化学学报 ›› 2011, Vol. 69 ›› Issue (15): 1795-1802. 上一篇    下一篇

研究论文

附子配伍过程中二萜类生物碱在Caco-2小肠吸收细胞模型中吸收转运的UPLC/MS研究

韩天娇1,3, 宋凤瑞1, 刘忠英2, 皮子凤*,1, 刘志强*,1, 刘淑莹1   

  1. (1中国科学院长春应用化学研究所 长春 130022)
    (2吉林大学药学院 长春 130021)
    (3中国科学院研究生院 北京 100039)
  • 投稿日期:2011-01-26 修回日期:2011-03-01 发布日期:2011-03-28
  • 通讯作者: 刘志强 E-mail:liuzq@ciac.jl.cn

Studies of the Intestinal Transport of the Diterpenoid Alkaloids in the Aconitum carmichaeli Combined with Different Medicinal Herbs in a Caco-2 Cell Culture System with UPLC/MS

Han Tianjiao1,3; Song Fengrui1; Liu Zhongying2; Pi Zifeng*,1; Liu Zhiqiang*,1; Liu Shuying1   

  1. (1 Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022)
    (2 School of Pharmacy, Jilin University, Changchun 130021)
    (3 Graduate School of the Chinese Academy of Sciences, Beijing 100039)
  • Received:2011-01-26 Revised:2011-03-01 Published:2011-03-28

利用Caco-2细胞单层模型和超高效液相色谱-三重四极杆电喷雾质谱联用方法, 考察附子中乌头类生物碱提取物的跨膜转运. 在相同浓度的附子乌头类生物碱溶液中, 加入干姜、甘草、半夏及浙贝母的水提物(折合药材质量比例为1∶1), 系统考察了加入前后的表观渗透系数(Papp). 结果表明, 加入配伍药材后附子中11种二萜类生物碱的Papp发生了明显的变化. 干姜、甘草和半夏水提物的加入能够明显地降低二萜类生物碱在小肠中的生物利用度, 尤其抑制其中毒性较大的双酯型生物碱的生物利用度|而浙贝母的水提物却在促进吸收和抑制外排两个方面共同作用, 使二萜类生物碱的生物利用度明显增加.

关键词: Caco-2单层细胞, UPLC/MS, 二萜类生物碱, 附子, 甘草, 干姜, 半夏, 浙贝母

A UPLC/MS method has been established to analyze the diterpenoid alkaloids transportation in the Aconitum carmichaeli with the Caco-2 cell monolayer. Different combination herbs water extracts including Radix Glycyrrhizae, Rhizoma Zingiberis, Rhizoma Pinelliae or Bulbus Frltillariae Thunbergii have been mixed with the same concentration of the Aconitum carmichaeli alkaloids extract solution. The mixing ratio was converted into their medicinal herbs mass of 1 to 1. The results demonstrated that the bioavailability of the diterpenoid alkaloids especially the diester-diterpenoid alkaloids has been decreased by the adding of the Radix Glycyrrhizae, Rhizoma Zingiberis or Rhizoma Pinelliae extracts, which are the most toxicity compounds in the Aconitum carmichaeli. However, the bioavailability of the diterpenoid alkaloids in the absorption and efflux has been increased by the adding of the Bulbus Frltillariae Thunbergii extract, respectively.

Key words: Caco-2 cell monolayer, UPLC/MS, diterpenoid alkaloids, Aconitum carmichaeli, Radix Glycyrrhizae, Rhizoma Zingiberis, Rhizoma Pinelliae, Bulbus Frltillariae Thunbergii