Journal of Capital Medical University ›› 2019, Vol. 40 ›› Issue (3): 424-428.doi: 10.3969/j.issn.1006-7795.2019.03.018

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Investigation on the inhibition of Sitagliptin by osmotic pump on CD26/DPPIV activity

Xue Xingkui1, Han Xinhua2, Cai Siqi1,3, Chen Xiaoling1, Melody Y. Zeng1   

  1. 1. Central Lab, The People's Hospital of Longhua Shenzhen, Shenzhen 518109, Guangdong Province, China;
    2. Department of Endocrinology, Shenzhen Shekou People's Hospital, Shenzhen 518109, Guangdong Province, China;
    3. Department of Laboratory Medicine and Biotechnology, Graduate School, Southern Medical University, Guangzhou 501505, China
  • Received:2019-02-15 Online:2019-05-21 Published:2019-06-13
  • Supported by:
    This study was supported by National Natural Sciences Foundation of China (31650110474),Shenzhen Science,Technology and Innovation Commission (JCYJ20160426094752965),Shenzhen Health Research Project (201601059),Funds for Innovation of Science and Technology in Longhua District,Shenzhen (20160831A1030180,20160831A0410020).

Abstract: Objective To investigate the effect of Sitagliptin on mice with subcutaneous osmotic pump. Methods Osmotic pump carrying with Sitaglipin was implanted into mice subcutaneously, and the plasma concentration of sitagliptin was measured with HPLC-MS. The skin inflammation reaction was evaluated with pathological slides. DPPIV enzyme activity was measured with ELISA. Furthermore, the CD26 expression of spleen T cell was detected with flow cytometry and T cell migration was determined with transwell system.Results The duration of plasm Sitagliptin in mice subject to instant shot was shorter while those delivered by osmotic pump was observed at 24h post implantation of osmotic pump. Inhibition of DPPIV activity, as measured by ELISA, was confirmed at 24 hours after pump implantation, highlighting the utility of this method as a longer term model for DPPIV inhibition in mice. T cell migration was stably inhibited after application of Sitagliptin with osmotic pump. Conclusion In vivo Sitagliptin administration by an osmotic pump offers an effective approach for longer-term and stable DPPIV inhibition in mice and avoids the necessity for multiple dosing of the inhibitor, making study on function of CD26/DPPIV more effective.

Key words: CD26/DPPIV, Sitagliptin, osmotic pump, T cells

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