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J E Pike

Publications and source records attributed to J E Pike.

At least 19 recordsLinked to original sources

Inhibition of platelet arachidonic acid 12-lipoxygenase by acetylenic acid compounds.

Eighteen acetylenic fatty acids were tested as inhibitors of human platelet arachidonic acid 12-lipoxygenase. 4,7,10,13-Eicosatetraynoic (4,7,10,13-ETYA) acid emerged as the most potent compound. Additional experiments have shown that 4,7,10,13-ETYA selectively blocked the 12-lipoxygenase in washed human platelets with lesser activity against the cyclooxygenase. The ID50 value for lipoxygenase was 7.8 microM in comparison with an ID50 of 100 microM for the cyclooxygenase. The commonly used inhibitor 5,8,11,14-eicosatetraynoic acid inhibited both enzymes with equal potency. It appears that 4,7,10,13-ETYA may be a valuable lead for selective modulation of the 12-lipoxygenase pathway in platelet or other target tissues.

5,8,11,14-Eicosatetraynoic Acid↗

The stability of 13,14-dihydro-15 keto-PGE2.

13,14-Dihydro-15 keto-PGE2 decomposes by first order reaction kinetics, dependent on pH, temperature and albumin concentration. Under common experimental conditions at or near neutrality in the absence of albumin decomposition is suspended with the formation of 13,14-dihydro-15-keto-PGA2. Cyclization into 11-deoxy-13,14-dihydro-15 keto-11,16-bicyclo-PGE2 occurs at elevated pH in purely aqueous buffers, and also at or near neutrality in the presence of albumin. Albumin accelerates, quantitatively, the decomposition of 13,14-dihydro-15 keto-PGE2 and promotes, qualitatively, the formation of the bicyclo rearrangement product. High performance liquid chromatographic analysis indicates that the cyclization product exists in at least three epimerically distinct forms. The two major epimers have been synthesized and isolated in pure form. They differ, mainly, by their optical rotation.

Albumins↗

Prostaglandins.

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Animals↗