三种乳源生物活性肽的二肽基肽酶-Ⅳ抑制活性研究  

Inhibition of dipeptidyl peptidase Ⅳ(DPP-Ⅳ) by three casein-derived bioactive peptides in vitro

作　　者：陈静[1] 李婉如[1] 李阜烁 汪超 范梦珠 占东升 李锡安 张少辉[1,2] 

机构地区：[1]上海交通大学农业与生物学院,上海200240 [2]浙江辉肽生命健康科技有限公司,浙江温州325800 [3]浙江熊猫乳集团股份有限公司,浙江温州325800

出　　处：《中国乳品工业》2018年第2期4-8,共5页China Dairy Industry

摘　　要：通过从分化成熟的人克隆结肠腺癌细胞(Caco-2细胞)中提取二肽基肽酶-Ⅳ(DPP-Ⅳ)建立体外筛选DPP-Ⅳ抑制剂的模型,用Ile-Pro-Ile(IPI)作为阳性对照测定其半抑制质量浓度(IC_(50))评价该模型,并测定3种来源于酪蛋白的四肽Leu-Pro-Leu-Pro(LPLP)、Gln-Glu-Pro-Val(QEPV)和Asp-Gln-Leu-Gln(DELQ)的抑制率,研究了DPP-Ⅳ抑制肽的抑制类型和复合抑制作用。实验结果表明:IPI的IC_(50)为(31.51±1.51)μg/m L,与文献报道的相近,证明该模型可以应用于DPP-Ⅳ抑制剂的筛选;LPLP的IC_(50)为(0.84±0.06)mg/m L,QEPV的IC_(50)为(14.45±1.07)mg/m L而DELQ的IC_(50)大于100 mg/m L,即LPLP和QEPV具有一定的抑制作用;LPLP和QEPV的作用均为非竞争性机制,并且两种多肽联合对DPP-Ⅳ抑制作用为协同抑制作用。The model of DPP-IV inhibitor was established by extracting DPP-IV from Caco-2 cells. Ile-Pro-Ile （IPI）, a positive control, was used to evaluate the selected model. The half concentration （IC50） of three casein-derived bioactive peptides, Leu-Pro-Leu-Pro （LPLP）, Gln-Glu-Pro-Val （QEPV） and Asp-Gln-Leu-Gln （DELQ）, were studied. The D＇PP-IV inhibitory types of three peptides and the inhibition rate of complex peptides were studied. The results showed that the IC50 of LPLP, QEPV and DELQ was 0.84± 0.06 mg/mL, 14.45- 1.07 mg/mL and more than 100mg/mL respectively. The DPP-IV inhibitory type of LPLP and QEPV was noncompetitive mecha- nisms. The combination of the LPLP and QEPV to DPP-IV inhibition was synergistic inhibition.

关 键 词：生物活性肽 人克隆结肠腺癌细胞 二肽基肽酶-Ⅳ抑制模型 复合作用 

分 类 号：Q93-33[生物学—微生物学]