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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 AC, Cunha AC, Ceravolo IP, Gonçalves RA, Oliveira AJ, Krettli AU - Mem. Inst. Oswaldo Cruz (2015)

Bottom Line: Several species of Aspidosperma plants are used to treat diseases in the tropics, including Aspidosperma ramiflorum, which acts against leishmaniasis, an activity that is experimentally confirmed.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).This plant species is likely to be useful in the further development of an antimalarial drug, but its pharmacological evaluation is still required.

View Article: PubMed Central - PubMed

Affiliation: Centro de Pesquisas René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, MG, Brasil.

ABSTRACT
Several species of Aspidosperma plants 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, yellow peroba, coffee-peroba and matiambu, grows in the Atlantic Forest of Brazil in the South to the Southeast regions. Through a guided biofractionation of A. ramiflorum extracts, the plant activity against Plasmodium falciparum was 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 berghei in 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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flowchart fractionation of Aspidosperma ramiflorumusingacid base crude extract from stem bark of the plant. IC50: half-maximal druginhibitory concentration.
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f02: flowchart fractionation of Aspidosperma ramiflorumusingacid base crude extract from stem bark of the plant. IC50: half-maximal druginhibitory concentration.

Mentions: A crude extract of the plant leaves (20.4 g) was subjected to a simplified acid-basepartition employing the same solvents (Tanaka et al.2007). Two alkaloid rich fractions were obtained (the acid fraction and thebasic fraction) and were concentrated under reduced pressure at 40ºC for solventevaporation and then lyophilised (Cunha et al.2012) (Fig. 2).


Aspidosperma (Apocynaceae) plant cytotoxicity and activity towards malaria parasites. Part II: experimental studies withAspidosperma ramiflorum in vivo and in vitro.

Aguiar AC, Cunha AC, Ceravolo IP, Gonçalves RA, Oliveira AJ, Krettli AU - Mem. Inst. Oswaldo Cruz (2015)

flowchart fractionation of Aspidosperma ramiflorumusingacid base crude extract from stem bark of the plant. IC50: half-maximal druginhibitory concentration.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4660620&req=5

f02: flowchart fractionation of Aspidosperma ramiflorumusingacid base crude extract from stem bark of the plant. IC50: half-maximal druginhibitory concentration.
Mentions: A crude extract of the plant leaves (20.4 g) was subjected to a simplified acid-basepartition employing the same solvents (Tanaka et al.2007). Two alkaloid rich fractions were obtained (the acid fraction and thebasic fraction) and were concentrated under reduced pressure at 40ºC for solventevaporation and then lyophilised (Cunha et al.2012) (Fig. 2).

Bottom Line: Several species of Aspidosperma plants are used to treat diseases in the tropics, including Aspidosperma ramiflorum, which acts against leishmaniasis, an activity that is experimentally confirmed.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).This plant species is likely to be useful in the further development of an antimalarial drug, but its pharmacological evaluation is still required.

View Article: PubMed Central - PubMed

Affiliation: Centro de Pesquisas René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, MG, Brasil.

ABSTRACT
Several species of Aspidosperma plants 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, yellow peroba, coffee-peroba and matiambu, grows in the Atlantic Forest of Brazil in the South to the Southeast regions. Through a guided biofractionation of A. ramiflorum extracts, the plant activity against Plasmodium falciparum was 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 berghei in 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.

Show MeSH
Related in: MedlinePlus