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浙江大学学报(医学版)  2021, Vol. 50 Issue (5): 659-665    DOI: 10.3724/zdxbyxb-2021-0170
综述     
磷酸二酯酶抑制剂治疗炎性肠病的研究进展
史建蓉1,马望前2,汤慧芳3,*()
1.浙江大学医学院附属儿童医院实验检验中心 国家儿童健康与疾病临床医学研究中心 国家儿童区域医疗中心,浙江 杭州 310052
2.浙江大学医学院附属第二医院消化内科,浙江 杭州 310009
3.浙江大学基础医学院药理学系,浙江 杭州 310058
Research progress of phosphodiesterase inhibitors in inflammatory bowel disease treatment
SHI Jianrong1,MA Wangqian2,TANG Huifang3,*()
1. Clinical Laboratory, Children’s Hospital, Zhejiang University School of Medicine, National Clinical Research Center for Child Health, National Children’s Regional Medical Center, Hangzhou 310052, China;
2. Department of Gastroenterology, the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310009, China;
3. Department of Pharmacology, School of Basic Medical Sciences, Zhejiang University, Hangzhou 310058, China
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摘要:

炎性肠病是一种慢性复发性肠道炎性疾病,尚无理想治疗方法。磷酸二酯酶(PDE)通过介导细胞内第二信使环磷酸腺苷和环磷酸鸟苷的水解影响细胞内信号级联反应,从而调控多种病理、生理过程。近年来,一系列研究结果显示,PDE抑制剂如多种PDE4抑制剂、PDE5抑制剂(西地那非、他达拉非及伐地那非)、PDE3抑制剂(西洛他唑)、PDE9抑制剂(PF-04447943)、PDE3/PDE4双抑制剂(pumafentrine)对实验性结肠炎具有改善作用;PDE4抑制剂阿普司特在临床试验中较替托司特的治疗优势更明显。本文就PDE抑制剂在炎性肠病治疗中的研究进展进行综述。

关键词: 炎性肠病磷酸二酯酶磷酸二酯酶抑制剂环磷酸腺苷环磷酸鸟苷综述    
Abstract:

Inflammatory bowel disease is a recurrent chronic intestinal inflammatory disease with unknown etiology and no effective treatment. Phosphodiesterase (PDE) regulates a variety of physiological and pathophysiological processes by mediating the hydrolysis of intracellular second messengers cyclic adenosine monophosphate and cyclic guanosine monophosphate. In recent years, a series of researches suggest that PDE inhibitors such as several PDE4 inhibitors, PDE5 inhibitors (sildenafil, tadalafil and vardenafil), PDE3 inhibitors (cilostazol), PDE9 inhibitor (PF-04447943) and PDE3/PDE4 double inhibitor (pumafentrine) have ameliorating effect on experimental colitis in animals. In clinical trials, PDE4 inhibitor apremilast showed more therapeutic advantage than tetomilast. This article reviews the recent research progress of PDE inhibitors in treatment of inflammatory bowel disease.

Key words: Inflammatory bowel disease    Phosphodiesterase    Phosphodiesterase inhibitor    Cyclic adenosine monophosphate    Cyclic guanosine monophosphate    Review
收稿日期: 2021-06-18 出版日期: 2021-12-29
:  R967  
基金资助: 国家自然科学基金(81402989); 浙江省基础公益研究计划(LGD20H010002)
通讯作者: 汤慧芳     E-mail: tanghuifang@zju.edu.cn
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史建蓉,马望前,汤慧芳. 磷酸二酯酶抑制剂治疗炎性肠病的研究进展[J]. 浙江大学学报(医学版), 2021, 50(5): 659-665.

SHI Jianrong,MA Wangqian,TANG Huifang. Research progress of phosphodiesterase inhibitors in inflammatory bowel disease treatment. J Zhejiang Univ (Med Sci), 2021, 50(5): 659-665.

链接本文:

https://www.zjujournals.com/med/CN/10.3724/zdxbyxb-2021-0170        https://www.zjujournals.com/med/CN/Y2021/V50/I5/659

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