论文部分内容阅读
目的研究老鼠簕生物碱A及其衍生物对-淀粉酶活性的影响,以期为-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-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-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-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-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-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-淀粉酶的水解活性。
Aim To study the effect of alkaloid A and its derivatives on the activity of amylase in rats, in order to provide the experimental and structural basis for the further study of amylase inhibitors and to expand the application of alkaloids A and its derivatives range. Methods The rat alkaloids A and its derivatives were taken as test samples and acarbose as positive control. The effects of each compound on amylase activity were compared by Bernfeld method. Results A-1, a-2, a-3, a-4, a-5 and b-7 showed inhibitory activity on amylase at the concentrations of 0.625,1.25,2.5,5.0 and 10.0 gL- The inhibitory rates were 10.24%, 71.52%, 63.79%, 19.71%, 52.76%, 38.96% at the concentration of 10.0 gL-1, respectively, in the experimental concentration range. While a-7, b-3, b-1 showed a trend of enhancing the activity of amylase hydrolysis with increasing concentration. Conclusions It is speculated that the phenolic hydroxyl group in the A structure of S. aureus is the basic pharmacophore of its inhibition on amylase. When structural modification of S. alkaloid A, Introduction of a chlorine atom, an acyl group or a hydroxyl group-containing substituent is advantageous for inhibiting the activity of amylase; the substitution of the acetoxy group for the 4-position phenolic hydroxyl group and the substitution of the 7-position for the carboxylic acid-containing substituent or for the 3- Or when substituted with small molecule groups, are beneficial for enhancing the hydrolytic activity of amylase.