Quassinoids Exhibit Greater Selectivity Against Plasmodium Falciparum Than Against Entamoeba Histolytica, Giardia Intestinalis Or Toxoplasma Gondii In Vitro

1993 ◽  
Vol 40 (3) ◽  
pp. 244-246 ◽  
Author(s):  
COLIN W. WRIGHT ◽  
MARGARET M. ANDERSON ◽  
DAVID ALLEN ◽  
J. DAVID PHILLIPSON ◽  
GEOFFREY C. KIRBY ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Toxoplasma Gondii ◽  
Entamoeba Histolytica ◽  
Giardia Intestinalis

Parasitic Infections

2012 ◽  
pp. 190-217
Author(s):  
Jon E. Rosenblatt ◽  
Bobbi S. Pritt
Keyword(s):  
Plasmodium Falciparum ◽  
Toxoplasma Gondii ◽  
Entamoeba Histolytica ◽  
Giardia Lamblia ◽  
Babesia Microti ◽  
Parasitic Infections ◽  
Blastocystis Hominis ◽  
Different Types ◽  
Eukaryotic Organisms ◽  
Parasitic Worms

This chapter covers protozoa, helminths, and arthropods. 1. Protozoa are single-celled, microscopic eukaryotic organisms like amebae and Giardia. Helminths are parasitic worms including nematodes (roundworms), cestodes (tapeworms), and trematodes (flukes). Arthropods, like ticks and mites, are generally considered parasites. Specific organisms reviewed include Giardia lamblia, Cyclospora cayetanensis, Blastocystis hominis, Entamoeba histolytica, Plasmodium falciparum, Babesia microti, and Toxoplasma gondii. Diagnosis and treatment of different types of infection are also reviewed.

In Vitro Effect of Nitazoxanide Against Entamoeba histolytica, Giardia intestinalis and Trichomonas vaginalis Trophozoites

2002 ◽  
Vol 49 (3) ◽  
pp. 201-208 ◽  
Author(s):  
ROBERTO CEDILLO-RIVERA ◽  
BIBIANA CHAVEZ ◽  
ARTURO GONZALEZ-ROBLES ◽  
AMPARO TAPIA ◽  
LILIAN YEPEZ-MULIA
Keyword(s):  
Entamoeba Histolytica ◽  
Trichomonas Vaginalis ◽  
Giardia Intestinalis ◽  
Vitro Effect

scholarly journals Inhibition of Toxoplasma gondii and Plasmodium falciparum Infections in Vitro by NSC3852, a Redox Active Antiproliferative and Tumor Cell Differentiation Agent

2009 ◽  
Vol 95 (1) ◽  
pp. 215-223 ◽  
Author(s):  
Jeannine S. Strobl ◽  
Christopher W. Seibert ◽  
Yunbo Li ◽  
Rana Nagarkatti ◽  
Sheila M. Mitchell ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Cell Differentiation ◽  
Toxoplasma Gondii ◽  
Tumor Cell ◽  
Redox Active ◽  
Tumor Cell Differentiation

scholarly journals Ligands of the Peripheral Benzodiazepine Receptor Are Potent Inhibitors of Plasmodium falciparum and Toxoplasma gondii In Vitro

2002 ◽  
Vol 46 (10) ◽  
pp. 3197-3207 ◽  
Author(s):  
Florence Dzierszinski ◽  
Alexandra Coppin ◽  
Marlene Mortuaire ◽  
Etienne Dewailly ◽  
Christian Slomianny ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Toxoplasma Gondii ◽  
Morphological Changes ◽  
Synergistic Effects ◽  
Benzodiazepine Receptor ◽  
Peripheral Benzodiazepine Receptor ◽  
Parasite Resistance ◽  
Antimalarial Agents ◽  
Parasite Replication

ABSTRACT The increase in resistance of the malaria parasite Plasmodium falciparum to currently available drugs demands the development of new antimalarial agents. In this quest, we have found that ligands to the peripheral benzodiazepine receptor such as flurazepam, an agonist of the benzodiazepine family, and PK11195, an antagonist derived from isoquinoline, were active against Plasmodium falciparum. These two compounds effectively and rapidly inhibited parasite growth in vitro, irrespective of parasite resistance to chloroquine and mefloquine. Treatment with both drugs induced a sharp and consistent decline in parasitemia, a complete inhibition of parasite replication, and the destruction of parasites within the host red blood cells. Using electron microscopy, we showed that dramatic morphological changes, involving swollen endoplasmic reticulum and the reduction of hemozoin, were consistent with parasite death. The potent activities of flurazepam and PK11195 were also evaluated for antagonist or synergistic effects with currently used antimalarial drugs such as chloroquine and mefloquine. Moreover, flurazepam was found to be active against Toxoplasma gondii, another member of the phylum Apicomplexa. Taken together, our results indicated that benzodiazepines could be considered promising candidates in the treatment of both malaria and toxoplasmosis.

Synthesis and in vitro activities of ferrocenic aminohydroxynaphthoquinones against Toxoplasma gondii and Plasmodium falciparum

2006 ◽  
Vol 14 (5) ◽  
pp. 1294-1302 ◽  
Author(s):  
Apiwat Baramee ◽  
Alexandra Coppin ◽  
Marlène Mortuaire ◽  
Lydie Pelinski ◽  
Stanislas Tomavo ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Toxoplasma Gondii

scholarly journals Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii and anti-cancer molecules

2015 ◽  
Vol 80 (11) ◽  
pp. 1339-1359 ◽  
Author(s):  
Dejan Opsenica ◽  
Jelena Radivojevic ◽  
Ivana Matic ◽  
Tijana Stajner ◽  
Slavica Knezevic-Usaj ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Toxoplasma Gondii ◽  
Mononuclear Cells ◽  
Antimalarial Activity ◽  
Human Cancer ◽  
Subcutaneous Administration ◽  
Peripheral Blood Mononuclear ◽  
Normal Peripheral Blood ◽  
Apicomplexan Parasites

New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. Derivatives showed moderate nM range antimalarial activities and low cytotoxicity. N-phenyl-urea derivative 24 exhibited best resistant indices (RIW2 = 0.44, RITM91C235 = 0.80), and was not toxic against human normal peripheral blood mononuclear cells (IC50 > 200 ?M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukemia K562 cells. One compound, derivative 21 with a primary amino-group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another Apicomplexan parasite. Subcutaneous administration at a dose of 10 mg/kg/day for 8 days allowed survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of Apicomplexan parasites.

scholarly journals New paradigms for understanding and step changes in treating active and chronic, persistent apicomplexan infections

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Martin McPhillie ◽  
Ying Zhou ◽  
Kamal El Bissati ◽  
Jitender Dubey ◽  
Hernan Lorenzi ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Toxoplasma Gondii ◽  
Gold Standard ◽  
Parasitic Infection ◽  
Drug Resistant ◽  
Direct Impact ◽  
Active Infection ◽  
Standard Criterion

Abstract Toxoplasma gondii, the most common parasitic infection of human brain and eye, persists across lifetimes, can progressively damage sight, and is currently incurable. New, curative medicines are needed urgently. Herein, we develop novel models to facilitate drug development: EGS strain T. gondii forms cysts in vitro that induce oocysts in cats, the gold standard criterion for cysts. These cysts highly express cytochrome b. Using these models, we envisioned, and then created, novel 4-(1H)-quinolone scaffolds that target the cytochrome bc1 complex Qi site, of which, a substituted 5,6,7,8-tetrahydroquinolin-4-one inhibits active infection (IC50, 30 nM) and cysts (IC50, 4 μM) in vitro, and in vivo (25 mg/kg), and drug resistant Plasmodium falciparum (IC50, <30 nM), with clinically relevant synergy. Mutant yeast and co-crystallographic studies demonstrate binding to the bc1 complex Qi site. Our results have direct impact on improving outcomes for those with toxoplasmosis, malaria, and ~2 billion persons chronically infected with encysted bradyzoites.

Ultrastructural observations on the in vitro cytoadherence of Plasmodium falciparum infected red blood cells

1990 ◽  
Vol 48 (3) ◽  
pp. 914-915
Author(s):  
D.J.P. Ferguson ◽  
A.R. Berendt ◽  
J. Tansey ◽  
K. Marsh ◽  
C.I. Newbold
Keyword(s):  
Plasmodium Falciparum ◽  
Red Blood Cells ◽  
Blood Cells ◽  
Umbilical Vein ◽  
Cell Types ◽  
Amelanotic Melanoma ◽  
Cytoplasmic Process ◽  
Umbilical Vein Endothelial Cells

In human malaria, the most serious clinical manifestation is cerebral malaria (CM) due to infection with Plasmodium falciparum. The pathology of CM is thought to relate to the fact that red blood cells containing mature forms of the parasite (PRBC) cytoadhere or sequester to post capillary venules of various tissues including the brain. This in vivo phenomenon has been studied in vitro by examining the cytoadherence of PRBCs to various cell types and purified proteins. To date, three Ijiost receptor molecules have been identified; CD36, ICAM-1 and thrombospondin. The specific changes in the PRBC membrane which mediate cytoadherence are less well understood, but they include the sub-membranous deposition of electron-dense material resulting in surface deformations called knobs. Knobs were thought to be essential for cytoadherence, lput recent work has shown that certain knob-negative (K-) lines can cytoadhere. In the present study, we have used electron microscopy to re-examine the interactions between K+ PRBCs and both C32 amelanotic melanoma cells and human umbilical vein endothelial cells (HUVEC).We confirm previous data demonstrating that C32 cells possess numerous microvilli which adhere to the PRBC, mainly via the knobs (Fig. 1). In contrast, the HUVEC were relatively smooth and the PRBCs appeared partially flattened onto the cell surface (Fig. 2). Furthermore, many of the PRBCs exhibited an invagination of the limiting membrane in the attachment zone, often containing a cytoplasmic process from the endothelial cell (Fig. 2).

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