Planta Med 2014; 80 - P1L84
DOI: 10.1055/s-0034-1394741

Evaluation of the antiparasitic activities of extracts and glycoalkaloids isolated of the fruit of the Solanum lycocarpum

GZ Martins 1, M do Céu R Souza 2, RMB Cicarelli 3, CS Planeta 3, RRD Moreira 3
  • 1University Center of the Educational Foundation of Barretos, Barretos, 14783 – 226, São Paulo State, Brazil
  • 2Faculty of Pharmacy, University of Coimbra, 3030 – 548, Coimbra, Portugal
  • 3Department Natural Active Principles and Toxicology, Faculty of Pharmaceutical Sciences, State University Paulista, 14801 – 902, Araraquara, São Paulo State, Brazil

Solanum lycocarpum St. Hill. (Solanaceae) is a medicinal plant used as complementary therapy for the treatment of Diabetes Mellitus and hypertension [1]. These effects are attributed to glycoalkaloids: solamargine and solasonine [2]. The objective of this work was to isolate solasonine and solamargine of ripe fruits of S. lycocarpum and evaluate their antiparasitic and cytotoxicity activities. The crude 96% ethanol extract (CE), resulting fractions and glycoalkaloids were screened for their antiparasitic (Giardia lamblia, Leishmania infantum, Trypanosoma cruzi and Trypanosoma brucei) and cytotoxic activities (Macrophages, J774). The isolation of the glycoalkaloids was performed by chromatographic techniques. The crude extract (CE) was purified initially by liquid-liquid partition (40% ethanol: mixture hexane:EtOAC), of the 40% ethanol fraction (EF), six fractions were obtained with CC [neutral alumina, type 1 (5 × 20 cm), 40% ethanol], and of the fraction F2, nine fractions were obtained by TLC [silica gel 60 F254 (0,25 µm, 20 × 20 cm), n-butanol/acid acetic/water 6:3:1, detection: 10% H2SO4) and from the sub-fractions 2.5 and 2.7 were isolated solasonine (Rf = 0.46) and solamargine (Rf = 0.57). Their structures were identified by NMR 1H (500 MHz, 1 mg/mL, pyridine-d5). The CE extract, EF and fraction F2 (40% ethanol) showed activity for all parasites tested. Fraction F1 (40% ethanol) showed antiparasitic activity for G. lamblia, T. brucei and L. infantum. Fraction F3 (40% ethanol) showed activity against L. infantum. Solamargine showed activity for epimastigote of T. cruzi. A mixture (1:1) of solasonine and solamargine (SS) showed a synergistic action against G. lamblia and L. infantum. The CE extract and solasonine showed high toxicity to macrophages at low concentrations. The inverse was verified for solamargine and SS. Antiparasitic action found for CE extract, F2 fraction and SS showed to be promising for the development of new therapeutic agents.

Acknowledgements: CNPq/CsF (244.285/2012 – 8).

Keywords: Solanum lycocarpum, Giardia lamblia, Leishmania infantum, Trypanosoma cruzi, Trypanosoma brucei, glycoalkaloids.

References:

[1] Soares-Mota, M. R., Schwarz, A., Bernardi, M. M., Maiorka, P. C., Spinosa, H. S. Toxicological evaluation of 10% Solanum lycocarpum St Hill fruit consumption in the diet of growing rats: Hematological, biochemical and histopathological effects. Exp Toxicol Pathol, 2009, doi:10.1016/j.etp.2009.07.006.

[2] Martins, G. Z., Santos, A. N., Vilela M. V. R., Ferreira, M. C., Oliveira, W. P., Moreira, R. R. D. Optimization of extraction conditions and antioxidant activity of Solanum lycocarpum fruits. J Applied Sci, 2013, 13: 147 – 153.