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Specific Turn-On Fluorescent Probe with Aggregation-Induced Emission Characteristics for SIRT1 Modulator Screening and Living-Cell Imaging

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journal contribution
posted on 19.05.2015, 00:00 by Yi Wang, Yaqi Chen, Haibo Wang, Yiyu Cheng, Xiaoping Zhao
SIRT1 is an important protein that catalyzes the nicotinamide adenine dinucleotide (NAD)+-dependent deacetylation reaction, which is regarded as a novel target to treat metabolic disorders and aging-related diseases. However, there is lack of appropriate approach for SIRT1 modulator screening and bioimaging of SIRT1 in living cells. We designed and synthesized a “turn-on” fluorescent probe by connecting a specifically recognized peptide to tetraphenylethene core. It exhibits excellent selectivity and sensitivity in homogeneous measurement of SIRT1 activity for screening both SIRT1 inhibitors and activators. 20­(S)-ginsenoside Rg3 and ophiopogonin D′ were found to activate SIRT1. It was also successfully applied to monitor SIRT1 modulation in the cardiomyocytes as well as in the wild-type and SIRT1–/– mesenchymal stem cells.