In vitro and in vivo evaluation of o-carboranylalanine as a potential boron delivery agent for neutron capture therapy.

摘要: o-Carboranylalanine (B10H10C2CH2CHNH2COOH) is a carborane-containing amino acid, which has been synthesized as potential capture agent for boron neutron therapy (BNCT) of cancer. The purpose the present study was to develop rational approach in vitro and vivo evaluation containing compounds that possibly might be used BNCT. uptake carboranylalanine (CBA) evaluated using two cell lines, human melanoma MRA 27, murine Harding-Passey melanoma. Uptake CBA by 27 cells ranged from 135-551 micrograms B/10(9) following 3 hrs incubation with medium 100-113 B/ml not reduced exposing tumor either rotenone, an inhibitor electron transport, or culturing them at ambient temperature (approximately 22 degrees C). Cellular elution occurred rapidly under conditions. slightly greater than boronophenylalanine (BPA). Following hr concentration 106 B/ml, content 255 cells, compared 192 when were incubated BPA 95 B/ml. In studies initially carried out melanoma, had implanted intramuscularly (i.m.) into right flank BALB/c mice. Tumors allowed grow 14 days time mice injected intraperitoneally (i.p.) (1.25 mgB/mouse), killed 3, 6 8 later. attained low blood ratio(1.0-1.4), levels 15.7-26.2 B/g 3.3-19.9 hrs. Higher lower observed all points BPA, suggesting taken up selectively Similar studies, rats bearing intra-cerebral gliomas, failed reveal detectable amounts tumor. From study, it can concluded does appear possess requisite properties useful delivery