Antileishmanial activity of an indole alkaloid from Peschiera australis

• Published in: Antimicrobial agents and chemotherapy Vol. 45; no. 5; pp. 1349 - 1354
• Main Authors: DELORENZI, Jan Carlo, ATTIAS, Marcia, GATTASS, Cerli R, ANDRADE, Marcelo, REZENDE, Claudia, CUNHA PINTO, Angelo D. A, HENRIQUES, Amélia T, BOU-HABIB, Dumith C, SARAIVA, Elvira M. B
• Format: Journal Article
• Language: English
• Published: Washington, DC American Society for Microbiology 01.05.2001
• Subjects: Alkaloids - pharmacology; Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Antiprotozoal Agents - pharmacology; Biological and medical sciences; General pharmacology; Ibogaine - analogs & derivatives; indole alkaloids; Indoles - pharmacology; Leishmania - drug effects; Leishmania - ultrastructure; Leishmania amazonensis; Macrophages, Peritoneal - drug effects; Macrophages, Peritoneal - metabolism; Macrophages, Peritoneal - ultrastructure; Magnoliopsida - chemistry; mastigotes; Mechanisms of Action: Physiological Effects; Medical sciences; Mice; Nitric Oxide - metabolism; Peschiera australis; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Plant Extracts - chemistry; South America; Brazil; America; Kinetoplastida; Protozoa; Pharmacognosy; Rodentia; In vitro; Biological activity; Medicinal plant; Vertebrata; Alkaloid; Mammalia; Mouse; Animal; Nitric oxide; Leishmania; Parasiticid; Plant origin; Indole derivatives; Macrophage
• ISSN: 0066-4804; 1098-6596
• DOI: 10.1128/AAC.45.5.1349-1354.2001

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.