Antileishmanial activity of an indole alkaloid from Peschiera australis.
In this study, we show the leishmanicidal effects of a chloroform fraction (CLF) and a purified indole alkaloid obtained from crude stem extract of Peschiera australis against Leishmania amazonensis, a causative agent of cutaneous leishmaniasis in the New World. In a bioassay-guided chemical fractionation, the leishmanicidal activity in CLF completely and irreversibly inhibited promastigote growth. This fraction was also active against amastigotes in infected murine macrophages. Chemical analysis of CLF identified an iboga-type indole alkaloid coronaridine as one of its major compounds. Coronaridine showed potent antileishmanial activity, inhibiting promastigote and amastigote growth. Promastigotes and amastigotes treated with CLF or coronaridine showed pronounced alterations in their mitochondria as assessed by transmission electron microscopy.
Delorenzi
J C
JC
Laboratório de Imunobiologia das Leishmanioses, Departamento de Imunologia-Instituto de Microbiologia, Rio de Janeiro, RJ, Brazil.
Attias
M
M
Gattass
C R
CR
Andrade
M
M
Rezende
C
C
da Cunha Pinto
A
A
Henriques
A T
AT
Bou-Habib
D C
DC
Saraiva
E M
EM
D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D007050:Ibogaine / Q000031:analogs & derivatives; D007211:Indoles / Q000494:pharmacology*; D007891:Leishmania / Q000187:drug effects* / Q000648:ultrastructure; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D019684:Magnoliopsida / Q000737:chemistry*; D051379:Mice; D009569:Nitric Oxide / Q000378:metabolism; D010936:Plant Extracts / Q000737:chemistry
D000470:Alkaloids; D000981:Antiprotozoal Agents; D007211:Indoles; D010936:Plant Extracts; D009569:Nitric Oxide; D007050:Ibogaine; C011734:coronardine