Related Experiment Video
Updated: Jan 17, 2026
Non-invasive In Vivo Fluorescence Optical Imaging of Inflammatory MMP Activity Using an Activatable Fluorescent Imaging Agent
Published on: May 8, 2017
Rational design of MAO-B-activated fluorescent probe for activity evaluation and its biomedical applications
Fei Yan1, Junxiang Niu2, Yue Zhang2
1Second Affiliated Hospital, Dalian Medical University, Dalian, 116023, China; General Hospital of Northern Theater Command, Department of Neurosurgery, Shenyang, 110801, China.
A new fluorescent probe, AHPC, enables real-time detection of monoamine oxidase B (MAO-B) activity and its changes under oxidative stress. This tool facilitated high-throughput screening of Chinese medicine, identifying Licoisoflavone B as a potent MAO-B inhibitor for potential disease treatment.
Area of Science:
- Biochemistry
- Neuroscience
- Pharmacology
Background:
- Monoamine oxidase B (MAO-B) is a key enzyme in neurotransmitter metabolism and a significant drug target for neurological disorders.
- MAO-B activity is implicated in various nervous system diseases, highlighting the need for effective inhibitors and detection methods.
Purpose of the Study:
- To design and develop a selective and sensitive fluorescent probe (AHPC) for real-time monitoring of MAO-B activity.
- To establish a high-throughput screening system for MAO-B inhibitors using the developed fluorescent probe.
- To identify potential MAO-B inhibitors from traditional Chinese medicine.
Main Methods:
- Design and synthesis of the fluorescent probe 3-aminopropyl (3-oxo-3H-phenoxazin-7-yl) carbamate (AHPC).
- Evaluation of AHPC's stability, cell permeability, and ability to detect endogenous MAO-B activity in real-time.
- Development of a high-throughput visual screening system for MAO-B inhibitors based on AHPC.
- Screening of 272 traditional Chinese medicines and isolation of active compounds.
Main Results:
- AHPC demonstrated good stability and cell membrane permeability, enabling real-time detection of MAO-B activity and its modulation under oxidative stress.
- The AHPC-based screening system successfully identified Glycyrrhizae radix et rhizome as a source of MAO-B inhibitors.
- Licoisoflavone B was isolated as the primary active component from Glycyrrhizae radix et rhizome, exhibiting significant MAO-B inhibition and potential as a lead compound.
Conclusions:
- AHPC serves as a valuable molecular tool for real-time assessment of MAO-B distribution and function in biological systems.
- The developed high-throughput screening method offers a promising approach for discovering MAO-B inhibitors from natural products.
- Licoisoflavone B represents a potential therapeutic lead for MAO-B-related diseases, warranting further investigation.
