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• Martínez-Luis, S
• Gómez, J
• Spadafora, C
• Guzmán, H
• Gutiérrez, M
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• Martínez-Luis, S
• Gómez, J
• Spadafora, C
• Guzmán, H
• Gutiérrez, M
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• Martínez-Luis, S
• Gómez, J
• Spadafora, C
• Guzmán, H
• Gutiérrez, M

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Molecules 2012, 17(9), 11146-11155; doi:10.3390/molecules170911146

Article

Antitrypanosomal Alkaloids from the Marine Bacterium Bacillus pumilus

Sergio Martínez-Luis ¹ , José Félix Gómez ^1,2 , Carmenza Spadafora ³ , Héctor M. Guzmán ⁴  and Marcelino Gutiérrez ^1,*

¹ Center for Biodiversity and Drug Discovery, Institute for Scientific Research and High Technology Services, City of Knowledge, P.O. Box 0843-01103, Panama ² Departamento de Química, Centro de Investigación y de Estudios Avanzados del IPN, México D.F. 07360, Mexico ³ Center for Cellular and Molecular Biology of Diseases, Institute for Scientific Research and High Technology Services, City of Knowledge, P.O. Box 0843-01103, Panama ⁴ Smithsonian Tropical Research Institute, Balboa, Ancon, P.O. Box 0843-03092, Panama

* Author to whom correspondence should be addressed.

Received: 18 July 2012; in revised form: 6 September 2012 / Accepted: 7 September 2012 / Published: 18 September 2012

(This article belongs to the Section Natural Products)

Download PDF Full-Text [210 KB, uploaded 18 September 2012 08:35 CEST]

Abstract: Fractionation of the ethyl acetate extract of the marine bacterium Bacillus pumilus isolated from the black coral Antipathes sp. led to the isolation of five compounds: cyclo-(L-Leu-L-Pro) (1), 3-hydroxyacetylindole (2), N-acetyl-b-oxotryptamine (3), cyclo-(L-Phe-L-Pro) (4), and 3-formylindole (5). The structures of compounds 1−5 were established by spectroscopic analyses, including HRESITOF-MS and NMR (¹H, ¹³C, HSQC, HMBC and COSY). Compounds 2, 3 and 5 caused the inhibition on the growth of Trypanosoma cruzi (T. cruzi), with IC₅₀ values of 20.6, 19.4 and 26.9 μM, respectively, with moderate cytotoxicity against Vero cells. Compounds 1−5 were found to be inactive when tested against Plasmodium falciparum and Leishmania donovani, therefore showing selectivity against T. cruzi parasites.

Keywords: indole alkaloids; Trypanosoma cruzi; Bacillus pumilus; Chagas disease

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