Journal
MOLECULAR NUTRITION & FOOD RESEARCH
Volume 56, Issue 9, Pages 1413-1423Publisher
WILEY-BLACKWELL
DOI: 10.1002/mnfr.201200021
Keywords
Bioavailability; Caco-2 cells; Coffee; Human plasma; Phenolic acids
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Funding
- Nestle Research Center, Lausanne, Switzerland
- Nestle
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Scope This study reports the 24 h human plasma pharmacokinetics of 3,4-dimethoxycinnamic acid (dimethoxycinnamic acid) after consumption of coffee, and the membrane transport characteristics of certain dimethoxycinnamic acid derivatives, as present in coffee. Methods and results Eight healthy human volunteers consumed a low-polyphenol diet for 24 h before drinking 400 mL of commercially available coffee. Plasma samples were collected over 24 h and analyzed by HPLC-MS2. Investigation of the mechanism of absorption and metabolism was performed using an intestinal Caco-2 cell model. For the first time, we show that dimethoxycinnamic acid appears in plasma as the free aglycone. The time to reach the Cmax value of approximately 0.5 mu M was rapid, Tmax = 30 min, and showed an additional peak at 24 h for several subjects. In contrast, smaller amounts of dimethoxy-dihydrocinnamic acid (Cmax 0.1 mu M) peaked between 8 and 12 h after coffee intake. In the cell model, dimethoxycinnamic acid was preferentially transported in the free form by passive diffusion, and a small amount of dimethoxycinnamoylquinic acid hydrolysis was observed. Conclusion These findings show that dimethoxycinnamic acid, previously identified in plasma after coffee consumption, was rapidly absorbed in the free form most likely by passive diffusion in the upper gastrointestinal tract.
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