摘要

Comparative studies of enzymatic acylation of troxerutin by the alkaline protease from Bacillus subtilis under ultrasound and shaking were carried out in nonaqueous media. Using divinyl dicarboxylates (CH(2)CH-OOC-(CH(2))(n)-COO-CHCH(2), n=2, 3, 4, 7, 8, 11) featuring different chain length as acyl donors, troxerutin was regioselectively acylated at B ethoxyl group, whether under ultrasound or shaking. Ultrasonic treatment increased the reaction rate and led to high conversion. Several factors, such as pre-irradiation on the enzyme, the power and frequency of the ultrasound, operation manner, as well as the length of the acyl donors were investigated. Using enzyme pre-irradiated for 8 h, the conversion of troxerutin was increased to 87.3% compared with 56.3% obtained from the untreated enzyme. Experimental results also showed that continual ultrasound caused greater rate acceleration than interval ultrasound. Powers of 100, 150 and 200 W, frequencies of 40, 80 and 100 kHz all showed significant improvement on the transesterification, with the greatest effect observed at 150 W, 80 kHz. The acceleration effect increased as the chain length of the acyl donors decreased from C(13) to C(4).

译文

在非水介质中,在超声波和振荡下,对枯草芽孢杆菌碱性蛋白酶对曲克芦丁的酶酰化作用进行了比较研究。使用二乙烯基二羧酸 (CH (2) CH-OOC-(CH (2)) (n)-COO-CHCH (2),n = 2,3,4,7,8,11) 以不同链长作为酰基供体,无论是在超声波下还是在摇动下,曲克芦丁在 B 乙氧基组被区域选择性酰化。超声波处理提高了反应速率并导致高转化率。研究了几个因素,如对酶的预照射、超声波的功率和频率、操作方式以及酰基供体的长度。使用预辐照 8 小时的酶,与未处理酶的 87.3% 相比,曲克芦丁的转化率提高到 56.3%。实验结果还表明,continual 超声比间隔超声产生更大的加速度。100 、 150 和 200 W 的功率,40 、 80 和 100 kHz 的频率都显示了对酯交换的显著改善,在 150 W 、 80 kHz 时观察到的效果最大。加速效应随着酰基供体的链长从 C (13) 减少到 C (4) 而增加。

Troxerutin

神经 防血栓 治疗药物
概述  :  

作用与用途药效学:本药是芦丁经羟乙基化半合成水溶性黄酮类化合物,对闭塞性血管病具有较好的疗效。药理作用:①抑制血小板聚集,防止血栓形成。②对抗5-羟色胺、缓激肽引起的血管损伤,增加毛细血管抵抗力,降低毛细血管通透性,从而防止血管通透性增高引起的水肿。③增加血氧含量和氧饱和度,促进新血管生成以增进侧支循环,对急性缺血性脑损伤有显著的保护作用。④可兴奋神经纤维,具有解痉作用。⑤还具有抗放射线损伤、抗炎症、抗过敏、抗溃疡等作用。药动学:口服吸收良好,给药后1~6小时达血药浓度峰值。药物体内分布广泛,可

troxerutin

释    义   曲克芦丁

例    句   To establish a method for the determination of other hydroxyethylated rutin derivatives in troxerutin for injection by HPLC. 建立了高效液相色谱法测定注射用曲克芦丁中其他羟乙基芦丁衍生物的方法。

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