ArticleAntimicrobial agents and chemotherapy1999
The new ketolide HMR3647 accumulates in the azurophil granules of human polymorphonuclear cells.
Article in Antimicrobial agents and chemotherapy, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers, 1 of them a synthesis that pooled it.
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Who cites it
18 citing papers in PubMed, 1 synthesis or guideline pooled it, 54 citations in OpenAlex.
- Influential predictors of azithromycin pharmacokinetics: a systematic review of population pharmacokinetics.Annals of medicine · 2025Pooled it
- Intracellular Penetration and Effects of Antibiotics onAntibiotics (Basel, Switzerland) · 2019Review
- Macrolide derivatives reduce proinflammatory macrophage activation and macrophage-mediated neurotoxicity.CNS neuroscience & therapeutics · 2019Article
- Designing Molecular Probes To Prolong Intracellular Retention: Application to Nitroxide Spin Probes.Bioconjugate chemistry · 2016Article
- Killing of Staphylococcus aureus in murine macrophages by chloroquine used alone and in combination with ciprofloxacin or azithromycin.Journal of inflammation research · 2015Article
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- Ketolides--the modern relatives of macrolides : the pharmacokinetic perspective.Clinical pharmacokinetics · 2009Review
- Cellular uptake and efflux of azithromycin, erythromycin, clarithromycin, telithromycin, and cethromycin.Antimicrobial agents and chemotherapy · 2005Article
- Activity of telithromycin and comparators against bacterial pathogens isolated from 1,336 patients with clinically diagnosed acute sinusitis.Annals of clinical microbiology and antimicrobials · 2004Article
- Interaction of the new ketolide ABT-773 (cethromycin) with human polymorphonuclear neutrophils and the phagocytic cell line PLB-985 in vitro.Antimicrobial agents and chemotherapy · 2004Article
- Telithromycin.Drugs · 2004Review
- Quantitative analysis of gentamicin, azithromycin, telithromycin, ciprofloxacin, moxifloxacin, and oritavancin (LY333328) activities against intracellular Staphylococcus aureus in mouse J774 macrophages.Antimicrobial agents and chemotherapy · 2003Article
- The ketolides: a critical review.Drugs · 2002Review
- Telithromycin is active against Mycobacterium avium in mice despite lacking significant activity in standard in vitro and macrophage assays and is associated with low frequency of resistance during treatment.Antimicrobial agents and chemotherapy · 2001Article
- Uptake, transport, and delivery of antimicrobial agents by human polymorphonuclear neutrophils.Antimicrobial agents and chemotherapy · 2001Article
- Telithromycin.Drugs · 2001Article
- Activities of antimicrobial agents against intracellular pneumococci.Antimicrobial agents and chemotherapy · 2000Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
HMR3647 is a semisynthetic representative of a new group of drugs, the ketolides, derived from erythromycin A. Since macrolides have been shown to accumulate in human polymorphonuclear cells (PMNs), we have investigated the ability of the molecule HMR3647 to enter human PMNs as well as other cell types, such as peripheral blood mononuclear cells and cell lines of hematopoietic and nonhematopoietic origin. In these experiments, HMR3647 was compared to erythromycin A, azithromycin, clarithromycin, and roxithromycin. Our results show that HMR3647 is specifically trapped in PMNs, where it is concentrated up to 300 times. In addition, it is poorly released by these cells, 80% of the compound remaining cell associated after 2 h in fresh medium. By contrast, it is poorly internalized and quickly released by the other cell types studied. This differs from the results obtained with the macrolide molecules, which behaved similarly in the different cells studied. In addition, subcellular fractionation of PMNs allowed us to identify the intracellular compartment where HMR3647 was trapped. In PMNs, more than 75% of the molecule was recovered in the azurophil granule fraction. Similarly, in NB4 cells differentiated into PMN-like cells, almost 60% of the molecules accumulated in the azurophil granule fraction. In addition, when HMR3647 was added to disrupted PMNs, 63% accumulated in the azurophil granules. Therefore, this study shows that the ketolide HMR3647 specifically accumulates in PMN azurophil granules, thus favoring its delivery to bacteria phagocytosed in these cells.
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