Inhibitory effects of sodium quercetin monosulfate on pig platelet aggregation induced by thrombin.

Zhongguo yao li xue bao = Acta pharmacologica Sinica Pub Date : 1999-07-01

W Liu, Z J Song, N C Liang, J She, L E Mo

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Abstract

Aim: To study the inhibitory effects of sodium quercetin monosulfate (SQMS) on pig platelet aggregation induced by thrombin.

Methods: Platelet aggregation was analyzed by turbidimetry. Cytosolic free calcium concentration ([Ca2+]i) was determined by Fura-2 fluorescence. Activity of protein kinase C (PKC) was assayed by incubating PKC with histone III S and [gamma-32 P] ATP. The cytoskeletal proteins were precipitated by Triton X-100 and separated by SDS-PAGE.

Results: SQMS inhibited the platelet aggregation induced by thrombin 500 U.L-1 with IC50 132 (50-347) mumol.L-1. SQMS inhibited Ca2+ influx in blood platelets induced by thrombin 500 U.L-1 in the presence of extracellular Ca2+ 1 mmol.L-1 with IC50 20 (9-46) mumol.L-1; SQMS inhibited the internal Ca2+ release in the absence of extracellular Ca2+. SQMS also decreased [Ca2+]i level in quiescent blood platelets. SQMS (10-160 mumol.L-1) inhibited the activity of cytosolic PKC from blood platelets in a concentration-dependent manner, but had no effect on membrane PKC. SQMS (20-80 mumol.L-1) inhibited the actin polymerization induced by thrombin 500 U.L-1 inblood platelets in a concentration-dependent manner.

Conclusion: SQMS inhibited pig platelet aggregation induced by thrombin and its mechanism might be due to its inhibitions of Ca2+ influx, internal Ca2- release, PKC activity, and actin polymerization.

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单硫酸槲皮素钠对凝血酶诱导的猪血小板聚集的抑制作用。

目的:研究槲皮素单硫酸钠(SQMS)对凝血酶诱导的猪血小板聚集的抑制作用。方法:用浊度法分析血小板聚集。用Fura-2荧光法测定胞质游离钙浓度([Ca2+]i)。蛋白激酶C (PKC)与组蛋白3s和[γ -32 P] ATP孵育，检测PKC的活性。细胞骨架蛋白用Triton X-100沉淀，SDS-PAGE分离。结果:SQMS抑制凝血酶500ul -1诱导的血小板聚集，IC50为132(50-347)。在细胞外Ca2+ 1 mmol存在的情况下，SQMS抑制凝血酶500 μ l -1诱导的血小板内流Ca2+。L-1, IC50为20 (9-46);在没有细胞外Ca2+的情况下，SQMS抑制了细胞内Ca2+的释放。SQMS还能降低静止血小板中的[Ca2+]i水平。SQMS (10- 160mol . l -1)对血小板胞浆PKC活性有浓度依赖性，但对膜PKC无影响。SQMS (20 ~ 80 μ mol. l -1)对凝血酶500 μ l -1诱导的血小板肌动蛋白聚合具有浓度依赖性。结论:SQMS抑制凝血酶诱导的猪血小板聚集，其机制可能与抑制Ca2+内流、Ca2-释放、PKC活性和肌动蛋白聚合有关。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Zhongguo yao li xue bao = Acta pharmacologica Sinica

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