Prostaglandin synthesis, analysis

The hypothesis that Cox-2 inhibitors are less toxic than NSAIDs on the GI tract because of sparing Cox-l-dependent GI prostaglandin synthesis is born out by these data. Furthermore, data from the rofecoxib phase II and III studies have been combined in order to compare the effects of rofecoxib with those of NSAIDs on clinical outcomes relevant to GI toxicity. In this prespecified, combined analysis of the clinical development program, rofecoxib produced a significantly reduced incidence of clinical GI ulcers, bleeds, and perforations compared with the... 

Analysis of the analgesic and anti-inflammatory effects of rimazolium, a pyrido-pyrimidine derivative, compared with that of prostaglandin synthesis inhibitors and morphine... 

Topical delivery of diclofenac in 2.5% HA has also been shown to inhibit the development and angiogenesis of colon-26 adenocarcinoma (112). In this work, HA-diclofenac reduced proliferation and viability of colon-26 adenocarcinoma cells in vitro, inhibited tumor prostaglandin synthesis, and retarded angiogenesis in mice (114). Analysis of the tumor vasculature showed that vascular development was retarded by 12 days. The effects of HA-diclofenac were likely related to enhanced transdermal delivery and binding properties of HA. 

Frolich, 3.C., Williams, W.M., Sweetman, B.3., Smigel, M., Carr, K., HoUifield, 3.W., Fleischer, S., Nies, A.S., Frisk-Holmberg and Oates, 3.A. Analysis of renal prostaglandin synthesis by competitive protein binding assay and gas chromatography -mass spectrometry. Adv. in Prostaglandin and Thromboxane Research Vol. 1 (D. Samuelsson, R. Paoletti, ed.) 65-80, 1976... 

One of the key Intermediates in Corey s total synthesis of prostaglandins is the lactone (35) whose optically active form was obtained by resolution of (+) 36. Upon analysis of the sequence of reactions from cy-clopentadiene to 35 one would readily visualize the possibility of carrying out microbial resolution of various Intermediates along the synthetic pathway. One such resolution has been accomplished by microbial reduction of the (+) ketone 37 with Saccharomyces drosophylarum to yield the (+) exo and (-) endo alcohols (38 and 39). These were separated by chromatography and were oxidized to the optically active ketones (37).63 One of these was converted to 36. 4... 

Shibuya M, Ebizuka Y, Noguchi H, litaka Y, Sankawa U (1983) Inhibition of prostaglandin biosynthesis by 4-0-methylcryptochlorophaeic acid synthesis of monomeric arylcarboxylic acids for inhibitory activity testing and X-ray analysis of 4-0-methylcryptochlorophaeic acid. Chem Pharm Bull 31 407-413... 

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