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RESEARCH PAPER
 
 

Neuroprotective activity of 2-amino-1,3,4-thiadiazole derivative 4BrABT – an in vitro study

Ewa Langner 2,  
 
1
Department of Medical Biology, Institute of Rural Health, Lublin, Poland
2
Department of Medical Biology, Institute of Rural Health, Lublin, Poland; Department of Pharmacology, Medical University, Lublin, Poland
3
Institute of Industrial Organic Chemistry, Warsaw, Poland
4
Department of Chemistry, University of Life Sciences, Lublin, Poland
5
Department of Medical Biology, Institute of Rural Health, Lublin, Poland; Department of Virology and Immunology, Institute of Microbiology and Biotechnology, Maria Curie-Sklodowska University, Lublin, Poland
Ann Agric Environ Med 2013;20(3):575–579
KEYWORDS:
ABSTRACT:
4BrABT (2-(4-Bromophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole) is a compound known for its interesting in vitro anticancer profile. 4BrABT inhibited proliferation and motility of several cancer cell lines in concentrations which were not toxic to normal cells. A major problem associated with cancer chemotherapy, but also caused by environmental factors such as pesticides, is neurotoxicity. Therefore, the aim of the presented study was an [i]in vitro[/i] evaluation of the neuroprotective activity of this compound. 4BrABT activity (1–100 μM) was tested in cultures of mouse neurons, rat astrocytes and rat oligodendrocytes. A possible protective action of the compound in different neurodegenerative models, as serum deprivation (SD), excitotoxicity (presence of 500 μM glutamate in culture medium), as well as cisplatin toxicity (astroglia – 50 μM and oligodendroglia – 100 μM) was investigated. Cell viability in the tested cultures was assessed with the use of LDH and MTT methods. Moreover, 4BrABT ability to prevent the cisplatin-induced apoptosis in astrocyte and oligodendrocyte cultures was analysed after Hoechst 33342 fluorostaining. The obtained results indicate that 4BrABT was not toxic to neurons, astrocytes and oligodendrocytes. Moreover, a decrease in the neuronal LDH level was observed, which may suggest the ability of 4BrABT to act as a trophic agent. Furthermore, the protective action of the studied compound was shown in neuronal cultures exposed to neurotoxic conditions (presence of glutamate and trophic stress) and in cisplatin-treated astrocytes and oligodendrocytes. The expression of anticancer and neuroprotective activity raises hopes for the potential use of 4BrABT as a safe anticancer drug, or neuroprotective agent in chemotherapy-associated neurotoxicity.
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eISSN:1898-2263
ISSN:1232-1966