title: A new boronated porphyrin (STA-BX909) for neutron capture therapy: an in vitro survival assay and in vivo tissue uptake study.
abstract: A new boronated porphyrin compound (STA-BX909) was developed as a possible agent for boron neutron capture therapy. The boron concentration was measured by an in vivo rat experimental brain tumor model and an in vitro cell culture study. This agent was compared to sodium borocaptate (BSH) which has been used in clinical trials of boron neutron capture therapy. In the 9L rat brain tumor model, STA-BX909 achieved a higher boron tumor/blood ratio 24 h after injection in comparison to BSH. A boron concentration study in cultured glioma cell lines (U-251, U-87, 9L) demonstrated an increased boron concentration as a function of exposure time to STA-BX909, while the boron concentration remained stable with increasing exposure time to BSH. Use of a colony forming assay with thermal neutron irradiation revealed more cytotoxicity with STA-BX909 than BSH when the same concentration of 10B was administered. We concluded that STA-BX909 may be an effective drug for use in boron neutron capture therapy and that it merits further investigation.
authors.affiliation: Department of Neurosurgery, Institute of Clinical Medicine, University of Tsukuba, Ibaraki, Japan. matsumur@md.tsukuba.ac.jp
authors.forename: A
authors.initials: A
authors.lastname: Matsumura
authors.forename: Y
authors.initials: Y
authors.lastname: Shibata
authors.forename: T
authors.initials: T
authors.lastname: Yamamoto
authors.forename: F
authors.initials: F
authors.lastname: Yoshida
authors.forename: T
authors.initials: T
authors.lastname: Isobe
authors.forename: K
authors.initials: K
authors.lastname: Nakai
authors.forename: Y
authors.initials: Y
authors.lastname: Hayakawa
authors.forename: M
authors.initials: M
authors.lastname: Kiriya
authors.forename: N
authors.initials: N
authors.lastname: Shimojo
authors.forename: K
authors.initials: K
authors.lastname: Ono
authors.forename: I
authors.initials: I
authors.lastname: Sakata
authors.forename: S
authors.initials: S
authors.lastname: Nakajima
authors.forename: M
authors.initials: M
authors.lastname: Okumura
authors.forename: T
authors.initials: T
authors.lastname: Nose
mesh_terms: D000818:Animals; D001894:Borohydrides / Q000493:pharmacokinetics / Q000494:pharmacology; D001895:Boron / Q000378:metabolism; D016754:Boron Neutron Capture Therapy; D001932:Brain Neoplasms / Q000378:metabolism*; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D005910:Glioma / Q000378:metabolism*; D008665:Metalloporphyrins / Q000493:pharmacokinetics* / Q000494:pharmacology*; D009368:Neoplasm Transplantation; D051381:Rats; D011916:Rats, Inbred F344; D013438:Sulfhydryl Compounds / Q000493:pharmacokinetics / Q000494:pharmacology; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured; D014410:Tumor Stem Cell Assay
chemical_list: D001894:Borohydrides; D008665:Metalloporphyrins; C120895:STA BX909; D013438:Sulfhydryl Compounds; C014651:mercaptoundecahydrododecaborate; D001895:Boron