The invention provides a phenolic acid polypeptide conjugate as well as a preparation method and application thereof. The phenolic acid polypeptide conjugate is formed by connecting phenolic acid and polypeptide through amido bonds, wherein the phenolic acid mainly comprises gallic acid, rosmarinic acid, ferulic acid, caffeic acid, protocatechuic acid, chlorogenic acid, sinapic acid and vanillic acid; and the amino acid sequence of the polypeptide is KLVFFAED. The preparation method comprises the following steps: (1) synthesizing KLVFFAED polypeptide by using a polypeptide solid-phase synthesis method; (2) under the protection of an inert atmosphere, dissolving a phenolic acid solution, a catalyst and an alkaline reagent into DMF to be coupled and reacted with the resin, and after reaction, cutting off the polypeptide from the resin by using a cutting reagent to obtain a phenolic acid polypeptide conjugate crude product; and (3) separating, purifying and freeze-drying to obtain the phenolic acid polypeptide conjugate. Compared with unmodified phenolic acid, the phenolic acid polypeptide conjugate has the advantages that fat solubility and stability can be improved, so that the phenolic acid polypeptide conjugate can be more easily taken by cells, a targeting effect can be realized, toxic and side effects on normal cells are reduced, and a drug treatment effect is efficiently played.