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A lysosomal polarity-specific two-photon fluorescent probe for visualization of autophagy

Chinese Chemical Letters 2021年第5期32卷 1803-1808页

作者： Zixiang Yuan Jun Chen Qin Zhou Ao Liu Zeming Qiang Min Fang Man Chen Yan Feng Haizhu Yu Xiuli Yang Xiangming Meng School of Chemistry and Chemical Engineering&Anhui Province Key Laboratory of Chemistry for Inorganic/Organic Hybrid Functionalized Materials Anhui UniversityHefei 230601China Key Laboratory for Advanced Technology in Environmental Protection of Jiangsu Province Yancheng Institute of TechnologyYancheng 224051China Institute of Physical Science and Information Technology Anhui UniversityHefei 230601China Anhui Golden Sun Biochemical Pharmaceuticals Limited Company Fuyang 236000China

Autophagy plays a vital role in maintaining the balance of normal physiological state of living *** this paper,a polarity-specific two-phot on fluorescent probe Lyso-NA based on naphthalimide was synthesized for the purpose of monitoring autophagy during biological *** results of photophysical properties and theoretical calculation con firmed that different polarities of solvents mainly effected fluorescent intensities of *** nt intensity,quantum yield and fluorescence lifetime of probe kept a good linear relationship with polarity *** addition,due to its low toxicity and selective accumulation in lysosomes,Lyso-NA is suitable for detecting changes in lysosomal polarity of living *** with the imaging results of plasmid transfection,a better performed realtime long-term fluoresce nt visualization of autophagy in living cells was *** Lyso-NA can work as an efficient and cost effective imaging tool for visualizing autophagy in living cells.

关键词： two-photon fluorescent probe Lysosomal polarity Autophagy Visualization Plasmid transfection

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High-Throughput Screening of Flavonoids Inhibitors of Catechol-O-Methyltransferase with a two-photon fluorescent probe

High-Throughput Screening of Flavonoids Inhibitors of Catech...

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中国药理学会分析药理学专业委员会成立大会、第三届全国分析药理学学术大会暨贵州省药学会药学青年专业委员会成立大会

作者： Fangyuan Wang Ping Wang Guangbo Ge Ling Yang Shanghai University of Traditional Chinese Medicine

Aim:Catechol O-methyltransferase（COMT）,which catalyzes the catechol compounds to O-methylated metabolites,plays a key role in the metabolism of endogenous catecholamine neurotransmitters and dopaminergic drug such as *** of human brain COMT is an important therapy approach for Parkinson's disease,because the potent COMT inhibitors can slow down the metabolism of levodopa and dopamine,resulting in the increase of dopamine level in the *** flavonoids have been long recognized as an interesting class of COMT inhibitors due to their catechol skeletons and abilities to bind the active sites of the ***:We first synthesize a two-photon fluorescent probe,3-BTD,for determination of COMT activity in various biological samples and bio-imaging of endogenous COMT in the living cells,which displays good reactivity and high specificity to the ***,a high-throughput screening method is developed for COMT inhibitors from natural flavonoids using the 3-BTD as a small-molecule *** further inhibition kinetics assays demonstrate the inhibition potentials of these flavonoid ***:In this study,the C-8 phenolic hydroxyl of 3-BTD is selectively methylated by COMT,and the corresponding product,3-BTMD,exhibits about 150-fold fluorescence enhancement at 380 nm excitation/510 nm *** fluorescence quantum yields of 3-BTD and 3-BTMD are determined to be 0.0003 and 0.673,*** 3-BTD probe has been successfully applied to the high-throughput screening of COMT inhibitors,and the inhibitory effects of 50 flavonoid compounds are *** them,only 3 compounds（baicalein,scutellarein,and hispidulin） exhibit stronger inhibitory effects on COMT activity,with the IC values of 0.039,0.053 and 0.036 μM,***:3-BTD exhibited extremely weak fluorescent signal because of the interactions between the photo-induced electron transfer of 8-phenolic hydroxyl and the intramolecular charge transfer of 7-phenolic h

关键词： Catechol O-methyltransferase(COMT) high-throughput screening natural flavonoids two-photon fluorescent probe

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