In vitro trypanocidal activity of phenolic derivatives from Peperomia obtusifolia.
The trypanocidal activity of crude extracts and fractions from the leaves and stems of Peperomia obtusifolia (Piperaceae) was evaluated in vitro against the epimastigote forms of Trypanosoma cruzi. Bioactivity-guided fractionation of the most active extracts afforded seven known compounds, including three chromanes, two furofuran lignans and two flavone C-diglycosides. The most active compounds were the chromanes peperobtusin A and 3,4-dihydro-5-hydroxy-2,7-dimethyl-8-(2''-methyl-2''-butenyl)-2-(4'-methyl-1',3'-pentadienyl)-2 H-1-benzopyran-6-carboxylic acid, with IC (50) values of 3.1 microM (almost three times more active than the positive control benznidazole, IC (50) 10.4 microM) and 27.0 microM, respectively. Cytotoxicity assays using peritoneal murine macrophages indicated that the chromanes were not toxic at the level of the IC (50) for trypanocidal activity. This is the first report on the trypanocidal activity besides unspecific cytotoxicity of chromanes from Peperomia species. Additionally it represents the first time isolation of 3,4-dihydro-5-hydroxy-2,7-dimethyl-8-(2''-methyl-2''-butenyl)-2-(4'-methyl-1',3'-pentadienyl)-2 H-1-benzopyran-6-carboxylic acid from P. obtusifolia.
da Silva Mota
Jonas
J
Institute of Chemistry, Mato Grossodo Sul State University, Dourados, MS, Brazil.
Leite
Ana Cristina
AC
Batista Junior
João Marcos
JM
Noelí López
Silvia
S
Luz Ambrósio
Daniela
D
Duó Passerini
Gabriela
G
Kato
Massuo Jorge
MJ
da Silva Bolzani
Vanderlan
V
Barretto Cicarelli
Regina Maria
RM
Furlan
Maysa
M
D000818:Animals; D002839:Chromans / Q000302:isolation & purification / Q000494:pharmacology*; D008018:Life Cycle Stages; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D009593:Nitroimidazoles / Q000494:pharmacology; D036941:Peperomia / Q000737:chemistry*; D010636:Phenols / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves; D018547:Plant Stems; D014344:Trypanocidal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D002839:Chromans; D009593:Nitroimidazoles; D010636:Phenols; D010936:Plant Extracts; D014344:Trypanocidal Agents; C009999:benzonidazole