Construction of Screening Model for Dipeptidyl Peptidase Ⅳ in vitro and Active Inhibitory Estimation of Related Compounds

JIANG Hui-xian1; LUO Chao2; LU Jun-xiong1; CAO Ying1; PANG Jian-xin1

doi:10.13422/j.cnki.syfjx.2012.04.080

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Construction of Screening Model for Dipeptidyl Peptidase Ⅳ in vitro and Active Inhibitory Estimation of Related Compounds

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- Construction of Screening Model for Dipeptidyl Peptidase Ⅳ in vitro and Active Inhibitory Estimation of Related Compounds
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 18, Issue 4, Pages: 210-215(2012)
- 作者机构：
  
  1. 南方医科大学药学院
  2. 2. 广州医学院第四附属医院药剂科
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2012.04.080
  CLC： R965
- Published：2012
- 稿件说明：
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[1]江慧贤,罗超,卢钧雄,曹莹,庞建新.构建二肽基肽酶-Ⅳ抑制剂体外筛选模型及相关化合物抑制活性的测定[J].中国实验方剂学杂志,2012,18(04):210-215.

JIANG Hui-xian1, LUO Chao2, LU Jun-xiong1, et al. Construction of Screening Model for Dipeptidyl Peptidase Ⅳ in vitro and Active Inhibitory Estimation of Related Compounds[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(4): 210-215.
[1]江慧贤,罗超,卢钧雄,曹莹,庞建新.构建二肽基肽酶-Ⅳ抑制剂体外筛选模型及相关化合物抑制活性的测定[J].中国实验方剂学杂志,2012,18(04):210-215. DOI： 10.13422/j.cnki.syfjx.2012.04.080.

JIANG Hui-xian1, LUO Chao2, LU Jun-xiong1, et al. Construction of Screening Model for Dipeptidyl Peptidase Ⅳ in vitro and Active Inhibitory Estimation of Related Compounds[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(4): 210-215. DOI： 10.13422/j.cnki.syfjx.2012.04.080.

摘要

目的:建立二肽基肽酶-IV（DPP-IV）抑制剂体外筛选模型

并测定相关化合物的抑制率。方法:提取Caco-2细胞中DPP-IV

测定酶不同活力单位的吸光度（A）

绘制活性-吸光度相关性曲线评价酶的活性与A的相关性;以sitagliptin为阳性对照测定其半抑制浓度（IC50）验证本实验模型;以该模型测定sitagliptin衍生物及对DPP-IV有抑制作用化合物的抑制活性。结果:酶的活性在一定范围内与A成直线相关;以本模型测定的sitagliptin IC50为18.354 nmol.L-1;JD-1

JD-2 IC50分别为3.4

2.6μmol.L-1

相关化合物的抑制率在21.45%～27.77%之间。结论:使用本DPP-IV抑制剂筛选模型测定的sitagliptin IC50与文献报道的相近

证明本模型的有效性

所测化合物有一定抑制活性。

Abstract

Objective:We aimed to establish a model to select dipeptidyl peptidase IV（DPP-IV）

and to test the inhibitory rate of the seven compounds.Method:DPP-IV was extracted from cultured Caco-2 cells and the values of absorbance（A） were tested in different activity units which were to evaluate the relation between the activity of DPP-IV and the value of A by the curve of activity-A.Sitagliptin as a positive control was used to evaluate the selected model.The derivatives from sitagliptin and the compounds were estimated inhibitory activity by the model.Result:The activity of DPP-IV was correlated to the value of A in a certain range.The IC50 values of sitagliptin

JD-1 and JD-2 were 18.354 nmol·L-1

3.4 μmol·L-1 and 2.6 μmol·L-1

respectively;the range of inhibitory activity for the compounds was between 21.45% and 27.77%.Conclusion:The IC50 of sitagliptin tested by this selected model is close to the value reported

which proves availability of the model.and meanwhile

the compounds estimated in this study contain inhibitory effect.

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