红景天提取物的结构鉴定及其生物活性研究  

Structural Identification and Biological Activity of Rhodiola crenulata Extract

作　　者：聂远洋[1] 曹玫[2] 刘素君[3] 颜亮[1] 江南[2] 张单[1] 张艳[1] 黎伟[1] 杨志荣[1] 赵建[1] 

机构地区：[1]四川大学生命科学学院生物资源与生态环境教育部重点实验室,四川成都610064 [2]四川省医学科学院.四川省人民医院临床医学中心实验室,四川成都610072 [3]乐山师范学院天然产物研究所,四川乐山614004

出　　处：《时珍国医国药》2011年第8期1962-1965,共4页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(No.30801359);四川省应用基础计划项目(No.2010JY0043)

摘　　要：目的从大花红景天中分离具有生物活性的多酚类单体化合物,并进行结构鉴定和生物活性研究。方法采用有机溶剂萃取和硅胶柱层析技术,从大花红景天中分离多酚类单体化合物,通过紫外、红外光谱法和核磁共振谱法进行结构鉴定;并采用牛津杯法和打孔法研究该提取物的抗菌活性,同时采用四甲基偶氮唑盐还原法和流式细胞术研究该物质的抗肿瘤细胞活性。结果 从大花红景天中分离到一种多酚类化合物,波谱学方法鉴定该物质为3,4,5-三羟基苯甲酸(TBA)。TBA对大肠杆菌、金黄色葡萄球菌、柑橘绿霉和黑曲霉无显著抗菌活性。TBA对MGC80-3人胃癌细胞体外增殖具有显著抑制作用,且呈剂量依赖性,拟合曲线,呈线性相关,拟合回归方程为Y=0.0350X+0.0782(r=0.9522),作用48 h后IC50为12.051μg/m l;DAPI染色结果显示,TBA作用后,MGC80-3细胞核出现染色质浓缩、细胞核固缩和核碎裂等;流式细胞术结果显示,IC50的TBA作用于细胞24 h后,MGC80-3细胞的凋亡率为13.1%。结论 从大花红景天中分离的多酚类化合物TBA具有显著的抗MGC80-3人胃癌细胞活性,但对大肠杆菌、金黄色葡萄球菌、柑橘绿霉和黑曲霉无显著抗菌活性。Objective To isolate bioactive polyphenolic compound from Rhodiola crenulata,identify its structure and study its biological activity.Methods The polyphenolic compound in Rhodiola cremulata was separated and purified by using organic solvent extraction and silica gelcolumn chromatography.The structure of polyphenolic compound obtained was identified by means of UV,IR,1H NMR and 13C NMR.The antibacterial activity of polyphenolic compound obtained was studied by Oxford Cup method and Drilling method.The anti-tumor activity of polyphenolic compound obtained was studied by means of 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide（MTT） reduction method and flow cytometry.Results The structure of polyphenolic compound obtained was identified to be 3,4,5-trihydroxybenzoic acid（TBA） by spectroscopy method.TBA had no significant antibacterial activity against Escherichia coli,Staphylococcus aureus,Penicillium digitatum and Aspergillus niger.TBA had a quite high activity for inhibiting the proliferation and inducing apoptosis of MGC80-3 cells.The inhibition of proliferation of MGC80-3 cells was correlated with the concentration of TBA in vitro.The curve fitting showed that the line regression equation was Y=0.0350X＋0.0782（r=0.9522）,and the IC50 of MGC80-3 cells treated by IC50 of TBA for 24 hours was 13.1%.Conclusion TBA has significant anti-tumor activity on MGC 80-3 cells,but has no significant antibacterial activity against Escherichia coli,Staphylococcus aureus,Penicillium digitatum and Aspergillus niger.

关 键 词：红景天 核磁共振 3 4 5-三羟基苯甲酸 抗肿瘤 流式细胞术 

分 类 号：R284.1[医药卫生—中药学]