Inspired by magnolol: design of NSAID-based compounds with excellent anti-inflammatory effects

Liu, Wenfeng; Yue, Yuan; Li, Yonglian; Zheng, Xi; Zhang, Kun; Du, Zhiyun

doi:10.1039/c5md00308c

Cited by 8 publications

(5 citation statements)

References 27 publications

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“…Compound 12 was more effective (up to 90 %) than magnolol in reducing terephthalic acid-induced ear edema (58.3 %) at 0.75 μM. [20]…”

Section: Replacing the Magnolol Hydroxy Groups With Mercapto Moietiesmentioning

confidence: 90%

“…The results demonstrated that Compound 12 reduced the production of IL‐1, IL‐6, and TNF‐ ɑ caused by TPA via the inhibitor of the kappa B kinase/nuclear factor kappa B signaling pathway and significantly reduced the average weight of mouse ear punches. Compound 12 was more effective (up to 90 %) than magnolol in reducing terephthalic acid‐induced ear edema (58.3 %) at 0.75 μM [20] …”

Section: Magnolol Structural Modifications and Biological Actionsmentioning

confidence: 99%

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Research Progress on the Structural Modification of Magnolol and Honokiol and the Biological Activities of Their Derivatives

Guo

Feng

et al. 2023

Chemistry & Biodiversity

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Magnolol and Honokiol are the primary active components that have been identified and extracted from Magnolia officinalis, and several investigations have demonstrated that they have significant pharmacological effects. Despite their therapeutic benefits for a wide range of illnesses, research on and the implementation of these compounds have been hindered by their poor water solubility and low bioavailability. Researchers are continually using chemical methods to alter their structures to make them more effective in treating and preventing diseases. Researchers are also continuously developing derivative drugs with high efficacy and few adverse effects. This article summarizes and analyzes derivatives with significant biological activities reported in recent research obtained by structural modification. The modification sites have mainly focused on the phenolic hydroxy groups, benzene rings, and diene bonds. Changes to the allyl bisphenol structure will result in unexpected benefits, including high activity, low toxicity, and good bioavailability. Furthermore, alongside earlier experimental research in our laboratory, the structure‐activity relationships of magnolol and honokiol were preliminarily summarized, providing experimental evidence for improving their development and utilization.

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“…Compound 12 was more effective (up to 90 %) than magnolol in reducing terephthalic acid-induced ear edema (58.3 %) at 0.75 μM. [20]…”

Section: Replacing the Magnolol Hydroxy Groups With Mercapto Moietiesmentioning

confidence: 90%

Section: Magnolol Structural Modifications and Biological Actionsmentioning

confidence: 99%

Research Progress on the Structural Modification of Magnolol and Honokiol and the Biological Activities of Their Derivatives

Guo

Feng

et al. 2023

Chemistry & Biodiversity

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“…According to our previous publication, the concentration at which the initial screening anti-inammatory activities of N and M were conducted was selected as 0.75 mM. 20 As shown in Fig. 2, ear oedema was induced by the topical application of TPA alone.…”

Section: Effects Of Naproxen In Combination With Magnolol On Tpa-indu...mentioning

confidence: 99%

Synergistic inhibitory effects of naproxen in combination with magnolol on TPA-induced skin inflammation in mice

et al. 2016

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“…Naproxen is one type of NSAID used for the treatment of inflammatory diseases, such as inflammatory bowel and rheumatic diseases, as well as myocarditis [16]. Current studies have revealed that naproxen combined with natural compounds, or structurally modified naproxen with active compounds derived from natural products are beneficial to enhance their bioactivity [17][18][19][20]. As shown in Figure 1a,b, it has been suggested that a naproxen derivative containing curcumin or magnolol reduced phorbol-12-myristate-13-acetate (TPA)-induced skin inflammation in a TPA-induced mouse ear edema model.…”

Section: Introductionmentioning

confidence: 99%

Naproxen-Derived New Compound Inhibits the NF-κB, MAPK and PI3K/Akt Signaling Pathways Synergistically with Resveratrol in RAW264.7 Cells

You

Yang

et al. 2023

Molecules

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Naproxen is widely used for anti-inflammatory treatment but it can lead to serious side effects. To improve the anti-inflammatory activity and safety, a novel naproxen derivative containing cinnamic acid (NDC) was synthesized and used in combination with resveratrol. The results showed that the combination of NDC and resveratrol at different ratios have a synergistic anti-inflammatory efficacy in RAW264.7 macrophage cells. It was indicated that the combination of NDC and resveratrol at a ratio of 2:1 significantly inhibited the expression of carbon monoxide (NO), tumor necrosis factor α (TNF-α), interleukin 6 (IL-6), induced nitric oxide synthase (iNOS), cyclooxygenase 2 (COX-2) and reactive oxygen species (ROS) without detectable side effects on cell viability. Further studies revealed that these anti-inflammatory effects were mediated by the activation of nuclear factor kappa-B (NF-κB), mitogen-activated protein kinase (MAPK) and phosphoinositide-3 kinase (PI3K)/protein kinase B (Akt) signaling pathways, respectively. Taken together, these results highlighted the synergistic NDC and resveratrol anti-inflammatory activity that could be further explored as a strategy for the treatment of inflammatory disease with an improved safety profile.

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Inspired by magnolol: design of NSAID-based compounds with excellent anti-inflammatory effects

Abstract: A10 was selected to elucidate the anti-inflammatory mechanism at the transcriptional level, suggesting its potential to serve as a novel anti-inflammatory agent.

Cited by 8 publications

References 27 publications

Research Progress on the Structural Modification of Magnolol and Honokiol and the Biological Activities of Their Derivatives

Research Progress on the Structural Modification of Magnolol and Honokiol and the Biological Activities of Their Derivatives

Synergistic inhibitory effects of naproxen in combination with magnolol on TPA-induced skin inflammation in mice

Naproxen-Derived New Compound Inhibits the NF-κB, MAPK and PI3K/Akt Signaling Pathways Synergistically with Resveratrol in RAW264.7 Cells

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