Abstract
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 GI50 values of around 1.5µM, while allyl-isothiocyanate exhibited values of 100 and 11µM, respectively. The compounds showed similar cytotoxic activities against human HL-60 cells with GI50 values of 1-4µM and MIC values of 10-100µM. Short-term experiments revealed that, with the exception of allyl-isothiocyanate, isothiocyanates at a concentration of 10µM kill trypanosomes within 1-4h 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 50mg/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.
| Original language | English |
|---|---|
| Journal | Planta Medica |
| DOIs | |
| Publication status | Published - 22 Jan 2014 |
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In Vitro and In Vivo studies of trypanocidal activity of dietary isothiocyanates. / Steverding, Dietmar; Michaels, Sarah; Read, Kevin D.
In: Planta Medica, 22.01.2014.Research output: Contribution to journal › Letter
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 - 2014/1/22
Y1 - 2014/1/22
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 GI50 values of around 1.5µM, while allyl-isothiocyanate exhibited values of 100 and 11µM, respectively. The compounds showed similar cytotoxic activities against human HL-60 cells with GI50 values of 1-4µM and MIC values of 10-100µM. Short-term experiments revealed that, with the exception of allyl-isothiocyanate, isothiocyanates at a concentration of 10µM kill trypanosomes within 1-4h 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 50mg/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 GI50 values of around 1.5µM, while allyl-isothiocyanate exhibited values of 100 and 11µM, respectively. The compounds showed similar cytotoxic activities against human HL-60 cells with GI50 values of 1-4µM and MIC values of 10-100µM. Short-term experiments revealed that, with the exception of allyl-isothiocyanate, isothiocyanates at a concentration of 10µM kill trypanosomes within 1-4h 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 50mg/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.
U2 - 10.1055/s-0033-1360262
DO - 10.1055/s-0033-1360262
M3 - Letter
C2 - 24452460
JO - Planta Medica
JF - Planta Medica
SN - 0032-0943
ER -