摘要
利用荧光转基因斑马鱼模型筛选来源于不同药性中药的主要成分,比较其抑制血管生成的作用差异,为研发抗肿瘤新药提供先导化合物。以TG(VEGFR2:GFP)系荧光转基因斑马鱼作为筛选模型,18种来源于不同药性中药的主要成分,按照25、50、100μg/m L的药物浓度分别作用于斑马鱼胚胎,观察对斑马鱼体节间血管(ISVs)生成的影响,并进行定量分析。结果发现,18种中药成分均有不同程度的抑制斑马鱼血管生成作用,其中来源于寒性和热性中药的主要成分抑制作用比较明显,来源于平性中药的成分抑制作用比较弱,5种效果很明显的成分分别是汉防己甲素、木通皂苷D、阿魏酸、丹参酮IIA、儿茶素,且具有一定的量效关系。本研究从中药寒热药性理论的角度,探讨了来源于不同药性中药的主要成分抑制血管生成的活性,筛选出的5种中药成分,具有很明显的抑制斑马鱼体节间血管(ISVs)生成作用,可以为抗肿瘤药物的研发提供先导化合物,为抗肿瘤先导化合物的筛选提供新的思路。
In order to provide lead compounds for further research and development of anti-tumor drug,fluorescent transgenic zebrafish model was used to screen for components with anti-angiogenesis activity from traditional Chinese medicine,and to compare their effects on inhibiting angiogenesis,VEGFR2： GFP transgenic zebrafish with fluorescent blood vessels was taken as model,and zebrafish embryos were treated with 18 components from different Chinese medicine with the concentration of 25,50 and 100 μg / m L,respectively. The effects of these components were observed and quantitatively analyzed. The results showed that 18 different compositions had effects on inhibiting angiogenesis in different degrees. Those components from Chinese medicine with cold or hot natures all had significant effect,while the other ones with neutral nature have little effect. Based on the theory of nature of Chinese medicine,the effects of the active components on inhibiting angiogenesis were analyzed,and five components were screened for developing new anti-cancer drug,including tetrandrine hormone,akeboside D,ferulic acid,tanshinone IIA and catechin. This study provided a new insight into screening lead components for developing new drug with anti-cancer activity based on the theory of traditional Chinese medicine.
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2015年第6期1064-1069,共6页
Natural Product Research and Development
基金
山东省人力资源和社会保障厅博士后创新项目(201102036)
国家自然科学基金(81473369)
科学技术部国家重点基础研究发展计划("973计划")项目(2007CB512601)
科学技术部国家高技术研究发展计划("863计划")项目(2013AA093001)
关键词
抗肿瘤活性成分
抑制血管生成
中药
斑马鱼
anti-tumor active components
anti-angiogenesis
traditional Chinese medicine
zebrafish
