國家衛生研究院 NHRI:Item 3990099045/13436
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    题名: DBPR108, a novel dipeptidyl peptidase-4 inhibitor with antihyperglycemic activity
    作者: Yeh, KC;Yeh, TK;Huang, CY;Hu, CB;Wang, MH;Huang, YW;Chou, LH;Ho, HH;Song, JS;Hsu, T;Jiaang, WT;Chao, YS;Chen, CT
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Aims: Dipeptidyl peptidase 4 (DPP-4) is a valid molecular drug target from which its inhibitors have been developed as medicines for treating diabetes. The present study evaluated a new synthetic DPP-4-specific inhibitor of small molecule DBPR108 for pharmacology and pharmacokinetic profiles. Main methods: DBPR108 of various doses was orally administered to rats, diabetic mice, and dogs and the systemic circulating DPP-4 activities in the animals were measured to demonstrate the pharmacological mechanisms of action via DPP-4 inhibition. Upon an oral administration of DBPR108, the serum active GLP-1 and insulin levels of the rats challenged with an oral glucose ingestion were measured. Oral glucose tolerance test in diet-induced obese mice was performed to examine if DBPR108 increases the glucose tolerability in animals. Key findings: Orally administered DBPR108 inhibited the systemic plasma DPP-4 activities in rats, dogs and diabetic mice in a dose-dependent manner. DBPR108 caused elevated serum levels of active GLP-1 and insulin in the rats. DBPR108 dose-dependently increased the glucose tolerability in diet-induced obese (DIO) mice and, furthermore, DIO mice treated with DBPR108 (0.1 mg/kg) in combination with metformin (50 or 100 mg/kg) showed a prominently strong increase in the glucose tolerability. Significance: DBPR108 is a novel DPP-4-selective inhibitor of small molecule that demonstrated potent in vivo pharmacological effects and good safety profiles in animals. DBPR108 is now a drug candidate being further developed in the clinical studies as therapeutics for treating diabetes.
    日期: 2021-08-01
    關聯: Life Sciences. 2021 Aug 1;278:Article number 119574.
    Link to: http://dx.doi.org/10.1016/j.lfs.2021.119574
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0024-3205&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000663320600010
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85105305416
    显示于类别:[陳炯東] 期刊論文
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    [蔣維棠] 期刊論文
    [葉燈光] 期刊論文

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