Table 3.
Compounds/Substances | Origin | Trypanocidal activities | Assays | References | |||
---|---|---|---|---|---|---|---|
in vitro | in vivo | Observations | Toxicity | Clinical | |||
[(2S)-methyl-2-methyl-8-(3-methylbut-2′-enyl)-2-(4-methylpent-3-enyl)-2Hchromene-6-carboxylate] |
Piper1 | T. cruzi epimastigote—IC50-value 2.82 μM | nd | nd | nd | nd | [143] |
3-(3,7-dimethyl-2,6-octadienyl)-4-methoxy-benzoic acid |
Piper aduncum | L. braziliensis promastigote—IC50-value 6.5 μg/mL | nd | nd | nd | nd | [144] |
4-hydroxy-3-(3-methyl-1-oxo-2-butenyl)-5-(3-methyl-2-butenyl)benzoic acid |
Piper aduncum | T. cruzi epimastigote—IC50 16.5 μg/mL | nd | nd | nd | nd | [144] |
methyl 4-hydroxy-3-(2-hydroxy-3-methyl-3-butenyl)benzoate |
Piper glabratum | T. cruzi epimastigote—IC50-value 15.6 μg/mL | nd | nd | nd | nd | [145] |
2,6-dihydroxi-4-metoxichalcone |
Piper aduncum | L. amazonensis promastigote—IC50-value 0.5 μg/mL amastigotes—IC50-value 24 μg/mL | nd | nd | nd | nd | [146] |
dihydrochalcone |
Piper elongatum | L. braziliensis promastigote—IC50-value 2.98 μg/mL | nd | nd | nd | nd | [147] |
Cubebin |
Piper cueba | L. donovani promastigotes—IC50-value 28 μg/mL | 100.0 mg/kg, i.p. in hamster infected with L. donovani | nd | nd | nd | [148] |
Conocarpan |
Piper regnellii | T. cruzi epimastigote—IC50-value 8.0 μg/mL | nd | nd | nd | nd | [149] |
Eupomatenoid |
Piper regnellii | T. cruzi epimastigote—IC50-value 7.0 μg/mL | nd | nd | Non-toxic in Vero cells (CC50 250 μg/mL) | nd | [149] |
Grandisin |
Piper solmsianum | T. cruzi trypomastigote—IC50-value 8.74 μg/mL | nd | nd | nd | nd | [150] |
Piperine |
Piper | T. cruzi epimastigote—IC50-value 7.36 μM amastigote—IC50-value 4.91 μM | nd | nd | nd | nd | [151] |
Piplartine |
Piper tuberculatum Piper retrofractum | T. cruzi epimastigote—IC50-value 10.5 μM L. donovani promastigotes—IC50-value 7.5 μg/mL | 30 mg/kg ip. in hamster infected with L. donovani | nd | nd | nd | [148,152] |
prenylated hydroquinone [1,4-dihydroxy-2-(3′,7′-dimethyl-1′-oxo-2′-E,6′-octadienyl)benzene |
Piper crassinervium | T. cruzi epimastigote—IC50-value 6.10 μg/mL | nd | nd | nd | nd | [153] |
methyl 3,4-dihydroxy-5-(3′-methyl-2′-butenyl)benzoate |
Piper glabratum | L. braziliensis, L. amazonensis and L. donovani—IC50-value 13.8–18.5 μg/mL) | nd | nd | nd | nd | [145] |
methyl 3,4-dihydroxy-5-(2-hydroxy-3-methylbutenyl)benzoate |
Piper glabratum | T cruzi epimestigote—IC50-value 16.4 μg/mL | nd | nd | nd | nd | [145] |
methyl 4-hydroxy-3-(2-hydroxy-3-methyl-3-butenyl)benzoate |
Piper glabratum | T cruzi epimestigote—IC50-value 15.6 μg/mL | nd | nd | nd | nd | [145] |
(15-acetoxy-8_-[(2-methylbutyryloxy)]-14-oxo-4,5-cis-acanthospermolide) |
Acanthospermum hispidum | T. brucei brucei—IC50-value 2.45 μM L. mexicana Mexicana —IC50-value 0.94 μM | nd | nd | nd | nd | [154] |
Veraguensin |
Nectandra megapotamica | L.donovani promastigotes—IC50-value 18 μg/mL and IC90-value 36 μg/mL | nd | nd | Non-toxic in Vero cells5 in 10 μg/ml | nd | [91] |
Methanol extract from stem bark | Acacia nilotica | na | 200 mg/kg body weight in mice infected with T. brucei brucei | Clear the parasites from circulation within 6 days of treatment | na | na | [136] |
Methanol stem bark extract | Bombax buonopozense | nd | 300 mg/kg body weight in mice infected with T. brucei brucei | Clear the parasites from circulation within 7 days of treatment | nd | nd | [136] |
Dichloromethane bark extract | Warburgia salutaris | T. brucei brucei—IC50 -value 10.68 μg/mL | nd | nd | nd | nd | [155] |
8-epixanthatin 1β,5β-epoxide |
Xanthium brasilicum Vell | T. brucei—IC50 0.09 μg/mL T. cruzi—IC50-value 2.95 μg/L L. donovani—IC50 0.16 μg/mL | nd | nd | nd | nd | [142] |
Synthetic compound derived from chromenes isolated from Piper aduncum and Piper gaudichaudianum;
Intraperitoneally, twice daily for 3 days;
per os, twice daily for 3 days;
Balb/c infected with L. amazonensis and treated for 28 days;
African green monkey kidney fibroblast.