The invention provides valerenic acid derivatives, pharmaceutical composition comprising the same and an anti-tumor application of the valerenic acid derivatives. Simple and available genipin as a natural product is taken as a raw material, structural constraint of a conventional natural extract is changed with a semisynthetic method, a series of valerenic acid derivatives with anti-tumor activity are designed and synthesized, the valerenic acid derivatives show better anti-tumor activity in in-vitro experiments, and the compounds can be applied to anti-tumor drug study through further experiments.