Disclosed is a trolox derivative-modified fat-soluble anti-cancer pharmaceutical compound having a structure as represented by formula I or II. An active moiety of the anti-cancer pharmaceutical compound, camptothecins or a camptothecin derivative, is covalently bonded to a lipophilic moiety, a trolox ester or a trolox amide, by a linking group to form the fat-soluble anti-cancer pharmaceutical compound. Also disclosed are a preparation, preparing method and use of the pharmaceutical compound.
