Killing of Human Lung Cancer Cells Using a New [¹¹¹In]Bleomycin Complex [¹¹¹In]BLMC

Abstract

The ability of a [111In]bleomycin complex [( 111In]BLMC) to kill five cell lines of human lung cancer (small cell lung cancer) was investigated. Cells were exposed to either 0.9% NaCl, [111In]Cl3, BLM, [111In]BLMC, nonradioactive InCl3, or In-BLMC for 60 minutes, plated in soft agarose, and assessed for colony formation. [111In]BLMC (40-200 microCi carried by 15-25 micrograms BLM/ml) was more cytotoxic than BLM (15-25 micrograms BLM/ml) by a factor of 1.6-5.3 for five cell lines. The percent survival of N417 cells was 28.4 for [111In]BLMC (40 microCi/15 micrograms BLM/ml) and 54.3 for BLM (15 micrograms/ml); 1.9 for [111In]BLMC (200 microCi/25 micrograms BLM/ml), and 10.0 for BLM (25 micrograms/ml). 111InCl3 (200 microCi/ml) and nonradioactive InCl3 failed to inhibit colony formation. The new [111In]BLMC may be useful for therapy of some lung cancer patients.

Chromosome aberrations of human small cell lung cancer induced by a new 111in‐bleomycin complex

“…Our previous data [9] also indicated that there were no significant difference in cell survival between the Table 11.…”

“…Human small cell lung cancer (SCLC) is sensitive to chemotherapy, radiotherapy, and combined chemo-radiotherapy [8]. Experiments with ' ' 'In-BLMC showed that it was more cytotoxic than BLM by a factor of I .6-5.3 times for killing five human SCLC cell lines [9].…”

“…Experiments with ' ' 'In-BLMC showed that it was more cytotoxic than BLM by a factor of I .6-5.3 times for killing five human SCLC cell lines [9].…”

Nikolai Sergeevich Dikanskii (on his sixtieth birthday)

“…Tumours were palpable after 12-14 days and were used after reaching a volume of approximately 8 cm 3 (longest dimension: 2.5 cm). Bleomycin (Blenoxane, Mead Johnson, Princeton, NJ) was labelled with 111 In by mixing 1 mCi (0.1 ml) of 111 InCl (Nycomed Amersham, Amersham, England) with 0.4 ml bleomycin solution (10 mg = 15 units bleomycin, per ml normal saline, acidified with cHCl to pH 1-3), letting the mixture stand for 1 h at room temperature with occasional mixing, and adding another 0.5 ml bleomycin solution and 1.0 ml acidified normal saline to the mixture [49][50][51]. Labelling efficiency was approximately 97% as determined by thin layer chromatography on silica gel (liquid phase: equal volumes of MeOH and 10% aqueous ammonium acetate; Rf approximately 0.7).…”

Radioimmunotherapy Dosimetry—A Review

“…Thus, Auger electron emitting radionuclides hold great promises in systemic radiotherapy if appropriate carriers can be found. Attempts have been made to develop chemo-Auger combination therapy with Auger emitters labelled to bleomycin (86,87) and carboplatin (88,89). Many cancer cells contain hormone receptors in the cytoplasm or on the cell membrane, to which hormones or anti-hormone drugs labelled with an Auger electron emitting radionuclide may be targeted.…”