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Heparin, a potential blood anti-coagulant, is also known for its binding ability to several kinds of proteins, inter alia angiogenic factors, through electrostatic interactions due to its polyanionic character.In order to improve the therapeutic effects and overcome the potential side effect of geparin as a potential blood anti-coagulant, low molecular weight heparin (LMWH) was conjugated to ursolic acid (UA) by binding the amine group of aminoethyl UA (UA-NH2) with the carboxylic groups of LMWH.The resulting conjugate showed reduced anticoagulant activity and could self-assemble into nanomicelles with a mean particles size of~ 200 nm.In vitro endothelial tubular formation assay and in vivo Matrigel plug assay were performed to verify the anti-angiogenic potential of LHU nanomicelles.Meanwhile, the antitumor effect of LHU nanomicelles was also evaluated using the in vivo model of B16-F10 melanoma.LHU nanomicelles were shown to inhibit angiogenesis in vitro and in vivo.In addition, the i.v.administration of LHU nanomicelles to the B16-F10 tumor-bearing mice resulted in a significant inhibition of tumor growth due to its anti-angiogenic effect which was evidenced by lower expression of CD31.These findings demonstrate the therapeutic potential of LHU nanomicelles as a new therapeutic remedy for cancer therapy.