国际呼吸杂志
國際呼吸雜誌
국제호흡잡지
INTERNATIONAL JOURNAL OF RESPIRATION
2012年
21期
1646-1651
,共6页
慢性阻塞性肺疾病%磷酸二酯酶4抑制剂%罗氟司特%抗炎作用
慢性阻塞性肺疾病%燐痠二酯酶4抑製劑%囉氟司特%抗炎作用
만성조새성폐질병%린산이지매4억제제%라불사특%항염작용
Chronic obstructive pulmonary disease%Phosphodiesterase 4 inhibitor%Roflumilast%Anti inflammatory effect
磷酸二酯酶4(Phosphodiesterase 4,PDE4)、特异性水解环磷酸腺苷(cyclic adenosine monophosphate,cAMP),广泛存在于多种炎症细胞及结构细胞中.选择性抑制PDE4使细胞内cAMP浓度增加,呈现抗炎作用.第二代PDE4抑制剂罗氟司特(roflumilast)具有抑制中性粒细胞、T细胞、巨噬细胞等多种炎症细胞及TNF-α、LTB4、活性氧、IFN-γ等多种炎症介质的抗炎作用,成为第一个应用于慢性阻塞性肺疾病临床治疗的PDE4抑制剂.罗氟司特的抗炎效果可能与炎症类型、药物剂量、免疫形式等影响因素有关.
燐痠二酯酶4(Phosphodiesterase 4,PDE4)、特異性水解環燐痠腺苷(cyclic adenosine monophosphate,cAMP),廣汎存在于多種炎癥細胞及結構細胞中.選擇性抑製PDE4使細胞內cAMP濃度增加,呈現抗炎作用.第二代PDE4抑製劑囉氟司特(roflumilast)具有抑製中性粒細胞、T細胞、巨噬細胞等多種炎癥細胞及TNF-α、LTB4、活性氧、IFN-γ等多種炎癥介質的抗炎作用,成為第一箇應用于慢性阻塞性肺疾病臨床治療的PDE4抑製劑.囉氟司特的抗炎效果可能與炎癥類型、藥物劑量、免疫形式等影響因素有關.
린산이지매4(Phosphodiesterase 4,PDE4)、특이성수해배린산선감(cyclic adenosine monophosphate,cAMP),엄범존재우다충염증세포급결구세포중.선택성억제PDE4사세포내cAMP농도증가,정현항염작용.제이대PDE4억제제라불사특(roflumilast)구유억제중성립세포、T세포、거서세포등다충염증세포급TNF-α、LTB4、활성양、IFN-γ등다충염증개질적항염작용,성위제일개응용우만성조새성폐질병림상치료적PDE4억제제.라불사특적항염효과가능여염증류형、약물제량、면역형식등영향인소유관.
Phosphodiesterase 4 is a cyclic adenosine monophosphate (cAMP)-specific enzyme which has a ubiquitous distribution in inflammatory and structural cells.Selective PDE4 inhibitors prevent the hydrolysis of cAMP,leading to broad spectrum anti-inflammatory effects.Among these drugs,the second-generation PDE4 inhibitor Roflumilast was the first to be developed and approved for market (in Europe and USA) as a COPD therapy.Roflumilast demonstrated great suppressing effects on a wide range of inflammatory cells,such as neutrophils,T lymphocytes,macrophages,eosinophils,and also on a variety of inflammatory mediators,such as TNF-α,LTB4,IFN-γ and reactive oxygen species.The anti inflammatory effect of roflumilast may be related to the inflammatory type,drug dose and immune form.
