Activity of the Lupane isolated from Combretum leprosum against Leishmania amazonensis promastigotes

Journal of the Brazilian Chemical Society

Silva-Jardim, Izaltina¹  Fiocruz, Porto Velho, Brazil¹  Instituto de Pesquisas em Patologias Tropicais de Rondônia, Porto Velho, Brazil¹  Teles, Carolina B. G¹  Zuliani, Juliana P¹  Silva, Alexandre de A. E¹  Facundo, Valdir A¹  Moreira, Leandro S¹  Universidade Federal de Rondônia, Porto Velho, Brazil¹  Stábeli, Rodrigo G¹ 

关键词: promastigotes;    Leishmania amazonensis;    Combretum leprosum;    triterpene;    synthetic derivatives;   

DOI  :  10.1590/S0103-50532011000500017

学科分类：化学（综合）

来源: SciELO

【 摘 要 】

This paper describes the activity of the ethanolic extract (EE), obtained from the fruits of Combretum leprosum, the triterpene 3β, 6β, 16β-trihydroxylup-20(29)-ene (1) and its synthetic derivatives 1a-1d on Leishmania amazonensis promastigotes. The EE displayed leishmanicidal activity and the IC50 was 24.8 mg mL-1. However, the triterpene 3β, 6β, 16β-trihydroxylup-20(29)-ene (1), at a concentration of 5.0 mg mL-1, showed a potent inhibitory activity on promastigotes proliferation (IC50 = 3.3 mg mL-1). Among the synthetic derivatives, only (1b) and (1d) were active against promastigotes (IC50 = 3.48 mg mL-1and 5.8 mg mL-1, respectively). Moreover, the synthetic derivative 1a showed no activity on promastigotes of L. amazonensis. EE, (1) and the synthetic derivatives 1a-1d showed no cytotoxic effect on mice peritoneal macrophages. These results provide evidence that the ethanolic extract and the lupane isolated from C. leprosum was active against promastigotes of L. amazonensis, and may be used as a tool in the studies of new antileishmanial drugs.

【 授权许可】

Unknown