The invention discloses a dioxabicyclo-octane compound, a preparation method and application thereof. The invention in particular discloses a compound in a formula I, wherein R1, R2 and R3 are respectively and independently selected from H or a function as shown in formula II; R4 is selected from H or C1-4 linear and branched alkyl or pharmaceutically-acceptable solvate, hydrate, isomer, ester or pharmaceutically-acceptable salt, solvate, hydrate, isomer of the ester. The invention also discloses the extracts containing the compound, the composition containing the compound or the extracts and the preparation method of the compound and the extracts. According to the compound and the extracts, the compound in the formula I or the extracts containing the compound in the formula I can obviously restrain the secretion activity of catecholamine neurotransmitter.