Discovery of talmapimod analogues as polypharmacological anti-inflammatory agents

Liu, Wandong; Cai-yun, Hou; Li, Jiaming; Ma, Xiaodong; Zhang, Yanchun; Hu, Mengqi; Huang, Yuanzheng

doi:10.1080/14756366.2019.1693703

Cited by 11 publications

(6 citation statements)

References 27 publications

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“…The in vitro enzymatic experiment identified compound 95 as a potent inhibitor against both p38a MAPK (IC 50 ¼1.95 mM) and COX-2 (IC 50 ¼0.036 mM). Furthermore, it had the ability to downregulate NF-jB and MAPK signalling pathways 110 . Talmon et al synthesised a series of novel vortioxetine derivatives.…”

Section: Piperazine Derivatives As Anti-inflammatory Agentsmentioning

confidence: 99%

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Bian

Wu³

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Inflammation and disease are closely related. Inflammation can induce various diseases, and diseases can promote inflammatory response, and two possibly induces each other in a bidirectional loop. Inflammation is usually treated using synthetic anti-inflammatory drugs which are associated with several adverse effects hence are not safe for long-term use. Therefore, there is need for anti-inflammatory drugs which are not only effective but also safe. Several researchers have devoted to the research and development of effective anti-inflammatory drugs with little or no side effects. In this review, we studied some small molecules with reported anti-inflammatory activities and hence potential sources of anti-inflammatory agents. The information was retrieved from relevant studies published between January 2019 and May, 2021 for review. This review study was aimed to provide relevant information towards the design and development of effective and safe anti-inflammation agents.

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Section: Piperazine Derivatives As Anti-inflammatory Agentsmentioning

confidence: 99%

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Bian

Wu³

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…During inflammatory responses, the NF-κB subunit p65 translocates from the cytoplasm to the nucleus, facilitated by the proteasome degradation and phosphorylation of the inhibitory IκBα. This then interacts with the gene promoter region in the nucleus, promoting the expression of various cytokines and inflammatory mediators (e.g., iNOS, COX-2, TNF-α, IL-6, and IL-1β). , Therefore, the inhibition of IκBα phosphorylation to block NF-κB activation presents a potential therapeutic strategy for inflammation-associated diseases . The effects of compounds 9c and 9j on the NF-κB signaling pathway in LPS-induced RAW264.7 cells were explored using Western blotting.…”

Section: Results and Discussionmentioning

confidence: 99%

Discovery of Coixol Derivatives as Potent Anti-inflammatory Agents

Cui

Qian

et al. 2023

J. Nat. Prod.

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Coixol, a derivative of 2-benzoxazolinone extracted from coix (Coix lachryma-jobi L. var. ma-yuen Stapf), has demonstrated promising anti-inflammatory activity and low cytotoxicity. In this study, 26 coixol derivatives were designed and synthesized by hybridization with cinnamic acid to identify new anti-inflammatory agents. The anti-inflammatory activities of the derivatives were screened using LPS-induced overexpression of nitric oxide (NO) in RAW264.7 macrophages. On the basis of the screening results, compounds containing furan (9c) or nitrofuran (9j) moieties displayed more pronounced activity than coixol and celecoxib. Mechanistic investigations revealed that 9c and 9j suppressed the expression of induced nitric oxide synthase (iNOS), tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β, which was associated with the inhibition of the nuclear factor (NF)-κB signaling pathway. In vivo studies confirmed the anti-inflammatory activity of 9c and 9j in a xylene-induced mice auricles edema model. The preliminary in vitro and in vivo research findings suggest that 9c and 9j have the potential to be developed as anti-inflammatory agents.

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“…Decreased levels of NF-κB are observed in conditions of reduced inflammation and apoptosis. [ 25 , 26 ] Most studies consider decreased NF-κB level as a sign of attenuated inflammation. [ 25 ] However, since it may play an anti-apoptotic or pro-apoptotic role depending on the conditions, an increase in NF-κB may also be observed in scenarios of decreased apoptosis.…”

Section: Discussionmentioning

confidence: 99%

Effects of lercanidipine on traumatic spinal cord injury: an experimental study

Türk

2024

Ulus Travma Acil Cerrahi Derg

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BACKGROUND: Spinal cord injury is a devastating trauma that leaves survivors at risk for several medical complications throughout their lives. Lercanidipine, a third-generation calcium channel blocker, possesses anti-apoptotic, anti-inflammatory, and antioxidative properties. This study aimed to evaluate the neuroprotective effects of lercanidipine in an experimental spinal cord trauma model. METHODS: Twenty-one Wistar rats were randomly assigned to three groups. Group 1 (G1) underwent laminectomy. Group 2 (G2) were subjected to trauma following laminectomy. Group 3 (G3) were exposed to trauma following laminectomy and treated with lercanidipine. Lercanidipine was administered intraperitoneally for seven days. Histopathological and immunohistochemical evaluations were conducted. RESULTS: Regarding Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) staining, there was no significant difference among the groups. However, nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) levels were significantly different across the groups. G2 had significantly higher NF-κB levels compared to G1 and G3. CONCLUSION: Lercanidipine, a third-generation calcium channel blocker, is effective against inflammatory responses induced in spinal cord injury. Further studies are required to determine its capability in preventing apoptosis or improving functional recovery. To the best of our knowledge, this study is the first in the literature to examine the neuroprotective effects of lercanidipine on spinal cord injury.

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Discovery of talmapimod analogues as polypharmacological anti-inflammatory agents

Cited by 11 publications

References 27 publications

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Discovery of Coixol Derivatives as Potent Anti-inflammatory Agents

Effects of lercanidipine on traumatic spinal cord injury: an experimental study

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