title: Antimicrobial activity of synthetic bornyl benzoates against Trypanosoma cruzi.
abstract: We report here for the first time the in vitro effects of (1S,2R,4S)-1,7,7-trimethyl-bicyclo[2·2·1]heptan-2-yl-3',4',5'-trimethoxy benzoate (1) and (1S,2R,4S)-1,7,7-trimethyl-bicyclo[2·2·1]heptan-2-yl  benzoate (2) on the growth and ultrastructure of Trypanosoma cruzi. These two synthetic compounds exerted an antiproliferative effect on the epimastigote forms of the parasite. The ICs(50/72h) of two synthetic L-bornyl benzoates, 1 and 2, was 10·1  and 12·8 μg/ml, respectively. Both compounds were more selective against epimastigotes than HEp-2 cells. Ultrastructural analysis revealed intense cytoplasmic vacuolization and the appearance of cytoplasmic materials surrounded by membranes. The treatment of peritoneal macrophages  with compounds 1 and 2 caused a significant decrease in the number of T. cruzi-infected cells. L-Bornyl benzoate derivatives may serve as a potential source for the development of more effective and safer chemotherapeutic agents against T. cruzi infections.
authors.affiliation: Universidade Estadual de Londrina, Londrina, Paraná, Brazil.
authors.forename: P R C
authors.initials: PR
authors.lastname: Corrêa
authors.forename: R R S
authors.initials: RR
authors.lastname: Miranda
authors.forename: L P
authors.initials: LP
authors.lastname: Duarte
authors.forename: G D F
authors.initials: GD
authors.lastname: Silva
authors.forename: S A Vieira
authors.initials: SA
authors.lastname: Filho
authors.forename: A A
authors.initials: AA
authors.lastname: Okuma
authors.forename: F
authors.initials: F
authors.lastname: Carazza
authors.forename: J A
authors.initials: JA
authors.lastname: Morgado-Díaz
authors.forename: P
authors.initials: P
authors.lastname: Pinge-Filho
authors.forename: L M
authors.initials: LM
authors.lastname: Yamauchi
authors.forename: C V
authors.initials: CV
authors.lastname: Nakamura
authors.forename: S F
authors.initials: SF
authors.lastname: Yamada-Ogatta
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D001565:Benzoates / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D001892:Camphanes / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D003593:Cytoplasm / Q000648:ultrastructure; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000469:parasitology; D051379:Mice; D008807:Mice, Inbred BALB C; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development / Q000648:ultrastructure
chemical_list: D000981:Antiprotozoal Agents; D001565:Benzoates; D001892:Camphanes