2. Academic Validation
  3. Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog

Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog

  • Bioorg Med Chem Lett. 2014 Jun 15;24(12):2631-4. doi: 10.1016/j.bmcl.2014.04.070.
Andreia Montoia 1,  Luiz F Rocha E Silva 1,  Zelina E Torres 2,  David S Costa 2,  Marycleuma C Henrique 3,  Emerson S Lima 3,  Marne C Vasconcellos 3,  Rita C Z Souza 4,  Monica R F Costa 5,  Andriy Grafov 6,  Iryna Grafova 6,  Marcos N Eberlin 4,  Wanderli P Tadei 2,  Rodrigo C N Amorim 2,  Adrian M Pohlit 7
Affiliations

Affiliations

  • 1 National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil; Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas, Brazil.
  • 2 National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil.
  • 3 Federal University of Amazonas, Avenida General Rodrigo Otávio Jordão Ramos, 3000, 69077-000 Manaus, Amazonas, Brazil.
  • 4 State University of Campinas, Campus Universitário Zeferino Vaz SN, 13083-970 Campinas, Brazil.
  • 5 Heitor Vieira Dourado Tropical Medicine Foundation, Avenida Pedro Teixeira, 25, 69040-000 Manaus, Amazonas, Brazil.
  • 6 University of Helsinki, A.I. Virtasen aukio 1, PL 55, FI-00014 Helsinki, Finland.
  • 7 National Institute for Amazon Research, Avenida André Araújo, 2936, 69067-375 Manaus, Amazonas, Brazil. Electronic address: ampohlit@inpa.gov.br.
PMID: 24813729 DOI: 10.1016/j.bmcl.2014.04.070
Abstract

Ellipticine has been shown previously to exhibit excellent in vitro antiplasmodial activity and in vivo antimalarial properties that are comparable to those of the control drug chloroquine in a mouse malaria model. Ellipticine derivatives and analogs exhibit antimalarial potential however only a few have been studied to date. Herein, ellipticine and a structural analog were isolated from Aspidosperma vargasii bark. A-ring brominated and nitrated ellipticine derivatives exhibit good in vitro inhibition of Plasmodium falciparum K1 and 3D7 strains. Several of the compounds were found not to be toxic to human fetal lung fibroblasts. 9-Nitroellipticine (IC50=0.55μM) exhibits greater antiplasmodial activity than ellipticine. These results are further evidence of the antimalarial potential of ellipticine derivatives.

Keywords

2-Methyl-1,2,3,4-tetrahydroellipticine; 7,9-Dibromoellipticine; 7-Nitroellipticine; 9-Nitroellipticine; Plasmodium falciparum.

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