Drug repositioning: antiprotozoal activity of terfenadine against Entamoeba histolytica trophozoites

Amebiasis caused by Entamoeba histolytica is nowadays a serious public health problem worldwide, especially in developing countries. Annually, up to 100,000 deaths occur across the world. Due to the resistance that pathogenic protozoa exhibit against commercial antiprotozoal drugs, a growing emphasis has been placed on plants used in traditional medicine to discover new antiparasitics. Previously, we reported the in vitro antiamoebic activity of a methanolic extract of Lippia graveolens Kunth (Mexican oregano). In this study, we outline the isolation and structure elucidation of antiamoebic compounds occurring in this plant. The subsequent work-up of this methanol extract by bioguided isolation using several chromatographic techniques yielded the flavonoids pinocembrin (1), sakuranetin (2), cirsimaritin (3), and naringenin (4). Structural elucidation of the isolated compounds was achieved by spectroscopic/spectrometric analyses and comparing literature data. These compounds revealed significant antiprotozoal activity against E. histolytica trophozoites using in vitro tests, showing a 50% inhibitory concentration (IC50) ranging from 28 to 154 µg/mL. Amebicide activity of sakuranetin and cirsimaritin is reported for the first time in this study. These research data may help to corroborate the use of this plant in traditional Mexican medicine for the treatment of dyspepsia.

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Evaluation of the antiprotozoal activity of neo-clerodane type diterpenes from Salvia polystachya against Entamoeba histolytica and Giardia lamblia

Phytotherapy Research ◽

10.1002/ptr.2938 ◽

2009 ◽

Vol 24 (5) ◽

pp. 662-665 ◽

Cited By ~ 8

Author(s):

Fernando Calzada ◽

Lilian Yepez-Mulia ◽

Amparo Tapia-Contreras ◽

Elihú Bautista ◽

Emma Maldonado ◽

...

Keyword(s):

Entamoeba Histolytica ◽

Giardia Lamblia ◽

Antiprotozoal Activity

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In vitro antiprotozoal activity from the roots of Geranium mexicanum and its constituents on Entamoeba histolytica and Giardia lamblia

Journal of Ethnopharmacology ◽

10.1016/j.jep.2005.01.019 ◽

2005 ◽

Vol 98 (1-2) ◽

pp. 191-193 ◽

Cited By ~ 43

Author(s):

Fernando Calzada ◽

J. Antonio Cervantes-Martínez ◽

Lilian Yépez-Mulia

Keyword(s):

Entamoeba Histolytica ◽

Giardia Lamblia ◽

Antiprotozoal Activity

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Antiprotozoal activity against Entamoeba histolytica of furocoumarins isolated from Ruta chalepensis

Planta Medica ◽

10.1055/s-0036-1596528 ◽

2016 ◽

Vol 81 (S 01) ◽

pp. S1-S381

Author(s):

R Quintanilla-Licea ◽

BD Mata-Cárdenas ◽

J Vargas-Villarreal ◽

AF Bazaldúa-Rodríguez ◽

MJ Verde-Star

Keyword(s):

Entamoeba Histolytica ◽

Antiprotozoal Activity ◽

Ruta Chalepensis

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Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning

PLoS ONE ◽

10.1371/journal.pone.0135556 ◽

2015 ◽

Vol 10 (8) ◽

pp. e0135556 ◽

Cited By ~ 39

Author(s):

Marcel Kaiser ◽

Pascal Mäser ◽

Leela Pavan Tadoori ◽

Jean-Robert Ioset ◽

Reto Brun

Keyword(s):

Drug Repositioning ◽

Antiprotozoal Activity ◽

Activity Profiling ◽

Starting Point ◽

Approved Drugs

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Thienopyrimidine sulphonamide hybrids: design, synthesis, antiprotozoal activity and molecular docking studies

RSC Advances ◽

10.1039/c6ra15181g ◽

2016 ◽

Vol 6 (93) ◽

pp. 90371-90383 ◽

Cited By ~ 5

Author(s):

Saadia Leeza Zaidi ◽

Subhash M. Agarwal ◽

Porntip Chavalitshewinkoon-Petmitr ◽

Thidarat Suksangpleng ◽

Kamal Ahmad ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Molecular Docking ◽

Entamoeba Histolytica ◽

Docking Studies ◽

Antiprotozoal Activity ◽

Design Synthesis ◽

Molecular Docking Studies ◽

Hybrid Compounds

A series of hybrid compounds containing the thienopyrimidine scaffold with sulphonamide piperazine skeleton were synthesized and evaluated against K1 strain of Plasmodium falciparum and the HM1:1MSS strain of Entamoeba histolytica, respectively

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Furanocoumarins from Ruta chalepensis with Amebicide Activity

Molecules ◽

10.3390/molecules26123684 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3684

Author(s):

Aldo Fabio Bazaldúa-Rodríguez ◽

Ramiro Quintanilla-Licea ◽

María Julia Verde-Star ◽

Magda Elizabeth Hernández-García ◽

Javier Vargas-Villarreal ◽

...

Keyword(s):

Traditional Medicine ◽

Entamoeba Histolytica ◽

Public Health Issue ◽

In Vitro Tests ◽

High Morbidity ◽

Antiprotozoal Activity ◽

Meoh Extract ◽

Ruta Chalepensis ◽

Medicinal Treatment

Entamoeba histolytica (protozoan; family Endomoebidae) is the cause of amoebiasis, a disease related to high morbidity and mortality. Nowadays, this illness is considered a significant public health issue in developing countries. In addition, parasite resistance to conventional medicinal treatment has increased in recent years. Traditional medicine around the world represents a valuable source of alternative treatment for many parasite diseases. In a previous paper, we communicated about the antiprotozoal activity in vitro of the methanolic (MeOH) extract of Ruta chalepensis (Rutaceae) against E. histolytica. The plant is extensively employed in Mexican traditional medicine. The following workup of the MeOH extract of R. chalepensis afforded the furocoumarins rutamarin (1) and chalepin (2), which showed high antiprotozoal activity on Entamoeba histolytica trophozoites employing in vitro tests (IC50 values of 6.52 and 28.95 µg/mL, respectively). Therefore, we offer a full scientific report about the bioguided isolation and the amebicide activity of chalepin and rutamarin.

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Erythrophagocytosis by Entamoeba histolytica.- Ultrastructural Study

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100094036 ◽

1972 ◽

Vol 30 ◽

pp. 156-157 ◽

Cited By ~ 1

Author(s):

Norberto Treviño ◽

Alfredo Feria-Velasco ◽

I. Ruiz de Chávez

Keyword(s):

Electron Microscopy ◽

Light Microscopy ◽

Entamoeba Histolytica ◽

Ultrastructural Study ◽

Saline Solution ◽

Physiological Saline ◽

Ultrastructural Level ◽

Hot Plate ◽

Physiological Saline Solution ◽

Axenic Conditions

Although erythrophagocytosis by various species of Entamoeba is a well known phenomenon this has not yet been studied in detail at the ultrastructural level. The present work deals with the description of the incorporation process of erythrocytes by trophozoites of E. histolytica. For this study, trophozoites of E. histolytica, HK-9:NIH strain cultured in axenic conditions and washed human erythrocytes were placed on a hot plate at 37°C in physiological saline solution. After 5 minutes, 2.5% glutarldehyde was added and the samples were processed according to conventional techniques for electron microscopy.Based upon light microscopy studies on living trophozoites in contact with erythrocytes, it seems that erythrophagocytosis only takes place in one pole of the parasite.

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Scanning electron microscopy of erythrophagocytosis by Entamoeba histolytica trophozoites

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s042482010012480x ◽

1992 ◽

Vol 50 (1) ◽

pp. 880-881

Author(s):

Victor Tsutsumi ◽

Adolfo Martinez-Palomo ◽

Kyuichi Tanikawa

Keyword(s):

Electron Microscopy ◽

Scanning Electron Microscopy ◽

Red Blood Cells ◽

Entamoeba Histolytica ◽

Causative Agent ◽

Blood Cells ◽

Protozoan Parasite ◽

Complex Phenomenon ◽

Great Capacity ◽

Scanning Electron

The protozoan parasite Entamoeba histolytica is the causative agent of amebiasis in man. The trophozoite or motile form is a highly dynamic and pleomorphic cell with a great capacity to destroy tissues. Moreover, the parasite has the singular ability to phagocytize a variety of different live or death cells. Phagocytosis of red blood cells by E. histolytica trophozoites is a complex phenomenon related with amebic pathogenicity and nutrition.

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