The present disclosure discloses a sterol derivative, a preparation method therefor and a use thereof. The sterol derivative includes a sterol compound with Structural Formula (I) or a pharmaceutically acceptable salt thereof, or an extract containing the sterol compound, or a composition containing the sterol compound, wherein Structural Formula (I) is as follows: where R1 is &mdashOH, &boxHO, H or C1-C3 alkyl R2 is &mdashOH, H or C1-C3 alkyl R3 is &mdashOH, &boxHO, H or C1-C3 alkyl R4 is &mdashOH, H or C1-C3 alkyl, and at least one of R1, R2, R3 and R4 is &mdashOH. The compound with Structural Formula (I) can be used for preparing a drug having inhibitory effect on 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity and the prepared drug can effectively inhibit the HMG-CoA reductase activity or be used for preparing an anti-cancer drug.本發明公開了一種甾醇類衍生物及其製備方法與應用。該甾醇類衍生物包括具有結構式(I)的甾醇類化合物或其藥學上可接受的鹽、或包含其的提取物、或包含其的組合物。其中,結構式(I)如下:其中,R1為-OH、=O、H、或C1-C3烷基;R2為-OH、H、或C1-C3烷基;R3為-OH、=O、H、或C1-C3烷基;R4為-OH、H、或C1-C3烷基,且R1、R2、R3、R4中的至少一個為-OH。該具有結構式(I)的化合物能夠用以製備具有HMG-CoA還原酶活性抑制作用的藥物,且其所製備的藥物能夠有效抑制HMG-CoA還原酶活性或者用於製備具有抗癌作用的藥物。
