In this study, we report a novel per-6-substituted β-cyclodextrin () featuring seven phosphoramidate moieties as an innovative host for inclusion. This structurally well-defined host has remarkable water solubility and was isolated in pure form. Analytical techniques such as NMR and ITC were used to probe the molecular interactions with different drug molecules. Our investigations revealed that host can form 2:1 inclusion complexes with various drugs. Further studies showed that the inclusions of drugs by β-CD host () are mostly enthalpy driven, highlighting the potential roles played by the phosphoramidate functionalities of the host. Comparatively, a per-O2, O3-acetylated analog () of compound was also obtained, which also shows unusual water solubility but diminished inclusion capability.
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http://dx.doi.org/10.3390/molecules29122714 | DOI Listing |
Chemistry
January 2025
Ulm University: Universitat Ulm, Organic Chemistry III, Albert-Einstein-Allee 11, 89081, Ulm, GERMANY.
The efficiency of kinase inhibiting cancer therapeutics is often limited by their poor solubility in water. PEGylation is one possible strategy to improve the solubility of the drug, however, means to cleave these after reaching the target is important to make use of the therapeutic effects of the native drug. Moreover, the length of the PEG chains will have an effect on the solubility and binding.
View Article and Find Full Text PDFHeliyon
January 2025
Department of Food Science and Technology, College of Agriculture, Isfahan University of Technology, 84156-83111, Isfahan, Iran.
Packaging films based on natural biopolymers often suffer from inadequate barrier and mechanical properties. To address these challenges, multilayer films have emerged as potential solutions. In this study, we prepared bilayer films using bitter vetch seed protein (BVSP) and polylactic acid (PLA).
View Article and Find Full Text PDFBiomed Opt Express
January 2025
Key Laboratory of Optoelectronic Devices and Systems of Ministry of Education and Guangdong Province, College of Physics and Optoelectronic Engineering, Shenzhen University, Shenzhen, China.
Multiphoton fluorescence microscopy (MFM), renowned for its noninvasiveness and high spatiotemporal resolution, is extensively applied in brain structure imaging in vivo. Three-photon fluorescence (3PF) imaging, excited at the NIR-III window, can penetrate the deepest mouse cerebrovascular. Evans blue, a substance known for its low toxicity, high water solubility, and resistance to metabolism, is frequently employed to assess blood-brain barrier (BBB) permeability.
View Article and Find Full Text PDFNarra J
December 2024
Department of Medicine, Faculty of Medicine, Universitas Sebelas Maret, Surakarta, Indonesia.
Skin aging is one of the degenerative processes influenced by tyrosinase, elastase, collagenase, hyaluronidase, and matrix metalloproteinase-9 (MMP9) activity. One promising avenue for discovering antiaging therapeutics is the peptides from the spine. The aim of this study was to explore the potential of peptides from spine as a multitarget inhibitor for recombinant antiaging therapies through in silico approaches.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Laboratory of Drug Design and Medicinal Chemistry, Showa Pharmaceutical University, 3-2-1 Higashi-Tamagawagakuen, Machida, Tokyo 194-8543, Japan.
The development of covalent drugs, particularly those utilizing Michael acceptors, has garnered significant attention in recent pharmaceutical research due to the ability of such molecules to irreversibly inhibit protein function. This study focusses on the synthesis and evaluation of ethynylsulfonamides, which are predicted to have superior covalent binding ability, metabolic stability, and water solubility compared to traditional amides. We developed a straightforward synthesis method for ethynylsulfonamides and comprehensively evaluated the covalent binding abilities of these compounds using NMR with various nucleophilic amino acids in different solvents.
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