化合物简介
The drug aprotinin (Trasylol, previously Bayer and now Nordic Group pharmaceuticals), is the small protein bovine pancreatic trypsin inhibitor (BPTI), an antifibrinolytic molecule that inhibits trypsin and related proteolytic enzymes. Under the trade name Trasylol, aprotinin was used as a medication administered by injection to reduce bleeding during complex surgery, such as heart and liver surgery. Its main effect is the slowing down of fibrinolysis, the process that leads to the breakdown of blood clots. The aim in its use was to decrease the need for blood transfusions during surgery, as well as end-organ damage due to hypotension (low blood pressure) as a result of marked blood loss. The drug was temporarily withdrawn worldwide in 2007 after studies suggested that its use increased the risk of complications or death; this was confirmed by follow-up studies. Trasylol sales were suspended in May 2008, except for very restricted research use. In February 2012 the European Medicines Agency (EMA) scientific committee reverted its previous standpoint regarding aprotinin, and has recommended that the suspension be lifted. Nordic became distributor of aprotinin in 2012.
基本信息
中文名称
抑肽酶
英文名称
Aprotinin
中文别名
英文别名
cas9004-04-0、Trypsin Inhibitor
CAS号
9087-70-1
分子式
分子量
精确质量
PSA
LOGP
编号系统
UNII
04XPW8C0FL
生产方法及用途
生产方法
抑肽酶可以从牛胰和肺组织中提取,也可以从人尿中提取。目前国内主要从牛肺中提取。 取新鲜牛肺冲洗干净,用绞肉机绞碎。然后加入5倍体积的水,搅拌均匀,用2.5mol/L的硫酸调节pH=2.0,搅拌提取8h,然后用双层纱布过滤,滤渣重复上述步骤再提取一次,合并两次提取液。向提取液中按每升277g加入硫酸铵,搅匀,再用5mol/L的硫酸调节pH=1.5,静置过夜。吸取上清液,过滤,滤液调节pH=5.5,再按每升加255g向滤液中加入硫酸铵,搅匀,静置48h,过滤,收集盐析物。盐析物用8~10倍水溶解,4℃下静置过夜,滤去沉淀,滤液中加入50%三氯乙酸(加量为滤液的1/20),搅匀,迅速加热至80℃后速冷到30℃,滤去沉淀,再用20%的氢氧化钠调pH=3.0,然后加入硫酸铵(每升滤液加610g),搅拌溶解,静置过夜,收集盐析物。盐析物再用5倍的
用途
1.对胰蛋白酶、糜蛋白酶、凝白酶、溶血纤维蛋白酶以及各种组织或血浆激肽释放酶有广谱抑制作用。可用于治疗急性胰腺炎,并对皮肤疾患、烧伤休克及产后大出血有独特的疗效。