In vitro Action of Chloramphenicol and Chloramphenicol-Analogues on the Metabolism of Human Immature Red Blood Cells

Erslev, Allan J.; Iossifides, I.

doi:10.1159/000207232

Cited by 16 publications

(6 citation statements)

References 8 publications

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“…Soon after its discovery and subsequent synthesis, CAM became very popular due to its antimicrobial effectiveness and low cost. However, in the following years when CAM was issued for general clinical use, it was realized that CAM can cause hematological disorders like bone marrow depression and aplastic anemia [ 55 ]. While an irreversible and fatal aplastic anemia appeared to be a rare complication, probably caused by nitrobenzene metabolites of CAM that act on DNA [ 56 , 57 , 58 ], mild and reversible bone marrow suppression was found to occur quite frequently and was ascribed to a mitochondrial protein synthesis inhibition, particularly in cases in which underlying mitochondrial mutations favor CAM binding to mitochondrial ribosome (mitoribosome) [ 59 , 60 ].…”

Section: Side Effects Of Cammentioning

confidence: 99%

Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions

et al. 2016

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Chloramphenicol (CAM) is the D-threo isomer of a small molecule, consisting of a p-nitrobenzene ring connected to a dichloroacetyl tail through a 2-amino-1,3-propanediol moiety. CAM displays a broad-spectrum bacteriostatic activity by specifically inhibiting the bacterial protein synthesis. In certain but important cases, it also exhibits bactericidal activity, namely against the three most common causes of meningitis, Haemophilus influenzae, Streptococcus pneumoniae and Neisseria meningitidis. Resistance to CAM has been frequently reported and ascribed to a variety of mechanisms. However, the most important concerns that limit its clinical utility relate to side effects such as neurotoxicity and hematologic disorders. In this review, we present previous and current efforts to synthesize CAM derivatives with improved pharmacological properties. In addition, we highlight potentially broader roles of these derivatives in investigating the plasticity of the ribosomal catalytic center, the main target of CAM.

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Section: Side Effects Of Cammentioning

confidence: 99%

Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions

et al. 2016

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“…Non-competitive type of inhibition mechanism has also been found depending on factors such as the nature of substrate, ionic buffer, or inhibitor concentration [4,5,6]. Clinical uses of CAM are, however, limited due to the development of a typical antibiotic-resistance through targeted mutations [7] and specific problems related to hematological disorders such as aplastic anemia [8].…”

Section: Introductionmentioning

confidence: 99%

Incorporation of Chloramphenicol Loaded Hydroxyapatite Nanoparticles into Polylactide

Rivas

Pelechà

Franco

et al. 2019

IJMS

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Chloramphenicol (CAM) has been encapsulated into hydroxyapatite nanoparticles displaying different morphologies and crystallinities. The process was based on typical precipitation of solutions containing phosphate and calcium ions and the addition of CAM once the hydroxyapatite nuclei were formed. This procedure favored a disposition of the drug into the bulk parts of the nanoparticles and led to a fast release in aqueous media. Clear antibacterial activity was derived, being slightly higher for the amorphous samples due to their higher encapsulation efficiency. Polylactide (PLA) microfibers incorporating CAM encapsulated in hydroxyapatite nanoparticles were prepared by the electrospinning technique and under optimized conditions. Drug release experiments demonstrated that only a small percentage of the loaded CAM could be delivered to an aqueous PBS medium. This amount was enough to render an immediate bacteriostatic effect without causing a cytotoxic effect on osteoblast-like, fibroblasts, and epithelial cells. Therefore, the prepared scaffolds were able to retain CAM-loaded nanoparticles, being a reservoir that should allow a prolonged release depending on the polymer degradation rate. The studied system may have promising applications for the treatment of cancer since CAM has been proposed as a new antitumor drug.

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“…Chloramphenicol, rifampicin, and clindamycin have been shown to be bactericidal against the pneumococcus in models of meningitis without inducing autolysis. ,− Chloramphenicol serves as an excellent example of an ideal meningitis drug: highly bactericidal to major meningeal pathogens, nonlytic, rapid penetration into the CNS, oral bioavailability, and low prevalence of resistance. It was used in the clinic extensively in the past; however, it is currently discouraged due to the side effects of bone marrow suppression. − In pneumococcal infection models, the use of clindamycin to treat both sepsis and meningitis markedly improves CNS pathology ,, in part because clindamycin appears to induce programmed cell death pathways leading to filamentation rather than lysis . However, all protein synthesis inhibitors are not necessarily good meningitis drugs.…”

Section: The Future Of Antibiotics For Abmmentioning

confidence: 99%

Acute Bacterial Meningitis: Challenges to Better Antibiotic Therapy

Kietzman

Tuomanen

2019

ACS Infect. Dis.

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Bacterial meningitis is a medical emergency requiring highly bactericidal antibiotics to achieve cure. Many challenges exist to achieving optimal patient outcome. First, antibiotics must pass the blood brain barrier. Once in the subarachnoid space, achieving bactericidal therapy involves circumventing antibiotic resistance and, more commonly, antibiotic tolerance arising from the slow growth of bacteria in the nutrient poor cerebrospinal fluid. Finally, bactericidal therapy is most often bacteriolytic, and debris from lysis is highly inflammatory. Controlling damage from lytic products may require adjunctive therapy to prevent neuronal death. These challenges are an extreme example of the different requirements for treating infections in different body sites.

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In vitro Action of Chloramphenicol and Chloramphenicol-Analogues on the Metabolism of Human Immature Red Blood Cells

Cited by 16 publications

References 8 publications

Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions

Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions

Incorporation of Chloramphenicol Loaded Hydroxyapatite Nanoparticles into Polylactide

Acute Bacterial Meningitis: Challenges to Better Antibiotic Therapy

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