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Antiprotozoal compounds from Mikania periplocifolia (Asteraceae).
Laurella, Laura C; Elso, Orlando G; Rodriguez, Rachel Nápoles; Viecenz, Juan M; Alonso, María Rosario; Bontempi, Esteban J; Malchiodi, Emilio; Catalán, Cesar A N; Cazorla, Silvia I; Sülsen, Valeria P.
Affiliation
  • Laurella LC; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Cátedra de Farmacognosia, Buenos Aires, Argentina; CONICET - Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Buenos Aires, Argentina.
  • Elso OG; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Cátedra de Farmacognosia, Buenos Aires, Argentina.
  • Rodriguez RN; CONICET - Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Buenos Aires, Argentina.
  • Viecenz JM; Instituto Nacional de Parasitología, ANLIS "Carlos G. Malbrán", Buenos Aires, Argentina.
  • Alonso MR; CONICET - Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Buenos Aires, Argentina.
  • Bontempi EJ; Instituto Nacional de Parasitología, ANLIS "Carlos G. Malbrán", Buenos Aires, Argentina.
  • Malchiodi E; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Cátedra de Inmunología, Buenos Aires, Argentina; CONICET - Universidad de Buenos Aires, Instituto de Estudios de la Inmunidad Humoral (IDEHU), Buenos Aires, Argentina.
  • Catalán CAN; Instituto de Química Orgánica, Facultad de Bioquímica, Química y Farmacia, Universidad Nacional de Tucumán, San Miguel de Tucumán, Tucumán, Argentina.
  • Cazorla SI; CONICET - Centro de Referencia para Lactobacilos (CERELA), San Miguel de Tucumán, Argentina.
  • Sülsen VP; Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Cátedra de Farmacognosia, Buenos Aires, Argentina; CONICET - Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Buenos Aires, Argentina. Electronic address: vsulsen@ffyb.uba.ar.
Fitoterapia ; 167: 105499, 2023 Jun.
Article in En | MEDLINE | ID: mdl-37019368
ABSTRACT
Chagas disease, African trypanosomiasis and Leishmaniasis are neglected parasitic diseases which affect millions of people worldwide. In a previous work, we report the antiprotozoal activity of the dichloromethane extract of Mikania periplocifolia Hook. & Arn. (Asteraceae). The aim of this work was to isolate and identify the bioactive compounds present in the extract. The fractionation of the dichloromethane extract has led to the isolation of the sesquiterpene lactone miscandenin and the flavonoid onopordin, together with the sesquiterpene lactones mikanolide, dihydromikanolide and deoxymikanolide, which have previously shown antiprotozoal activity. Miscandenin and onopordin were assayed in vitro against Trypanosoma cruzi, T. brucei and Leishmania braziliensis. Miscandenin was active against T. cruzi trypomastigotes and amastigotes with IC50 values of 9.1 and 7.7 µg/ml, respectively. This sesquiterpene lactone and the flavonoid onopordin showed activity against T. brucei trypomastigotes (IC50 = 0.16 and 0.37 µg/ml) and L. braziliensis promastigotes (IC50 = 0.6 and 1.2 µg/ml), respectively. The CC50 values on mammalian cells were 37.9 and 53.4 µg/ml for miscandenin and onopordin, respectively. Besides, the pharmacokinetic and physicochemical properties of miscandenin were assessed in silico, showing a good drug-likeness profile. Our results highlight this compound as a promising candidate for further preclinical studies in the search of new drugs for the treatment of trypanosomiasis and leishmaniasis.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Sesquiterpenes / Trypanosoma cruzi / Leishmaniasis / Asteraceae / Mikania / Antiprotozoal Agents Limits: Animals / Humans Language: En Journal: Fitoterapia Year: 2023 Document type: Article Affiliation country: Argentina

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Sesquiterpenes / Trypanosoma cruzi / Leishmaniasis / Asteraceae / Mikania / Antiprotozoal Agents Limits: Animals / Humans Language: En Journal: Fitoterapia Year: 2023 Document type: Article Affiliation country: Argentina