The potential biological effects of quercetin based on pharmacokinetics and multi-targeted mechanism<i>in vivo</i>

Keranmu, Adili; Pan, Li-Bin; Yu, Hang; Fu, Jie; Liu, Yifang; Amuti, Siyiti; Han, Pei; Ma, Shu‐Rong; Xu, Hui; Zhang, Zhengwei; Chen, Dong; Yang, Feiya; Wang, Ming-Shuai; Wang, Yan; Xing, Nianzeng; Jiang, Jian‐Dong

doi:10.1080/10286020.2022.2045965

Cited by 3 publications

(2 citation statements)

References 226 publications

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“…Quercetin is a flavonoid that has been extensively examined in many studies that have demonstrated its antioxidant and anti-inflammatory properties in therapeutic applications. It is only relatively recently that interest has focused on quercetin metabolites and their biological properties [ 364 ]. The use of quercetin to treat OA rats has also been shown to influence gut bacterial populations with an elevation in the numbers of members of the Clostridia, Bacteroidia , and Bacilli families [ 365 ].…”

Section: Bioactive Quercetin Metabolitesmentioning

confidence: 99%

The Potential of Flavonoids and Flavonoid Metabolites in the Treatment of Neurodegenerative Pathology in Disorders of Cognitive Decline

Melrose

2023

Antioxidants

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Flavonoids are a biodiverse family of dietary compounds that have antioxidant, anti-inflammatory, antiviral, and antibacterial cell protective profiles. They have received considerable attention as potential therapeutic agents in biomedicine and have been widely used in traditional complimentary medicine for generations. Such complimentary medical herbal formulations are extremely complex mixtures of many pharmacologically active compounds that provide a therapeutic outcome through a network pharmacological effects of considerable complexity. Methods are emerging to determine the active components used in complimentary medicine and their therapeutic targets and to decipher the complexities of how network pharmacology provides such therapeutic effects. The gut microbiome has important roles to play in the generation of bioactive flavonoid metabolites retaining or exceeding the antioxidative and anti-inflammatory properties of the intact flavonoid and, in some cases, new antitumor and antineurodegenerative bioactivities. Certain food items have been identified with high prebiotic profiles suggesting that neutraceutical supplementation may be beneficially employed to preserve a healthy population of bacterial symbiont species and minimize the establishment of harmful pathogenic organisms. Gut health is an important consideration effecting the overall health and wellbeing of linked organ systems. Bioconversion of dietary flavonoid components in the gut generates therapeutic metabolites that can also be transported by the vagus nerve and systemic circulation to brain cell populations to exert a beneficial effect. This is particularly important in a number of neurological disorders (autism, bipolar disorder, AD, PD) characterized by effects on moods, resulting in depression and anxiety, impaired motor function, and long-term cognitive decline. Native flavonoids have many beneficial properties in the alleviation of inflammation in tissues, however, concerns have been raised that therapeutic levels of flavonoids may not be achieved, thus allowing them to display optimal therapeutic effects. Dietary manipulation and vagal stimulation have both yielded beneficial responses in the treatment of autism spectrum disorders, depression, and anxiety, establishing the vagal nerve as a route of communication in the gut-brain axis with established roles in disease intervention. While a number of native flavonoids are beneficial in the treatment of neurological disorders and are known to penetrate the blood–brain barrier, microbiome-generated flavonoid metabolites (e.g., protocatechuic acid, urolithins, γ-valerolactones), which retain the antioxidant and anti-inflammatory potency of the native flavonoid in addition to bioactive properties that promote mitochondrial health and cerebrovascular microcapillary function, should also be considered as potential biotherapeutic agents. Studies are warranted to experimentally examine the efficacy of flavonoid metabolites directly, as they emerge as novel therapeutic options.

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Section: Bioactive Quercetin Metabolitesmentioning

confidence: 99%

The Potential of Flavonoids and Flavonoid Metabolites in the Treatment of Neurodegenerative Pathology in Disorders of Cognitive Decline

Melrose

2023

Antioxidants

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“…Extracellular regulated protein kinase (ERK) (Guo et al., 2020) is the main member of the mitogen‐activated protein kinase family, which mainly regulates apoptosis, proliferation, and differentiation (Karisch et al., 2011). Phosphatase 1 (SHP‐1, also known as PTPN6) containing the Src homologous region 2 (SH2) domain is a non‐receptor protein tyrosine phosphatase (PTP) (Xu et al., 2012), a tyrosine phosphatase expressed in hematopoietic cells (Chen et al., 2022), containing two structures of SH2, the SHP‐1 gene is located in the p12–p13 region of chromosome 12, and the expressed product SHP‐1 is composed of 641 amino acid residues with a molecular weight of 70,510 Da, It plays an important role in cell signaling (Keranmu et al., 2022). Protein tyrosine phosphatase 1B (PTP1B) can bind directly to protein tyrosine kinase receptors, including IRs and epidermal growth factor receptors.…”

Section: Introductionmentioning

confidence: 99%

Network pharmacology and experiment indicated that medicinal food homologous components play important roles in insomnia

Xu,

Liu,

et al. 2023

Food Frontiers

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Insomnia refers to a subjective experience where insufficient sleep duration and quality affect daytime social functioning. This study aims to screen bioactive components with medicinal food homologous (MFH), such as quercetin, beta‐sitosterol, kaempferol, stigmasterol, and capsaicin, which can treat insomnia and demonstrate that quercetin acts as a direct inhibitor of insomnia‐related glucosylceramidase and as an insulin receptor tyrosine phosphatase inhibitor in the upstream insulin signaling pathway, affecting insomnia targets in the downstream pathway for the treatment of insomnia, using network pharmacology and cell experiment approaches. The results showed that 703 components in 44 MFH were enriched in 139 metabolic pathways and acted on 210 potential targets of insomnia. The protein–protein interaction network is analyzed by cytoNCA, according to the topological analysis results, quercetin, beta‐sitosterol, kaempferol, stigmasterol, and capsaicin of betweenness ranked in the top 10. Quercetin and glucosylceramidase were shown to directly inhibit insomnia proteins through reverse molecular docking. Quercetin was used to culture and stimulate HepG2 cells to detect tyrosine phosphorylation of key cellular proteins in the insulin signaling pathway, concluding that quercetin inhibits the activity of tyrosine phosphatase in a dose‐dependent manner, activating the insulin signaling pathway, triggering a cascade reaction, and affecting the expression of insomnia targets in the downstream pathway. The molecular docking of tyrosine phosphatase and quercetin revealed that quercetin interacted with it near the catalytic site, thereby inhibiting its interaction with the substrate. Overall, this study facilitates the development of medicinal food homologous, which exerts good pharmacological effects in the treatment of insomnia.

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Dietary herbs that interact with gut microbiota: roles as anti-stroke agents

Li,

Liu,

Wang

et al. 2024

Food Sci Biotechnol

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The potential biological effects of quercetin based on pharmacokinetics and multi-targeted mechanismin vivo

Cited by 3 publications

References 226 publications

The Potential of Flavonoids and Flavonoid Metabolites in the Treatment of Neurodegenerative Pathology in Disorders of Cognitive Decline

The Potential of Flavonoids and Flavonoid Metabolites in the Treatment of Neurodegenerative Pathology in Disorders of Cognitive Decline

Network pharmacology and experiment indicated that medicinal food homologous components play important roles in insomnia

Dietary herbs that interact with gut microbiota: roles as anti-stroke agents

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