Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity

Liu, Wenfeng; Li, Yonlian; Yue, Yuan; Zhang, Kun; Chen, Qian; Wang, Huaqian; Lu, Yu‐Jing; Huang, Mou‐Tuan; Zheng, Xi; Du, Zhiyun

doi:10.1016/j.bmcl.2015.04.077

Cited by 40 publications

(27 citation statements)

References 18 publications

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“…Furthermore, the complex of polyethylene glycol (PEG) and curcumin inhibits NF-κB p65 nuclear translocation and c-Jun phosphorylation, and activation of nuclear factor (erythroid-derived 2)-like 2 (Nrf2), interfering with multiple targets involved in the inflammatory response [ 53 ]. Curcumin derivatives containing nonsteroidal anti-inflammatory components have been found to block the phosphorylation of IκB-α and suppress the activation of p65 and IκB-α [ 54 ]. The diarylpentadienone derivatives of curcumin inhibit LPS-induced inducible nitric oxide synthase (iNOS) expression, and slightly reduces the activation of p65 in nuclei [ 55 ].…”

Section: Bioactivity Of Curcuminmentioning

confidence: 99%

Bioactivity, Health Benefits, and Related Molecular Mechanisms of Curcumin: Current Progress, Challenges, and Perspectives

et al. 2018

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Curcumin is a principal curcuminoid of turmeric (Curcuma longa), which is commonly used as a spice in cooking and a yellow pigment in the food processing industry. Recent studies have demonstrated that curcumin has a variety of biological activities and pharmacological performances, providing protection and promotion of human health. In addition to presenting an overview of the gut metabolism of curcumin, this paper reviews the current research progress on its versatile bioactivity, such as antioxidant, anti-inflammatory, and immune-regulatory activities, and also intensively discusses its health benefits, including the protective or preventive effects on cancers and diabetes, as well as the liver, nervous system, and cardiovascular systems, highlighting the potential molecular mechanisms. Besides, the beneficial effects of curcumin on human are further stated based on clinical trials. Considering that there is still a debate on the beneficial effects of curcumin, we also discuss related challenges and prospects. Overall, curcumin is a promising ingredient of novel functional foods, with protective efficacy in preventing certain diseases. We hope this comprehensive and updated review will be helpful for promoting human-based studies to facilitate its use in human health and diseases in the future.

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Section: Bioactivity Of Curcuminmentioning

confidence: 99%

Bioactivity, Health Benefits, and Related Molecular Mechanisms of Curcumin: Current Progress, Challenges, and Perspectives

et al. 2018

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“…This decrease in prostaglandin synthesis is associated with the occurrence of several unwanted effects accompanied with the use of NSAIDs, especially gastrointestinal (GI) irritation and ulceration. Additionally, several NSAIDs have a free carboxylic acid group (5) ; therefore, oral administration is linked with the side effects on the gastric system (6) , which are due to direct GI irritation. NSAIDs can be categorized by the site of action into nonselective (COX) inhibitors which target COX I and COX II and selective (COX) inhibitors that selectively target COX II though decrease gastric side effect that comes with COX I inhibitors (7) .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Preliminary Anti-inflammatory Evaluation of New Etodolac Derivatives

Hassan¹,

Sarsam²

2019

IJPS

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Three new hydrazone derivatives of Etodolac were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy, and 1HNMR analysis. The synthesis of the target (P1-P3) compounds was accomplished following multistep reaction procedures. The synthesized target compounds were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac).

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“…However, its poor water-solubility and low bioavailability restrict its use. To address this problem, a number of derivatives and analogs of Cur have been developed in our lab, such as FM0807 (2-hydroxy-4-[(1E, 6E)-7-(4-hydroxy-3-methoxyphenyl)-3,5-dioxo-1,6-heptadien-1-yl]-2-methoxyphenyl ester), which incorporated a 2-hydroxy-benzoic acid chain into Cur that retains the β-diketone structure and exhibits better anti-inflammatory activity than that of Cur [ 19 ]. FM0807 can also be considered as the combined compound of Cur and aspirin (the structures of Cur, aspirin, and FM0807 are shown in Figure 1 A–C).…”

Section: Introductionmentioning

confidence: 99%

Effects of FM0807, a novel curcumin derivative, on lipopolysaccharide-induced inflammatory factor release via the ROS/JNK/p53 pathway in RAW264.7 cells

Liu

Wu³

et al. 2018

Bioscience Reports

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Purpose: Sepsis is a systemic inflammatory response caused by infection. Curcumin is known to have antioxidant and anti-inflammatory activities. FM0807, a curcumin derivative, was investigated in the present study to determine its effect on cytokines and the possible molecular mechanism. Main methods: The experiments were carried out in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Cell viability was measured by MTT assay. ELISA, Griess assays, fluorescence-based quantitative PCR, flow cytometric analysis, 2′,7′-dichlorodihydrofluorescein diacetate (DCFH-DA) experiments, and Western blotting were carried out to assess the potential effects of FM0807 on LPS-induced RAW 264.7 cells. Significant findings: FM0807 had no cytotoxic effects on RAW 264.7 cells. Furthermore, pretreatment with FM0807 inhibited the inflammatory factor tumor necrosis factor-α (TNF-α), interleukin (IL) 1β (IL-1β), IL-6, and inducible nitric oxide synthase (iNOS) at the protein and gene levels. FM0807 also inhibited the production of reactive oxygen species (ROS) and apoptosis. In addition, the activation of the ROS/JNK (c-jun NH2-terminal kinase)/p53 signaling pathway was inhibited by FM0807 in RAW 264.7 cells in vitro. Conclusion: FM0807 has anti-inflammatory activity in vitro, which suggests a potential clinical application in sepsis. The anti-inflammatory activity of FM0807 may be mediated by the ROS/JNK/p53 signaling pathway.

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Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity

Cited by 40 publications

References 18 publications

Bioactivity, Health Benefits, and Related Molecular Mechanisms of Curcumin: Current Progress, Challenges, and Perspectives

Bioactivity, Health Benefits, and Related Molecular Mechanisms of Curcumin: Current Progress, Challenges, and Perspectives

Synthesis, Characterization and Preliminary Anti-inflammatory Evaluation of New Etodolac Derivatives

Effects of FM0807, a novel curcumin derivative, on lipopolysaccharide-induced inflammatory factor release via the ROS/JNK/p53 pathway in RAW264.7 cells

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