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Metabolism of the Endocannabinoids, 2-Arachidonylglycerol and Anandamide, into Prostaglandin, Thromboxane, and Prostacyclin Glycerol Esters and Ethanolamides*
TLDR
The results define the in vitrodiversity of endocannabinoid-derived prostanoids and will permit focused investigations into their production and potential biological actions in vivo.
Thromboxane A2 is a mediator of cyclooxygenase-2-dependent endothelial migration and angiogenesis.
TLDR
It is shown that thromboxane A2 (TXA2) is one of several eicosanoid products generated by activated human microvascular endothelial cells that functions as a critical intermediary of angiogenesis.
Aspirin-like molecules that covalently inactivate cyclooxygenase-2.
TLDR
Aspirin-like molecules were designed that preferentially acetylate and irreversibly inactivate COX-2, and these compounds may lead to the development of aspirin-like drugs for the treatment or prevention of immunological and proliferative diseases without gastrointestinal or hematologic side effects.
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.
TLDR
Indomethacin amides are orally active, nonulcerogenic, anti-inflammatory agents in an in vivo model of acute inflammation and can be envisioned for the modification of all carboxylic acid-containing NSAIDs into selective COX-2 inhibitors.
Peroxynitrite, the coupling product of nitric oxide and superoxide, activates prostaglandin biosynthesis.
TLDR
The hypothesis that peroxynitrite is an important modulator of cyclooxygenase activity in inflammatory cells is supported and it is established that superoxide anion serves as a biochemical link between NO and prostaglandin biosynthesis.
Metabolism of Prostaglandin Glycerol Esters and Prostaglandin Ethanolamides in Vitro and in Vivo *
TLDR
The results suggest that endocannabinoid-derived PG-like compounds may be sufficiently stable in humans to exert actions systemically and suggest that the rat is not an adequate model for investigating the biological activities of 2-arachidonylglycerol or glyceryl prostaglandins in humans.
The glyceryl ester of prostaglandin E2 mobilizes calcium and activates signal transduction in RAW264.7 cells
TLDR
PGE2-G triggers Ca2+ mobilization, IP3 synthesis, and activation of PKC in RAW264.7 macrophage cells at low concentrations, and induces a concentration-dependent increase in the levels of phosphorylated extracellular signal regulated kinases 1 and 2 through a pathway that requires the activities ofPKC, IP 3 receptor, and phospholipase C β.
Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.
TLDR
Conversion of indomethacin into ester and amide derivatives provides a facile strategy for generating highly selective COX-2 inhibitors and eliminating the gastrointestinal side effects of the parent compound.
Elevated CSF prostaglandin E2 levels in patients with probable AD.
TLDR
Increased CSF PGE2 concentration in probable AD patients suggest that cyclo-oxygenase inhibitors may benefit AD patients by limiting PG production and quantitative marker of lipid peroxidation in vivo is increased.
Regulation of Prostaglandin Biosynthesis by Nitric Oxide Is Revealed by Targeted Deletion of Inducible Nitric-oxide Synthase*
TLDR
The hypothesis that NO and/or NO-derived species modulate cyclooxygenase activity and eicosanoid production in vivo is supported by the effects of targeted deletion of the inducible NO synthase (iNOS) gene.
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