穿心莲总内酯的NO抑制活性研究  

Study on NO Inhibitory Activity of Total Lactones from Andrographis paniculata

作　　者：徐芳芳[1,2] 金治全[2,3] 石伟[1,3] 马毅敏[2,3] 周军[2,3] 王振中[2,3] 毕宇安[2,3] 王智民[3] 萧伟[2,3] 

机构地区：[1]南京中医药大学药学院,南京210000 [2]江苏康缘药业股份有限公司,连云港222001 [3]中药制药过程新技术国家重点实验室,连云港222001

出　　处：《世界科学技术-中医药现代化》2015年第5期1061-1065,共5页Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology

基　　金：科学技术部国家重点基础研究发展计划(973计划)(2012CB724001):基于释药动力学的多组分缓控释给药体系的评价方法研究;负责人:王智民

摘　　要：目的:考察穿心莲总内酯对巨噬细胞释放一氧化氮的抑制作用。方法:以脂多糖(LPS)刺激小鼠巨噬细胞RAW264.7建立体外炎症模型,采用Griess Reagent法检测细胞培养上清一氧化氮(NO)含量并计算抑制率,通过MTT法评价细胞毒性。结果:穿心莲总内酯在5-50μmol·L-1浓度范围内对LPS诱导的小鼠巨噬细胞RAW264.7释放的NO具有明显的抑制作用,并呈现良好的剂量依赖关系,IC50分别为8.58μmol·L-1,11.52μmol·L-1,8.94μmol·L-1;其主要活性成分穿心莲内酯(5-60μmol·L-1)、脱水穿心莲内酯(5-100μmol·L-1)、新穿心莲内酯(5-100μmol·L-1)对LPS诱导的小鼠巨噬细胞RAW 264.7释放的NO亦表现出抑制作用,并呈现良好的剂量依赖关系,其IC50分别为17.54μmol·L-1,49.54μmol·L-1,41.80μmol·L-1。结论:穿心莲总内酯的NO抑制作用优于三个单体,以上结果可为穿心莲总内酯的制剂开发及临床应用提供一定的理论基础及科学依据。This study was aimed to explore the suppression of nitric oxide（NO） production in RAW264.7 cells by total lactones fraction from Andrographis paniculata. The inflammatory model in vitro was established by stimulating the RAW264.7 cells with lipopolysaccharide（LPS）. The NO production and inhibitory rate were determined by Griess assay. Cytotoxicity was evaluated by MTT method. The results showed that total lactones fraction of A. paniculata suppressed NO production in a concentration-dependent manner in the concentration range from 5 to 50 μmol·L^-1 and their IC50 values were 8.58 μmol·L^-1, 11.52 μmol·L^-1 and 8.94 μmol·L^-1, respectively. In this condition, major constituents were andrographolide（5-60 μmol·L^-1）, dehydroandrographolide（5-100 μmol·L^-1） and neoandrographolide（5-100 μmol·L^-1） inhibited NO production in a dose-dependent manner with an IC50 values of 17.54 μmol·L^-1, 49.54 μmol·L^-1 and 41.80 μmol·L^-1, respectively. It was concluded that the NO inhibitory activity of total lactones from A. paniculata was better than three active ingredients, which may be able to provide a theoretical foundation and scientific basis for the preparation and clinical application of total lactones fraction from A. paniculata.

关 键 词：穿心莲 总内酯 穿心莲内酯 一氧化氮 抑制率 

分 类 号：R285[医药卫生—中药学]