The recognition of a specific protein in blood serum amidst similar proteins is a challenging and vital endeavor in clinical diagnostics. Herein, we have described a small-molecule probe (DFPAC-OH) that can induce self-assembly of human serum albumin (HSA) and bovine serum albumin (BSA) to generate a highly sustainable fluorescent organic nanoparticle (NP), useful for imaging and in vitro drug-delivery applications. In the midst of similar proteins, DFPAC-OH selectively binds in a noncovalent manner to serum albumin. The specific binding tailors the fluorescence properties of DFPAC-OH. The lowest detection limit for BSA is 47 nM with a binding constant of 1.03 × 10 5 M −1 . The probe can efficiently detect HSA in an artificial urine sample. Furthermore, the subsequent bovine albumin self-assembled nanoparticle (DFPAC-OH@BSA-NPs) displays a strong emission at 580 nm both in solution and in solid state. The nanoparticle is highly stable over a long pH range, covering the physiologic pH, and shows an excellent bioavailability to be used for sustainable cell imaging and drug-delivery applications. In addition, the cellular internalization and the pH-responsive drug-release behavior of a hydrophobic drug thymoquinone (TQ) encapsulated in DFPAC-
Since inception, the magic bullets
developed against leishmaniasis
traveled a certain path and then dropped down due to either toxicity
or the emergence of resistance. The route of administration is also
an important concern. We developed a series of water-soluble ferrocenylquinoline
derivatives, targeting Leishmania donovani, among which CQFC1 showed the highest efficacy even in comparison
to other drugs, in use or used, both in oral and intramuscular routes.
It did not induce any toxicity to splenocytes and on hematopoiesis,
induced protective cytokines, and did not hamper the drug-metabolizing
enzymes in hosts. It acts through the reduction and the inhibition
of parasites’ survival enzyme trypanothione reductase of replicating
amastigotes in hosts’ reticuloendothelial tissues. Unlike conventional
drugs, this molecule did not induce the resistance-conferring genes
in laboratory-maintained resistant L. donovani lines. Experimentally, this easily bioavailable preclinical drug
candidate overcame all of the limitations causing the discontinuation
of the other conventional antileishmanial drugs.
Diethyl chlorophosphate (DCP) has similar reactivity to sarin widely known as nerve agent usually used in terrorist attacks. As DCP lacks high toxicity, it can be used as a model...
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