Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes
In continuation of the investigation on the bithiophene structure as potential Aβ probes, two halogenated chalcone derivatives containing bithiophene moiety were designed and evaluated as imaging probes for Aβ plaques. In vitro fluorescence staining indicated that they could stain Aβ plaques in the...
Main Authors: | , , , |
---|---|
Format: | Article |
Language: | zho |
Published: |
Editorial Board of Journal of Isotopes
2015-11-01
|
Series: | Journal of Isotopes |
Subjects: | |
Online Access: | http://www.tws.org.cn/CN/10.7538/tws.2015.28.04.0253 |
id |
doaj-e4a4c8f4461d4d22853300266a3dcb75 |
---|---|
record_format |
Article |
spelling |
doaj-e4a4c8f4461d4d22853300266a3dcb752020-11-25T02:22:17ZzhoEditorial Board of Journal of IsotopesJournal of Isotopes1000-75121000-75122015-11-0128425325810.7538/tws.2015.28.04.0253 Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ ProbesPENG Cheng0CUI Meng-chao1LIANG Zhi-gang2LIU Ting-ting3Xuanwu Hospital,Capital Medical UniversityKey Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education,College of ChemistryXuanwu Hospital,Capital Medical UniversityXuanwu Hospital,Capital Medical UniversityIn continuation of the investigation on the bithiophene structure as potential Aβ probes, two halogenated chalcone derivatives containing bithiophene moiety were designed and evaluated as imaging probes for Aβ plaques. In vitro fluorescence staining indicated that they could stain Aβ plaques in the brain sections of AD model mice specifically, in vitro binding assay further confirmed that they displayed high binding affinities to Aβ aggregates (Ki=2.33 nM and 0.88 nM). One radio-iodinated probe, 125I labeleled chalcone derivatives was obtained via iododestannylation reaction with high radiochemical yield and purity (>99%). Moreover, the 125I-labeling compound displayed specific labeling of Aβ plaques in the brain sections of AD model mice with low background, and the specific labeling could be confirmed by thioflavin-S staining. In vivo biodistribution in normal mice indicated that the 125I labeling compound exhibited low initial brain uptake (1.19%ID/g at 2 min) and rapid clearance. These preliminary results suggest that 125I labeling compound may serve as novel Aβ imaging probe, although further modifications are needed to improve initial brain uptake. http://www.tws.org.cn/CN/10.7538/tws.2015.28.04.0253 Alzheimer’s diseaseA&betaplaquesautoradiographybiodistribution |
collection |
DOAJ |
language |
zho |
format |
Article |
sources |
DOAJ |
author |
PENG Cheng CUI Meng-chao LIANG Zhi-gang LIU Ting-ting |
spellingShingle |
PENG Cheng CUI Meng-chao LIANG Zhi-gang LIU Ting-ting Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes Journal of Isotopes Alzheimer’s disease A&beta plaques autoradiography biodistribution |
author_facet |
PENG Cheng CUI Meng-chao LIANG Zhi-gang LIU Ting-ting |
author_sort |
PENG Cheng |
title |
Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes |
title_short |
Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes |
title_full |
Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes |
title_fullStr |
Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes |
title_full_unstemmed |
Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes |
title_sort |
synthesis and evaluation of 125i labeled chalcone derivatives containing bithiophene moiety as potential aβ probes |
publisher |
Editorial Board of Journal of Isotopes |
series |
Journal of Isotopes |
issn |
1000-7512 1000-7512 |
publishDate |
2015-11-01 |
description |
In continuation of the investigation on the bithiophene structure as potential Aβ probes, two halogenated chalcone derivatives containing bithiophene moiety were designed and evaluated as imaging probes for Aβ plaques. In vitro fluorescence staining indicated that they could stain Aβ plaques in the brain sections of AD model mice specifically, in vitro binding assay further confirmed that they displayed high binding affinities to Aβ aggregates (Ki=2.33 nM and 0.88 nM). One radio-iodinated probe, 125I labeleled chalcone derivatives was obtained via iododestannylation reaction with high radiochemical yield and purity (>99%). Moreover, the 125I-labeling compound displayed specific labeling of Aβ plaques in the brain sections of AD model mice with low background, and the specific labeling could be confirmed by thioflavin-S staining. In vivo biodistribution in normal mice indicated that the 125I labeling compound exhibited low initial brain uptake (1.19%ID/g at 2 min) and rapid clearance. These preliminary results suggest that 125I labeling compound may serve as novel Aβ imaging probe, although further modifications are needed to improve initial brain uptake.
|
topic |
Alzheimer’s disease A&beta plaques autoradiography biodistribution |
url |
http://www.tws.org.cn/CN/10.7538/tws.2015.28.04.0253 |
work_keys_str_mv |
AT pengcheng synthesisandevaluationof125ilabeledchalconederivativescontainingbithiophenemoietyaspotentialabprobes AT cuimengchao synthesisandevaluationof125ilabeledchalconederivativescontainingbithiophenemoietyaspotentialabprobes AT liangzhigang synthesisandevaluationof125ilabeledchalconederivativescontainingbithiophenemoietyaspotentialabprobes AT liutingting synthesisandevaluationof125ilabeledchalconederivativescontainingbithiophenemoietyaspotentialabprobes |
_version_ |
1724862279863762944 |