Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity

Scopoletin is a coumarin synthesized by diverse medicinal and edible plants, which plays a vital role as a therapeutic and chemopreventive agent in the treatment of a variety of diseases. In this review, an overview of the pharmacology, pharmacokinetics, and toxicity of scopoletin is provided. In ad...

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Main Authors: Xiao-Yan Gao, Xu-Yang Li, Cong-Ying Zhang, Chun-Ying Bai
Format: Article
Language:English
Published: Frontiers Media S.A. 2024-02-01
Series:Frontiers in Pharmacology
Subjects:
Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2024.1268464/full
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author Xiao-Yan Gao
Xiao-Yan Gao
Xiao-Yan Gao
Xu-Yang Li
Xu-Yang Li
Cong-Ying Zhang
Cong-Ying Zhang
Cong-Ying Zhang
Chun-Ying Bai
Chun-Ying Bai
author_facet Xiao-Yan Gao
Xiao-Yan Gao
Xiao-Yan Gao
Xu-Yang Li
Xu-Yang Li
Cong-Ying Zhang
Cong-Ying Zhang
Cong-Ying Zhang
Chun-Ying Bai
Chun-Ying Bai
author_sort Xiao-Yan Gao
collection DOAJ
description Scopoletin is a coumarin synthesized by diverse medicinal and edible plants, which plays a vital role as a therapeutic and chemopreventive agent in the treatment of a variety of diseases. In this review, an overview of the pharmacology, pharmacokinetics, and toxicity of scopoletin is provided. In addition, the prospects and outlook for future studies are appraised. Scopoletin is indicated to have antimicrobial, anticancer, anti-inflammation, anti-angiogenesis, anti-oxidation, antidiabetic, antihypertensive, hepatoprotective, and neuroprotective properties and immunomodulatory effects in both in vitro and in vivo experimental trials. In addition, it is an inhibitor of various enzymes, including choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies have demonstrated the low bioavailability, rapid absorption, and extensive metabolism of scopoletin. These properties may be associated with its poor solubility in aqueous media. In addition, toxicity research indicates the non-toxicity of scopoletin to most cell types tested to date, suggesting that scopoletin will neither induce treatment-associated mortality nor abnormal performance with the test dose. Considering its favorable pharmacological activities, scopoletin has the potential to act as a drug candidate in the treatment of cancer, liver disease, diabetes, neurodegenerative disease, and mental disorders. In view of its merits and limitations, scopoletin is a suitable lead compound for the development of new, efficient, and low-toxicity derivatives. Additional studies are needed to explore its molecular mechanisms and targets, verify its toxicity, and promote its oral bioavailability.
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spelling doaj.art-f3133e612f0741ccb5d99b6702b72a352024-02-23T17:15:57ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122024-02-011510.3389/fphar.2024.12684641268464Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicityXiao-Yan Gao0Xiao-Yan Gao1Xiao-Yan Gao2Xu-Yang Li3Xu-Yang Li4Cong-Ying Zhang5Cong-Ying Zhang6Cong-Ying Zhang7Chun-Ying Bai8Chun-Ying Bai9Basic Medicine College, Chifeng University, Chifeng, ChinaInner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, ChinaKey Laboratory of Mechanism and Evaluation of Chinese and Mongolian Pharmacy at Chifeng University, Chifeng University, Chifeng, ChinaBasic Medicine College, Chifeng University, Chifeng, ChinaInner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, ChinaBasic Medicine College, Chifeng University, Chifeng, ChinaInner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, ChinaKey Laboratory of Mechanism and Evaluation of Chinese and Mongolian Pharmacy at Chifeng University, Chifeng University, Chifeng, ChinaBasic Medicine College, Chifeng University, Chifeng, ChinaInner Mongolia Key Laboratory of Human Genetic Disease Research, Chifeng University, Chifeng, ChinaScopoletin is a coumarin synthesized by diverse medicinal and edible plants, which plays a vital role as a therapeutic and chemopreventive agent in the treatment of a variety of diseases. In this review, an overview of the pharmacology, pharmacokinetics, and toxicity of scopoletin is provided. In addition, the prospects and outlook for future studies are appraised. Scopoletin is indicated to have antimicrobial, anticancer, anti-inflammation, anti-angiogenesis, anti-oxidation, antidiabetic, antihypertensive, hepatoprotective, and neuroprotective properties and immunomodulatory effects in both in vitro and in vivo experimental trials. In addition, it is an inhibitor of various enzymes, including choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies have demonstrated the low bioavailability, rapid absorption, and extensive metabolism of scopoletin. These properties may be associated with its poor solubility in aqueous media. In addition, toxicity research indicates the non-toxicity of scopoletin to most cell types tested to date, suggesting that scopoletin will neither induce treatment-associated mortality nor abnormal performance with the test dose. Considering its favorable pharmacological activities, scopoletin has the potential to act as a drug candidate in the treatment of cancer, liver disease, diabetes, neurodegenerative disease, and mental disorders. In view of its merits and limitations, scopoletin is a suitable lead compound for the development of new, efficient, and low-toxicity derivatives. Additional studies are needed to explore its molecular mechanisms and targets, verify its toxicity, and promote its oral bioavailability.https://www.frontiersin.org/articles/10.3389/fphar.2024.1268464/fullscopoletinplant sourcespharmacological activitiespharmacokineticstoxicology
spellingShingle Xiao-Yan Gao
Xiao-Yan Gao
Xiao-Yan Gao
Xu-Yang Li
Xu-Yang Li
Cong-Ying Zhang
Cong-Ying Zhang
Cong-Ying Zhang
Chun-Ying Bai
Chun-Ying Bai
Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity
Frontiers in Pharmacology
scopoletin
plant sources
pharmacological activities
pharmacokinetics
toxicology
title Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity
title_full Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity
title_fullStr Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity
title_full_unstemmed Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity
title_short Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity
title_sort scopoletin a review of its pharmacology pharmacokinetics and toxicity
topic scopoletin
plant sources
pharmacological activities
pharmacokinetics
toxicology
url https://www.frontiersin.org/articles/10.3389/fphar.2024.1268464/full
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