摘要
目的建立二肽基肽酶Ⅳ抑制剂的筛选模型。方法以Gly-Pro-PNA为反应底物,通过发色底物法检测DPPIV的活性,对酶量、底物浓度、最佳温度、pH及反应时间进行了优化。结果确定反应条件为酶量0.5U.L-1、底物浓度0.262μmol·L-1、温度37℃、pH8.2。在上述反应条件下对多种中药进行了筛选,发现中药水蛭、茯神、密蒙花提取物具有DPPIV抑制作用。结论此方法可作为DPPIV抑制剂的体外筛选模型。
Aim To develop a model for screening DPPIV inhibitor from Chinese Herbal medicine. Methods With GlyPro-PNA as a substrate,DPPⅣ activity was assayed by the chromogenic substrate. The concentration of DPPIV and Gly-Pro- PNA, temperature, pH and reaction time were optimized. Resuits The optimal enzymatic reaction system was as follows： DPPIV 0. 5 U·L^-1 , Gly-Pro-PNA 0. 262umol·L^-1 , 37%,pH 8.2, reaction for 60 min. Further more, many kinds of herbal abstracts were screened and some had the DPPIV inhibitory function, such as Leech, Poria cum Radix Pini and Buddleja officinalis Maxim. Conclusion The model can be used to screen for DPPⅣ inhibitors in vitro.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2009年第3期411-414,共4页
Chinese Pharmacological Bulletin
基金
国家高技术研究发展计划(863计划)重点资助项目(No2007AA021506)
教育部新世纪优秀人才支持计划资助项目(NoNCET-07-0380)
