Abstract: Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.