Effects of Artesunate on Tracheal Smooth Muscle from the Guinea-pig  

作　　者：Mao－ShengYang Jian－ChuXiao 

机构地区：[1]DepartmentofPharmacology,SunYat－senUniversityofMdeicalSciences,Guangzhou510089 [2]DepartmentofPharmacolo

出　　处：《Journal of Chinese Pharmaceutical Sciences》1997年第4期228-229,共2页中国药学（英文版）

摘　　要：Artesunate is a derivative of qinghaosu, with a sesquiterpene structure. The specific action and the clinical uses of artesunate are on the preliminary stage. On the one hand, artesunate has specific action of both antiinflammation and antivirus, and also has protective effect on the pulmonary alveolar macrophages, which may be advantageous to the treatment of the airway non specific inflammation of asthma. On the other hand, qinghaosu has the activities to relax vascular smooth muscle and to cause hypotension. The expectorant action, the antitussive action and the antiasthmatic action of qinghaosu were reported. Artesunate may also have antiasthmatic activity, because the antimalarial potency of artesunate is stronger than that of qinghaosu, and Artesunate can block Ca 2+ influx by inhibiting calcium dependent chloride current. The main aims of this paper are to investigate the site, the mode, and the mechanism of artesunate action on isolated tracheal smooth muscle from the guinea pig. The isolated tracheal smooth muscle and isolated aortic strip circle were suspended in 10 ml Thornton and 5 ml Krebs solution gassed with 95% O 2+5% CO 2 at 37℃ respectively, and stretched with an initial tension of 1.5 g. After a stabilization period of over two hours, drug effects were plotted from cumulative doses. The tension changes were recorded by a forcedisplacement transducer connected to a two pen recorder (XWTD 264 made in Shanghai Dahua Apparatus Factory). Our experiments on isolated tracheal smooth muscle have demonstrated that artesunate is able to relax tracheal smooth muscle by its action on the tracheal smooth muscle cells. In concentrations ranging from 10 pmol·L 1 to 100 nmol·L 1 , artesunate can reduce the tone of the trachea in a concentration dependent manner. Its pD 2 is 8.76±0.74 (epithelium removed, n=6) and its potency is seventy four percent of isoprenaline′s. Artesunate is able to antagonize noncompetitively the effects of spasmogens like acetylcholine and histaminＥｆｅｃｔｓｏｆＡｒｔｅｓｕｎａｔｅｏｎＴｒａｃｈｅａｌＳｍｏｏｔｈＭｕｓｃｌｅｆｒｏｍｔｈｅＧｕｉｎｅａｐｉｇＰｏｓｔｇｒａｄｕａｔｅ∶ＭａｏＳｈｅｎｇＹａｎｇＳｕｐｅｒｖｉｓｏｒ∶ＡｓｏｃｉａｔｅＰｒｏｆ．ＪｉａｎＣｈｕＸｉａｏＤｅｐａ...

关 键 词：Artesunate ester Tracheal smooth muscle ACETYLCHOLINE HISTAMINE Potassium chloride Cyclic AMP 

分 类 号：R965[医药卫生—药理学] R974.3[医药卫生—药学]