Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetin

Abstract Fisetin is one of the most popular flavonoids found in vegetables and fruits with several health benefits such as antidiabetic, anticancer, and anti‐inflammatory activities. Biotechnology or chemosynthesis tools were used for the synthesis of fisetin and its analogs to improve their yield a...

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Main Authors: Ruting Zhong, Mohamed A. Farag, Meiwan Chen, Chengwei He, Jianbo Xiao
Format: Article
Language:English
Published: Wiley 2022-04-01
Series:eFood
Subjects:
Online Access:https://doi.org/10.1002/efd2.3
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author Ruting Zhong
Mohamed A. Farag
Meiwan Chen
Chengwei He
Jianbo Xiao
author_facet Ruting Zhong
Mohamed A. Farag
Meiwan Chen
Chengwei He
Jianbo Xiao
author_sort Ruting Zhong
collection DOAJ
description Abstract Fisetin is one of the most popular flavonoids found in vegetables and fruits with several health benefits such as antidiabetic, anticancer, and anti‐inflammatory activities. Biotechnology or chemosynthesis tools were used for the synthesis of fisetin and its analogs to improve their yield and efficacy. Structure activity relationships (SARs) revealed that the aromatic hydroxyl groups especially the 3,4‐dihydroxylation at ring B were crucial for fisetin biological activities, whereas substitution of several hydroxyl groups in fisetin appeared to impact its original effects. The ongoing or upcoming clinical trials containing fisetin are applied in drugs and dietary supplements. Noteworthily, fisetin has been successfully incorporated into nutraceuticals in the market. Furthermore, the delivery system of fisetin‐loaded nanocochleates showed the best bioavailability compared to other formulations. This review presents the latest research progress of fisetin on its synthesis, structure–activity relationships, pharmacokinetics, biological activities, and underlying mechanisms, bioavailability, delivery systems, and clinical trials to provide a comprehensive insight into the research and application of this valuable natural compound.
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spelling doaj.art-423b0b8b87a94516bb487e1f49e3416c2022-12-22T04:21:37ZengWileyeFood2666-30662022-04-0131-2n/an/a10.1002/efd2.3Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetinRuting Zhong0Mohamed A. Farag1Meiwan Chen2Chengwei He3Jianbo Xiao4Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine University of Macau Macau ChinaPharmacognosy Department, College of Pharmacy Cairo University Cairo EgyptInstitute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine University of Macau Macau ChinaInstitute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine University of Macau Macau ChinaDepartment of Analytical and Food Chemistry, Faculty of Sciences Universidade de Vigo Ourense SpainAbstract Fisetin is one of the most popular flavonoids found in vegetables and fruits with several health benefits such as antidiabetic, anticancer, and anti‐inflammatory activities. Biotechnology or chemosynthesis tools were used for the synthesis of fisetin and its analogs to improve their yield and efficacy. Structure activity relationships (SARs) revealed that the aromatic hydroxyl groups especially the 3,4‐dihydroxylation at ring B were crucial for fisetin biological activities, whereas substitution of several hydroxyl groups in fisetin appeared to impact its original effects. The ongoing or upcoming clinical trials containing fisetin are applied in drugs and dietary supplements. Noteworthily, fisetin has been successfully incorporated into nutraceuticals in the market. Furthermore, the delivery system of fisetin‐loaded nanocochleates showed the best bioavailability compared to other formulations. This review presents the latest research progress of fisetin on its synthesis, structure–activity relationships, pharmacokinetics, biological activities, and underlying mechanisms, bioavailability, delivery systems, and clinical trials to provide a comprehensive insight into the research and application of this valuable natural compound.https://doi.org/10.1002/efd2.3bioactivitiesbioavailabilityclinical trialsfisetinformulationsmolecular mechanism
spellingShingle Ruting Zhong
Mohamed A. Farag
Meiwan Chen
Chengwei He
Jianbo Xiao
Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetin
eFood
bioactivities
bioavailability
clinical trials
fisetin
formulations
molecular mechanism
title Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetin
title_full Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetin
title_fullStr Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetin
title_full_unstemmed Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetin
title_short Recent advances in the biosynthesis, structure–activity relationships, formulations, pharmacology, and clinical trials of fisetin
title_sort recent advances in the biosynthesis structure activity relationships formulations pharmacology and clinical trials of fisetin
topic bioactivities
bioavailability
clinical trials
fisetin
formulations
molecular mechanism
url https://doi.org/10.1002/efd2.3
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