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Development and validation of a sensitive LC-MS/MS assay for the quantification of anserine in human plasma and urine and its application to pharmacokinetic study

Inge Everaert (UGent) , Giovanna Baron, Silvia Barbaresi (UGent) , Ettore Gilardoni, Crescenzo Coppa, Marina Carini, Giulio Vistoli, Tine Bex (UGent) , Jan Stautemas (UGent) , Laura Blancquaert, et al.
(2019) AMINO ACIDS. 51(1). p.103-114
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Organization
Abstract
Carnosine (beta-alanyl-l-histidine) and its methylated analogue anserine are present in relevant concentrations in the omnivore human diet. Several studies reported promising therapeutic potential for carnosine in various rodent models of oxidative stress and inflammation-related chronic diseases. Nevertheless, the poor serum stability of carnosine in humans makes the translation of rodent models hard. Even though anserine and carnosine have similar biochemical properties, anserine has better serum stability. Despite this interesting profile, the research on anserine is scarce. The aim of this study was to explore the bioavailability and stability of synthesized anserine by (1) performing in vitro stability experiments in human plasma and molecular modelling studies and by (2) evaluating the plasma and urinary pharmacokinetic profile in healthy volunteers following different doses of anserine (4-10-20mg/kg body weight). A bio-analytical method for measuring anserine levels was developed and validated using liquid chromatography-electrospray mass spectrometry. Both plasma (C-MAX: 0.54-1.10-3.12 mu M) and urinary (C-MAX: 0.09-0.41-0.72mg/mg creatinine) anserine increased dose-dependently following ingestion of 4-10-20 anserine mg/kg BW, respectively. The inter-individual variation in plasma anserine was mainly explained by the activity (R-2=0.75) and content (R-2=0.77) of the enzyme serum carnosinase-1. Compared to carnosine, a lower interaction energy of anserine with carnosinase-1 was suggested by molecular modelling studies. Conversely, the two dipeptides seems to have similar interaction with the PEPT1 transporter. It can be concluded that nutritionally relevant doses of synthesized anserine are well-absorbed and that its degradation by serum carnosinase-1 is less pronounced compared to carnosine. This makes anserine a good candidate as a more stable carnosine-analogue to attenuate chronic diseases in humans.
Keywords
Anserine, Carnosine, Pharmacokinetics, Carnosinase-1, GLYCATION END-PRODUCTS, CARNOSINE SUPPLEMENTATION, DIABETIC-NEPHROPATHY, INTESTINAL-ABSORPTION, LEUCINE REPEAT, RENAL-DISEASE, DOUBLE-BLIND, HISTIDINE, INGESTION, GLUCOSE

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MLA
Everaert, Inge, et al. “Development and Validation of a Sensitive LC-MS/MS Assay for the Quantification of Anserine in Human Plasma and Urine and Its Application to Pharmacokinetic Study.” AMINO ACIDS, vol. 51, no. 1, 2019, pp. 103–14, doi:10.1007/s00726-018-2663-y.
APA
Everaert, I., Baron, G., Barbaresi, S., Gilardoni, E., Coppa, C., Carini, M., … Regazzoni, L. (2019). Development and validation of a sensitive LC-MS/MS assay for the quantification of anserine in human plasma and urine and its application to pharmacokinetic study. AMINO ACIDS, 51(1), 103–114. https://doi.org/10.1007/s00726-018-2663-y
Chicago author-date
Everaert, Inge, Giovanna Baron, Silvia Barbaresi, Ettore Gilardoni, Crescenzo Coppa, Marina Carini, Giulio Vistoli, et al. 2019. “Development and Validation of a Sensitive LC-MS/MS Assay for the Quantification of Anserine in Human Plasma and Urine and Its Application to Pharmacokinetic Study.” AMINO ACIDS 51 (1): 103–14. https://doi.org/10.1007/s00726-018-2663-y.
Chicago author-date (all authors)
Everaert, Inge, Giovanna Baron, Silvia Barbaresi, Ettore Gilardoni, Crescenzo Coppa, Marina Carini, Giulio Vistoli, Tine Bex, Jan Stautemas, Laura Blancquaert, Wim Derave, Giancarlo Aldini, and Luca Regazzoni. 2019. “Development and Validation of a Sensitive LC-MS/MS Assay for the Quantification of Anserine in Human Plasma and Urine and Its Application to Pharmacokinetic Study.” AMINO ACIDS 51 (1): 103–114. doi:10.1007/s00726-018-2663-y.
Vancouver
1.
Everaert I, Baron G, Barbaresi S, Gilardoni E, Coppa C, Carini M, et al. Development and validation of a sensitive LC-MS/MS assay for the quantification of anserine in human plasma and urine and its application to pharmacokinetic study. AMINO ACIDS. 2019;51(1):103–14.
IEEE
[1]
I. Everaert et al., “Development and validation of a sensitive LC-MS/MS assay for the quantification of anserine in human plasma and urine and its application to pharmacokinetic study,” AMINO ACIDS, vol. 51, no. 1, pp. 103–114, 2019.
@article{8584305,
  abstract     = {{Carnosine (beta-alanyl-l-histidine) and its methylated analogue anserine are present in relevant concentrations in the omnivore human diet. Several studies reported promising therapeutic potential for carnosine in various rodent models of oxidative stress and inflammation-related chronic diseases. Nevertheless, the poor serum stability of carnosine in humans makes the translation of rodent models hard. Even though anserine and carnosine have similar biochemical properties, anserine has better serum stability. Despite this interesting profile, the research on anserine is scarce. The aim of this study was to explore the bioavailability and stability of synthesized anserine by (1) performing in vitro stability experiments in human plasma and molecular modelling studies and by (2) evaluating the plasma and urinary pharmacokinetic profile in healthy volunteers following different doses of anserine (4-10-20mg/kg body weight). A bio-analytical method for measuring anserine levels was developed and validated using liquid chromatography-electrospray mass spectrometry. Both plasma (C-MAX: 0.54-1.10-3.12 mu M) and urinary (C-MAX: 0.09-0.41-0.72mg/mg creatinine) anserine increased dose-dependently following ingestion of 4-10-20 anserine mg/kg BW, respectively. The inter-individual variation in plasma anserine was mainly explained by the activity (R-2=0.75) and content (R-2=0.77) of the enzyme serum carnosinase-1. Compared to carnosine, a lower interaction energy of anserine with carnosinase-1 was suggested by molecular modelling studies. Conversely, the two dipeptides seems to have similar interaction with the PEPT1 transporter. It can be concluded that nutritionally relevant doses of synthesized anserine are well-absorbed and that its degradation by serum carnosinase-1 is less pronounced compared to carnosine. This makes anserine a good candidate as a more stable carnosine-analogue to attenuate chronic diseases in humans.}},
  author       = {{Everaert, Inge and Baron, Giovanna and Barbaresi, Silvia and Gilardoni, Ettore and Coppa, Crescenzo and Carini, Marina and Vistoli, Giulio and Bex, Tine and Stautemas, Jan and Blancquaert, Laura and Derave, Wim and Aldini, Giancarlo and Regazzoni, Luca}},
  issn         = {{0939-4451}},
  journal      = {{AMINO ACIDS}},
  keywords     = {{Anserine,Carnosine,Pharmacokinetics,Carnosinase-1,GLYCATION END-PRODUCTS,CARNOSINE SUPPLEMENTATION,DIABETIC-NEPHROPATHY,INTESTINAL-ABSORPTION,LEUCINE REPEAT,RENAL-DISEASE,DOUBLE-BLIND,HISTIDINE,INGESTION,GLUCOSE}},
  language     = {{eng}},
  number       = {{1}},
  pages        = {{103--114}},
  title        = {{Development and validation of a sensitive LC-MS/MS assay for the quantification of anserine in human plasma and urine and its application to pharmacokinetic study}},
  url          = {{http://doi.org/10.1007/s00726-018-2663-y}},
  volume       = {{51}},
  year         = {{2019}},
}
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