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beta diketone/radang
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Inhibitory effects of 1,3-bis-(2-substituted-phenyl)-propane-1,3-dione, β-diketone structural analogues of curcumin, on chemical-induced tumor promotion and inflammation in mouse skin.
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Dibenzoylmethane (DBM), a β-diketone structural analogue of curcumin, has been reported to exhibit anti-tumorigenic and chemopreventive activities. Due to the structural resemblance of DBM to the anti-inflammatory curcumin and an aspirin-like skeleton of DBM derivatives, we tested the
Synthesis and biological evaluation of curcuminoid pyrazoles as new therapeutic agents in inflammatory bowel disease: effect on matrix metalloproteinases.
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Seven N-unsubstituted curcuminoid pyrazoles have been synthesized from the corresponding beta-diketones (including curcumin). We evaluated the possibility of curcuminoid pyrazoles regulating the activity of matrix metalloproteinases (MMPs) by human intestinal epithelial cells in vitro. Zymographic
Synthesis, biological evaluation and molecular modeling study of 5-trifluoromethyl-Δ²-pyrazoline and isomeric 5/3-trifluoromethylpyrazole derivatives as anti-inflammatory agents.
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Searching for new anti-inflammatory agents, we have prepared a series of potential COX-2 inhibitors, 1-(4,6-dimethylpyrimidin-2-yl)-5-hydroxy-5-trifluoromethyl-Δ(2)-pyrazolines (3) and 1-(4,6-dimethylpyrimidin-2-yl)-3-trifluoromethylpyrazoles (4), by refluxing 2-hydrazino-4,6-dimethylpyrimidine (1)
Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors.
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Two series of celecoxib analogues having 1,5-diaryl relationship were synthesized. The key strategy of the molecular design was oriented towards exploring bioisosteric modifications of the sulfonamide moiety of celecoxib. First series (2a-2i) of celecoxib analogues bearing cyano functionality in
Inhibitory effect of beta-diketones and their metal complexes on TNF-alpha induced expression of ICAM-1 on human endothelial cells.
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Recent reports show that the natural beta-diketone curcumin displays important biological properties regarding the intercellular adhesion molecule-1 (ICAM-1), which plays a critical role in the immune responses and inflammation. In this study the ICAM-1 inhibitory activity of beta-diketone
Synthesis and anti-inflammatory activities of mono-carbonyl analogues of curcumin.
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Curcumin has been extensively studied for its anti-inflammatory activities. However, its potential beneficial effects on various disease preventions and treatments are limited by its unstable structure. The beta-diketone moiety renders curcumin to be rapidly metabolized by aldo-keto reductase in
Synthesis, crystal structure and anti-inflammatory properties of curcumin analogues.
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Curcuminoids have been reported to possess multifunctional bioactivities, especially the ability to inhibit proinflammatory induction. Since it has been suggested that the seven-carbon beta-diketone linker in curcumin is responsible for its instability, nine mono-carbonyl five-carbon linker
Dibenzoylmethane ameliorates lipid-induced inflammation and oxidative injury in diabetic nephropathy.
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Dibenzoylmethane (DBM) is a beta-diketone analog of curcumin. Numerous studies have shown the beneficial effects of curcumin on diabetes, obesity and diabetic complications including diabetic nephropathy. Recently, we investigated the beneficial metabolic effects of DBM on high-fat diet-induced
Modulation of arachidonic acid metabolism by curcumin and related beta-diketone derivatives: effects on cytosolic phospholipase A(2), cyclooxygenases and 5-lipoxygenase.
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Aberrant arachidonic acid metabolism is involved in the inflammatory and carcinogenic processes. In this study, we investigated the effects of curcumin, a naturally occurring chemopreventive agent, and related beta-diketone derivatives on the release of arachidonic acid and its metabolites in the
New MD2 inhibitors derived from curcumin with improved anti-inflammatory activity.
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An overactive Toll-like receptor (TLR) signaling complex is a significant pathogenic factor of acute and chronic inflammatory diseases. The natural product curcumin is reported to inhibit the TLR4 co-receptor, MD2 (myeloid differentiation protein 2), but its low in vivo bioavailability limits its
Inhibition of LPS-induced production of inflammatory factors in the macrophages by mono-carbonyl analogues of curcumin.
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Curcumin (diferuloylmethane) is an orange-yellow compound from turmeric (Curcuma longa), a spice found in curry powder. Traditionally known for its anti-inflammatory effects, curcumin has established itself in the last two decades to be a potent immunomodulatory agent that can regulate the
Biologically active novel N, N, O donor tridentate water soluble hydrazide based O-carboxymethyl chitosan Schiff base Cu (II) metal complexes: Synthesis and characterisation.
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Water soluble hydrazide based O-carboxymethyl chitosan Schiff base ligands have been prepared from chitosan and a mixture of benzoic acidhydrazide with β-diketone by carboxymethylation using mono chloroaceticacid (MCA) through in-situ reaction. The degree of deacetylation of chitosan was determined
Paramagnetic Fluorinated Nanoemulsions for in vivo F-19 MRI.
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Curcumin blocks prostaglandin E2 biosynthesis through direct inhibition of the microsomal prostaglandin E2 synthase-1.
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Prostaglandin E(2) (PGE(2)) plays a crucial role in the apparent link between tumor growth and chronic inflammation. Cyclooxygenase (COX)-2 and microsomal PGE(2) synthase-1, which are overexpressed in many cancers, are functionally coupled and thus produce massive PGE(2) in various tumors. Curcumin,
The molecular mechanisms for the antitumorigenic effect of curcumin.
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Curcumin, an active yellow pigment of turmeric and curry, possesses anti-inflammatory, antioxidative and anticarcinogenic properties. Analysis of its structure revealed the presence of beta-diketone moiety and phenolic hydroxy groups that were believed to contribute to antioxidation. And vanillin,
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