The invention relates to application of Synsepalum dulcificum leaf extract in the preparation of molecular targeting drugs; the Synsepalum dulcificum leaf extract is extracted via the steps of homogenizing and crushing Synsepalum dulcificum leaf into Synsepalum dulcificum leaf powder, ultrasonically extracting with 70-90% (v/v) ethanol solution, and centrifugally collecting supernate; distilling the supernate under reduced pressure, and lyophilizing to obtain Synsepalum dulcificum leaf crude extract; dissolving the Synsepalum dulcificum leaf crude extract in water, treating with macroporous resin, eluting with an eluent, and collecting eluant; distilling the eluant under reduced pressure, and lyophilizing to obtain Synsepalum dulcificum leaf extract powder. Molecular targeting drugs containing the Synsepalum dulcificum leaf extract are small toxic and side effects, have significant effect in resisting tumor angiogenesis and are good in safety and reliability.