The pH-responsive polymer prodrugs were designed to maintain sufficient stability in the bloodstream and promptly release the active drugs when entering the acidic microenvironments, such as tumor tissue and cells. This kind of polymer-drug conjugates has become increasingly intriguing given the specific advantages over traditional drug delivery system. In our work, dextran (Dex) was oxidized into aldehyde-functionalized Dex-CHO before conjugating with doxorubicin (DOX) via efficient Schiff base reaction. The amphiphilic product Dex-DOX aggregated into uniform spherical nanoparticle in aqueous condition. The imine bond in Dex-DOX stayed tough in neutral solution yet quickly fractured when pH was lowered, in which way DOX was locally released and functioned in tumor cells. Our findings proved that the newly-constructed Dex-DOX could obviously promote the pH-dependent drug release, highlight the cell uptake efficiency, and strengthen the antitumor ability toward mouse B16F10 melanoma. In addition, it also largely averted the adverse effects to vital organs, which guaranteed higher level of security. Therefore, Dex-DOX held great potential of becoming a qualified chemotherapeutic drug delivery system.
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http://dx.doi.org/10.1016/j.msec.2017.03.201 | DOI Listing |
RSC Med Chem
December 2024
Department of Pharmaceutical Chemistry, College of Pharmacy, The University of Mashreq Baghdad 10023 Iraq.
Many cancers have displayed resistance to chemotherapeutic drugs over the past few decades. EGFR has emerged as a leading target for cancer therapy inhibiting tumor angiogenesis. Besides, studies strongly suggest that blocking telomerase activity could be an effective way to control the growth of certain cancer cells.
View Article and Find Full Text PDFInorg Chem
January 2025
Department of Chemistry, University College of Science, University of Calcutta, 92 A.P.C. Road, Kolkata 700009, India.
The well-known inhibitory strength of 3d metal Schiff base complexes against urease enzymes has long been acknowledged, but their untapped potential to act as ureolytic mimics of active metallobiosites remained unexplored. To break the new ground, we present pyrrolidine-based mononuclear Ni(II)-azide complex {[NiL(HL)(N)]·1.5(HO)} using the N,N,O donor ligand, namely ()-4-bromo-2-(((2-(pyrrolidin-1-yl)ethyl)imino)methyl)phenol.
View Article and Find Full Text PDFMini Rev Med Chem
January 2025
Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru 81310, Johor, Malaysia.
Indole, a ubiquitous structural motif in bioactive compounds, has played a pivotal role in drug discovery. Among indole derivatives, indole-3-carboxaldehyde (I3A) has emerged as a particularly promising scaffold for the development of therapeutic agents. This review delves into the recent advancements in the chemical modification of I3A and its derivatives, highlighting their potential applications in various therapeutic areas.
View Article and Find Full Text PDFR Soc Open Sci
January 2025
Department of Industrial Chemistry, College of Natural and Applied Sciences, Addis Ababa Science and Technology University, PO Box 16417, Addis Ababa, Ethiopia.
The asymmetric Schiff base prepared from ethylenediamine and pyridine-2-carboxaldehyde reacts with Fe(ClO)·6HO to form the Fe(II) complex [FeL](ClO) with L = ,-diethyl-'-(pyridin-2-yl)methylene)ethane-1,2-diamine, where the Fe(III) starting material has been unexpectedly reduced to Fe(II). This complex was characterized by elemental analysis, infrared spectra, single crystal and powder X-ray diffraction measurements, variable temperature DC magnetic measurement and room temperature Mössbauer spectroscopy. The asymmetric ligand L coordinates in a tridentate fashion through its pyridyl, azomethine and amino nitrogen atoms, generating a distorted octahedral geometry around the central metal ion.
View Article and Find Full Text PDFInorg Chem
January 2025
School of Chemistry and Chemical Engineering, Northwestern Polytechnical University, Xi'an 710072, P. R. China.
Air-stable single-molecule magnets (SMMs) can be obtained by confining Dy ion in a coordination environment; however, most of the current efforts were focused on modifying the rigidity of the macrocycle ligand. Herein, we attempt to assemble air-stable SMMs based on macrocycles with a replaceable coordination site. By using an in situ 1 + 1 Schiff-base reaction of dialdehyde with diamine, three air-stable SMMs have been obtained in which one of the equatorial coordination sites can be varied from -NH- (for ), -O- (for ), and -NMe- (for ).
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