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Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda.

  • Rocha VPC Laboratório de Engenharia Tecidual e Imunofarmacologia, Instituto Gonçalo Moniz, Fundação Oswaldo Cruz (Fiocruz), Avenida Waldemar Falcão, 121, Candeal⁻Salvador-BA 40296-710, Brazil. viny_rocha@hotmail.com.
  • Quintino da Rocha C Departamento de Química, Universidade Federal do Maranhão, São Luiz 65080-805, MA, Brazil. claudiarocha3@yahoo.com.br.
  • Ferreira Queiroz E School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, CMU, 1, Rue Michel Servet, 1211 Geneva, Switzerland. emerson.ferreira@unige.ch.
  • Marcourt L School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, CMU, 1, Rue Michel Servet, 1211 Geneva, Switzerland. laurence.marcourt@unige.ch.
  • Vilegas W UNESP-Campus Experimental do Litoral Paulista, Praça Infante Dom Henrique s/n°, Parque Bitaru, São Vicente⁻SP 11330-900, Brazil. vilegasw@clp.unesp.br.
  • Grimaldi GB Laboratório de Engenharia Tecidual e Imunofarmacologia, Instituto Gonçalo Moniz, Fundação Oswaldo Cruz (Fiocruz), Avenida Waldemar Falcão, 121, Candeal⁻Salvador-BA 40296-710, Brazil. gabrielagrimaldi16.1@bahiana.edu.br.
  • Furrer P School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, CMU, 1, Rue Michel Servet, 1211 Geneva, Switzerland. pascal.furrer@unige.ch.
  • Allémann É School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, CMU, 1, Rue Michel Servet, 1211 Geneva, Switzerland. eric.allemann@unige.ch.
  • Wolfender JL School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, CMU, 1, Rue Michel Servet, 1211 Geneva, Switzerland. jean-luc.wolfender@unige.ch.
  • Soares MBP Laboratório de Engenharia Tecidual e Imunofarmacologia, Instituto Gonçalo Moniz, Fundação Oswaldo Cruz (Fiocruz), Avenida Waldemar Falcão, 121, Candeal⁻Salvador-BA 40296-710, Brazil. milena@bahia.fiocruz.br.
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  • 2018-12-23
Published in:
  • Molecules (Basel, Switzerland). - 2018
Arrabidaea brachypoda
Leishmania
flavonoids
high content
Amphotericin B
Animals
Antiprotozoal Agents
Bignoniaceae
Flavonoids
Leishmania
Mice
Mice, Inbred BALB C
Microscopy, Electron
Molecular Structure
English Leishmaniasis are diseases caused by parasites belonging to Leishmania genus. The treatment with pentavalent antimonials present high toxicity. Secondary line drugs, such as amphotericin B and miltefosine also have a narrow therapeutic index. Therefore, there is an urgent need to develop new drugs to treat leishmaniasis. Here, we present the in vitro anti-leishmanial activity of unusual dimeric flavonoids purified from Arrabidaea brachypoda. Three compounds were tested against Leishmana sp. Compound 2 was the most active against promastigotes. Quantifying the in vitro infected macrophages revealed that compound 2 was also the most active against intracellular amastigotes of L. amazonensis, without displaying host cell toxicity. Drug combinations presented an additive effect, suggesting the absence of interaction between amphotericin B and compound 2. Amastigotes treated with compound 2 demonstrated alterations in the Golgi and accumulation of vesicles inside the flagellar pocket. Compound 2-treated amastigotes presented a high accumulation of cytoplasmic vesicles and a myelin-like structure. When administered in L. amazonensis-infected mice, neither the oral nor the topical treatments were effective against the parasite. Based on the high in vitro activity, dimeric flavonoids can be used as a lead structure for the development of new molecules that could be useful for structure-active studies against Leishmania.
Language
  • English
Open access status
gold
Identifiers
Persistent URL
https://sonar.ch/global/documents/43746
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