摘要
为肿瘤特异性药物研制提供参考,以40种中药材总生物碱提取物及12种天然viridin类似物为材料,使用体外激酶测定方法评估化合物对PI3K的抑制强度,通过使用基于萤光素酶的发光测定法测量激酶反应后产生ADP的量来确定PI3K酶活性,以寻求天然的磷脂酰肌醇3-激酶(PI3K)高活性的抑制剂。结果表明:槲寄生、马齿苋、粉防己、大青叶和川芎的总生物碱提取物及化合物12(Wortmannine C)具有明显的PI3K抑制活性,其抑制率分别为81.0%、80.8%、80.7%、86.6%、77.5%和74%,其IC50在0.1~20.6μg/mL。其余的植物总生物碱及天然化合物无显著的抗PI3K活性。
12 natural viridian analogs and 40 total alkaloid extracts from 40 traditional Chinese medicinal materials were used to detect their inhibition strength against phosphatidylinositol 3-kinase(PI3K)by an vitro kinase assay and the activity of PI3K enzyme was determined by measuring ADP amount produced from kinase reaction by means of luciferase-based luminescence assay to provide a refereace for development of tumor-specific drugs and screen inhibitors with higher activity against PI3K.Result:The inhibition rate of total alkaloid extracts from Viscum coloratum,Portulaca oleracea,Stephania tetrandra,Isatis indigotica and Ligusticum chuanxiong and Compound 12(Wortmannine C)against PI3K is 81.0%,80.8%,80.7%,86.6%,77.5%and 74%respectively and the IC 50 is 0.1-20.6μg/mL.Other tested total alkaloid extracts and natural compounds all have no significant anti-PI3K activity.
作者
杨立军
杨中铎
YANG Lijun;YANG Zhongduo(College of Life Science and Engineering,Lanzhou University of Technology,Lanzhou,Gamsu 730050,China)
出处
《贵州农业科学》
CAS
2019年第7期127-130,共4页
Guizhou Agricultural Sciences
基金
国家自然科学基金项目“踝节菌属真菌中具有PI3K抑制活性的新型Viridin类似物的高通量发现研究”（21762027）
