TY - JOUR
T1 - In vitro and in vivo studies of trypanocidal activity of dietary isothiocyanates
AU - Steverding, Dietmar
AU - Michaels, Sarah
AU - Read, Kevin D.
PY - 2014
Y1 - 2014
N2 - Six dietary isothiocyanates, allyl-isothiocyanate, benzyl-isothiocyanate, phenylethyl-isothiocyanate, sulforaphane, erucin, and iberin, were tested for their trypanocidal activities in vitro using culture-adapted bloodstream forms of Trypanosoma brucei. All isothiocyanates showed a dose-dependent effect on the growth of trypanosomes. Five compounds displayed MIC values of 10 μM and GI values of around 1.5 μM, while allyl-isothiocyanate exhibited values of 100 and 11 μM, respectively. The compounds showed similar cytotoxic activities against human HL-60 cells with GI values of 1-4 μM and MIC values of 10-100 μM. Short-term experiments revealed that, with the exception of allyl-isothiocyanate, isothiocyanates at a concentration of 10 μM kill trypanosomes within 1-4 h of incubation. In contrast, HL-60 cells were not affected by any of the compounds in short-term incubation experiments. Sulforaphane, the most intensively studied isothiocyanate, was also investigated for its in vivo trypanocidal activity. However, administration of 50 mg/kg sulforaphane orally or intraperitoneally for four days had no effect on the parasitaemia in mice infected with T. brucei compared to control animals treated with vehicle alone.
AB - Six dietary isothiocyanates, allyl-isothiocyanate, benzyl-isothiocyanate, phenylethyl-isothiocyanate, sulforaphane, erucin, and iberin, were tested for their trypanocidal activities in vitro using culture-adapted bloodstream forms of Trypanosoma brucei. All isothiocyanates showed a dose-dependent effect on the growth of trypanosomes. Five compounds displayed MIC values of 10 μM and GI values of around 1.5 μM, while allyl-isothiocyanate exhibited values of 100 and 11 μM, respectively. The compounds showed similar cytotoxic activities against human HL-60 cells with GI values of 1-4 μM and MIC values of 10-100 μM. Short-term experiments revealed that, with the exception of allyl-isothiocyanate, isothiocyanates at a concentration of 10 μM kill trypanosomes within 1-4 h of incubation. In contrast, HL-60 cells were not affected by any of the compounds in short-term incubation experiments. Sulforaphane, the most intensively studied isothiocyanate, was also investigated for its in vivo trypanocidal activity. However, administration of 50 mg/kg sulforaphane orally or intraperitoneally for four days had no effect on the parasitaemia in mice infected with T. brucei compared to control animals treated with vehicle alone.
UR - http://www.scopus.com/inward/record.url?scp=84894279873&partnerID=8YFLogxK
U2 - 10.1055/s-0033-1360262
DO - 10.1055/s-0033-1360262
M3 - Article
AN - SCOPUS:84894279873
SN - 0032-0943
VL - 80
SP - 183
EP - 186
JO - Planta Medica
JF - Planta Medica
IS - 2-3
ER -