PubMed · 109921
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J L Marx. 1979-07-13. Dysmenorrhea: basic research leads to a rational therapy.. https://doi.org/10.1126/science.109921
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The effects of 12-O-tetradecanoyl-phorbol-13-acetate (TPA) on the mRNA levels of two enzymes, thromboxane synthase (TXS) and prostaglandin endoperoxide synthase (PES), responsible for the synthesis of thromboxane A2 from arachidonic acid, were studied in human erythroleukemia (HEL) cells by RNA blot analysis. TPA induced both TXS and PES mRNAs in HEL cells in a dose-dependent manner at 36 h. The half-maximal and maximal effects for the induction of both mRNAs were at approximately 3 x 10(-9) M and at 10(-8) M, respectively. TXS and PES mRNA levels increased in a time-dependent fashion by TPA, and reached to 7- and 3.5-fold of the control, respectively after 48 h of TPA treatment. These results suggest that expression of TXS and PES genes in HEL cells were simultaneously stimulated by TPA.
The role of endogenous prostaglandins in the modulation of lower oesophageal sphincter (LES) function has been assessed by giving three structurally unrelated cyclooxygenase inhibitors and monitoring their acute effects on LES tonus and platelet thromboxane (TX) B2 production in 20 healthy volunteers. In a double-blind, placebo-controlled, cross-over study, IV injection of soluble salts of acetylsalicylic acid and indomethacin elicited a transient increase in LES tonus of approximately 50% over baseline. A similar pattern was observed after the rectal administration of indomethacin. In contrast, indoprofen had no measurable effect on LES tones, despite comparable inhibition of platelet cyclooxygenase activity. This may have been due to the markedly different tissue distribution of the drug. The results suggest that endogenous prostaglandins physiologically exert an inhibitory influence on LES function.
The root heartwood of Dalbergia odorifera T. Chen (Leguminosae) is a Chinese medicinal drug (Japanese name koshinko) used for a stagnant blood syndrome (stagnation of disordered blood; Japanese, oketsu). In addition to 10 known compounds, five new phenolic compounds, isomucronustyrene and hydroxyobtustyrene (cinnamylphenols), (+)-isoduartin (isoflavan), odoriflavene (isoflav-3-ene) and (-)-odoricarpan (pterocarpan) were isolated and their structures were elucidated on the basis of chemical and spectroscopic methods. Of the fifteen compounds isolated, cinnamylphenols, isoflavans, isoflavene and benzoic acid derivative significantly inhibited prostaglandin biosynthesis as well as platelet aggregation induced by arachidonic acid.