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| 題名: | YC-1 INHIBITED HUMAN PLATELET-AGGREGATION THROUGH NO-INDEPENDENT ACTIVATION OF SOLUBLE GUANYLATE-CYCLASE |
| 作者: | WU, CC;KO, FN;KUO, SC;LEE, FY;TENG, CM |
| 貢獻者: | 藥學院藥化所;NATL TAIWAN UNIV,COLL MED,INST PHARMACOL,TAIPEI,TAIWAN;CHINA MED COLL,GRAD INST PHARMACEUT CHEM,TAICHUNG,TAIWAN;YUNG SHIN PHARMACEUT IND CO LTD,TAICHUNG,TAIWAN |
| 日期: | 1995 |
| 上傳時間: | 2010-09-24 15:05:58 (UTC+8) |
| 出版者: | STOCKTON PRESS |
| 摘要: | Acetylshikonin, teracrylshikonin, beta,beta-dimethylacrylshikonin and shikonin, isolated from Amebia euchroma, inhibited collagen (10 mu g/ml)-induced aggregation of washed rabbit platelets in a concentration-dependent manner with IC50 values of 2.1 +/- 0.2, 2.8 +/- 0.3, 4.2 +/- 0.5 and 10.7 +/- 0.7 mu M, respectively. Acetylshikonin also inhibited the aggregation and ATP release of washed rabbit platelets induced by arachidonic acid (AA, 100 mu M), U46619 (1 mu M), platelet-activating factor (PAF, 3.6 nM) and thrombin (0.1 U/ml) in a concentration-dependent manner. The IC(5)0 values of acetylshikonin on the inhibition of these four agonists-induced platelet aggregation were 3.1 +/- 0.4, 2.2 +/- 0.2, 8.0 +/- 0.6 and 12.7 +/- 1.0 mu M, respectively. The thromboxane B-2 formation caused by collagen, PAF and thrombin was inhibited by acetylshikonin, while formations of thromboxane B-2 and prostaglandin D-2 caused by AA were not inhibited. Acetylshikonin did not inhibit cyclooxygenase activity since it did not attenuate prostaglandin E(2) formation after incubation of sheep vesicular gland microsomes with AA. Acetylshikonin suppressed both the rise of intracellular Ca2+ concentration and the generation of [H-3]inositol monophosphate caused by these five aggregation inducers. Platelet cyclic AMP level was unaffected by acetylshikonin. These data indicate that acetylshikonin inhibits platelet activation by suppression of phosphoinositide breakdown. |
| 關聯: | BRITISH JOURNAL OF PHARMACOLOGY 116(3):1973-1978 |
| 顯示於類別: | [藥物化學研究所] 期刊論文
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