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Modulation of GSTP1-1 oligomerization by electrophilic inflammatory mediators and reactive drugs.

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Glutathione S transferase P1-1 plays a key role in the metabolism of inflammatory mediators and drugs, thus modulating the inflammatory response. Active GSTP1-1 is a homodimer with cysteine residues close to the active site that can undergo oligomerization in response to stress, a process that

A meroterpenoid NF-kappaB inhibitor and drimane sesquiterpenoids from Asafetida.

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Investigation of an acetone extract from Asafetida afforded two drimane sesquiterpene dienones (fetidones A and B, 1a,b) and several known sesquiterpene coumarin ethers, one of which (8-acetoxy-5-hydroxyumbelliprenin, 2a) showed potent and specific NF-kappaB-inhibiting properties. This, coupled to a

Novel Curcumin Inspired Antineoplastic 1-Sulfonyl-4-Piperidones: Design, Synthesis and Molecular Modeling Studies.

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Curcumin is a well-known example of plant origin exhibiting promising diverse biological properties such as, anti-inflammatory and antitumor as well as poor pharmacokinetic/pharmacodynamic properties. This is why effective agents based on its chemical scaffold were

Curcumin structure-function, bioavailability, and efficacy in models of neuroinflammation and Alzheimer's disease.

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Curcumin can reduce inflammation and neurodegeneration, but its chemical instability and metabolism raise concerns, including whether the more stable metabolite tetrahydrocurcumin (TC) may mediate efficacy. We examined the antioxidant, anti-inflammatory, or anti-amyloidogenic effects of dietary

Anti-oxidant activities of curcumin and related enones.

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The natural product curcumin (diferuloylmethane, 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione), obtained from the spice turmeric, exhibits numerous biological activities including anti-cancer, anti-inflammatory, and anti-angiogenesis activities. Some of these biological activities may

TPA-induced up-regulation of activator protein-1 can be inhibited or enhanced by analogs of the natural product curcumin.

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The activator protein-1 (AP-1) family of transcription factors, including the most common member c-Jun-c-Fos, participates in regulation of expression of numerous genes involved in proliferation, apoptosis, and tumorigenesis in response to a wide array of stimuli including pro-inflammatory

New 1,4-Dienonesteroids from the Octocoral Dendronephthya sp.

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Two new steroids, dendronesterones D (1) and E (2), featuring with 1,4-dienone moiety, along with three known steroids, methyl 3-oxochola-4,22-diene-24-oate (3), 5α,8α-epidioxy-24(S)- methylcholesta-6,22-dien-3β-ol (4), and

Strategies toward Organic Carbon Monoxide Prodrugs.

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Carbon monoxide is widely acknowledged as an important gasotransmitter in the mammalian system with importance on par with that of nitric oxide. It has also been firmly established as a potential therapeutic agent with a wide range of indications including organ transplantation, cancer, bacterial

Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin.

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Inflammation and oxidative stress are common in many chronic diseases. Targeting signaling pathways that contribute to these conditions may have therapeutic potential. The transcription factor Nrf2 is a major regulator of phase II detoxification and anti-oxidant genes as well as anti-inflammatory

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