Quercetin derivatives: Drug design, development, and biological activities, a review

Alizadeh, Seyedeh Roya; Ebrahimzadeh, Mohammad Ali

doi:10.1016/j.ejmech.2021.114068

Cited by 119 publications

(54 citation statements)

References 115 publications

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“…The representatives of phenolic acids include protocatechuic acid, caffeic acid, and paeonol; they all had a wide range of pharmacological activities, including antioxidant, immunomodulatory, neuroprotective, organ protective effects, and other anti-aging effects ( 73 – 76 ). Several quercetin derivatives were the representatives of flavonoids, which exhibited a wide range of biological activities by regulating multiple targets and signaling pathways, and they are popular candidate compounds in the field of anti-aging and against aging-related diseases ( 77 ). Plant tannins are a group of polyphenols with different molecular weights and complexity.…”

Section: Discussionmentioning

confidence: 99%

The anti-aging effects of Renshen Guben on thyrotoxicosis mice: Improving immunosenescence, hypoproteinemia, lipotoxicity, and intestinal flora

Feng

Li²,

Xia³

et al. 2022

Front. Immunol.

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With the rapid aging of the population, the control of age-related disease susceptibility and prognosis faces greater challenges. There is an urgent need for a strategy to maintain the vitality of elderly people. In this study, the effect of Renshen Guben (RSGB) oral liquid was investigated on an accelerated aging mice model of thyrotoxicosis by conventional detection methods combined with multiomics technology. The results showed that RSGB increased the number of neutrophils and lymphocytes, enhanced the function of lymphocytes, and increased the levels of complement and antimicrobial peptides, which indicated that RSGB improved the immunity of thyrotoxicosis mice at the cellular and molecular levels. RSGB corrected malnutrition in thyrotoxicosis mice by improving anemia, hypoalbuminemia, ion transporters, and vitamin-binding proteins. RSGB significantly reduced the lipotoxicity by reducing the level of fatty acids, triglyceride, sphingolipids, and glucocorticoids, thus increasing the level of docosapentaenoic acid (DPA) and bile acids, which contributed to improve immunosenescence. The intestinal defense ability of thyrotoxicosis mice was enhanced with the increase of bile acids and lactic acid bacteria by the RSGB treatment. The plant metabolomics analysis showed that there were various active components in RSGB oral liquid and medicated serum, including terpenoids, phenolic acids, flavonoids, tannin, alkaloids, organic acids, phenolamines, amino acids, and others. They have antioxidant, immune regulation, and anti-aging effects, which was the material basis of RSGB. Totally, RSGB protected the thyrotoxicosis mice against aging by improving immunosenescence, hypoproteinemia, lipotoxicity, and the intestinal flora. It will be beneficial for improving the disease susceptibility and prognosis of the elderly.

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Section: Discussionmentioning

confidence: 99%

The anti-aging effects of Renshen Guben on thyrotoxicosis mice: Improving immunosenescence, hypoproteinemia, lipotoxicity, and intestinal flora

Feng

Li²,

Xia³

et al. 2022

Front. Immunol.

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“…Que is a common flavonoid found in a variety of vegetables and fruits [17]. Owing to its strong antioxidative, anti-inflammatory, immunomodulatory, vascular-protective, and other biological activities, Que has been widely studied in the field of ophthalmology [18][19][20]. Que can penetrate the blood-brain barrier to exert its effects of antioxidation and neuroprotection [21,22].…”

Section: Discussionmentioning

confidence: 99%

Mechanisms of Qing-Gan Li-Shui Formulation in Ameliorating Primary Open Angle Glaucoma: An Analysis Based on Network Pharmacology

Dong

Zhang

2022

Evidence-Based Complementary and Alternative Medicine

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Objective. In this study, we investigated the mechanism of Qing-Gan Li-Shui formulation (QGLSF) in treating primary open glaucoma (POAG) by network pharmacology and in vitro experiments. Methods. The active pharmaceutical ingredients (APIs) of GLQSF (prepared with Prunella vulgaris, Kudzu root, Plantago asiatica, and Lycium barbarum) were obtained from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) and Yet Another Traditional Chinese Medicine database (YATCM). The targets of POAG were screened out with GeneCards, OMIM, PharmGKB, Therapeutic Target Database (TTD), and DrugBank databases. The Venny platform was used to summarize the core targets. Topological analysis was performed using Cytoscape3.8.0. A protein-protein interaction network was plotted by STRING online. The key targets were subjected to GO and KEGG enrichment analyses. Finally, the effects of APIs were verified by a model of chloride hexahydrate (CoCl2)-induced retinal ganglion cells-5 (RGC-5). Results. The main APIs were selected as quercetin (Que) by network pharmacology. Nine clusters of QGLSF targets were obtained by the PPI network analysis, including AKT-1, TP53, and JUN. KEGG enrichment analysis showed that these targets were mainly involved in the AGE-RAGE signaling pathway. By in vitro experiments, Que promoted cell proliferation. The secretion of AKT-1, TP53, JUN, AGE, and RAGE in the cell culture supernatant decreased, as shown by ELISA. The mRNA levels of AKT-1, TP53, JUN, and RAGE decreased, as shown by RT-PCR. QGLSF may employ the AGE-RAGE signaling pathway to counter POAG. Conclusion. This study preliminarily elucidates the efficacy and mechanism of QGLSF in the treatment of POAG.

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“…Natural compounds quercetin, fisetin and curcumin all belong to the class of senolytics. Natural compounds are mainly found in food and are therefore referred to as “nutraceuticals” ( 92 ). Quercetin is a plant flavonoid with powerful antioxidant activity.…”

Section: Senotherapeuticsmentioning

confidence: 99%

Senescence in Vascular Smooth Muscle Cells and Atherosclerosis

Zha

Zhuang

Yang

et al. 2022

Front. Cardiovasc. Med.

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Vascular smooth muscle cells (VSMCs) are the primary cell type involved in the atherosclerosis process; senescent VSMCs are observed in both aged vessels and atherosclerotic plaques. Factors associated with the atherosclerotic process, including oxidative stress, inflammation, and calcium-regulating factors, are closely linked to senescence in VSMCs. A number of experimental studies using traditional cellular aging markers have suggested that anti-aging biochemical agents could be used to treat atherosclerosis. However, doubt has recently been cast on such potential due to the increasingly apparent complexity of VSMCs status and an incomplete understanding of the role that these cells play in the atherosclerosis process, as well as a lack of specific or spectrum-limited cellular aging markers. The utility of anti-aging drugs in atherosclerosis treatment should be reevaluated. Promotion of a healthy lifestyle, exploring in depth the characteristics of each cell type associated with atherosclerosis, including VSMCs, and development of targeted drug delivery systems will ensure efficacy whilst evaluation of the safety and tolerability of drug use should be key aims of future anti-atherosclerosis research. This review summarizes the characteristics of VSMC senescence during the atherosclerosis process, the factors regulating this process, as well as an overview of progress toward the development and application of anti-aging drugs.

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Quercetin derivatives: Drug design, development, and biological activities, a review

Cited by 119 publications

References 115 publications

The anti-aging effects of Renshen Guben on thyrotoxicosis mice: Improving immunosenescence, hypoproteinemia, lipotoxicity, and intestinal flora

The anti-aging effects of Renshen Guben on thyrotoxicosis mice: Improving immunosenescence, hypoproteinemia, lipotoxicity, and intestinal flora

Mechanisms of Qing-Gan Li-Shui Formulation in Ameliorating Primary Open Angle Glaucoma: An Analysis Based on Network Pharmacology

Senescence in Vascular Smooth Muscle Cells and Atherosclerosis

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