Evaluation of anti-inflammatory activity of kaurenol: Experimental evaluation and mechanistic insights

IF 2.1 4区医学 Q3 PHARMACOLOGY & PHARMACY

Fundamental & Clinical Pharmacology Pub Date : 2023-09-21 DOI:10.1111/fcp.12957

Ricardo Andrade Furtado, Samir A. Ross, Silvio de Almeida Junior, Rafael Paranhos de Mendonça, Cristiane Teixeira Vilhena Bernardes, Mauro Nogueira da Silva, Karina Furlani Zoccal, Lúcia Helena Faccioli, Jairo Kenupp Bastos

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引用次数: 0

Abstract

Background

Kaurenol, a diterpene alcohol found in Copaifera langsdorffii Desf. (known as “copaiba”), is historically used in traditional medicine for inflammatory conditions.

Objectives

This study aims to comprehensively assess the potential anti-inflammatory and antinociceptive properties of kaurenol.

Methods

To this end, the following experiments were conducted to evaluated toxicity: locomotor performance and acute toxicity; nociception: acetic acid-induced writhing and formalin-induced antinociception; and anti-inflammatory activity: carrageenan and dextran-induced paw edema at 10, 20, and 40 mg/kg, and measurement of nitric oxide (NO), tumor necrosis factor alpha (TNF-α), interleukin-6 (IL-6), and interleukin-10 (IL-10) in macrophages at 1, 3, and 9 μg/ml.

Results

Kaurenol did not show significant locomotor changes, acute toxicity, and central analgesic activity in the first phase of formalin test at dosages tested. Kaurenol showed 53%, 64%, 64%, and 58% of inhibition in the acetic acid-induced writhing, second phase of formalin test, carrageenan and dextran-induced paw edema, respectively.

Conclusion

The anti-inflammatory activity was associated with the regulation of NO release and probably with the regulation of mediators, such as serotonin and prostaglandin in vascular permeability, as well as by being associated with the regulation of IL-6 and IL-10. Kaurenol display anti-inflammatory activity but has no analgesic activity.

查看原文本刊更多论文

卡脲醇抗炎活性的评估：实验评估和机制见解。

背景：考瑞诺，一种二萜醇，存在于狼毒中。（被称为“copaiba”），在传统医学中用于治疗炎症。目的：本研究旨在全面评估卡脲醇潜在的抗炎和镇痛作用。方法：为此，进行以下实验来评估毒性：运动性能和急性毒性；伤害感受：醋酸致扭体和福尔马林致镇痛感受；和抗炎活性：卡拉胶和右旋糖酐在10、20和40时诱导的爪水肿 mg/kg，并在1、3和9时测量巨噬细胞中的一氧化氮（NO）、肿瘤坏死因子α（TNF-α）、白细胞介素-6（IL-6）和白细胞介蛋白-10（IL-10） μg/ml。结果：在福尔马林试验的第一阶段，在所测试的剂量下，考雷诺没有显示出显著的运动变化、急性毒性和中枢镇痛活性。Kaurenol对乙酸诱导的扭体反应、福尔马林第二阶段试验、卡拉胶和右旋糖酐诱导的足跖水肿的抑制率分别为53%、64%、64%和58%。结论：抗炎活性与NO释放的调节有关，可能与5-羟色胺和前列腺素等介质对血管通透性的调节有关。Kaurenol表现出抗炎活性，但没有镇痛活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Fundamental & Clinical Pharmacology 医学-药学

CiteScore

5.30

自引率

6.90%

发文量

111

审稿时长

6-12 weeks

期刊介绍： Fundamental & Clinical Pharmacology publishes reports describing important and novel developments in fundamental as well as clinical research relevant to drug therapy. Original articles, short communications and reviews are published on all aspects of experimental and clinical pharmacology including: Antimicrobial, Antiviral Agents Autonomic Pharmacology Cardiovascular Pharmacology Cellular Pharmacology Clinical Trials Endocrinopharmacology Gene Therapy Inflammation, Immunopharmacology Lipids, Atherosclerosis Liver and G-I Tract Pharmacology Metabolism, Pharmacokinetics Neuropharmacology Neuropsychopharmacology Oncopharmacology Pediatric Pharmacology Development Pharmacoeconomics Pharmacoepidemiology Pharmacogenetics, Pharmacogenomics Pharmacovigilance Pulmonary Pharmacology Receptors, Signal Transduction Renal Pharmacology Thrombosis and Hemostasis Toxicopharmacology Clinical research, including clinical studies and clinical trials, may cover disciplines such as pharmacokinetics, pharmacodynamics, pharmacovigilance, pharmacoepidemiology, pharmacogenomics and pharmacoeconomics. Basic research articles from fields such as physiology and molecular biology which contribute to an understanding of drug therapy are also welcomed.