[Bone targeting of antitumor conjugate phenamine acid aryolysine-hexanedioic acid bridge grafting-bisphosphonates].
OBJECTIVE
To develop a new bone targeting antitumor therapy system which uses diphosphonate and bone-seeking nuclide to enhance the coordinated effects of chemotherapy and radiotherapy on bones, and to validate the targeting of the new therapy system in vitro and in vivo.


METHODS
Phenamine acid caryolysine was connected to bisphosphonates, and then combined with radioactive nuclide 153Sm to establish a new bone targeting chemotherapeutic and radioactive drug for bone cancers. The targeting of this new therapy system was validated by hydroxyapatite crystal absorbing test and body distribution in vivo methods.


RESULTS
The optical spectrum of the phenamine acid caryolysine-bisphosphonates conjugate detected by the nuclear magnetic resonance was consistent with the standard structure of synthesized drugs. The conjugate had good absorbability to hydroxyapatite crystals. The body distribution of the conjugate showed higher radiocounting in bones than in other tissues.


CONCLUSIONS
The conjugate has a structure that is consistent with the active compound targeting bone tumors.
Li
Wei
W
Department of Orthopaedic Surgery, West China Hospital, Sichuan University, Chengdu 610041, China.
Zeng
Jian-Cheng
JC
Yang
Jing
J
Shen
Bin
B
Pei
Fu-Xing
FX
D000179:Acrylates / Q000008:administration & dosage; D000272:Adipates / Q000008:administration & dosage; D000661:Amphetamine / Q000008:administration & dosage; D001859:Bone Neoplasms / Q000628:therapy*; D004164:Diphosphonates / Q000008:administration & dosage*; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D009588:Nitrogen Mustard Compounds / Q000008:administration & dosage; D011868:Radioisotopes / Q000008:administration & dosage*; D012493:Samarium / Q000008:administration & dosage*
D000179:Acrylates; D000272:Adipates; D004164:Diphosphonates; D009588:Nitrogen Mustard Compounds; D011868:Radioisotopes; D012493:Samarium; C029900:adipic acid; D000661:Amphetamine