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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Vendrametto, Michele Cristina Santos, Adriana Oliveira dos Nakamura, Celso Vataru Dias Filho, Benedito Prado Cortez, Diógenes Aparício Garcia Ueda-Nakamura, Tânia |
| Description | Country affiliation: Brazil Author Affiliation: Vendrametto MC ( Programa de Pós-graduação em Ciências Farmacêuticas, Departamento de Análises Clínicas, Universidade Estadual de Maringá, Av. Colombo 5790, Paraná, Brazil.) |
| 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. |
| File Format | HTM / HTML |
| ISSN | 13835769 |
| Issue Number | 2 |
| Volume Number | 59 |
| e-ISSN | 18730329 |
| Journal | Parasitology International |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2010-06-01 |
| Publisher Place | Netherlands |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Parasitology Antiprotozoal Agents Pharmacology Benzofurans Leishmania Drug Effects Phenols Piper Chemistry Plant Leaves Animals Isolation & Purification Toxicity Cell Line Cells, Cultured Dose-response Relationship, Drug Classification Growth & Development Ultrastructure Leishmaniasis Drug Therapy Parasitology Macrophages Macrophages, Peritoneal Mice Mice, Inbred Balb C Microscopy, Electron, Transmission Parasitic Sensitivity Tests Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Infectious Diseases Parasitology |
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