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A sensitive LC-MS assay using derivatization with boron trifluoride to quantify curcuminoids in biological samples
Alexander J Yoon1, Haiqiang Wu2, Roy D Pan3
1Pasarow Mass Spectrometry Laboratory, Jane and Terry Semel Institute for Neuroscience and Human Behavior and Department of Psychiatry & Biobehavioral Sciences, David Geffen School of Medicine at UCLA, Los Angeles, CA 90095, USA.
Analytical Biochemistry
|February 22, 2020
Summary
This study introduces a sensitive method to quantify curcuminoids and their metabolites in biological samples. The procedure enables detailed pharmacokinetic analysis of curcumin compounds in humans.
Area of Science:
- Pharmacology
- Analytical Chemistry
- Biochemistry
Background:
- Curcuminoids, including curcumin (C), demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC), are natural compounds with potential therapeutic properties.
- Understanding their metabolism and pharmacokinetics is crucial for assessing efficacy and safety.
- Existing analytical methods may lack the sensitivity or scope to measure the full range of curcuminoids and their metabolites in complex biological matrices.
Purpose of the Study:
- To develop and validate a highly sensitive analytical procedure for quantifying curcuminoids (C, DMC, BDMC), tetrahydrocurcumin (TC), and their glucuronidated metabolites (CG, DMCG, BDMCG).
- To analyze these compounds in various biological samples, including plasma, brain, liver, and tumor tissues.
- To investigate the pharmacokinetic profile of orally administered curcuminoids in a human subject.
Main Methods:
- Analyte derivatization using boron difluoride.
- Analysis via combined liquid chromatography coupled to an ion trap mass spectrometer (LC-MSn).
- Detection in negative ion mode with high sensitivity.
Main Results:
- The method achieved excellent limits of detection: 0.01 nM for curcuminoids and 0.5 nM for TC and glucuronidated metabolites.
- Representative chromatograms demonstrated the method's applicability to real biological samples.
- A human pharmacokinetic study revealed peak and changing concentrations of circulating curcuminoids after daily oral consumption.
Conclusions:
- The developed LC-MSn method provides a sensitive and robust tool for analyzing curcuminoids and their metabolites in diverse biological samples.
- This analytical capability is essential for advancing research into the pharmacokinetics and therapeutic potential of curcuminoids.
- The study provides initial insights into the human pharmacokinetic profile of curcuminoids from over-the-counter products.

