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, R 1 is selected from the group consisting of -OH, =O(carbonyl), H, and C 1 -C 3 alkyl; R 2 is selected from the group consisting of -OH, H, and C 1 -C 3 alkyl; R 3 is selected from the group consisting of -OH, =O, H, and C 1 -C 3 alkyl; R 4 is selected from the group consisting of -OH, H, and C 1 -C 3 alkyl; and none, one, two, three or four of R 1 , R 2 , R 3 , and R 4 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.