YC-1 INHIBITED HUMAN PLATELET-AGGREGATION THROUGH NO-INDEPENDENT ACTIVATION OF SOLUBLE GUANYLATE-CYCLASE

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Title:	YC-1 INHIBITED HUMAN PLATELET-AGGREGATION THROUGH NO-INDEPENDENT ACTIVATION OF SOLUBLE GUANYLATE-CYCLASE
Authors:	WU, CC;KO, FN;KUO, SC;LEE, FY;TENG, CM
Contributors:	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
Date:	1995
Issue Date:	2010-09-24 15:05:58 (UTC+8)
Publisher:	STOCKTON PRESS
Abstract:	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.
Relation:	BRITISH JOURNAL OF PHARMACOLOGY 116(3):1973-1978
Appears in Collections:	[Graduate Institute of Pharmaceutical Chemistry] Journal articles

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