Human Serum Albumin-Occupying-Based Fluorescence Turn-On Analysis of Antiepileptic Drug Tiagabine Hydrochloride

Abstract

Tiagabine hydrochloride (TGB) is a clinically frequently used drug for anticonvulsion and reducing epileptic frequency. Over administration of TGB could bring about adverse effects, such as speech disorder, depression, and even suicidal tendencies. Therefore, accessible and sensitive assay for analysis of TGB becomes an urgent need toward guiding clinical medication. Here, we present the first report on fluorescence turn-on detection of TGB in urine testing. In this protocol, a fluorescent dye, perylene tetracarboxylic acid imide derivative (PTAI), is found specifically occupying the Sudlow site II of human serum albumin (HSA) and displays a new phenomenon of binding-induced quenching (BIQ). In presence of TGB, competitive binding of the TGB to the site II of HSA will trigger release of PTAI, thus successfully lighting up the fluorescence of PTAI. This label-free assay enjoys a broader working range (1–350 μM) and lower detection limit (0.218 μM) than the traditional liquid chromatography method and is uninterfered by the miscellaneous in the artificial urine. The BIQ probe highlights the merits of HSA as a quencher and a molecular recognition unit, and it opens up a way for studying drug-HSA interaction mechanism and noninvasive pharmaceutical testing.

Thermal Reversibility and Structural Stability in Lysozyme Induced by Epirubicin Hydrochloride

“…The functional aspects of a protein strongly depend on the interactions with ligands and drug molecules. Such interactions with drugs can lead to significant variations in the structural morphology and dynamics of the protein. − Hence, determining the activity and toxicity of the drug inside the living body is rather crucial for the protein to function normally. The pharmacokinetics and pharmacodynamics of a drug depend upon the extent of binding to proteins .…”

An Activatable and Switchable Nanoaggregate Probe for Detecting H2S and Its Application in Mice Brains

“…Basically, longer wavelength means weaker energy, thus a direct NIR sensing usually need a subsequent procedure of amplification. Common enlarging strategies include instrumental calibration, [22] Aggregation-Induced Emission (AIE), [23,24] proteinassistant amplification, [25,26] nanocarrier-based signal transmission, [27] and so on. One step further, we still hope that the signal switching could be regulated by an "all-or-nothing" biomolecule which itself is the marker of specific physiological or pathological models, for example, glutathione in solid tumor [28] or caspase-3 in apoptosis.…”

Engineering a selective fluorescent sensor with a high signal-to-background ratio for microalbumin detection and imaging

“…Furthermore, most of the current HSA probes mainly bind to two commonly used drug binding sites of HSA, subdomains IIA and IIIA. [22][23][24][25] Although these binding sites work well for many drugs and dyes, however, they can make these probes subject to severe interference from bovine serum albumin (BSA), which is 75% similar in physiological structure to HSA, resulting in nonspecific detection to HSA. 26 It is well known that the entire structure of HSA consists of domains I, II, and III, each of which is subdivided into two subdomains A and B.…”