P. Lemmen et al., UPTAKE AND DISTRIBUTION OF THE BORON-CONTAINING ETHER LIPID B-ET-11-OME IN TUMOR-BEARING MICE, Anti-cancer drugs, 6(6), 1995, pp. 744-748
Ether lipids in general are accumulated in tumor tissue with a favorab
le tumor/healthy tissue ratio. The uptake of the boron-containing anal
og carboranyl)nonyl-2-methyl-glycero-3-phosphocholine (B-Et-11-OMe) wa
s studied in C3H mice bearing the murine mammary carcinoma AT17 and in
BALB/c mice bearing an osteosarcoma. Boron concentrations of tumor, b
lood, liver and kidney were followed up to 48 h by inductively coupled
plasma emission spectrometry and inductively coupled plasma mass spec
trometry. Boron concentration in AT17 mamma carcinoma rose up to 2 mg/
kg and the tumor/blood ratio rose to 0.5. The bulk was taken up by the
liver. Osteosarcoma did not take up 8-Et-11-OMe. This result constitu
tes a significant contrast to the behavior of published (non-boron-con
taining) analogs. It is interpreted in terms of critical micellar conc
entration (CMC). Whereas earlier work with ether lipids was done well
below CMC, this study was undertaken above. Further studies will conce
ntrate on syntheses of high CMC analogs.