Characterization of DPP-IV Inhibitory Peptides Using an In Vitro Cell Culture Model of the Intestine

文献类型： 外文期刊

第一作者： Jin, Ritian

作者： Jin, Ritian;Shang, Jiaqi;Teng, Xiangyu;Zhang, Ligang;Liao, Minhe;Kang, Jiaxin;Ren, Haowei;Liu, Ning;Jin, Ritian;Shang, Jiaqi;Teng, Xiangyu;Zhang, Ligang;Liao, Minhe;Kang, Jiaxin;Ren, Haowei;Liu, Ning;Jin, Ritian;Shang, Jiaqi;Teng, Xiangyu;Kang, Jiaxin;Liu, Ning;Meng, Ran;Wang, Dangfeng

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关键词： DPP-IV inhibitory peptide; Caco-2 monolayer membrane; transport mechanism; tight junction protein

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：4.192； 五年影响因子：4.289 ）

ISSN： 0021-8561

年卷期： 2021 年 69 卷 9 期

页码：

收录情况： SCI

摘要： Here, we characterize the activities of two depeptidyl peptidase-IV (DPP-IV) inhibitory peptides, VLATSGPG and LDKVFER, using the Caco-2 monolayer model for the intestine. VLATSGPG and LDKVFR inhibited the DPP-IV in the cells via a mixed-type inhibition mode, with in situ IC50 values of 207.3 and 148.5 mu M, respectively. Furthermore, VLATSGPG and LDKVFR were transported intact across the cells, with P-app values of 2.41 +/- 0.16 and 4.23 +/- 0.29 x 10(-7) cm/s, respectively. Fragmented peptides were identified in the basolateral side of the membrane. Two of these, GPG and VLA, exhibited high inhibitory activities of 83.6 +/- 3.3 and 58.5 +/- 2.5%, respectively, at 100 mu M concentration. Although 3 mM VLATSGPG and LDKVFR were transported across the epithelium in a concentration-dependent manner, their transport did not damage the tight junction proteins, ZO-1 and occludin. This study demonstrates that the two peptides potentially regulate DPP-IV activity in the intestine.

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