北豆根根茎中生物碱类化学成分及其生物活性研究

摘要

目的:对北豆根根茎中的生物碱类化合物进行分离、结构鉴定及抗炎活性研究.方法:将药材北豆根干燥,粉碎,用HCl水溶液(pH 3.0)渗漉提取.提取液调节pH至7.0,减压回收得干浸膏,过碱性硅胶柱色谱、ODS柱色谱富集得到生物碱部位.以甲醇-水为流动相,用高效液相色谱对生物碱部位进行分离纯化.对得到的单体化合物,运用NMR、ESIMS等多种谱学技术进行结构鉴定.结果:从北豆根根茎中分离鉴定了10个生物碱化合物,分别为阿普菲类生物碱lakshminine(1),telazoline(2),daurioxoisoporphine A(3),daurioxoisoporphine B(4),吗啡烷类生物碱scrodentoside A(5),双苄基异喹啉类生物碱(-)-1,3,4-dehydrocepharanthine(6),(+)-1,3,4-dehydrocepharanthine-2′β-N-oxide(7),cissampentine A(8),cissampentine B(9)和(-)-pseudocurine(10).体外抗炎活性研究表明,化合物6,8,9和10具有抑制大鼠巨噬细胞一氧化氮生成的作用,IC50分别为6.0、12.0、8.5、9.7 μmol·L-1.结论:生物碱化合物1~10均首次从该植物中获得.%Objective:To study the chemical structures and anti-inflammatory activity of alkaloids from Menispermum dauricum.Methods:The dried rhizome of M. dauricum were powdered and percolated with HCl(pH 3.0).The extract was concentrated under reduced pressure after adjusted to pH 7.0 and subjected to alkaline silica gel and ODS column chromatogra-phies to obtain alkaloids portion.The alkaloid-containing portion was purified by preparative HPLC,using MeOH-H2O as the mobile phase.The structures were identified by extensive spectroscopic analyses,including ESIMS and NMR.Results:Ten al-kaloids were isolated from the plant and identified as lakshminine(1),telazoline(2),daurioxoisoporphine A(3),daurioxoi-soporphine B(4),scrodentoside A(5),(-)-1,3,4-dehydrocepharanthine(6),(+)-1,3,4-dehydrocepharanthine-2′β-N-oxide(7),cissampentine A(8),cissampentine B(9),and(-)-pseudocurine(10).Compounds 6,8,9,and 10 exhib-ited anti-inflammatory activities in vitro,with IC50values of 6.0,12.0,8.5,and 9.7 μmol·L-1,respectively. Conclusion:Compounds 1-10 were obtained from the rhizomes of M.dauricum for the first time.