Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia

It is known that sunflower (<i>Helianthus annuus</i> 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 (sc...

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Autores principales:	Huining Dai, Shuai Lv, Xueqi Fu, Wannan Li
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	sunflower calathide scopoletin chlorogenic acid urate transporters xanthine oxidase inhibitor molecular docking Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/d7fbf9f76ec14803b0209415aead44b2
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spelling	oai:doaj.org-article:d7fbf9f76ec14803b0209415aead44b22021-11-11T15:20:07ZIdentification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia10.3390/app1121103062076-3417https://doaj.org/article/d7fbf9f76ec14803b0209415aead44b22021-11-01T00:00:00Zhttps://www.mdpi.com/2076-3417/11/21/10306https://doaj.org/toc/2076-3417It is known that sunflower (<i>Helianthus annuus</i> 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 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mrow><mrow><mi mathvariant="sans-serif">μ</mi><mi mathvariant="normal">M</mi></mrow></mrow></semantics></math></inline-formula>, despite the IC<sub>50</sub> of scopoletin (577.7 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mrow><mrow><mi mathvariant="sans-serif">μ</mi><mi mathvariant="normal">M</mi></mrow></mrow></semantics></math></inline-formula>) being lower than that chlorogenic acid (844.7 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mrow><mrow><mi mathvariant="sans-serif">μ</mi><mi mathvariant="normal">M</mi></mrow></mrow></semantics></math></inline-formula>) 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 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mi mathvariant="sans-serif">μ</mi></semantics></math></inline-formula>g/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.Huining DaiShuai LvXueqi FuWannan LiMDPI AGarticlesunflower calathidescopoletinchlorogenic acidurate transportersxanthine oxidase inhibitormolecular dockingTechnologyTEngineering (General). Civil engineering (General)TA1-2040Biology (General)QH301-705.5PhysicsQC1-999ChemistryQD1-999ENApplied Sciences, Vol 11, Iss 10306, p 10306 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	sunflower calathide scopoletin chlorogenic acid urate transporters xanthine oxidase inhibitor molecular docking Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999
spellingShingle	sunflower calathide scopoletin chlorogenic acid urate transporters xanthine oxidase inhibitor molecular docking Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999 Huining Dai Shuai Lv Xueqi Fu Wannan Li Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia
description	It is known that sunflower (<i>Helianthus annuus</i> 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 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mrow><mrow><mi mathvariant="sans-serif">μ</mi><mi mathvariant="normal">M</mi></mrow></mrow></semantics></math></inline-formula>, despite the IC<sub>50</sub> of scopoletin (577.7 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mrow><mrow><mi mathvariant="sans-serif">μ</mi><mi mathvariant="normal">M</mi></mrow></mrow></semantics></math></inline-formula>) being lower than that chlorogenic acid (844.7 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mrow><mrow><mi mathvariant="sans-serif">μ</mi><mi mathvariant="normal">M</mi></mrow></mrow></semantics></math></inline-formula>) 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 <inline-formula><math xmlns="http://www.w3.org/1998/Math/MathML" display="inline"><semantics><mi mathvariant="sans-serif">μ</mi></semantics></math></inline-formula>g/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.
format	article
author	Huining Dai Shuai Lv Xueqi Fu Wannan Li
author_facet	Huining Dai Shuai Lv Xueqi Fu Wannan Li
author_sort	Huining Dai
title	Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia
title_short	Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia
title_full	Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia
title_fullStr	Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia
title_full_unstemmed	Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia
title_sort	identification of scopoletin and chlorogenic acid as potential active components in sunflower calathide enzymatically hydrolyzed extract towards hyperuricemia
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/d7fbf9f76ec14803b0209415aead44b2
work_keys_str_mv	AT huiningdai identificationofscopoletinandchlorogenicacidaspotentialactivecomponentsinsunflowercalathideenzymaticallyhydrolyzedextracttowardshyperuricemia AT shuailv identificationofscopoletinandchlorogenicacidaspotentialactivecomponentsinsunflowercalathideenzymaticallyhydrolyzedextracttowardshyperuricemia AT xueqifu identificationofscopoletinandchlorogenicacidaspotentialactivecomponentsinsunflowercalathideenzymaticallyhydrolyzedextracttowardshyperuricemia AT wannanli identificationofscopoletinandchlorogenicacidaspotentialactivecomponentsinsunflowercalathideenzymaticallyhydrolyzedextracttowardshyperuricemia
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Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia

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