bims-antpol 2024-01-14 papers

Issue of 2024‒01‒14
two papers selected by
Rick Sheridan, EMSKE Phytochem

Crit Rev Food Sci Nutr. 2024 Jan 08. 1-37

A critical examination of human data for the biological activity of quercetin and its phase-2 conjugates.

This critical review examines evidence for beneficial effects of quercetin phase-2 conjugates from clinical intervention studies, volunteer feeding trials, and in vitro work. Plasma concentrations of quercetin-3-O-glucuronide (Q3G) and 3'-methylquercetin-3-O-glucuronide (3'MQ3G) after supplementation may produce beneficial effects in macrophages and endothelial cells, respectively, especially if endogenous deglucuronidation occurs, and lower blood uric acid concentration via quercetin-3'-O-sulfate (Q3'S). Unsupplemented diets produce much lower concentrations (<50 nmol/l) rarely investigated in vitro. At 10 nmol/l, Q3'S and Q3G stimulate or suppress, respectively, angiogenesis in endothelial cells. Statistically significant effects have been reported at 100 nmol/l in breast cancer cells (Q3G), primary neuron cultures (Q3G), lymphocytes (Q3G and3'MQ3G) and HUVECs (QG/QS mixture), but it is unclear whether these translate to a health benefit in vivo. More sensitive and more precise methods to measure clinically significant endpoints are required before a conclusion can be drawn regarding effects at normal dietary concentrations. Future requirements include better understanding of inter-individual and temporal variation in plasma quercetin phase-2 conjugates, their mechanisms of action including deglucuronidation and desulfation both in vitro and in vivo, tissue accumulation and washout, as well as potential for synergy or antagonism with other quercetin metabolites and metabolites of other dietary phytochemicals.

Keywords: Quercetin; endothelial function; flavonoid; glucuronide; sulfate

DOI: https://doi.org/10.1080/10408398.2023.2299329

Nutrients. 2024 Jan 04. pii: 161. [Epub ahead of print]16(1):

Flavonoid Metabolites in Serum and Urine after the Ingestion of Selected Tropical Fruits.

Lalita Chomphen, Paveena Yamanont, Noppawan Phumala Morales.

The serum concentration and urinary excretion of flavonoids after the ingestion of guava, pineapple, and pomelo were determined using liquid chromatography-mass spectroscopy (LC-MS/MS). Each group of healthy volunteers was given 200 g of fresh fruit after overnight fasting and a 24-h flavonoid-free diet. The results demonstrate that only the glucuronic-conjugated metabolites of luteolin, quercetin, kaempferol, and myricetin were detected after fruit ingestion. The metabolites were first detected after 2 h, with the time to maximum concentration (Tmax) at 6 h. The most abundant metabolites for guava, pineapple, and pomelo were the glucuronide metabolites of quercetin (AUC0-8 5.4 ± 1.3 μg·h/mL), kaempferol (AUC0-8 9.9 ± 2.3 μg·h/mL), and luteolin (AUC0-8 6.4 ± 1.1 μg·h/mL), respectively. The flavonoids found in the 24-h urinary excretions were glucuronic- and mainly sulfate-conjugated metabolites. Quercetin metabolites were the most abundant after guava and pineapple ingestion, accounting for 900 and 700 μg, respectively. Luteolin metabolites were the most abundant after pomelo ingestion, accounting for 450 μg. The serum and urinary metabolite profiles suggested that guava and pineapple are good sources of quercetin, pineapple is a good source of kaempferol, and pomelo is a good source of luteolin. The study of flavonoid profiles may provide information for the selection of fruits as functional foods for their health benefits to help with various health conditions.

Keywords: bioavailability; conjugated metabolites; flavonoids; kaempferol; luteolin; myricetin; quercetin

DOI: https://doi.org/10.3390/nu16010161