ArticleLipids2007
Inward translocation of the phospholipid analogue miltefosine across Caco-2 cell membranes exhibits characteristics of a carrier-mediated process.
Article in Lipids, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 34 citations in OpenAlex.
- Population pharmacokinetics of a combination of miltefosine and paromomycin in Eastern African children and adults with visceral leishmaniasis.The Journal of antimicrobial chemotherapy · 2023Trial
- Simultaneous population pharmacokinetic modelling of plasma and intracellular PBMC miltefosine concentrations in New World cutaneous leishmaniasis and exploration of exposure-response relationships.The Journal of antimicrobial chemotherapy · 2018Trial
- Optimal dosing of miltefosine in children and adults with visceral leishmaniasis.Antimicrobial agents and chemotherapy · 2012Trial
- Determining tissue distribution of the oral antileishmanial agent miltefosine: a physiologically-based pharmacokinetic modeling approach.Antimicrobial agents and chemotherapy · 2024Article
- Skin pharmacokinetics of miltefosine in the treatment of post-kala-azar dermal leishmaniasis in South Asia.The Journal of antimicrobial chemotherapy · 2024Article
- Characterizing the non-linear pharmacokinetics of miltefosine in paediatric visceral leishmaniasis patients from Eastern Africa.The Journal of antimicrobial chemotherapy · 2020Article
- Structure and Antiparasitic Activity Relationship of Alkylphosphocholine Analogues againstMicroorganisms · 2020Article
- Functional Validation of ABCA3 as a Miltefosine Transporter in Human Macrophages: IMPACT ON INTRACELLULAR SURVIVAL OF LEISHMANIA (VIANNIA) PANAMENSIS.The Journal of biological chemistry · 2016Article
- Naegleria fowleri: pathogenesis, diagnosis, and treatment options.Antimicrobial agents and chemotherapy · 2015Review
- Quantification of miltefosine in peripheral blood mononuclear cells by high-performance liquid chromatography-tandem mass spectrometry.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2015Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Miltefosine (hexadecylphosphocholine, HePC) is the first effective oral agent for the treatment of visceral leishmaniasis. The characteristics of HePC incorporation into the human intestinal epithelial cell line Caco-2 were investigated in order to understand its oral absorption mechanism. The results provide evidence for the involvement of a carrier-mediated mechanism, since the association of HePC at the apical pole of Caco-2 cells was (1) saturable as a function of time with a rapid initial incorporation over 5 min followed by a more gradual increase; (2) saturable as a function of concentration over the range studied (2-200 microM) with a saturable component which followed Michaelis-Menten kinetics (apparent K (m) 15.7 micromol/L, V (max) 39.2 nmol/mg protein/h) and a nonspecific diffusion component; (3) partially inhibited by low temperature and ATP depletion, indicating the temperature and energy-dependence of the uptake process. Moreover, we demonstrated, by an albumin back-extraction method, that HePC is internalized via translocation from the outer to the inner leaflet of the plasma membrane and that HePC may preferentially diffuse through intact raft microdomains. In conclusion, our results suggest that incorporation of HePC at the apical membrane of Caco-2 cells may occur through a passive diffusion followed by a translocation in the inner membrane leaflet through an active carrier-mediated mechanism.
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