Anticarcinoma activity of a novel drug, 3-ethyl-3'-methyl-thiatelluracarbocyanine iodide (Te), a tellurium-containing cyanine targeted at mitochondria.
Lipophilic cationic compounds such as rhodamine 123, AA1, and dequalinium chloride have been reported to constitute a new class of anticarcinoma agents based on their selective localization, accumulation, and retention within the mitochondria of certain carcinoma cells. After screening more than 1000 lipophilic cationic compounds in clonogenic assays, we found that a tellurium-containing cyanine, 3-ethyl-3'-methyl-thiatelluracarbocyanine iodide (Te), exhibits significant anticarcinoma activity. In vitro testing showed that Te was 64-fold more toxic to the carcinoma cell line CX-1 than to the normal epithelial cell line CV-1. In vivo testing showed that Te significantly prolonged the survival of mice implanted with tumors. For C57BL x DBA/2 F1 mice implanted with the mouse bladder carcinoma cell line MB49, the treated:control (T:C) ratio ranged from 250 to 268%. For Swiss nu/nu mice implanted with the human melanoma cell line LOX, the T:C ratio ranged from 176 to 270%. For Swiss nu/nu mice implanted with the human ovarian tumor cell line OVCA-III, the T:C ratio was 344%. These anticarcinoma activities warrant further investigation of Te as a potential anticarcinoma agent.
Sun
X
X
Department of Chemistry, Biochemistry, and Molecular Biology, Oregon Graduate Institute of Science and Technology, Portland, Oregon 97291-1000, USA.
Wong
J R
JR
Song
K
K
Chen
L B
LB
D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008811:Mice, Inbred DBA; D008819:Mice, Nude; D008928:Mitochondria / Q000378:metabolism*; D009374:Neoplasms, Experimental / Q000188:drug therapy; D009942:Organometallic Compounds / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
C116939:3-ethyl-3'-methyl-thiatelluracarbocyanine iodide; D000970:Antineoplastic Agents; D009942:Organometallic Compounds