1 research outputs found
Novel Benzothiazole Derivatives as Fluorescent Probes for Detection of β‑Amyloid and α‑Synuclein Aggregates
Deposits
of β-amyloid (Aβ) and α-synuclein (α-syn)
are the hallmark of Alzheimer’s disease (AD) and Parkinson’s
disease (PD), respectively. The detection of these protein aggregates
with fluorescent probes is particularly of interest for preclinical
studies using fluorescence microscopy on human brain tissue. In this
study, we newly designed and synthesized three push–pull benzothiazole
(PP-BTA) derivatives as fluorescent probes for detection of Aβ
and α-syn aggregates. Fluorescence intensity of all PP-BTA derivatives
significantly increased upon binding to Aβ(1–42) and
α-syn aggregates in solution. In in vitro saturation binding
assays, PP-BTA derivatives demonstrated affinity for both Aβ(1–42)
(<i>K</i><sub>d</sub> = 40–148 nM) and α-syn
(<i>K</i><sub>d</sub> = 48–353 nM) aggregates. In
particular, PP-BTA-4 clearly stained senile plaques composed of Aβ
aggregates in the AD brain section. Moreover, it also labeled Lewy
bodies composed of α-syn aggregates in the PD brain section.
These results suggest that PP-BTA-4 may serve as a promising fluorescent
probe for the detection of Aβ and α-syn aggregates