Background/Purpose: Tart cherries (TC) contain high levels of anthocyanins that exert potent antioxidant and anti-inflammatory effects. Approximately 50% of gout patients report using TC to help manage their gout, and preliminary data have demonstrated reduced gout flares in patients consuming TC. Our study aimed to characterize the major anthocyanins in Tart Cherry Juice Concentrate (TCJC) and identify the most prominently available anthocyanins in gout patients consuming TCJC.

Methods: Anthocyanins were determined using liquid chromatography-mass spectroscopy (LCMS). TCJC was diluted with deionized water and anthocyanins analyzed by LCMS using a Dionex UltiMate 3000 LC coupled with a Thermo Q Exactive HF, a Phenomenex Kinetex C18 column, and a gradient of 10% aqueous formic acid: acetonitrile. Cyanidin-3-arabinoside was used as an internal standard. anthocyaninswere identified by their fragmentation patterns and/or authentic standards. All available standards were purchased from Sigma Aldrich (St. Louis, MO), except for cyanidin-3-glucosylrutinoside, purchased from Diagnocine LLC (Hackensack, NJ). Individuals with gout (n=10) were administered either 60 or 120 mL of TCJC in a crossover design. Serial blood samples were drawn and used to characterize the pharmacokinetics and pharmacodynamics of anthocyanins in plasma.

Results: Cyanidin-3-glucosylrutinoside (C3GR) and cyanidin-3-rutinoside (C3R) were the main anthocyanins identified in the TCJC (Table 1). Various anthocyanins were bioavailable with C3GR and C3R achieving the highest plasma concentration in a dose-dependent manner.

Administration of oral TCJC resulted in a significant fold change in antioxidant mRNA gene expression NRF-2, HO-1, and NQO-1 (mean peak fold change 1.3, 1.6, and 1.4 versus baseline, p< 0.05; respectively) appreciated as early as 30 minutes after dose administration.

A significant reduction in iNOS and TNF-α mRNA gene expression (mean peak fold change 0.7 and 0.8 versus baseline, p< 0.05; respectively) was also observed and peaked at 2 hours post-dose. Only the high dose resulted in significant changes in gene expression. Pharmacokinetic analyses are ongoing.

TABLE 1. Quantitation of major anthocyanins identified in TCJC.

Conclusion: The present study identifies the main anthocyanins present in the TCJC and patient plasma after oral administration of TCJC, as cyanidin 3-glucosylrutinoside and cyanidin 3-rutinoside. Since these anthocyanins are known to have anti-inflammatory and antioxidant effects, they may explain the benefit of TC in patients with gout.

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ACR Meeting Abstracts - https://acrabstracts.org/abstract/pharmacokinetics-and-pharmacodynamics-of-anthocyanins-after-oral-administration-of-oral-tart-cherry-juice-concentrate-to-gout-patients/