Doxofylline is a methylxanthine bronchodilator used to treat asthma, COPD and bronchospasm, whiel the anti-asthmatic effects are mediated primarily through inhibiting the activities of the phosphodiesterase (PDE) enzyme.
Doxofylline is an orally active inhibitor of phosphodiesterase IV (PDE IV) and an antagonist of the A1 adenosine receptor (A1AR). It is recognized for its anti-inflammatory effects on epithelial cells by inhibiting mitochondrial reactive oxygen species (ROS) production and improving various cellular pathways, such as the NLRP3-TXNIP inflammasome pathway. Doxofylline is particularly relevant for research into asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm[1].[2].[3].
体内研究
In mice, intraperitoneal injections of Doxofylline at doses of 0.3 and 1 mg/kg effectively inhibit LPS-induced pulmonary inflammation[2].
A pre-treatment dose of 0.3 mg/kg also significantly reduces cellular adhesion to vascular tissue and suppresses the expression of ICAM-1 induced by LPS in vivo[2].
体外研究
In vitro, Doxofylline demonstrates significant anti-inflammatory activity in 16HBE epithelial cells. At concentrations of 5 and 10 µM over 48 hours, it effectively reduces the levels of prostaglandin E2 (PGE2), nitric oxide (NO), and mitochondrial ROS, which are induced by lipopolysaccharide (LPS)[1].
Doxofylline also decreases the expression of NADPH oxidase subunits and TXNIP in these cells, further suppressing inflammation[1].
Additionally, Doxofylline inhibits the activation of the NLRP3 inflammasome and the secretion of inflammatory cytokines IL-1β and IL-18, and mitigates the reduction of SIRT1 caused by LPS exposure[1].
In experimental models using bone marrow (BM) cells, Doxofylline markedly reduces leukocyte migration induced by fMLP (Formyl-Methionyl-Leucyl-Phenylalanine) at concentrations ranging from 0.1 to 10 µM within a short exposure time of 15 minutes[2].
China, Anhui
... 展开 >> Suzhou municipal hospital
Suzhou, Anhui, China
China, Hebei
the second hospital of Hebei medcial university
Shijiazhuang, Hebei, China
China, Henan
Henan Province Hospital of Traditional Chinese Medicine
Zhengzhou, Henan, China
China, Liaoning
Jinzhou central hospital
Jinzhou, Liaoning, China 收起 <<
Turkey
... 展开 >> Cukurova University Faculty of Medicine, Chest Diseases Department
Adana, Turkey
Health Sciences University, Sureyyapasa Chest Diseases and Thoracic Surgery Training and Research Hospital
Istanbul, Turkey 收起 <<
China, Anhui
... 展开 >> Suzhou municipal hospital
Suzhou, Anhui, China
China, Hebei
the second hospital of Hebei medcial university
Shijiazhuang, Hebei, China
China, Henan
Henan Province Hospital of Traditional Chinese Medicine
Zhengzhou, Henan, China
China, Liaoning
Jinzhou central hospital
Jinzhou, Liaoning, China 收起 <<
Turkey
... 展开 >> Cukurova University Faculty of Medicine, Chest Diseases Department
Adana, Turkey
Health Sciences University, Sureyyapasa Chest Diseases and Thoracic Surgery Training and Research Hospital
Istanbul, Turkey 收起 <<
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