility by 60% and freezing behavior by 62% in open field test, and enhanced the latency of hot plate by 30%. Gentisic acid prevented carrageenan induced paw swelling by 82% at 3 h and vanillic acid prevented histamine induced edema by 80%, which was better than cetirizine. ELISA indicated that both Gentisic acid and catechin were the most effective in reducing high levels of IL-1β and TNF-α levels in serum and brain tissue from 4.55 to 2.035 pg/mL.

Conclusion: Acer oblongifolium and its phenolic constituents, principally Gentisic acid and vanillic acid, showed analgesic, anti-inflammatory, and anxiolytic-like activity in this preclinical model, potentially mediated via modulation of pro-inflammatory cytokines.

用高效液相色谱表征的长叶槭酚类物质可减轻炎症、疼痛和中枢神经系统相关紊乱:停靠、水肿、伤害和行为研究。
背景:植物来源的酚类化合物是很有前途的替代品,但长叶槭及其成分的潜力尚未得到研究。目的:用体外、体内和生化方法评价槭叶提取物及其主要酚类物质儿茶素、丁香酸、香草酸和龙胆酸的镇痛、抗炎和抗焦虑作用。方法:采用高效液相色谱法测定植物提取物中酚类物质的含量。已知化合物与TNF α、IL-6和IL-1β的结合通过分子对接进行评估。采用孔板实验、露天实验、热板实验、扭体实验、角叉菜胶诱导足跖水肿和组胺诱导足跖水肿等体内实验评价其药用潜力。ELISA法检测各组血清及组织中IL-6、IL-1β、TNF-α水平。结果:HPLC验证了龙胆酸、香草酸、儿茶素、丁香酸等4种酚类化合物的存在。龙胆酸与TNF-α和IL-1β具有较强的氢结合。其中,香草酸的抗焦虑活性最显著,可降低60%的不动性和62%的冻结性,并可提高30%的热板潜伏期。龙胆酸对角叉菜胶诱导的足跖肿胀的抑制率为82%,香草酸对组胺诱导的足跖肿胀的抑制率为80%,均优于西替利嗪。酶联免疫吸附试验结果显示,龙胆酸和儿茶素均能有效降低血清和脑组织中IL-1β和TNF-α水平,从4.55降至2.035 pg/mL。结论:在这个临床前模型中,长叶槭及其酚类成分,主要是龙胆酸和香草酸,显示出镇痛、抗炎和抗焦虑样活性,可能是通过调节促炎细胞因子介导的。
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来源期刊
Inflammopharmacology
Inflammopharmacology IMMUNOLOGYTOXICOLOGY-TOXICOLOGY
CiteScore
8.00
自引率
3.40%
发文量
200
期刊介绍: Inflammopharmacology is the official publication of the Gastrointestinal Section of the International Union of Basic and Clinical Pharmacology (IUPHAR) and the Hungarian Experimental and Clinical Pharmacology Society (HECPS). Inflammopharmacology publishes papers on all aspects of inflammation and its pharmacological control emphasizing comparisons of (a) different inflammatory states, and (b) the actions, therapeutic efficacy and safety of drugs employed in the treatment of inflammatory conditions. The comparative aspects of the types of inflammatory conditions include gastrointestinal disease (e.g. ulcerative colitis, Crohn''s disease), parasitic diseases, toxicological manifestations of the effects of drugs and environmental agents, arthritic conditions, and inflammatory effects of injury or aging on skeletal muscle. The journal has seven main interest areas: -Drug-Disease Interactions - Conditional Pharmacology - i.e. where the condition (disease or stress state) influences the therapeutic response and side (adverse) effects from anti-inflammatory drugs. Mechanisms of drug-disease and drug disease interactions and the role of different stress states -Rheumatology - particular emphasis on methods of measurement of clinical response effects of new agents, adverse effects from anti-rheumatic drugs -Gastroenterology - with particular emphasis on animal and human models, mechanisms of mucosal inflammation and ulceration and effects of novel and established anti-ulcer, anti-inflammatory agents, or antiparasitic agents -Neuro-Inflammation and Pain - model systems, pharmacology of new analgesic agents and mechanisms of neuro-inflammation and pain -Novel drugs, natural products and nutraceuticals - and their effects on inflammatory processes, especially where there are indications of novel modes action compared with conventional drugs e.g. NSAIDs -Muscle-immune interactions during inflammation [...]
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