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Activity-Based Dicyanoisophorone Derivatives: Fluorogenic Toolbox Enables Direct Visualization and Monitoring of
P Kavyashree1, Atri Bhattacharya1,2, Lidong Du3
1Bionanotechnology Lab, Department of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal Bypass Road, Bhauri, Bhopal 462066, Madhya Pradesh, India.
Analytical Chemistry
|November 1, 2024
Summary
Researchers developed novel fluorogenic ester substrates (DCIP-R) to visualize and monitor esterase activity in liver disease models. The DCIP-R1 probe demonstrated high sensitivity and efficiency for detecting endogenous esterase activity in vitro and in vivo.
Area of Science:
- Biochemistry
- Molecular Biology
- Medical Diagnostics
Background:
- Endogenous esterase activity is vital for liver disease diagnosis and treatment.
- Current methods for monitoring esterase activity have limitations.
Purpose of the Study:
- To develop and evaluate novel fluorogenic ester substrates for visualizing and monitoring endogenous esterase activity.
- To assess the efficacy of these probes in liver disease models.
Main Methods:
- Developed dicyanoisophorone-based fluorogenic ester substrates (DCIP-R).
- Employed substrate hydrolysis-enzymatic activity (SHEA) approach.
- Utilized two-photon imaging for comparative studies.
- Tracked esterase activity in diethylnitrosamine (DEN)-induced and HepG2-transplanted liver tumor models.
Main Results:
- Esterase-mediated hydrolysis yielded fluorescent DCIP-OH with nanomolar detection limits.
- DCIP-R1 exhibited high turnover number (4.73 s⁻¹) and catalytic efficiency (10⁶ M⁻¹ s⁻¹).
- Alkyl-substituted substrates (DCIP-R1) showed enhanced enzymatic cleavage over phenyl-substituted ones (DCIP-R4).
- Successfully monitored time-dependent esterase variations in healthy and liver tumor models.
Conclusions:
- DCIP-R probes, particularly DCIP-R1, are highly effective for in vitro and in vivo detection of esterase activity.
- These probes show significant potential for biomedical applications in liver disease diagnostics.
- The SHEA approach provides a sensitive method for evaluating esterase preferences and activity.
