Efficacy of anticancer alkylphosphocholines in Trypanosoma brucei subspecies
| Autor: | S.M. Konstantinov, U. Zillmann, R Kaminsky, R Brun, M.R. Berger |
|---|---|
| Rok vydání: | 1997 |
| Předmět: |
Phosphorylcholine
Veterinary (miscellaneous) medicine.medical_treatment Trypanosoma brucei brucei Cell volume Antineoplastic Agents Moderate activity Microbial Sensitivity Tests Trypanosoma brucei Pharmacology Mice chemistry.chemical_compound Piperidines In vivo medicine Phenylbutazone Animals Platelet Activating Factor Chemotherapy Molecular Structure biology Anti-Inflammatory Agents Non-Steroidal Drug Synergism biology.organism_classification In vitro Specific Pathogen-Free Organisms Trypanosomiasis African Infectious Diseases chemistry Insect Science Drug Therapy Combination Female Parasitology Growth inhibition medicine.drug |
| Zdroj: | Acta Tropica. 64:145-154 |
| ISSN: | 0001-706X |
| Popis: | Tetradecylphosphocholine (TPC), hexadecylphosphocholine (HPC), hexadecylphospho(N-N-N-trimethyl)hexanolamine (HPC6), octadecylphosphocholine (OPC), and octadecyl-[2-(N-methylpiperidinio)ethyl]-phosphate (OMPEP) were investigated for antitrypanosomal activity in vitro and in vivo. OMPEP showed the best trypanocidal efficacy in vitro: it was superior to the model compound HPC and comparable to the reference compound α-DFMO. HPC showed moderate activity in vivo in terms of increased life expectancy (up to 35% in the acute NMRI-mouse model or 49% if combined with phenylbutazone) and increased packed cell volume, if administered daily. However, HPC and the other alkylphosphocholines failed to prolong survival time of treated mice if given intermittently. Phenylbutazone had no own trypanocidal effect but increased the efficacy of alkylphosphocholines in vitro and in vivo: the combination of HPC and phenylbutazone acted apparently synergistic. |
| Databáze: | OpenAIRE |
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