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

作　　者：阳春苗[1] 郑广进[1] 龙盛京[1] 陈永好[1] 韦贤[1] 

机构地区：[1]广西医科大学药学院,南宁530021

出　　处：《中国现代应用药学》2012年第3期205-208,共4页Chinese Journal of Modern Applied Pharmacy

基　　金：广西科学基金资助项目(桂科基0342003-4)

摘　　要：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。OBJECTIVE To provide an evidence to do further study on inhibiting a-amylase and explore the application areas of Ilicifolius Alkaloids A （4-Hydroxy-2-benzoxazolone, HBOA）. The effects of HBOA and its derivatives on a-amylase activity were also studied in this paper. METHODS With Acarbose as positive control, the effects of HBOA and its derivatives on a-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 or-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 a-amylase. CONCLUSION The author suggested that in order to better define the inhibition effects of a-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 a-amylase.

关 键 词：老鼠簕生物碱A 衍生物 a-淀粉酶 抑制作用 

分 类 号：R962.1[医药卫生—药理学]