The invention relates to the field of medicine, and discloses a gelsemic acid derivative shown as a general formula (I) and a preparation method and an application thereof. In the prepration method, the compound shown as the general formula I is obtained by reacting substituted aminophenylacetyl chloride with 7-hydroxyl-6-herniarin. As proved by a pharmacological experiment, the compound shown as the general formula (I) has antitumor activity.