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.