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Aspidosperma (Apocynaceae) plant cytotoxicity and activity towards malaria parasites. Part II: experimental studies withAspidosperma ramiflorum in vivo and in vitro
Aguiar, Anna CC; Cunha, Ananda C; Ceravolo, Isabela Penna; Gonçalves, Regina A Correia; Oliveira, Arildo JB; Krettli, Antoniana Ursine.
  • Aguiar, Anna CC; Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte. BR
  • Cunha, Ananda C; Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte. BR
  • Ceravolo, Isabela Penna; Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte. BR
  • Gonçalves, Regina A Correia; Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte. BR
  • Oliveira, Arildo JB; Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte. BR
  • Krettli, Antoniana Ursine; Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte. BR
Mem. Inst. Oswaldo Cruz ; 110(7): 906-913, Nov. 2015. tab, graf
Article in English | LILACS | ID: lil-764592
ABSTRACT
Several species of Aspidospermaplants are used to treat diseases in the tropics, including Aspidosperma ramiflorum, which acts against leishmaniasis, an activity that is experimentally confirmed. The species, known as guatambu-yellow, yellowperoba, coffee-peroba andmatiambu, grows in the Atlantic Forest of Brazil in the South to the Southeast regions. Through a guided biofractionation of A. ramiflorumextracts, the plant activity against Plasmodium falciparumwas evaluated in vitro for toxicity towards human hepatoma G2 cells, normal monkey kidney cells and nonimmortalised human monocytes isolated from peripheral blood. Six of the seven extracts tested were active at low doses (half-maximal drug inhibitory concentration < 3.8 µg/mL); the aqueous extract was inactive. Overall, the plant extracts and the purified compounds displayed low toxicity in vitro. A nonsoluble extract fraction and one purified alkaloid isositsirikine (compound 5) displayed high selectivity indexes (SI) (= 56 and 113, respectively), whereas compounds 2 and 3 were toxic (SI < 10). The structure, activity and low toxicity of isositsirikine in vitro are described here for the first time in A. ramiflorum, but only the neutral and precipitate plant fractions were tested for activity, which caused up to 53% parasitaemia inhibition of Plasmodium bergheiin mice with blood-induced malaria. This plant species is likely to be useful in the further development of an antimalarial drug, but its pharmacological evaluation is still required.
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Full text: Available Index: LILACS (Americas) Main subject: Plasmodium berghei / Plasmodium falciparum / Plant Extracts / Aspidosperma / Antimalarials Limits: Animals / Humans Language: English Journal: Mem. Inst. Oswaldo Cruz Journal subject: Tropical Medicine / Parasitology Year: 2015 Type: Article / Project document Affiliation country: Brazil Institution/Affiliation country: Fundação Oswaldo Cruz/BR

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Full text: Available Index: LILACS (Americas) Main subject: Plasmodium berghei / Plasmodium falciparum / Plant Extracts / Aspidosperma / Antimalarials Limits: Animals / Humans Language: English Journal: Mem. Inst. Oswaldo Cruz Journal subject: Tropical Medicine / Parasitology Year: 2015 Type: Article / Project document Affiliation country: Brazil Institution/Affiliation country: Fundação Oswaldo Cruz/BR