The invention provides sesquiterpenoids capable of reversing ABCB1-mediated
lung cancer drug resistance activity in
tripterygium wilfordii as well as a preparation method and application of the sesquiterpenoids. The method comprises the following steps: adding an
ethanol-water
solvent into a
tripterygium wilfordii root tuber for extracting by a
percolation method, concentrating an extracting solution under reduced pressure to obtain an extract, adding water for dispersing, sequentially extracting by using
petroleum ether,
ethyl acetate and n-butyl
alcohol, carrying out reduced pressure concentration on an
ethyl acetate extracting solution to obtain a dry
solid component, sequentially carrying out
gradient elution by using
petroleum ether-
ethyl acetate through
silica gel column chromatography, and carrying out vacuum concentration on the dry
solid component to obtain the
tripterygium wilfordii extract. The preparation method comprises the following steps: carrying out
gradient elution by using
methanol-water through medium-pressure ODS
column chromatography, carrying out
dichloromethane-
methanol elution through
sephadex column chromatography, collecting an eluent, carrying out
isocratic elution by using
methanol-water or
acetonitrile-water with different concentrations through semi-preparative
high performance liquid chromatography, and recovering a
solvent under reduced pressure to obtain a compound 1 and a compound 2. The method is easy to operate, the product purity is high, the method can be used for preparing the
medicine for reversing the ABCB1 mediated
lung cancer drug-resistant activity, and other medicinal values of the
tripterygium wilfordii except for the traditional anti-inflammatory effect are developed.