Abstract
It is known that sunflower (Helianthus annuus L.) calathide enzymatically hydrolyzed extract (SCHE) contributes to the regulation of serum uric acid (UA); however, evidence regarding its bioactive components and mechanism are lacking. We identified two water-soluble components (scopoletin and chlorogenic acid) that are abundant in sunflower calathide, especially evaluated for the inhibition of xanthine oxidase (XO) and the expression levels of urate transporters with SCHE. Molecular docking of a chlorogenic acid–XO complex was more stable than that of the Scopoletin–XO, and its binding pockets, which closed the Mo = S center, was similar to xanthine pockets. Moreover, chlorogenic acid exhibited stronger inhibition than that of the scopoletin below 260 μM, despite the IC50 of scopoletin (577.7 μM) being lower than that chlorogenic acid (844.7 μM) on the UA generation assessed by a spectrophotometer in vitro. It revealed that chlorogenic acid and scopoletin were competitive inhibitors of XO. In addition, the SCHE (300 μg/mL) and chlorogenic acid (0.75 mM) obviously inhibited urate transporter 1 (URAT1) and glucose transporter 9 (GLUT9) expression levels, while scopoletin significantly upregulated the expression of GLUT9. To summarize, chlorogenic acid served a crucial role in UA regulation consistent with the SCHE and functioned as an important ingredient of SCHE. The strategic analysis of SCHE combined with scopoletin and chlorogenic acid may contribute to the development of food supplemental alternatives on UA metabolism and the reduction of agricultural byproduct waste.
Highlights
With the incremental incidence of hyperuricemia (HUA), a metabolic disorder of uric acid (UA), that has attracted great attention in the past few decades, clinical trials and medical research regarding UA regulation became topics of current interest [1]
Sunflower calathide, which could be used as a byproduct of food and agriculits potential to lower the effects of high uric acid and perhaps less toxicity than ture, showed its medicine, potential to lower the effects of high uric acid and and febuxostat perhaps less toxicity clinical such as allopurinol, benzbromarone
Scopoletin (6-methoxy-7-hydroxycoumarin), a naturally occurring phenolic coumarin isolated from medicinal herbs [21,22], has been verified to lower UA levels in hyperuricemic mice induced by potassium oxyzinate [23] or yeast extract/potassium oxyzinate [24], even if the uricase acts in parallel on hyperuricemic mice; it is essential to investigate the regulation of urate transporters and xanthine oxidase (XO) activities in vitro
Summary
With the incremental incidence of hyperuricemia (HUA), a metabolic disorder of uric acid (UA), that has attracted great attention in the past few decades, clinical trials and medical research regarding UA regulation became topics of current interest [1]. As it is well known, HUA is a metabolic disease caused by a decrease in UA excretion or an increase in the production of UA due to purine metabolism disorders, and is associated with the incidence of metabolic syndrome, diabetes, hypertension, and kidney disease [2,3]. Sunflower (Helianthus annuus L.) calathide, a type of Chinese folk medicine, has been used for the treatment of hypertension, headache, and analgesic and hemostatic disorders according to the Chinese Materia Medica and the Dictionary of Traditional Chinese
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