In Vitro Schistosomicidal Activity of Balsaminol F and Karavilagenin C

Autor(es)

Ramalhete, Catia ^[1] ; Magalhaes, Lizandra G. ^[2] ; Rodrigues, Vanderlei ^[3] ; Mulhovo, Silva ^[4] ; Da Silva Filho, Ademar A. ^[5] ; Ferreira, Maria-Jose U. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Lisbon, Fac Farm, Res Inst Med & Pharmaceut Sci iMed UL, P-1649003 Lisbon - Portugal

^[2] Univ Franca, Nucleo Pesquisas Ciencias Exatas & Tecnol, Franca, SP - Brazil

^[3] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Bioquim & Imunol, Ribeirao Preto, SP - Brazil

^[4] Univ Pedagogica, Ctr Estudos Mocambicanos & Etnociencias, Maputo - Mozambique

^[5] Univ Fed Juiz de Fora, Fac Farm, Dept Ciencias Farmaceut, Juiz De Fora, MG - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Planta Medica; v. 78, n. 18, p. 1912-1917, DEC 2012.
• Citações Web of Science: 11

Resumo

Five cucurbitane-type triterpenes (1-5), previously isolated from the African medicinal plant Momordica balsamina, along with five ester derivatives (6-10) of karavilagenin C (2), were evaluated for their potential schistosomicidal activity against Schistosoma mansoni adult worms. The natural compounds were isolated from the ethyl acetate-soluble fraction of the methanol extract of the aerial parts of M. balsamina. In a preliminary study, a significant schistosomicidal activity was observed for both the crude methanol extract and the ethyl acetate fraction. The compounds responsible for the activity were found to be balsaminol F (1) and karavilagenin C (2) with LC50 values of 14.7 +/- 1.5 and 28.9 +/- 1.8 mu M, respectively, after 24 h of incubation (positive control praziquantel, LC50 = 1.2 +/- 0.1 mu M). Both compounds (1, 2), at 10-50 mu M, induced significant reductions in the motor activity of the worms and significantly decreased the egg production. Furthermore, they were able (at 10-100 mu M) to separate the adult worm pairs into male and female after 24 h. Compounds 3-5, bearing a sugar moiety as a substituent, and the acylated derivatives of karavilagenin C (6-10) were inactive, suggesting that the presence of free hydroxyl groups in the tetracyclic skeleton might be important for the activity. A correlation between activity and the molecular volume/weight of compounds was also found. (AU)

• Processo FAPESP: 06/60132-4 - Investigação das atividades esquistossomicida, tripanocida e leishmanicida de lignanas e neolignanas obtidas por acoplamento oxidativo in vitro de fenilpropanóides
• Beneficiário: Ademar Alves da Silva Filho
• Modalidade de apoio: Auxílio à Pesquisa - Jovens Pesquisadores