Abstract: Disclosed in the present invention are a lignan derivative, a preparation method therefor and the use thereof. The structure of the lignan derivative is as shown in a formula I, wherein in the formula, the definition of each substituent is as described in the description and claims. The lignan derivative of the present invention can be used as an inhibitor of mitochondrial respiratory chain complex I to inhibit mitochondrial oxidative phosphorylation and ATP generation, and can also be used for preventing and/or treating diseases associated with the elevated activity or expression of the mitochondrial respiratory chain complex I or enhanced mitochondrial oxidative phosphorylation.