The invention relates to a preparation method for two novel compounds with antitumor activity extracted from isodon excisoides and an application of the two novel compounds. The novel compounds are extracted from the isodon excisoides and are applied to the preparation of antitumor drugs. The method comprises the steps: adding water into the isodon excisoides, carrying out boiling extraction, introducing an extract sample to a macroporous adsorption resin column, and carrying out gradient elution by using water and ethanol, so as to obtain Fr. A, Fr. B, Fr. C and Fr. D; subjecting part of Fr. C to gel column chromatography and methanol-water gradient elution, so as to obtain Fr. C1, Fr. C2, Fr. C3 and Fr. C4; and subjecting part of Fr. C2 to silica-gel column chromatography and petroleum ether-acetone and methanol gradient elution, so as to obtain Fr. B1-1, Fr. B1-2, Fr. C2a, Fr. C2b, Fr. C2c and Fr. C2d, subjecting Fr. C2c to methanol recrystallization so as to obtain an acetonitrile-water for white powder as eluate, carrying out semipreparative HPLC purification, collecting chromatographic peaks at 56.4min and 61.2min, separately placing products in a solvent, and carrying out anhydrous sodium sulfate dehydrating and nitrogen gas drying-up, thereby obtaining a compound 1 and a compound 2. The preparation method provided by the invention is easy in operation, high in orienting property, high in separating rate, high in efficiency and high in product purity and can be effectively used for preparing the antitumor drugs.