伊犁贝母的化学成分研究

目的研究伊犁贝母Fritillariapallidiflora中的化学成分。方法运用柱色谱方法进行分离纯化,结合波谱技术与理化常数鉴定化合物结构。结果从伊犁贝母95%乙醇提取物中分离得到了16个化合物,包括酚酸类、酯类、生物碱类等,分别鉴定为1,4-联苯基丁烷(1)、顺式肉桂酸(2)、4-羟基-3-甲氧基苯甲醛(3)、香草乙酮(4)、油酸甲酯(5)、阿魏酸甲酯(6)、1-O-阿魏酸甘油(7)、反式异阿魏酸(8)、丁香脂素(9)、松脂醇(10)、2,3-O-二阿魏酸甘油(11)、1,3-O-二阿魏酸甘油(12)、环(L-脯-L-丙)二肽(13)、环(L-亮-L-缬)二肽(14)、双(二乙二醇)邻苯二甲酸酯(15)、环(苯丙-缬)二肽(16)。结论所有化合物均为首次从伊犁贝母中分离得到,其中化合物1、3～8、10～13、15、16为该属植物中首次分离得到。     

热毒宁注射液化学成分研究(Ⅳ)

目的对中药复方热毒宁注射液的解热抗炎活性成分进行研究。方法采用脂多糖(LPS)诱导小鼠内毒素休克模型对热毒宁注射液解热抗炎活性部位进行筛选,综合应用HP-20大孔树脂、硅胶、MCI、ODS和Sephadex LH-20柱色谱以及反相MPLC、HPLC等各种现代色谱技术对解热抗炎活性部位进行系统地分离纯化,根据化合物的光谱数据和理化性质进行结构鉴定。结果经活性筛选,热毒宁注射液经大孔吸附树脂95%乙醇洗脱部位为解热抗炎活性部位,从中分离鉴定了14个化合物,分别鉴定为邻苯二甲酸二丁酯(1)、异香草酸(2)、香草乙酮(3)、苯丙酸(4)、京尼平苷(5)、jasmigeniposide B(6)、京尼平苷酸(7)、京尼平龙胆二糖苷(8)、6″-O-反-对香豆酰基京尼平龙胆二糖(9)、6″-O-反-阿魏酰基京尼平龙胆二糖苷(10)、6″-O-反-芥子酰基京尼平龙胆二糖苷(11)、jasmigeniposide A(12)、6″-O-反-桂皮酰基京尼平龙胆二糖苷(13)、2′-O-反-咖啡酰基栀子新苷(14)。结论化合物1~4、13均为首次从热毒宁注射液中分离得到;经UPLC定性分析及文献对照,化合物5、7~13均为来源于栀子中的化学成分。     

Alpha-lipoic acid decreases thiol reactivity of the insulin receptor and protein tyrosine phosphatase 1B in 3T3-L1 adipocytes

Alpha-lipoic acid is known to increase insulin sensitivity in vivo and to stimulate glucose uptake into adipose and muscle cells in vitro. In this study, alpha-lipoic acid was demonstrated to stimulate the autophosphorylation of insulin receptor and glucose uptake into 3T3-L1 adipocytes by reducing the thiol reactivity of intracellular proteins. To elucidate mechanism of this effect, role of protein thiol groups and H(2)O(2) in insulin receptor autophosphorylation and glucose uptake was investigated in 3T3-L1 adipocytes following stimulation with alpha-lipoic acid. Alpha-lipoic acid or insulin treatment of adipocytes increased intracellular level of oxidants, decreased thiol reactivity of the insulin receptor beta-subunit, increased tyrosine phosphorylation of the insulin receptor, and enhanced glucose uptake. Alpha-lipoic acid or insulin-stimulated glucose uptake was inhibited (i) by alkylation of intracellular, but not extracellular, thiol groups downstream of insulin receptor activation, and (ii) by diphenylene iodonium at the level of the insulin receptor autophosphorylation. alpha-Lipoic acid also inhibited protein tyrosine phosphatase activity and decreased thiol reactivity of protein tyrosine phosphatase 1B. These findings indicate that oxidants produced by alpha-lipoic acid or insulin are involved in activation of insulin receptor and in inactivation of protein tyrosine phosphatases, which eventually result in elevated glucose uptake into 3T3-L1 adipocytes.