Bioscience, biotechnology, and biochemistry, 2012, Vol.76 (11), p.2038-2043
2012
Details
- Autor(en) / Beteiligte
- Titel
- JJK694, a Synthesized Obovatol Derivative, Inhibits Platelet Activation by Suppressing Cyclooxygenase and Lipoxygenase Activities
- Ist Teil von
- Bioscience, biotechnology, and biochemistry, 2012, Vol.76 (11), p.2038-2043
- Ort / Verlag
- Tokyo: Japan Society for Bioscience, Biotechnology, and Agrochemistry
- Erscheinungsjahr
- 2012
- Link zum Volltext
- Quelle
- EZB Electronic Journals Library
- Beschreibungen/Notizen
- Obovatol has various biological activities, including anti-proliferative, neurotrophic, anti-fibrillogenic, anti-platelet, anti-fungal and anti-inflammatory activities. In this study, we investigated the effects of JJK694, a synthesized obovatol derivative, on rabbit platelet activation and its molecular mechanisms. JJK694 significantly inhibited washed rabbit platelet aggregation and serotonin secretion induced by collagen and arachidonic acid, but had little effect on thrombin- or U46619-induced aggregation. These results suggest that JJK694 selectively inhibits collagen- and arachidonic acid-mediated signaling. JJK694 also showed a concentration-dependent decrease in cytosolic Ca(2+) mobilization, but it had no effect on arachidonic acid liberation. On the other hand, it significantly inhibited the formation of arachidonic acid metabolites, including thromboxane A(2) (TXA(2)), prostaglandin D(2), and 12-hydroxy-5,8,10,14-eicosatetraenoic acid (12-HETE), by suppression of cyclooxygenase (COX)-1 and lipoxygenase (LOX) activities. These results indicate that JJK694 hasanti-platelet activities through inhibition of arachidonic acid metabolite production by suppression of COX-1 and LOX activities.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0916-8451eISSN: 1347-6947DOI: 10.1271/bbb.120369Titel-ID: cdi_pascalfrancis_primary_27771329
- Format
- –
- Schlagworte
- 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid - biosynthesis, Animals, anti-platelet activity, Antiinflammatory agents, arachidonic acid metabolites, Biological and medical sciences, Biphenyl Compounds - chemical synthesis, Biphenyl Compounds - chemistry, Biphenyl Compounds - pharmacology, Calcium - metabolism, Catechols - chemical synthesis, Catechols - chemistry, Catechols - pharmacology, Cell Survival - drug effects, cyclooxygenase, Cyclooxygenase Inhibitors - chemical synthesis, Cyclooxygenase Inhibitors - chemistry, Cyclooxygenase Inhibitors - pharmacology, Cytosol - drug effects, Cytosol - metabolism, Dinoprostone - biosynthesis, Fundamental and applied biological sciences. Psychology, lipoxygenase, Lipoxygenase - metabolism, Lipoxygenase Inhibitors - chemical synthesis, Lipoxygenase Inhibitors - chemistry, Lipoxygenase Inhibitors - pharmacology, Male, obovatol derivative, Phenyl Ethers - chemical synthesis, Phenyl Ethers - chemistry, Phenyl Ethers - pharmacology, Platelet Activation - drug effects, Platelet Aggregation - drug effects, Platelet Aggregation Inhibitors - chemical synthesis, Platelet Aggregation Inhibitors - chemistry, Platelet Aggregation Inhibitors - pharmacology, Prostaglandin-Endoperoxide Synthases - metabolism, Rabbits, Serotonin - secretion