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Abstract:

The trypanocidal action of green tea catechins against two different developmental stages of Trypanosoma cruzi is reported for the first time. This activity was assayed with the nonproliferative bloodstream trypomastigote and with the intracellular replicative amastigote parasite forms. An ethyl acetate fraction from Camellia sinensis green tea leaves, which contains most of the polyphenolic compounds and the maximal trypanocidal activity, was obtained by fractionation of the aqueous extract with organic solvents. The active compounds present in this extract were further purified by LH-20 column chromatography and were identified by high-performance liquid chromatography analysis with a photo diode array detector and gas chromatography coupled to mass spectroscopy. The following flavan-3-ols derivatives, known as catechins, were identified: catechin, epicatechin, gallocatechin, epigallocatechin, catechin gallate, epicatechin gallate, gallocatechin gallate, and epigallocatechin gallate. The purified compounds lysed more than 50% of the parasites present in the blood of infected BALB/c mice at concentrations as low as 0.12 to 85 pM. The most active compounds were gallocatechin gallate and epigallocatechin gallate, with minimal bactericidal concentrations that inhibited 50% of isolates tested of 0.12 and 0.53 pM, respectively. The number of amastigotes in infected Vero cells decreased by 50% in the presence of each of these compounds at 100 nM. The effects of the catechins on the recombinant T. cruzi arginine kinase, a key enzyme in the energy metabolism of the parasite, were assayed. The activity of this enzyme was inhibited by about 50% by nanomolar concentrations of catechin gallate or gallocatechin gallate, whereas the other members of the group were less effective. On the basis of these results, we suggest that these compounds could be used to sterilize blood and, eventually, as therapeutic agents for Chagas' disease.

Registro:

Documento: Artículo
Título:Anti-Trypanosoma cruzi Activity of Green Tea (Camellia sinensis) Catechins
Autor:Paveto, C.; Güida, M.C.; Esteva, M.I.; Martino, V.; Coussio, J.; Flawiá, M.M.; Torres, H.N.
Filiación:Inst. Invest. Ing. Genet., Fac. de Ciencias Exactas y Naturales, CONICET-UBA, 1428 Buenos Aires, Argentina
Inst. Nac. Parasitol. Dr. M. F. C., 1063 Buenos Aires, Argentina
Inst. de Quim./Metabol. del Farmaco, Facultad de Farmacia y Bioquimica, CONICET-UBA, 1113 Buenos Aires, Argentina
INGEBI, Vuelta de Obligado 2490, 1428 Buenos Aires, Argentina
Palabras clave:acetic acid ethyl ester; arginine kinase; catechin; catechin gallate; epicatechin; epicatechin gallate; epigallocatechin; epigallocatechin gallate; flavanol derivative; gallocatechin; gallocatechin gallate; green tea extract; organic solvent; polyphenol derivative; unclassified drug; amastigote; animal cell; animal experiment; animal model; antiprotozoal activity; aqueous solution; article; bactericidal activity; blood; blood flow; column chromatography; concentration response; controlled study; developmental stage; diode; drug determination; drug effect; drug efficacy; drug identification; drug mechanism; drug purification; drug screening; energy metabolism; enzyme inactivation; enzyme inhibition; fractionation; gas chromatography; high performance liquid chromatography; lysis; male; mass spectrometry; minimum inhibitory concentration; mouse; nonhuman; plant leaf; priority journal; protein function; protozoal infection; tea; Trypanosoma cruzi; trypomastigote; Vero cell; Animals; Arginine Kinase; Camellia; Catechin; Cercopithecus aethiops; Chagas Disease; Chromatography, Gas; Chromatography, High Pressure Liquid; Dose-Response Relationship, Drug; Indicators and Reagents; Male; Mice; Mice, Inbred BALB C; Plant Extracts; Trypanocidal Agents; Trypanosoma cruzi; Vero Cells
Año:2004
Volumen:48
Número:1
Página de inicio:69
Página de fin:74
DOI: http://dx.doi.org/10.1128/AAC.48.1.69-74.2004
Título revista:Antimicrobial Agents and Chemotherapy
Título revista abreviado:Antimicrob. Agents Chemother.
ISSN:00664804
CODEN:AMACC
CAS:acetic acid ethyl ester, 141-78-6; arginine kinase, 9026-70-4; catechin, 13392-26-2, 154-23-4; epicatechin gallate, 863-03-6; epicatechin, 490-46-0; epigallocatechin gallate, 989-51-5; epigallocatechin, 970-74-1; gallocatechin, 970-73-0; Arginine Kinase, EC 2.7.3.3; Catechin, 154-23-4; Indicators and Reagents; Plant Extracts; Trypanocidal Agents
PDF:https://bibliotecadigital.exactas.uba.ar/download/paper/paper_00664804_v48_n1_p69_Paveto.pdf
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00664804_v48_n1_p69_Paveto

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Citas:

---------- APA ----------
Paveto, C., Güida, M.C., Esteva, M.I., Martino, V., Coussio, J., Flawiá, M.M. & Torres, H.N. (2004) . Anti-Trypanosoma cruzi Activity of Green Tea (Camellia sinensis) Catechins. Antimicrobial Agents and Chemotherapy, 48(1), 69-74.
http://dx.doi.org/10.1128/AAC.48.1.69-74.2004
---------- CHICAGO ----------
Paveto, C., Güida, M.C., Esteva, M.I., Martino, V., Coussio, J., Flawiá, M.M., et al. "Anti-Trypanosoma cruzi Activity of Green Tea (Camellia sinensis) Catechins" . Antimicrobial Agents and Chemotherapy 48, no. 1 (2004) : 69-74.
http://dx.doi.org/10.1128/AAC.48.1.69-74.2004
---------- MLA ----------
Paveto, C., Güida, M.C., Esteva, M.I., Martino, V., Coussio, J., Flawiá, M.M., et al. "Anti-Trypanosoma cruzi Activity of Green Tea (Camellia sinensis) Catechins" . Antimicrobial Agents and Chemotherapy, vol. 48, no. 1, 2004, pp. 69-74.
http://dx.doi.org/10.1128/AAC.48.1.69-74.2004
---------- VANCOUVER ----------
Paveto, C., Güida, M.C., Esteva, M.I., Martino, V., Coussio, J., Flawiá, M.M., et al. Anti-Trypanosoma cruzi Activity of Green Tea (Camellia sinensis) Catechins. Antimicrob. Agents Chemother. 2004;48(1):69-74.
http://dx.doi.org/10.1128/AAC.48.1.69-74.2004