中國醫藥大學機構典藏 China Medical University Repository, Taiwan:Item 310903500/3784
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    题名: Inhibition on platelet activation by shikonin derivatives isolated from Arnebia euchroma
    作者: 張永勳(Yuan Shiun Chang)
    贡献者: 藥學院中國藥學研究所;中國附醫藥劑部中藥局
    关键词: Phosphoinositide breakdown;Platelet;Shikonin derivative;Arnebia euchroma
    日期: 1993
    上传时间: 2009-08-20 19:03:32 (UTC+8)
    摘要: Acetylshikonin, teracrylshikonin, β,β-dimethylacrylshikonin and shikonin, isolated from Arnebia euchroma, inhibited collagen (10 μg/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 μM, respectively. Acetylshikonin also inhibited the aggregation and ATP release of washed rabbit platelets induced by arachidonic acid (AA, 100 μM), U46619 (1 μM), platelet-activating factor (PAF, 3.6 nM) and thrombin (0.1 U/ml) in a concentration-dependent manner. The IC50 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 μM, respectively. The thromboxane B2 formation caused by collagen, PAF and thrombin was inhibited by acetylshikonin, while formations of thromboxane B2 and prostaglandin D2 caused by AA were not inhibited. Acetylshikonin did not inhibit cyclooxygenase activity since it did not attenuate prostaglandin E2 formation after incubation of sheep vesicular gland microsomes with AA. Acetylshikonin suppressed both the rise of intracellular Ca2+ concentration and the generation of [3H]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: Biochimica et Biophysica Acta 1268(3):329-334
    显示于类别:[中國藥學研究所(已停用)] 期刊論文

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