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제125회 대한화학회 학술발표회 및 총회 Discovery of Two-Photon MAO-B Fluorescence Probes for Neurodegenerative Diseases

2020년 2월 5일 17시 07분 49초
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Medicinal Chemistry
저자 및
Rina Kwag, Hyunah Choo*
Center of Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology, Korea
Monoamine oxidase B (MAO-B) catalyzes the oxidation of neuroactive amines and has been proposed as a biomarker for patients with neurodegenerative diseases such as Alzheimer’s disease and Parkinson’s disease. There have been many MAO-B chemical probes discovered. However, there are few MAO-B-specific probes in vivo applicable. Here we designed and synthesized novel two-photon fluoroscence probes (A and B) for highly sensitive and selective detection of MAO-B. Carboxylic acid and acetyl moieties were introduced to the reported MAO-B probe U1 to improve BBB penetration. Both probes exhibited good microsomal stability, which could make real-time imaging of MAO-B activity in small animals like a mouse. With the MAO-B probes (A and B) and the reference U1, cellular imaging of MAO-B activity was taken in HepG2, U87MG, and SHSY5Y cells. Especially probe A showed fluorescence with high intensity which can be a proof of concept for our designed MAO-B probes. The design, synthesis and biological properties of the MAO-B probes will be presented in detail.