老鼠簕生物碱A及其衍生物对α-淀粉酶活性的影响

Study on Effect of Ilicifolius Alkaloids A (4-Hydroxy -2-benzoxazolone, HBOA) and Its Derivatives on α-Amylase Activity

关键词:  老鼠簕生物碱A  衍生物  α-淀粉酶  抑制作用

Key words:  ilicifolius alkaloids A  derivatives  a-amylase  inhibition effects

摘要:

目的 研究老鼠簕生物碱A及其衍生物对a-淀粉酶活性的影响，以期为a-淀粉酶抑制剂的进一步深入研究提供实验基础及结构依据，并拓展老鼠簕生物碱A及其衍生物的应用范围。方法 以老鼠簕生物碱A及其衍生物为待测样品，阿卡波糖为阳性对照，采用Bernfeld法测定比较各化合物对a-淀粉酶活性的影响。结果 a-1、a-2、a-3、a-4、a-5、b-7在样品浓度为0.625，1.25，2.5，5.0，10.0 g·L^-1时均对a-淀粉酶有抑制作用，且在实验浓度范围内随着浓度增加抑制率增大，浓度为10.0 g·L^-1时抑制率分别为10.24%、71.52%、63.79%、19.71%、52.76%、38.96%。而a-7、b-3、b-1随浓度的增大，表现出增强a-淀粉酶水解活性的趋势。结论 推测老鼠簕生物碱A结构中的酚羟基是其对a-淀粉酶起抑制作用的基本药效基团，对老鼠簕生物碱A进行结构修饰时，保留4-位酚羟基并在7-位引入氯原子、酰基或含羟基取代基均有利于抑制a-淀粉酶的活性；而以乙酰氧基取代4-位酚羟基，并使7-位用含羧酸取代基取代或3-位无取代或以小分子基团取代时均有利于增强a-淀粉酶的水解活性。

Abstract:

To provide an evidence to do further study on inhibiting α-amylase and explore the application areas of Ilicifolius Alkaloids A (4-Hydroxy-2-benzoxazolone, HBOA). The effects of HBOA and its derivatives on α-amylase activity were also studied in this paper. METHODS With Acarbose as positive control, the effects of HBOA and its derivatives on α-amylase activity were compared by Bernfeld method. RESULTS a-1, a-2, a-3, a-4, a-5, b-7 could inhibit the activity of α-amylase, and the inhibition rate increased when the concentration increased in the experimental concentration range. Their inhibition rates were 10.24%, 71.52%, 63.79%, 19.71%, 52.76%, 38.96% on the 10.0 g·L^-1 concentration. While a-7, b-3, b-1 could reinforce the activity of α-amylase. CONCLUSION The author suggested that in order to better define the inhibition effects of α-amylase there is a need to synthesize some HBOA derivatives which carry chlorine atom, acyl group or hydroxyl group at position 7 of the HBOA and retain the phenolic hydroxyl group at position 4. However, taking acetoxyl group at position 4 and carboxyl group at position 7 or small group can non-yl at position 3 could reinforce the activity of α-amylase.