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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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major monoterpenoid indole alkaloids from Aspidospermaramiflorum. Drawing, displaying and characterising the chemicalstructures, substructures and reactions were performed using Marvin 5.4.1.1, 2011(ChemAxon) (chemaxon.com).
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f01: major monoterpenoid indole alkaloids from Aspidospermaramiflorum. Drawing, displaying and characterising the chemicalstructures, substructures and reactions were performed using Marvin 5.4.1.1, 2011(ChemAxon) (chemaxon.com).

Mentions: The extracts and compounds purified from Aspidospermaramiflorum(Apocynaceae), known as gua- tambu-yellow andyellowperoba, matiambu,matambu,guatambu-grande, peroba-caféandpequiá, are now being studied. The species is native in the Atlanticriver forests of Brazil from the South Region [states of Santa Catarina and Paraná (PR)] tothe Southeast Region [states of Rio de Janeiro and Minas Gerais (MG)]. Several plantfractions are active against Leishmania amazonensisparasites. Thecompounds responsible for the activity are the monoterpenoid indole alkaloids (Cunha et al. 2012), which are present in large amountsin the plant and were again isolated (Fig. 1) andstudied for activity against P. falciparum in vitro. Some extracts weretested against malaria in mice withPlasmodium berghei.


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)

major monoterpenoid indole alkaloids from Aspidospermaramiflorum. Drawing, displaying and characterising the chemicalstructures, substructures and reactions were performed using Marvin 5.4.1.1, 2011(ChemAxon) (chemaxon.com).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

f01: major monoterpenoid indole alkaloids from Aspidospermaramiflorum. Drawing, displaying and characterising the chemicalstructures, substructures and reactions were performed using Marvin 5.4.1.1, 2011(ChemAxon) (chemaxon.com).
Mentions: The extracts and compounds purified from Aspidospermaramiflorum(Apocynaceae), known as gua- tambu-yellow andyellowperoba, matiambu,matambu,guatambu-grande, peroba-caféandpequiá, are now being studied. The species is native in the Atlanticriver forests of Brazil from the South Region [states of Santa Catarina and Paraná (PR)] tothe Southeast Region [states of Rio de Janeiro and Minas Gerais (MG)]. Several plantfractions are active against Leishmania amazonensisparasites. Thecompounds responsible for the activity are the monoterpenoid indole alkaloids (Cunha et al. 2012), which are present in large amountsin the plant and were again isolated (Fig. 1) andstudied for activity against P. falciparum in vitro. Some extracts weretested against malaria in mice withPlasmodium berghei.

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