防治心脑血管疾病药物——灯盏细辛酚的研究与开发

灯盏细辛是著名的传统中药，全草用于治疗脑血管病中风及其后遗症偏瘫有良好疗效的中药材。自20世纪80年代，已开发了两种制剂（片剂和注射剂）在临床上用于治疗脑栓塞、脑血栓形成、脑血栓引起的瘫痪、冠心病、心绞痛、急性肾功能衰退以及肾变病综合症等。在临床上有很好疗效。为此，灯盏细辛已收载于2005年版《中华人民共和国药典》一部。自1992年始，我们再次对灯盏细辛的化学和活性成分进行了深入研究，发现了一系列二咖啡酰基奎宁酸酯类化合物同样为其主要活性成分，这些酚性成分为：1,5-，3,5-和4,5-二咖啡酰基奎宁酸和飞蓬酯乙等。为此，我们研发了包括灯盏乙素和上述系列酚类化合物为有效部位的、名"灯盏细辛酚"的注射液。已于2007年7月完成III期临床研究，正在申请新药证书。经临床研究表明，与同类药物相比是起效快、对重症病人疗效尤为显著、总有效率达98%以上的，有效成分清楚，质量可控，疗效确切的新一代制剂。

A Drug for Treating Cardio-Cerebrovascular Diseases——Phenolic Compds of Erigeron breviscapus

Erigeron breviscapus (Vant.) Hand.-Mazz. (compositae) is a well known drug as traditional Chinese medicine. The whole herb is used to treat a variety of paralysis and its sequelae originated from apoplexy and atherothrombotic of brain. Two kinds of drugs (injection liquid and tablets) developed from this medicine have been used in clinic for the cerebral embolism, cerebral thrombosis, paralysis arisen from cerebral embolism, coronary heart disease, angina pectoris, acute rend function failure, and nephritic syndrome etc., since 1980s. It has been collected in "Pharmacopoeia of P. R. China(2005) ". Our research group have reinvestigated and recognized the chemical and bioactive constituents from E. breviscapus since 1992. As the results, we found a series of phenolic compds, such as, 1,5-, 3,5- and 4,5-dicarffeoylquinic esters, and erigoster A and B, which also possessed same bioactivities with sculellarin isolated and identified by Guan and Zhang^4,5] in 1980s. Based on the above investigation, the new drug "Injection of Dengzhanxixin phenols" developed by our research team has completed phase III clinical trial in June 2007. The production certificate is in application. This new drug, with clear bioactive ingredient composition, well-controlled quality, solid therapeutic effect, and complete intellectual property, is believed as new generation drug in the treatment of brain and heart vas related diseases. Contens
1 Introduction
2 Medicinal history of Erigeron breviscapus
3 Bioactive ingredient composition of E. breviscapus
4 Investigation of the pharmacology and toxicology of Dengzhanxixin phenols
5 Comprehensive analysis and appraisal
6 Brief summary