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Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes.
Martins, Ligia F; Mesquita, Juliana T; Pinto, Erika G; Costa-Silva, Thais A; Borborema, Samanta E T; Galisteo Junior, Andres J; Neves, Bruno J; Andrade, Carolina H; Shuhaib, Zainab Al; Bennett, Elliot L; Black, Gregory P; Harper, Philip M; Evans, Daniel M; Fituri, Hisham S; Leyland, John P; Martin, Claire; Roberts, Terence D; Thornhill, Andrew J; Vale, Stephen A; Howard-Jones, Andrew; Thomas, Dafydd A; Williams, Harri L; Overman, Larry E; Berlinck, Roberto G S; Murphy, Patrick J; Tempone, Andre G.
Afiliação
  • Martins LF; Centre for Parasitology and Mycology, Instituto Adolfo Lutz , Avenida Dr. Arnaldo, 351, 8° andar, 01246-000 São Paulo, SP, Brazil.
  • Mesquita JT; Centre for Parasitology and Mycology, Instituto Adolfo Lutz , Avenida Dr. Arnaldo, 351, 8° andar, 01246-000 São Paulo, SP, Brazil.
  • Pinto EG; Centre for Parasitology and Mycology, Instituto Adolfo Lutz , Avenida Dr. Arnaldo, 351, 8° andar, 01246-000 São Paulo, SP, Brazil.
  • Costa-Silva TA; Instituto de Medicina Tropical, Universidade de São Paulo , Avenida Dr. Enéas de Carvalho Aguiar, 470, 05403-000 São Paulo, SP, Brazil.
  • Borborema SE; Centre for Parasitology and Mycology, Instituto Adolfo Lutz , Avenida Dr. Arnaldo, 351, 8° andar, 01246-000 São Paulo, SP, Brazil.
  • Galisteo Junior AJ; Centre for Parasitology and Mycology, Instituto Adolfo Lutz , Avenida Dr. Arnaldo, 351, 8° andar, 01246-000 São Paulo, SP, Brazil.
  • Neves BJ; Instituto de Medicina Tropical, Universidade de São Paulo , Avenida Dr. Enéas de Carvalho Aguiar, 470, 05403-000 São Paulo, SP, Brazil.
  • Andrade CH; LabMol, Laboratory for Molecular Modeling and Drug Design, Faculdade de Farmácia, Universidade Federal de Goiás , Goiânia, Brazil.
  • Shuhaib ZA; LabMol, Laboratory for Molecular Modeling and Drug Design, Faculdade de Farmácia, Universidade Federal de Goiás , Goiânia, Brazil.
  • Bennett EL; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Black GP; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Harper PM; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Evans DM; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Fituri HS; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Leyland JP; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Martin C; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Roberts TD; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Thornhill AJ; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Vale SA; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Howard-Jones A; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Thomas DA; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Williams HL; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Overman LE; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
  • Berlinck RG; University of California, Irvine , 4042A Frederick Reines Hall, Irvine, California 92697, United States.
  • Murphy PJ; Instituto de Química de São Carlos, Universidade de São Paulo , CP 780, CEP 13560-970, São Carlos, SP, Brazil.
  • Tempone AG; School of Chemistry, Bangor University , Bangor, Gwynedd, Wales, U.K. LL57 2UW.
J Nat Prod ; 79(9): 2202-10, 2016 09 23.
Article em En | MEDLINE | ID: mdl-27586460
Synthetic analogues of marine sponge guanidine alkaloids showed in vitro antiparasitic activity against Leishmania (L.) infantum and Trypanosoma cruzi. Guanidines 10 and 11 presented the highest selectivity index when tested against Leishmania. The antiparasitic activity of 10 and 11 was investigated in host cells and in parasites. Both compounds induced depolarization of mitochondrial membrane potential, upregulation of reactive oxygen species levels, and increased plasma membrane permeability in Leishmania parasites. Immunomodulatory assays suggested an NO-independent effect of guanidines 10 and 11 on macrophages. The same compounds also promoted anti-inflammatory activity in L. (L.) infantum-infected macrophages cocultived with splenocytes, reducing the production of cytokines MCP-1 and IFN-γ. Guanidines 10 and 11 affect the bioenergetic metabolism of Leishmania, with selective elimination of parasites via a host-independent mechanism.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Poríferos / Trypanosoma cruzi / Leishmania infantum / Guanidinas Limite: Animals Idioma: En Revista: J Nat Prod Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Brasil País de publicação: Estados Unidos
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Poríferos / Trypanosoma cruzi / Leishmania infantum / Guanidinas Limite: Animals Idioma: En Revista: J Nat Prod Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Brasil País de publicação: Estados Unidos