温度对超声辅助合成阿魏酸甲酯及其抗血小板试验的影响

J. Ekowati, Rian Putra Pratama, K. A. Nofianti, N. Diyah
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引用次数: 3

摘要

阿魏酸(FA)已被报道通过间接抑制P2Y12受体具有抗血小板活性。为了提高FA的活性,通过改善其亲脂性,使其更容易进入细胞,通过Fisher酯化法合成阿魏酸甲酯。在55℃和65℃两种温度下,以水为介质,利用超声波作为能量源发射。本研究的目的是在55°C和65°C的温度下制备阿魏酸甲酯,并测定其反应常数速率(k)和能量活化度(Ea)。此外,研究了20 mg/kg BW剂量下的抗血小板活性。采用凝血时间法和出血时间法进行抗血小板试验。结果采用单因素方差分析(P<0.05)。在55℃和65℃条件下,阿魏酸甲酯的收率分别为50.3%和67.1%。55℃时k值为4x10-5 cons-1min-1, 65℃时k值为9x10-5 cons-1min-1。阿魏酸甲酯的凝血时间和出血时间分别为265秒和175秒。阿魏酸甲酯的抗血小板活性优于阿魏酸。
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The Temperature Effect on Ultrasonic-assisted of Synthesis Methyl Ferulate and Its Antiplatelet Assay
Ferulic acid (FA) has been reported to have antiplatelet activity through indirectly inhibiting P2Y12 receptor. In order to increase the activity of FA, by improving its lipophilicity, so that it is easier to enter the cell, synthesis methyl ferulate was conducted through Fisher esterification. Ultrasonic waves were utilized as source of energy emitted through water as the medium at two various of temperature, i.e., 55 °C and 65 °C. The purposes of this study are to produce methyl ferulate and to determine the reaction constant rate (k) and its energy activation (Ea), at temperature of 55 °C and 65 °C. Moreover, the biological activity as antiplatelet was investigated at dose 20 mg/kg BW. The antiplatelet assay was conducted by clotting time and bleeding time methods. The results were analyzed by one way ANOVA program (P<0.05). The yield of methyl ferulate are 50.3% and 67.1% at 55 °C and 65 °C, respectively. The k value at 55°C is 4x10-5 cons-1min-1, while that of at 65 °C is 9x10-5 cons-1min-1. The clotting time and bleeding time of methyl ferulate obtained were 265 sec and 175 sec, respectively. The antiplatelet activity of methyl ferulate is better than ferulic acid.
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