ArticleDrug design, development and therapy2014
Discovery and evaluation of novel anti-inflammatory derivatives of natural bioactive curcumin.
Article in Drug design, development and therapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 29 citations in OpenAlex.
- Bioactive Diarylpentanoids: Insights into the Biological Effects beyond Antitumor Activity and Structure-Activity Relationships.Molecules (Basel, Switzerland) · 2022Review
- Improved Synthesis of Asymmetric Curcuminoids and Their Assessment as Antioxidants.Molecules (Basel, Switzerland) · 2022Article
- Curcumin induces apoptosis and autophagy inhuman renal cell carcinoma cells via Akt/mTOR suppression.Bioengineered · 2021Article
- Phytonutrient and Nutraceutical Action against COVID-19: Current Review of Characteristics and Benefits.Nutrients · 2021Review
- Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines.Scientia pharmaceutica · 2018Article
- Anti-inflammatory effects of curcumin are associated with down regulating microRNA-155 in LPS-treated macrophages and mice.Pharmaceutical biology · 2017Article
- Anti-Inflammatory Pyranochalcone Derivative Attenuates LPS-Induced Acute Kidney Injury via Inhibiting TLR4/NF-κB Pathway.Molecules (Basel, Switzerland) · 2017Article
- Phenolic 1,3-diketones attenuate lipopolysaccharide-induced inflammatory response by an alternative magnesium-mediated mechanism.British journal of pharmacology · 2017Article
- Selective Targeting of Cancer Cells by Oxidative Vulnerabilities with Novel Curcumin Analogs.Scientific reports · 2017Article
- Immunosuppressive Effects of Natural α,β-Unsaturated Carbonyl-Based Compounds, and Their Analogs and Derivatives, on Immune Cells: A Review.Frontiers in pharmacology · 2017Review
- A novel imidazopyridine derivative, X22, attenuates sepsis-induced lung and liver injury by inhibiting the inflammatory response in vitro and in vivo.Drug design, development and therapy · 2016Article
- Attenuation of myocardial fibrosis with curcumin is mediated by modulating expression of angiotensin II AT1/AT2 receptors and ACE2 in rats.Drug design, development and therapy · 2015Article
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Curcumin is a natural active product that has various pharmacological activities such as anti-inflammatory effects. Here, we report the synthesis and evaluation of 34 monocarbonyl curcumin analogs as novel anti-inflammatory agents. Among the analogs, the symmetrical heterocyclic type displayed the strongest inhibition of lipopolysaccharide (LPS)-stimulated expression of pro-inflammatory cytokines in macrophages. Analogs S1-S5 and AS29 reduced tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) production in a dose-dependent manner and also displayed excellent stability and low cytotoxicity in vitro. In addition, analog S1 dose-dependently inhibited LPS-induced extracellular signal-regulated kinase (ERK) phosphorylation. Furthermore, analogs S1 and S4 displayed a significant protective effect on LPS-induced septic death in mouse models, with 40% and 50% survival rates, respectively. These data demonstrate that the heterocyclic monocarbonyl curcumin analogs have potential therapeutic effects in acute inflammatory diseases.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.