Anti-inflammatory Effect of Predimenol, A Bioactive Extract from Phaleria macrocarpa, through the Suppression of NF-κB and COX-2.

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Accounts of Chemical Research Pub Date : 2022-01-19 DOI:10.2174/2772270816666220119122259

Yurike Yuliana, Olivia M Tandrasasmita, Raymond R Tjandrawinata

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Abstract

Background: Inflammation is the response to the reaction of any type of bodily injury by elevating cellular metabolism and releasing soluble mediators. It is also a contributing factor of pain. Predimenol, which has previously been known as DLBS1442, is a bioactive extract from Phaleria macrocarpa (Scheff.) Boerl (Thymelaceae). It can be an alternative treatment for pain relief, especially for long-term use.

Objective: The objective of this study is to evaluate the anti-inflammatory activities of predimenol through the evaluation of several parameters involved in the inflammatory pathway.

Methods: Cyclooxygenase 2 (COX-2), inducible nitric oxide synthase (iNOS), tumor necrosis factor-  (TNF-), interleukin-1β (IL-1β), interleukin-2 (IL-2), interleukin-6 (IL-6), and nuclear factor B (NF-B) were observed after 24 h exposure of predimenol (0-180 µg/mL) to lipopolysaccharides (LPS)-activated RAW 264.7 cell. The inflammatory markers were measured using nitric oxide (NO) assay and enzyme-linked immunosorbent assay (ELISA) for COX-2 inhibitor assay. The gene expressions of TNF-α, IL-1β, IL-2 and IL-6 were quantified using the polymerase chain reaction (PCR) method. Western blotting was applied to detect phosphorylated IB kinase (IKK) protein to confirm the activation of NF-κB.

Results: Our study showed a similar mechanism with most non-steroidal anti-inflammatory drugs (NSAIDs). Predimenol consistently downregulated the expression of iNOS and inhibited COX-2 activity. Moreover, predimenol significantly inhibited the LPS-induced production of NO, TNF-α, IL-1β, IL-2 and IL-6. Down-regulation of these markers was suggested due to the reduction of NF-κB transcription level and activation by predimenol.

Conclusion: Predimenol exhibits anti-inflammatory activities through NF-kB inactivation-mediated COX-2 suppression, which may suggest that predimenol is a potential analgesic and anti-inflammatory agent.

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红景天生物活性提取物 Predimenol 通过抑制 NF-κB 和 COX-2 发挥抗炎作用

背景：炎症是对任何类型的身体损伤的反应，它通过提高细胞新陈代谢和释放可溶性介质来实现。它也是导致疼痛的一个因素。Predimenol 以前被称为 DLBS1442，是从 Phaleria macrocarpa (Scheff.) Boerl（百里香科）中提取的一种生物活性提取物。它可以作为缓解疼痛的替代疗法，尤其适合长期使用：本研究的目的是通过评估参与炎症途径的几个参数来评估predimenol的抗炎活性：方法：将predimenol（0-180 µg/mL）暴露于脂多糖（LPS）激活的RAW 264.7细胞24小时后，观察环氧化酶2（COX-2）、诱导型一氧化氮合酶（iNOS）、肿瘤坏死因子- （TNF-）、白细胞介素-1β（IL-1β）、白细胞介素-2（IL-2）、白细胞介素-6（IL-6）和核因子B（NF-B）。使用一氧化氮（NO）检测法和 COX-2 抑制剂检测法的酶联免疫吸附试验（ELISA）测量炎症标志物。采用聚合酶链反应（PCR）方法定量检测 TNF-α、IL-1β、IL-2 和 IL-6 的基因表达。用 Western 印迹法检测磷酸化的 IB 激酶（IKK）蛋白，以确认 NF-κB 的激活：结果：我们的研究显示了与大多数非甾体抗炎药（NSAIDs）相似的机制。Predimenol 可持续下调 iNOS 的表达并抑制 COX-2 的活性。此外，Predimenol 还能明显抑制 LPS 诱导的 NO、TNF-α、IL-1β、IL-2 和 IL-6 的产生。这些指标的下调可能是由于 predimenol 降低了 NF-κB 的转录水平和激活所致：结论：Predimenol通过NF-kB失活介导的COX-2抑制作用表现出抗炎活性，这可能表明Predimenol是一种潜在的镇痛和抗炎药物。

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

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.