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Natural Product Research: Formerly Natural Product Letters Publication details, including instructions for authors and subscription information: http://www.tandfonline.com/loi/gnpl20
In vitro antiplasmodial activity, cytotoxicity and chemical profiles of sponge species of Cuban coasts a
b
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Judith Mendiola , Erik L. Regalado , Alexis Díaz-García , Olivier d
a
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P. Thomas , Aymé Fernández-Calienes , Hermis Rodríguez , Abilio b
Laguna & Olga Valdés
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Department of Parasitology and Cellular Cultures Laboratory, Institute of Tropical Medicine ‘Pedro Kourí’ (IPK), Autopista Novia del Mediodía km 6 1/2, PO Box 601, Marianao 13, Havana, Cuba b
Department of Chemistry, Center of Marine Bioproducts (CEBIMAR), Loma y 37, Alturas del Vedado, C.P. 10400, Havana, Cuba c
Biological and Pharmaceutical Laboratories (Labiofam), Ave Independencia km 16 1/2, Boyeros, Havana, Cuba d
Université de Nice-Sophia Antipolis, Institut de Chimie de Nice UMR 7272 CNRS – PCRE, Faculté des Science, Parc Valrose, 06108, Nice Cedex 02, France Published online: 04 Dec 2013.
To cite this article: Judith Mendiola, Erik L. Regalado, Alexis Díaz-García, Olivier P. Thomas, Aymé Fernández-Calienes, Hermis Rodríguez, Abilio Laguna & Olga Valdés , Natural Product Research (2013): In vitro antiplasmodial activity, cytotoxicity and chemical profiles of sponge species of Cuban coasts, Natural Product Research: Formerly Natural Product Letters, DOI: 10.1080/14786419.2013.861835 To link to this article: http://dx.doi.org/10.1080/14786419.2013.861835
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Natural Product Research, 2013 http://dx.doi.org/10.1080/14786419.2013.861835
In vitro antiplasmodial activity, cytotoxicity and chemical profiles of sponge species of Cuban coasts Judith Mendiolaa*, Erik L. Regaladob, Alexis Dı´az-Garcı´ac, Olivier P. Thomasd, Ayme´ Ferna´ndez-Calienesa, Hermis Rodrı´gueza, Abilio Lagunab and Olga Valde´sb
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a
Department of Parasitology and Cellular Cultures Laboratory, Institute of Tropical Medicine ‘ Pedro Kourı´’ (IPK), Autopista Novia del Mediodı´a km 6 1/2, PO Box 601, Marianao 13, Havana, Cuba; b Department of Chemistry, Center of Marine Bioproducts (CEBIMAR), Loma y 37, Alturas del Vedado, C.P. 10400 Havana, Cuba; cBiological and Pharmaceutical Laboratories (Labiofam), Ave Independencia km 16 1/2, Boyeros, Havana, Cuba; dUniversite´ de Nice-Sophia Antipolis, Institut de Chimie de Nice UMR 7272 CNRS – PCRE, Faculte´ des Science, Parc Valrose, 06108 Nice Cedex 02, France (Received 6 May 2013; final version received 30 October 2013) Aqueous and organic fractions from the crude extracts of 17 sponge species collected at Boca de Calderas, Havana, Cuba were analysed. The organic fractions of Mycale laxissima, Clathria echinata and Agelas cerebrum exhibited values of concentrations causing 50% inhibition of in vitro growth of Plasmodium berghei (IC50) of 42.3 ^ 5.1, 52 ^ 9.7 and 60.3 ^ 10.6 mg/mL, respectively, while their selectivity indexes for fibroblast cell lines were 9.45, 4.24 and 8.7, correspondingly. These fractions reduced parasitemia of infected Balb/c mice as well. Selective cytotoxicity indexes against tumour HeLa cells focused an interest on the aqueous fraction of M. laxissima (. 7.12) and organic fractions of Polymastia nigra (5.95), A. cerebrum (5.48) and Niphates erecta (.4.2). Triterpenoids/steroids and alkaloids detected in the organic fractions of M. laxissima, C. echinata and A. cerebrum should be isolated for future investigation. Keywords: Plasmodium berghei; Agelas; Clathria; Niphates; Mycale; Polymastia
1. Introduction Parasite resistance to antimalarial medicines and mosquito resistance to insecticides are major threats for the control of malaria in endemic countries. In addition to the focus on case management of uncomplicated and severe malaria, there are other key challenges in the context of malaria eradication for the continuing need to develop new antimalarials or to modify existing antimalarials (Anthony et al. 2012). Prominently, the concern about the drop of efficacy of artemisinin derivatives in the near future is present (WHO 2010). In view of their proven use, rodent models remain a standard part of the drug discovery and development pathway. When using rodent models for in vivo antiplasmodial evaluations of compounds, several key variables need to be considered during experimental design and interpretation. Most important is the choice of rodent malaria species and mouse strains (Fidock et al. 2004). The host immune system and drug pharmacokinetics have to be also considered (Somsak et al. 2011). Therefore, in vitro schizont maturation assays of Plasmodium berghei allow the assessment of intrinsic antimalarial activity, without interference of host factors. It is important to note that the drug sensitivity of a given rodent malaria species does not always mirror that of Plasmodium falciparum, but are mostly shared (Janse & Waters 1995; Fidock et al. 2004; Orjuela-Sa´nchez et al. 2012).
*Corresponding author. Email:
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results. Indeed, these fractions produced important and direct effects against parasites in line with endpoint criteria for plant extracts. Antitumoural compounds could be isolated concurrently in these sources. The initial chemical characterisation of M. laxissima, A. cerebrum and C. echinata organic fractions promotes future investigation of new antimalarial and antitumoural substances. Supplementary material Supplementary material relating to this article is available online, including Experimental section, Tables S1 and S2 and Figures S1– S6.
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