The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by simultaneous modification on 4-site and 7-site of brefeldin A. Particularly, the invention relates to 4,7-site difurazan NO donor substituted brefeldin A derivatives, and a preparation method of the derivatives and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.