The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R1 is selected from the group consisting of -OH, =O(carbonyl), H, and C1-C3 alkyl; R2 is selected from the group consisting of -OH, H, and C1-C3 alkyl; R3 is selected from the group consisting of -OH, =O, H, and C1-C3 alkyl; R4 is selected from the group consisting of -OH, H, and C1-C3 alkyl; and none, one, two, three or four of R1, R2, R3, and R4 are -OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cellsand lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.