Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil

Revista da Sociedade Brasileira de Medicina Tropical

Nadja Soares Vila-nova²  Selen Maia De Morais²  Maria José Cajazeiras Falcão¹  Lyeghyna Karla Andrade Machado¹  Cláudia Maria Leal Beviláqua²  Igor Rafael Sousa Costa¹  Nilce Viana Gramosa Pompeu De Sousa Brasil¹  Heitor Franco De Andrade Júnior¹ 

[1] ,Universidade Estadual do Ceará Faculdade de Medicina Veterinária Programa de Pós-Graduação em Ciências VeterináriasFortaleza CE

关键词: Leishmaniasis;    Benzylisoquinolinic alkaloids;    Acetogenins;    Annona squamosa;    Annona muricata;    Leishmaniose;    Alcaloide benzilisoquinolinico;    Acetogenina;    Annona squamosa;    Annona muricata;   

DOI  :  10.1590/S0037-86822011000500007

来源: SciELO

【 摘 要 】

INTRODUCTION: Visceral leishmaniasis is endemic in 88 countries, with a total of 12 million people infected and 350 million at risk. In the search for new leishmanicidal agents, alkaloids and acetogenins isolated from leaves of Annona squamosa and seeds of Annona muricata were tested against promastigote and amastigote forms of Leishmania chagasi. METHODS: Methanol-water (80:20) extracts of A. squamosa leaves and A. muricata seeds were extracted with 10% phosphoric acid and organic solvents to obtain the alkaloid and acetogenin-rich extracts. These extracts were chromatographed on a silica gel column and eluted with a mixture of several solvents in crescent order of polarity. The compounds were identified by spectroscopic analysis. The isolated compounds were tested against Leishmania chagasi, which is responsible for American visceral leishmaniasis, using the MTT test assay. The cytotoxicity assay was evaluated for all isolated compounds, and for this assay, RAW 264.7 cells were used. RESULTS: O-methylarmepavine, a benzylisoquinolinic alkaloid, and a C37 trihydroxy adjacent bistetrahydrofuran acetogenin were isolated from A. squamosa, while two acetogenins, annonacinone and corossolone, were isolated from A. muricata. Against promastigotes, the alkaloid showed an IC50 of 23.3 µg/mL, and the acetogenins showed an IC50 ranging from 25.9 to 37.6 µg/mL; in the amastigote assay, the IC50 values ranged from 13.5 to 28.7 µg/mL. The cytotoxicity assay showed results ranging from 43.5 to 79.9 µg/mL. CONCLUSIONS: These results characterize A. squamosa and A. muricata as potential sources of leishmanicidal agents. Plants from Annonaceae are rich sources of natural compounds and an important tool in the search for new leishmanicidal therapies.

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