Several aminomethylene analogs and a ketomethylene analog of reversins were synthesized in order to evaluate their ability to inhibit P-glycoprotein-mediated drug efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein. These analogs retained good activity compared to cyclosporin A and the original reversins.
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http://dx.doi.org/10.1016/j.bmcl.2006.07.059 | DOI Listing |
J Pharmacokinet Pharmacodyn
January 2025
Division of Systems Pharmacology and Pharmacy, Leiden Academic Center for Drug Research, Leiden University, Einsteinweg 55, Leiden, 2333 CC, The Netherlands.
P-glycoprotein (P-gp) is a key efflux transporter and may be involved in drug-drug interactions (DDIs) at the blood-brain barrier (BBB), which could lead to changes in central nervous system (CNS) drug exposure. Morphine is a P-gp substrate and therefore a potential victim drug for P-gp mediated DDIs. It is however unclear if P-gp inhibitors can induce clinically relevant changes in morphine CNS exposure.
View Article and Find Full Text PDFAdv Sci (Weinh)
December 2024
College of Chemistry and Molecular Sciences, Wuhan University, 299 Bayi Road, Wuhan, 430072, P. R. China.
Exosome-based drug delivery holds significant promise for cancer chemotherapy. However, current methods for loading drugs into exosomes are inefficient and cost-prohibitive for practical application. In this study, boron clusters are mixed with doxorubicin (DOX) and exosomes, enabling the efficient encapsulation of DOX into exosomes through a superchaotropic effect.
View Article and Find Full Text PDFJ Agric Food Chem
December 2024
Jilin Provincial Key Laboratory of Nutrition and Functional Food, College of Food Science and Engineering, Jilin University, Changchun 130062, China.
The fusion assembly strategy of supramolecular chemistry combined with dynamic covalent chemistry has provided novel insights into the design of precision nutrition and intelligent drug delivery carriers. This work involved the development of a supramolecular self-assembly originating from entropy- and enthalpy-driven dynamic covalent bonding on Schiff bases between egg white-derived peptide Gln-Ile-Gly-Leu-Phe (QIGLF) and glutaraldehyde (GA), denoted QIGLF-GA. The assembly exhibited outstanding assembly characteristics and multiwavelength autofluorescence properties.
View Article and Find Full Text PDFSci Rep
October 2024
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Damascus University, Damascus, Syria.
Chemotherapy for hepatoblastoma is limited by organ toxicity and poor outcomes, prompting the search for new, more effective treatments with minimal side effects. Vincristine sulfate, a potent chemotherapeutic, faces challenges due to P-glycoprotein-mediated resistance and its systemic toxicity. Nanoparticles offer a promising solution by improving pharmacokinetics, targeting tumor cells, thus reducing side effects.
View Article and Find Full Text PDFACS Nano
October 2024
Department of Ultrasound in Medicine, The Second Affiliated Hospital of Zhejiang University School of Medicine, No. 88 Jiefang Road, Shangcheng District, Hangzhou 310009, P. R. China.
Multidrug resistance (MDR) has emerged as a major barrier to effective breast cancer treatment, contributing to high rates of chemotherapy failure and disease recurrence. There is thus a pressing need to overcome MDR and to facilitate the efficient and precise treatment of breast cancer in a targeted manner. In this study, endogenous functional lipid droplets (IR780@LDs-FeO/OA) were developed and used to effectively overcome the limited diffusion distance of reactive oxygen species owing to their amenability to cascade-targeted delivery, thereby facilitating precise and effective sonodynamic therapy (SDT) for MDR breast cancer.
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