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

Revista da Sociedade Brasileira de Medicina Tropical

Falcão, Maria José Cajazeiras¹  Andrade Júnior, Heitor Franco de¹  Beviláqua, Cláudia Maria Leal¹  Vila-Nova, Nadja Soares¹  Universidade Federal do Ceará, Fortaleza¹  Universidade Estadual do Ceará, Fortaleza¹  Costa, Igor Rafael Sousa¹  Machado, Lyeghyna Karla Andrade¹  Universidade Estadual do Ceará¹  Morais, Selen Maia de¹  Brasil, Nilce Viana Gramosa Pompeu de Sousa¹  Universidade de São Paulo, São Paulo¹ 

关键词: Leishmaniasis;    Benzylisoquinolinic alkaloids;    Acetogenins;    Annona squamosa;    Annona muricata;   

DOI  :  10.1590/S0037-86822011000500007

学科分类：农业科学（综合）

来源: Sociedade Brasileira de Medicina Tropical

【 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.

【 授权许可】

Unknown