首页|角茴香中1个新的吡嗪类生物碱

角茴香中1个新的吡嗪类生物碱

扫码查看
采用硅胶、ODS、MCI等柱色谱以及半制备液相等现代色谱分离技术对角茴香(Hypecoum erectum L。)正丁醇萃取部位的化学成分进行分离纯化,得到4个吡嗪类生物碱。运用现代波谱学方法(1DNMR、2DNMR、UV、IR、MS 等)鉴定结构分别为 hyperectpyrazin A(1)、1'S-(6-methylpyrazin-2-yl)-ethane-1',2'-diol(2)、2-hydroxymethyl-6-methylpyrazin(3)和pyrazine-2-carboxylic acid(4)。化合物1为1个新的吡嗪类生物碱,化合物2~4为首次从角茴香中分离得到,并首次通过Mo2(OAc)4诱导的CD谱确定了化合物2的绝对构型。采用乙酰胆碱酯酶抑制模型和脂多糖诱导的RAW264。7 巨噬细胞炎症模型,对化合物1~4进行体外活性评价,其中化合物2和4表现出一定的乙酰胆碱酯酶抑制活性,在终浓度为50 μmol·L-1时对乙酰胆碱酯酶的抑制率分别为44。40%和43。99%。
A new pyrazine from Hypecoum erectum L.
Four pyrazines were isolated from the n-butanol fraction of Hypecoum erectum L.by using various chromatographic methods,including MCI gel,ODS,silica gel and semi-preparative HPLC.The structures of the isolated compounds were identified as hyperectpyrazin A(1),1'S-(6-methylpyrazin-2-yl)-ethane-1',2'-diol(2),2-hydroxymethyl-6-methylpyrazin(3)and pyrazine-2-carboxylic acid(4)by spectroscopy methods(1D NMR,2D NMR,UV,IR,MS,etc.).The absolute configuration of compound 2 was determined by using the Mo2(OAc)4 induced CD analysis for the first time.Compound 1 was a new compound,compounds 2-4 were isolated from H.erectum for the first time.Compounds 1-4 were evaluated for their inhibition against acetylcholinesterase and nitric oxide generation induced by lipopolysaccharide-RAW264.7 macrophage cells.At a concentration of 50 μmol·L-1,compounds 2 and 4 displayed inhibitory effects on acetylcholinesterase with the inhibition rates of 44.40%and 43.99%,respectively.

Hypecoum erectum L.chemical constituentpyrazineshyperectpyrazin Aacetylcholinesterase inhibitory activity

刘云、胡梦雅、张文静、范雨欣、徐瑞雯、朱登辉、孙彦君、冯卫生、陈辉

展开 >

河南中医药大学药学院,河南郑州 450046

呼吸疾病中医药防治省部共建协同创新中心,河南郑州 450046

角茴香 化学成分 吡嗪类生物碱 hyperectpyrazin A 乙酰胆碱酯酶抑制活性

国家自然科学基金

22177027

2024

药学学报
中国药学会 中国医学科学院药物研究所

药学学报

CSTPCD北大核心
影响因子:1.274
ISSN:0513-4870
年,卷(期):2024.59(1)
  • 13