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Evaluation of antileishmanial activity of eupomatenoid-5, a compound isolated from leaves of Piper regnellii var. pallescens.
- Source :
-
Parasitology international [Parasitol Int] 2010 Jun; Vol. 59 (2), pp. 154-8. Date of Electronic Publication: 2010 Jan 11. - Publication Year :
- 2010
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Abstract
- Infection with Leishmania spp. causes a disease with multifaceted clinical manifestations in humans. The treatment for leishmaniasis is dependent on a limited range of drugs. Here we investigated the antileishmanial activity of eupomatenoid-5, a neolignan isolated from leaves of Piper regnellii var. pallescens. We showed that eupomatenoid-5 had a dose-dependent activity during 72h of treatment, exhibiting IC(50) of 9.0microg/mL and 13.0microg/mL for promastigote and axenic amastigote forms, respectively, and IC(50) of 5.0microg/mL for intracellular amastigote forms of Leishmania amazonensis. When L. amazonensis was treated with eupomatenoid-5, it underwent considerable ultrastructural alterations, as shown by transmission electron microscopy. Among the alterations was the appearance of intense exocytic activity in the region of the flagellar pocket, myelin-like figures, and vacuoles in the cytoplasm of parasites treated with 9.0microg/mL. Cells treated with 25.0microg/mL showed a very large structure, apparently an extension of the endoplasmic reticulum. Also, mitochondrial swelling was detected at this concentration, indicating damage and significant change in this organelle. A cytotoxicity assay showed that the action of the isolated compound is more specific for protozoa and it is not toxic to macrophages. Our studies indicated that eupomatenoid-5 might be a potential new drug for the treatment of leishmaniasis, because this compound displays interesting antileishmanial activity in vitro against promastigote, axenic amastigote, and intracellular amastigote forms of L. amazonensis.
- Subjects :
- Animals
Antiprotozoal Agents chemistry
Antiprotozoal Agents isolation & purification
Antiprotozoal Agents toxicity
Benzofurans chemistry
Benzofurans isolation & purification
Benzofurans toxicity
Cell Line
Cells, Cultured
Dose-Response Relationship, Drug
Leishmania classification
Leishmania growth & development
Leishmania ultrastructure
Leishmaniasis drug therapy
Leishmaniasis parasitology
Macrophages drug effects
Macrophages, Peritoneal parasitology
Mice
Mice, Inbred BALB C
Microscopy, Electron, Transmission
Parasitic Sensitivity Tests
Phenols chemistry
Phenols isolation & purification
Phenols toxicity
Antiprotozoal Agents pharmacology
Benzofurans pharmacology
Leishmania drug effects
Phenols pharmacology
Piper chemistry
Plant Leaves chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1873-0329
- Volume :
- 59
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Parasitology international
- Publication Type :
- Academic Journal
- Accession number :
- 20064628
- Full Text :
- https://doi.org/10.1016/j.parint.2009.12.009