Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil
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 promast...
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| Format: | Article |
| Language: | English |
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Sociedade Brasileira de Medicina Tropical (SBMT)
2011-10-01
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| Series: | Revista da Sociedade Brasileira de Medicina Tropical |
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| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0037-86822011000500007&lng=en&tlng=en |
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| author | Nadja Soares Vila-Nova Selen Maia de Morais Maria José Cajazeiras Falcão Lyeghyna Karla Andrade Machado Cláudia Maria Leal Beviláqua Igor Rafael Sousa Costa Nilce Viana Gramosa Pompeu de Sousa Brasil Heitor Franco de Andrade Júnior |
| author_facet | Nadja Soares Vila-Nova Selen Maia de Morais Maria José Cajazeiras Falcão Lyeghyna Karla Andrade Machado Cláudia Maria Leal Beviláqua Igor Rafael Sousa Costa Nilce Viana Gramosa Pompeu de Sousa Brasil Heitor Franco de Andrade Júnior |
| author_sort | Nadja Soares Vila-Nova |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-12T10:43:48Z |
| format | Article |
| id | doaj.art-90a6b09c235a4e80bca2497867876e05 |
| institution | Directory Open Access Journal |
| issn | 1678-9849 |
| language | English |
| last_indexed | 2024-04-12T10:43:48Z |
| publishDate | 2011-10-01 |
| publisher | Sociedade Brasileira de Medicina Tropical (SBMT) |
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| series | Revista da Sociedade Brasileira de Medicina Tropical |
| spelling | doaj.art-90a6b09c235a4e80bca2497867876e052022-12-22T03:36:30ZengSociedade Brasileira de Medicina Tropical (SBMT)Revista da Sociedade Brasileira de Medicina Tropical1678-98492011-10-0144556757110.1590/S0037-86822011000500007S0037-86822011000500007Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern BrazilNadja Soares Vila-Nova0Selen Maia de Morais1Maria José Cajazeiras Falcão2Lyeghyna Karla Andrade Machado3Cláudia Maria Leal Beviláqua4Igor Rafael Sousa Costa5Nilce Viana Gramosa Pompeu de Sousa Brasil6Heitor Franco de Andrade Júnior7Universidade Estadual do CearáUniversidade Estadual do CearáUniversidade Estadual do CearáUniversidade Estadual do CearáUniversidade Estadual do CearáUniversidade Estadual do CearáUniversidade Federal do CearáUniversidade de São PauloINTRODUCTION: 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.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0037-86822011000500007&lng=en&tlng=enLeishmanioseAlcaloide benzilisoquinolinicoAcetogeninaAnnona squamosaAnnona muricata |
| spellingShingle | Nadja Soares Vila-Nova Selen Maia de Morais Maria José Cajazeiras Falcão Lyeghyna Karla Andrade Machado Cláudia Maria Leal Beviláqua Igor Rafael Sousa Costa Nilce Viana Gramosa Pompeu de Sousa Brasil Heitor Franco de Andrade Júnior Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil Revista da Sociedade Brasileira de Medicina Tropical Leishmaniose Alcaloide benzilisoquinolinico Acetogenina Annona squamosa Annona muricata |
| title | Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil |
| title_full | Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil |
| title_fullStr | Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil |
| title_full_unstemmed | Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil |
| title_short | Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil |
| title_sort | leishmanicidal activity and cytotoxicity of compounds from two annonacea species cultivated in northeastern brazil |
| topic | Leishmaniose Alcaloide benzilisoquinolinico Acetogenina Annona squamosa Annona muricata |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0037-86822011000500007&lng=en&tlng=en |
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