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Apple-derived extracellular vesicles modulate the expression of human intestinal bile acid transporter ASBT/SLC10A2 via downregulation of transcription factor RAR α
CONCLUSIONS: Suppression of ASBT by APEVs was indirectly mediated by the downregulation of RARα, and its stability was lowered by microRNAs present in APEVs. This study suggested that macromolecules in food directly affect intestinal function by means of EVs that stabilize them and facilitate their cellular uptake.PMID:37517353 | DOI:10.1016/j.dmpk.2023.100512 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - July 30, 2023 Category: Drugs & Pharmacology Authors: Shinya Usui Qiunan Zhu Hisakazu Komori Yui Iwamoto Takumi Nishiuchi Yoshiyuki Shirasaka Ikumi Tamai Source Type: research

Development of a fluorescent-labeled trapping reagent to evaluate the risk posed by acyl-CoA conjugates
Drug Metab Pharmacokinet. 2023 Apr 10;52:100509. doi: 10.1016/j.dmpk.2023.100509. Online ahead of print.ABSTRACTAlthough acyl-CoA conjugates are known to have higher reactivity than acyl glucuronides, few studies have been conducted to evaluate the risk of the conjugates. In the present study, we aimed to develop a trapping assay for acyl-CoA conjugates using trapping reagents we have developed previously. It was revealed that Cys-Dan, which has both a thiol and an amino group, was the most effective in forming stable adducts containing an amide bond after intramolecular acyl migration. Additionally, we also developed a he...
Source: Drug Metabolism and Pharmacokinetics - July 29, 2023 Category: Drugs & Pharmacology Authors: Chikako Shibazaki Tadahiko Mashino Tomoyuki Ohe Source Type: research

Population pharmacokinetic modeling of treosulfan and rationale for dose recommendation in children treated for conditioning prior to allogeneic hematopoietic stem cell transplantation
Drug Metab Pharmacokinet. 2023 May 30;52:100515. doi: 10.1016/j.dmpk.2023.100515. Online ahead of print.ABSTRACTIntravenously infused treosulfan was evaluated in adult and pediatric patients for conditioning regimen prior to allogeneic hematopoietic stem cell transplantation. A population pharmacokinetic (PK) model was initially developed on 116 adult and pediatric PK profiles from historical trials, to support treosulfan dose recommendations for children in 2 prospective trials. The aim was to assess and update the initial population PK model by inclusion of additional 83 pediatric PK profiles from these 2 trials. The fin...
Source: Drug Metabolism and Pharmacokinetics - July 23, 2023 Category: Drugs & Pharmacology Authors: Xieran Li Krzysztof Kalwak Rita Beier Jochen Kehne Ann-Kristin M öller Joachim Baumgart Dietrich W Beelen Ralf A Hilger Ajay Vora Karl-Walter Sykora Source Type: research

Characterization of LysoTracker Red uptake by in  vitro model cells of the outer blood-retinal barrier: Implication of lysosomal trapping with cytoplasmic vacuolation and cytotoxicity
Drug Metab Pharmacokinet. 2023 Apr 23;51:100510. doi: 10.1016/j.dmpk.2023.100510. Online ahead of print.ABSTRACTLysosomal trapping, a physicochemical process in which lipophilic cationic compounds are sequestered in lysosomes, can affect drug disposition and cytotoxicity. To better understand lysosomal trapping at the outer blood-retinal barrier (BRB), we investigated the distribution of LysoTracker Red (LTR), a probe compound for lysosomal trapping, in conditionally immortalized rat retinal pigment epithelial (RPE-J) cells. LTR uptake by RPE-J cells was dependent on temperature and attenuated by ammonium chloride and prot...
Source: Drug Metabolism and Pharmacokinetics - July 14, 2023 Category: Drugs & Pharmacology Authors: Yuma Tega Toshinari Takeuchi Masatoshi Nagano Reina Makino Yoshiyuki Kubo Shin-Ichi Akanuma Ken-Ichi Hosoya Source Type: research