Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors

Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (...
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Autor*in:	Chun-Mei Hu [verfasserIn] Yong-Xin Luo [verfasserIn] Wen-Jing Wang [verfasserIn] Jian-Ping Li [verfasserIn] Meng-Yue Li [verfasserIn] Yu-Fei Zhang [verfasserIn] Di Xiao [verfasserIn] Li Lu [verfasserIn] Zhuang Xiong [verfasserIn] Na Feng [verfasserIn] Chen Li [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2022

Schlagwörter:	coumarin chalcone α-glucosidase enzyme inhibitor docking

Übergeordnetes Werk:	In: Frontiers in Chemistry - Frontiers Media S.A., 2014, 10(2022)
Übergeordnetes Werk:	volume:10 ; year:2022

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3389/fchem.2022.926543

Katalog-ID:	DOAJ042404770

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allfields	10.3389/fchem.2022.926543 doi (DE-627)DOAJ042404770 (DE-599)DOAJa9f0db83f64f4e1d99de6f1bf6dff68d DE-627 ger DE-627 rakwb eng QD1-999 Chun-Mei Hu verfasserin aut Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (KI = 18.82 μM, KIS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t. coumarin chalcone α-glucosidase enzyme inhibitor docking Chemistry Yong-Xin Luo verfasserin aut Wen-Jing Wang verfasserin aut Jian-Ping Li verfasserin aut Meng-Yue Li verfasserin aut Yu-Fei Zhang verfasserin aut Di Xiao verfasserin aut Li Lu verfasserin aut Zhuang Xiong verfasserin aut Na Feng verfasserin aut Chen Li verfasserin aut In Frontiers in Chemistry Frontiers Media S.A., 2014 10(2022) (DE-627)742224538 (DE-600)2711776-5 22962646 nnns volume:10 year:2022 https://doi.org/10.3389/fchem.2022.926543 kostenfrei https://doaj.org/article/a9f0db83f64f4e1d99de6f1bf6dff68d kostenfrei https://www.frontiersin.org/articles/10.3389/fchem.2022.926543/full kostenfrei https://doaj.org/toc/2296-2646 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022
spelling	10.3389/fchem.2022.926543 doi (DE-627)DOAJ042404770 (DE-599)DOAJa9f0db83f64f4e1d99de6f1bf6dff68d DE-627 ger DE-627 rakwb eng QD1-999 Chun-Mei Hu verfasserin aut Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (KI = 18.82 μM, KIS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t. coumarin chalcone α-glucosidase enzyme inhibitor docking Chemistry Yong-Xin Luo verfasserin aut Wen-Jing Wang verfasserin aut Jian-Ping Li verfasserin aut Meng-Yue Li verfasserin aut Yu-Fei Zhang verfasserin aut Di Xiao verfasserin aut Li Lu verfasserin aut Zhuang Xiong verfasserin aut Na Feng verfasserin aut Chen Li verfasserin aut In Frontiers in Chemistry Frontiers Media S.A., 2014 10(2022) (DE-627)742224538 (DE-600)2711776-5 22962646 nnns volume:10 year:2022 https://doi.org/10.3389/fchem.2022.926543 kostenfrei https://doaj.org/article/a9f0db83f64f4e1d99de6f1bf6dff68d kostenfrei https://www.frontiersin.org/articles/10.3389/fchem.2022.926543/full kostenfrei https://doaj.org/toc/2296-2646 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022
allfields_unstemmed	10.3389/fchem.2022.926543 doi (DE-627)DOAJ042404770 (DE-599)DOAJa9f0db83f64f4e1d99de6f1bf6dff68d DE-627 ger DE-627 rakwb eng QD1-999 Chun-Mei Hu verfasserin aut Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (KI = 18.82 μM, KIS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t. coumarin chalcone α-glucosidase enzyme inhibitor docking Chemistry Yong-Xin Luo verfasserin aut Wen-Jing Wang verfasserin aut Jian-Ping Li verfasserin aut Meng-Yue Li verfasserin aut Yu-Fei Zhang verfasserin aut Di Xiao verfasserin aut Li Lu verfasserin aut Zhuang Xiong verfasserin aut Na Feng verfasserin aut Chen Li verfasserin aut In Frontiers in Chemistry Frontiers Media S.A., 2014 10(2022) (DE-627)742224538 (DE-600)2711776-5 22962646 nnns volume:10 year:2022 https://doi.org/10.3389/fchem.2022.926543 kostenfrei https://doaj.org/article/a9f0db83f64f4e1d99de6f1bf6dff68d kostenfrei https://www.frontiersin.org/articles/10.3389/fchem.2022.926543/full kostenfrei https://doaj.org/toc/2296-2646 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022
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allfieldsSound	10.3389/fchem.2022.926543 doi (DE-627)DOAJ042404770 (DE-599)DOAJa9f0db83f64f4e1d99de6f1bf6dff68d DE-627 ger DE-627 rakwb eng QD1-999 Chun-Mei Hu verfasserin aut Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (KI = 18.82 μM, KIS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t. coumarin chalcone α-glucosidase enzyme inhibitor docking Chemistry Yong-Xin Luo verfasserin aut Wen-Jing Wang verfasserin aut Jian-Ping Li verfasserin aut Meng-Yue Li verfasserin aut Yu-Fei Zhang verfasserin aut Di Xiao verfasserin aut Li Lu verfasserin aut Zhuang Xiong verfasserin aut Na Feng verfasserin aut Chen Li verfasserin aut In Frontiers in Chemistry Frontiers Media S.A., 2014 10(2022) (DE-627)742224538 (DE-600)2711776-5 22962646 nnns volume:10 year:2022 https://doi.org/10.3389/fchem.2022.926543 kostenfrei https://doaj.org/article/a9f0db83f64f4e1d99de6f1bf6dff68d kostenfrei https://www.frontiersin.org/articles/10.3389/fchem.2022.926543/full kostenfrei https://doaj.org/toc/2296-2646 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022
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callnumber-first	Q - Science
author	Chun-Mei Hu
spellingShingle	Chun-Mei Hu misc QD1-999 misc coumarin misc chalcone misc α-glucosidase misc enzyme inhibitor misc docking misc Chemistry Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors
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topic_title	QD1-999 Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors coumarin chalcone α-glucosidase enzyme inhibitor docking
topic	misc QD1-999 misc coumarin misc chalcone misc α-glucosidase misc enzyme inhibitor misc docking misc Chemistry
topic_unstemmed	misc QD1-999 misc coumarin misc chalcone misc α-glucosidase misc enzyme inhibitor misc docking misc Chemistry
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title	Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors
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title_full	Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors
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title_sort	synthesis and evaluation of coumarin-chalcone derivatives as α-glucosidase inhibitors
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title_auth	Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors
abstract	Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (KI = 18.82 μM, KIS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t.
abstractGer	Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (KI = 18.82 μM, KIS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t.
abstract_unstemmed	Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (KI = 18.82 μM, KIS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t.
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title_short	Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors
url	https://doi.org/10.3389/fchem.2022.926543 https://doaj.org/article/a9f0db83f64f4e1d99de6f1bf6dff68d https://www.frontiersin.org/articles/10.3389/fchem.2022.926543/full https://doaj.org/toc/2296-2646
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Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors

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