The invention discloses a stevioside derivative as well as a preparation method and application thereof. The stevioside derivative is a compound or pharmaceutically acceptable salt shown in a formulaI which is shown in the specification, wherein a. a sign shown in the specification represents a single bond or double bonds; b. R1, R4 and R5 are respectively independently selected from a hydrogen atom, methylene, an oxygen atom and amino alkyl having a substituent group of C1 to C10; R1 and R5 are precursor structures capable of replacing carbonyl or methylene, such as Mannich alkali and iminesalt; c. R2 and R3 are respectively independently selected from methylene, an oxygen atom, NOH, NR7, NOR8 and the like; d. R6 is selected from methyl, hydroxyl, OR9 and OCOR10; (OCO represents an ester group); e. R7, R8, R9 and R10 are respectively independently selected from hydrocarbyl of C1 to C10 (such as alkyl, a naphthenic base, alkenyl and alkynyl), aryl (such as phenyl, naphthyl replaced at any position, and all pentabasic, hexahydric and macrocyclic aromatic heterocyclic groups or various substitutional aryl), hydroxyl, carboxyl, an ester group, benzyl, metal (such as K, Na and Li) oran ion (such as NH<4+>).