A pyrane based fluorescence probe for noninvasive prediction of cerebral β-amyloid fibrils.
A potential fluorescence probe for in vivo detection of cerebral β-amyloid fibrils, (E)-2-(2-(2-(5-(dimethylamino)thiophen-2-yl)vinyl)-6-methyl-4H-pyran-4-ylidene)malononitrile (PT-1), was synthesized and evaluated. In experiments in vitro, PT-1 exhibited clear labeling of β-amyloid fibrils and significant fluorescence changes upon binding to aggregated β-amyloid fibrils. It also showed favorite kinetics in the brain, which is critical for cerebral imaging. In vivo fluorescence imaging with PT-1 and semi-quantitative analysis of the images further confirmed noninvasive visualization of cerebral β-amyloid fibrils in vivo and obvious distinction between APP/PS1 transgenic mice and wild-type controls. The results demonstrate the potential of PT-1 as a novel fluorescence probe for noninvasive prediction of cerebral β-amyloid fibrils.
Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University, Chengdu 610041, China. Electronic address: yancheng@scu.edu.cn.
Yan
Y
Cheng
Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Bi-Yue
BY
Zhu
Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Xue
X
Li
State Key Laboratory of Biotherapy/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
Guo-Bo
GB
Li
State Key Laboratory of Biotherapy/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
Sheng-Yong
SY
Yang
Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University, Chengdu 610041, China. Electronic address: zrzzl@vip.sina.com.
Zhi-Rong
ZR
Zhang
D016229:Amyloid beta-Peptides / Q000032:analysis*; D000818:Animals; D005453:Fluorescence; D005456:Fluorescent Dyes / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry*; D007275:Injections, Intravenous; D051379:Mice; D008810:Mice, Inbred C57BL; D008822:Mice, Transgenic; D008958:Models, Molecular; D015394:Molecular Structure; D009570:Nitriles / Q000138:chemical synthesis / Q000737:chemistry*; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry*
C000606695:2-(2-(2-(5-(dimethylamino)thiophen-2-yl)vinyl)-6-methyl-4H-pyran-4-ylidene)malononitrile; D016229:Amyloid beta-Peptides; D005456:Fluorescent Dyes; D009570:Nitriles; D013876:Thiophenes
Fluorescence probe; Neurodegenerative disease; β-Amyloid fibrils