口腔疾病防治 ›› 2021, Vol. 29 ›› Issue (3): 198-201.doi: 10.12016/j.issn.2096-1456.2021.03.010

• 综述 • 上一篇    下一篇

氯喹/羟氯喹的作用机制及其在口腔疾病中的应用

林琳(),吴开慧,王文梅()   

  1. 南京大学医学院附属口腔医院,南京市口腔医院口腔黏膜病科,江苏 南京(210008)
  • 收稿日期:2020-05-07 修回日期:2020-07-03 出版日期:2021-03-20 发布日期:2021-01-12
  • 通讯作者: 王文梅 E-mail:lin.09.11@163.com;wangwenmei0102@163.com
  • 作者简介:林琳,医师,硕士,Email:lin.09.11@163.com
  • 基金资助:
    国家自然科学基金(81570978)

The mechanism of chloroquine/hydroxychloroquine and its application in stomatological diseases

LIN Lin(),WU Kaihui,WANG Wenmei()   

  1. Department of Oral Mucosa Disease, Nanjing Stomatological Hospital, Medical School of Nanjing University, Jiangsu Nanjing 210008, China
  • Received:2020-05-07 Revised:2020-07-03 Online:2021-03-20 Published:2021-01-12
  • Contact: Wenmei WANG E-mail:lin.09.11@163.com;wangwenmei0102@163.com
  • Supported by:
    National Natural Science Foundation of China(81570978)

摘要:

氯喹/羟氯喹同为4-氨基喹啉类的经典抗疟药物,两者化学结构相似,作用机制相近,由于羟氯喹的毒性和副作用低于氯喹,目前临床应用以羟氯喹为主,具有良好的有效性与安全性。氯喹和羟氯喹因具有免疫抑制、抗炎、抗病毒、抗肿瘤、光保护等作用而在临床中应用广泛。氯喹/羟氯喹免疫抑制作用的主要机制包括:抑制溶酶体活性和自噬;抑制免疫反应的信号通路;抑制促炎细胞因子的产生。氯喹具有稳定溶酶体膜,减少溶酶体酶释放的作用;同时其作为前列腺素拮抗剂,减少前列腺素及白三烯的生成,从而发挥抗炎作用。氯喹/羟氯喹可通过抑制病毒血管紧张素转化酶2受体糖基化,在病毒复制的早期阶段抑制增殖,发挥抗病毒的作用。目前发现羟氯喹在盘状红斑狼疮、口腔扁平苔藓、慢性唇炎、落叶型天疱疮、干燥综合征等口腔疾病中均有显著疗效,然而眼部损害是羟氯喹最需关注的不良反应,其发生与药物的累积剂量有关。

关键词: 氯喹; 羟氯喹; 免疫抑制; 口腔疾病; 盘状红斑狼疮; 口腔扁平苔藓; 慢性唇炎; 落叶型天疱疮; 副作用

Abstract:

Chloroquine and hydroxychloroquine are both classic 4-aminoquinoline antimalarial drugs with similar chemical structures and mechanisms of action. As the toxicity and side effects of hydroxychloroquine are lower than those of chloroquine, hydroxychloroquine is the main clinical application at present, with good efficacy and safety. Chloroquine and hydroxychloroquine are widely used in the clinic because of their immunosuppressive, anti-inflammatory, antiviral, antitumor and photoprotective effects. The main mechanisms by which chloroquine/hydroxychloroquine inhibits immunity include inhibiting lysosome activity, autophagy, immune response signaling pathways production of proinflammatory cytokines. Chloroquine stabilizes the lysosomal membrane and reduces the release of lysosomal enzymes. As a prostaglandin antagonist, chloroquine can reduce the production of prostaglandins and leukotrienes, thus playing an anti-inflammatory role. Chloroquine/hydroxychloroquine can inhibit virus proliferation in the early stage of virus replication by inhibiting the glycosylation of the angiotensin converting enzyme 2 receptor. At present, hydroxychloroquine has been found to have significant efficacy in discoid lupus erythematosus, oral lichen planus, chronic cheilitis, pemphigus foliaceus, Sj?gren’s syndrome and other stomatological diseases. However, eye damage is the most important adverse reaction of hydroxychloroquine, and its occurrence is related to the cumulative dose of drugs.

Key words: chloroquine; hydroxychloroquine; immunosuppression; stomatological diseases; discoid lupus erythematosus; oral lichen planus; chronic cheilitis; pemphigus foliaceus; side effects

中图分类号: 

  • R78