Antibiotics for prophylaxis of Plasmodium falciparum infections: in vitro activity of doxycycline against Senegalese isolates.

Pradines, Bruno; Spiegel, André; Rogier, Christophe; Tall, Adama; Mosnier, Joël; Fusaı̈, Thierry; Trape, Jean‐François; Parzy, Daniel

doi:10.4269/ajtmh.2000.62.82

Cited by 58 publications

(40 citation statements)

References 27 publications

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“…Moreover, it appears to act faster than any of the other tetracyclines, exhibiting the highest activity at Day 3. The IC 50 values of classic tetracyclines and clindamycin in this study are consistent with those from previous studies using a similar approach [6,[11][12][13]. This underlines that prolonged incubation is required to assess adequately the antimalarial potential of most antibiotics in vitro.…”

Section: Discussionsupporting

confidence: 90%

In vitro activity of tigecycline in Plasmodium falciparum culture-adapted strains and clinical isolates from Gabon

Held¹,

Zanger²,

Issifou³

et al. 2010

International Journal of Antimicrobial Agents

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In vitro activity of tigecycline in Plasmodium falciparum culture-adapted strains and clinical isolates from Gabon. International Journal of Antimicrobial Agents, Elsevier, 2010, 35 (6) This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. nM) for clindamycin. Tigecycline was found to act faster against plasmodia than any of the other antibiotics tested. This study demonstrates the potential of tetracycline derivatives in the development of improved antimalarials.

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Section: Discussionsupporting

confidence: 90%

In vitro activity of tigecycline in Plasmodium falciparum culture-adapted strains and clinical isolates from Gabon

Held¹,

Zanger²,

Issifou³

et al. 2010

International Journal of Antimicrobial Agents

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“…In this specific case, tests must be extended to include longer incubation periods since toxic effects that are effective during the first exposure cycle will only be fully detectable at the end of the second cycle. Removing drugs at 48 h allows verifying that the lethal target was exerted during the first cycle (11,33).…”

Section: Discussionmentioning

confidence: 99%

Reliability of Antimalarial Sensitivity Tests Depends on Drug Mechanisms of Action

Wein

Maynadier

et al. 2010

J Clin Microbiol

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In vitro antimalarial activity tests play a pivotal role in malaria drug research or for monitoring drug resistance in field isolates. We applied two isotopic tests, two enzyme-linked immunosorbent assays (ELISA) and the SYBR green I fluorescence-based assay, to test artesunate and chloroquine, the metabolic inhibitors atovaquone and pyrimethamine, our fast-acting choline analog T3/SAR97276, and doxycycline, which has a delayed death profile. Isotopic tests based on hypoxanthine and ethanolamine incorporation are the most reliable tests provided when they are applied after one full 48-h parasite cycle. The SYBR green assay, which measures the DNA content, usually requires 72 h of incubation to obtain reliable results. When delayed death is suspected, specific protocols are required with increasing incubation times up to 96 h. In contrast, both ELISA tests used (pLDH and HRP2) appear to be problematic, leading to disappointing and even erroneous results for molecules that do not share an artesunatelike profile. The reliability of these tests is linked to the mode of action of the drug, and the conditions required to get informative results are hard to predict. Our results suggest some minimal conditions to apply these tests that should give rise to a standard 50% inhibitory concentration, regardless of the mechanism of action of the compounds, and highlight that the most commonly used in vitro antimalarial activity tests do not have the same potential. Some of them might not detect the antimalarial potential of new classes of compounds with innovative modes of action, which subsequently could become promising new antimalarial drugs.Malaria is a major global health problem, with an estimated 250 to 300 million clinical cases annually and 3.3 billion people at risk, causing nearly a million deaths, mostly among children under 5 years old in sub-Saharan Africa (18, 47). The resistance of Plasmodium falciparum, the most deadly malaria parasite to most antimalarial drugs, is a major obstacle to the eradication of this disease (46). It is also of considerable concern in the light of a recent report on decreased sensitivity to artemesinin drugs in Southeast Asia (14, 28). New chemotherapeutic approaches are thus urgently needed, based on optimization of current drugs and, more importantly, on the discovery of new antimalarial drugs. The latter implies systematic screening of drug libraries, a series of natural compounds, or a structure-based drug design targeting novel targets. In all cases, in vitro evaluation of the thousands of new molecules for their antimalarial activity is an early and necessary step. This early step aims at detecting the antimalarial potential of individual or series of compounds. It is performed in vitro against P. falciparum laboratory strains and, at a later stage, against field isolates, including multidrug-resistant strains. Assays must provide a first indication on the potency of the pharmacological activity, usually expressed as the concentration required to inhibit the parasite viability ...

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“…Although omeprazole, clarithromycin, and amoxicillin (or metronidazole) are standard therapy, the role of tetracycline may increase as more clarithromycin-and methronidazole-resistant H. pylori isolates are encountered (303). Tetracyclines are active against malaria, and this has unexpectedly become important for prophlylaxis following the rapid increase of mefloquine-resistant P. falciparum strains (28,211,264). Table 6 provides a summary of current anti-infective applications of the tetracyclines in humans.…”

Section: Human Therapy and Prophylacticsmentioning

confidence: 99%

Tetracycline Antibiotics: Mode of Action, Applications, Molecular Biology, and Epidemiology of Bacterial Resistance

Chopra

Roberts

2001

Microbiol Mol Biol Rev

3,635

2,643

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Tetracyclines were discovered in the 1940s and exhibited activity against a wide range of microorganisms including gram-positive and gram-negative bacteria, chlamydiae, mycoplasmas, rickettsiae, and protozoan parasites. They are inexpensive antibiotics, which have been used extensively in the prophlylaxis and therapy of human and animal infections and also at subtherapeutic levels in animal feed as growth promoters. The first tetracycline-resistant bacterium, Shigella dysenteriae, was isolated in 1953. Tetracycline resistance now occurs in an increasing number of pathogenic, opportunistic, and commensal bacteria. The presence of tetracycline-resistant pathogens limits the use of these agents in treatment of disease. Tetracycline resistance is often due to the acquisition of new genes, which code for energy-dependent efflux of tetracyclines or for a protein that protects bacterial ribosomes from the action of tetracyclines. Many of these genes are associated with mobile plasmids or transposons and can be distinguished from each other using molecular methods including DNA-DNA hybridization with oligonucleotide probes and DNA sequencing. A limited number of bacteria acquire resistance by mutations, which alter the permeability of the outer membrane porins and/or lipopolysaccharides in the outer membrane, change the regulation of innate efflux systems, or alter the 16S rRNA. New tetracycline derivatives are being examined, although their role in treatment is not clear. Changing the use of tetracyclines in human and animal health as well as in food production is needed if we are to continue to use this class of broad-spectrum antimicrobials through the present century

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Antibiotics for prophylaxis of Plasmodium falciparum infections: in vitro activity of doxycycline against Senegalese isolates.

Cited by 58 publications

References 27 publications

In vitro activity of tigecycline in Plasmodium falciparum culture-adapted strains and clinical isolates from Gabon

In vitro activity of tigecycline in Plasmodium falciparum culture-adapted strains and clinical isolates from Gabon

Reliability of Antimalarial Sensitivity Tests Depends on Drug Mechanisms of Action

Tetracycline Antibiotics: Mode of Action, Applications, Molecular Biology, and Epidemiology of Bacterial Resistance

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