石上柏化学成分及生物活性的研究  

Chemical constituents from Selaginella doederleinii and their bioactivities

作　　者：赵倩[1] 王彩霞[1] 李艳玲[1] 刘翠艳[1] 容彦华[1] 

机构地区：[1]石药集团中奇制药技术(石家庄)有限公司,河北石家庄050035

出　　处：《中草药》2013年第23期3270-3275,共6页Chinese Traditional and Herbal Drugs

基　　金：科技部"十一五"重大新药创制(2008ZX09401-004)

摘　　要：目的研究石上柏Selaginella doederleinii的化学成分及其生物活性。方法采用硅胶柱色谱、Sephadex LH-20柱色谱、反相C18柱色谱等分离纯化,利用理化性质和波谱学数据鉴定化合物结构。并对醋酸乙酯部位进行体内外抑制肿瘤细胞的活性测试。结果从石上柏醋酸乙酯部位中分离得到11个化合物,分别鉴定为穗花杉双黄酮(1)、粗贝壳杉黄酮4′-甲醚(2)、5,5″,7,7″,4′,4′′′-六羟基(2′,8″)双黄酮(3)、7,4′,7″,4′′′-四甲氧基穗花杉双黄酮(4)、5,5″,7,7″,4′,4′′′-六羟基(2′,6″)双黄酮(5)、银杏双黄酮(6)、异银杏双黄酮(7)、槲皮素-3-O-α-D-阿拉伯糖苷(8)、川陈皮素(9)、没食子酸(10)、莽草酸(11);从正丁醇部位中分离得到2个生物碱,分别鉴定为小檗碱(12)、巴马汀(13)。体外药理研究表明石上柏醋酸乙酯部位能显著抑制HeLa与HepG2细胞的生长,IC50分别为0.12 mg/mL和0.60 mg/mL。体内实验表明醋酸乙酯部位对S180荷瘤小鼠抑瘤率为43%。结论化合物5为一新天然产物,化合物3、6～10、12、13为首次从该植物中分离得到。Objective To study the chemical constituents from Selaginella doederleinii and their bioactivities. Methods Column chromatography on silica gel, RP-C18, and Sephadex LH-20 columns was used to separate and purify the chemical constituents. The structures were elucidated by physicochemical properties and spectroscopic analyses. The inhibition of EtOAc fraction on the tumor cells was tested in vivo and in vitro. Results Eleven compounds were obtained from EtOAc fraction and identified as flavonoids and phenolic acids. These compounds were asamentoflavone （1）, robustafavone 4＇-methyl ether （2）, 5, 5＂, 7, 7＂, 4＇, 4＇＂-hexahydroxy-（2＇, 8＂）-biflavone （3）, 7, 4＇, 7＂, 4＇＂-tetra-O-amentoflavone （4）, 5, 5＂, 7, 7＂, 4＇, 4＇＂-hexahydroxy-（2＇, 6＂）-biflavone （5）, ginkgetin （6）, isoginkgetin （7）, quercetin-3-O-a-D-arabinfuranosi （8）, nobiletin （9）, gallic acid （10）, and shikimic acid （11）. Two alkaloids, berberine （12） and palmatine （13） were obtained from n-BuOH fraction. The bioassays indicated that EtOAc fraction could inhibit the growth of HeLa and HepG2 in vitro with ICs0 values of 0.12 and 0.60 mg/mL, respectively. The tumor-inhibition rate in S180-bearing mice was 43%. Conclusion Compound 5 is a new natural product, and compounds 3, 6--10, 12, and 13 are isolated from the plant for the first time

关 键 词：石上柏 5 5” 7 7” 4’ 4-六羟基(2’ 6”)双黄酮 银杏双黄酮 没食子酸 巴马汀 

分 类 号：R284.1[医药卫生—中药学]