The invention discloses heterocyclic matrine derivatives and preparation methods and applications thereof. Structural formulas of the heterocyclic matrine derivatives are as shown in a formula (I). Two obtained matrine derivatives have an obvious inhibition effect on tumor cells or insect cells, the technical disadvantages in the field are filled, and the matrine derivatives can be applied to research and development of anti-tumor drugs or insecticides. Therefore, a candidate compound is provided for development of novel anti-tumor matrine derivatives or matrine derivatives with insecticidal activity, and the matrine derivatives are of great significance in overall development of the medical activity and the agricultural activity of matrine. The invention further provides preparation methods of the two derivatives. Indole or cyclohexane heterocyclic ring is introduced to the 13th key of a lead compound matrine, so that the biological activity of the matrine is significantly improved; and the preparation method is mild, simple and feasible. The formula is as shown in the specification.