TY - JOUR
T1 - High antitrypanosomal activity of plant-derived sulphur-containing amides
AU - Astelbauer, Florian
AU - Obwaller, Andreas
AU - Raninger, Adriane
AU - Brem, Brigitte
AU - Greger, Harald
AU - Duchêne, Michael
AU - Wernsdorfer, Walther
AU - Walochnik, Julia
N1 - Copyright © 2010 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.
PY - 2010/12
Y1 - 2010/12
N2 - Chagas disease, caused by Trypanosoma cruzi, represents an important public health problem in endemic geographic regions in Middle and South America, affecting 15 million infected people. Treatment options are still limited due to the toxicity of available drugs, parasite resistance and poor drug activity during the chronic phase of the disease. In this study, we investigated the in vitro antitrypanosomal activity of 15 tropical plant-derived compounds with the aim of finding new drug candidates. Three novel sulphur-containing amides (methyldambullin, methylgerambullin and sakambullin) showed promising antitrypanosomal activities, with 50% effective concentrations (EC₅₀ values) after 72 h exposure of 1.7, 1.23 and 5.18 μM, respectively, compared with EC₅₀ values for amphotericin B and benznidazole of 0.71 μM and 30.89 μM, respectively.
AB - Chagas disease, caused by Trypanosoma cruzi, represents an important public health problem in endemic geographic regions in Middle and South America, affecting 15 million infected people. Treatment options are still limited due to the toxicity of available drugs, parasite resistance and poor drug activity during the chronic phase of the disease. In this study, we investigated the in vitro antitrypanosomal activity of 15 tropical plant-derived compounds with the aim of finding new drug candidates. Three novel sulphur-containing amides (methyldambullin, methylgerambullin and sakambullin) showed promising antitrypanosomal activities, with 50% effective concentrations (EC₅₀ values) after 72 h exposure of 1.7, 1.23 and 5.18 μM, respectively, compared with EC₅₀ values for amphotericin B and benznidazole of 0.71 μM and 30.89 μM, respectively.
KW - Chemotherapy
KW - Methyldambullin
KW - Methylgerambullin
KW - Sakambullin
KW - Trypanosoma cruzi
KW - Humans
KW - Antiprotozoal Agents/isolation & purification
KW - Plants/chemistry
KW - Amides/isolation & purification
KW - Plant Extracts/isolation & purification
KW - Sulfur Compounds/isolation & purification
KW - Inhibitory Concentration 50
KW - Trypanosoma cruzi/drug effects
UR - http://www.scopus.com/inward/record.url?scp=78249275863&partnerID=8YFLogxK
U2 - 10.1016/j.ijantimicag.2010.07.003
DO - 10.1016/j.ijantimicag.2010.07.003
M3 - Article
C2 - 20851577
AN - SCOPUS:78249275863
SN - 0924-8579
VL - 36
SP - 570
EP - 572
JO - International Journal of Antimicrobial Agents
JF - International Journal of Antimicrobial Agents
IS - 6
ER -