Natural Product Communications
·
2018
·
IF 0.809
Yike Yue,Yongsheng Chen,Sheng Geng,Guizhao Liang,Benguo Liu
Fisetin is a flavonoid widespread in vegetables, fruits and medicinal plants. The in vitro antioxidant and α-glucosidase inhibitory activities of fisetin were systemically investigated in this study. The DPPH and ABTS radical scavenging performance of fisetin was higher than that of BHA. In the ORAC and PSC assays, fisetin also exhibited strong antioxidant activity. The α-glucosidase inhibitory activity of fisetin (IC50, 9.38±0.35 μg/mL) was significantly superior to that of acarbose (IC50, 1.07±0.15 mg/mL). Its inhibition type was determined to be a mixed competitive and non-competitive inhibition mode. Molecular docking analysis suggested it could exert the α-glucosidase inhibitory role by forming hydrogen bonds with the TRP391, ASP392, ARG428 and ASP568 residues of α-glucosidase.
研究领域:
药理学
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生物化学
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产品关联
DOI
高影响因子
PHYTOTHERAPY RESEARCH
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2025
·
IF 6.3
Xiao-Man Ji,Xin-Xin Dong,Jia-Peng Li,Guang-Jie Tai,Shu Qiu,Wei Wei,Ceaser Wankumbu Silumbwe,Davaadagva Damdinjav,Joseph Nicolao Otieno,Xiao-Xue Li,Ming Xu
Vascular aging is a major contributor to age-related cardiovascular diseases (CVDs) and type 2 diabetes mellitus (T2DM) induced early arterial aging and excessive senescent cells (SCs) burden in vessels. Inhibiting cellular senescence or eliminating SCs could effectively improve aging-related CVDs. Fisetin, a flavonoid extracted from cotinus coggygria scop, has shown potential in alleviating aging by clearing SCs. This study investigated the unexplored mechanisms and efficacy of fisetin in alleviating T2DM-related aortic aging. The T2DM mouse model was induced using a high-fat diet and low-dose streptozotocin injection. Chronic fisetin treatment's protective effects against aortic aging were assessed via senescence-associated beta-galactosidase (SA-β-Gal) staining, histopathology, and vasomotor function. RNA-sequencing and western blotting identified relevant signaling pathways and protein expression. Fisetin's effects on SCs and senescence-associated secretory phenotype (SASP) factors were evaluated through cell viability, apoptosis, and co-culture assays. Docking simulations suggested fisetin as a potential Phosphoinositide 3-kinase (Pi3k) inhibitor. In vivo, chronic fisetin treatment reduced aortic SCs burden, alleviating T2DM-related and natural aortic aging. In vitro, fisetin selectively induced apoptosis of senescent endothelial cells via regulating the Pi3k-Protein Kinase B (Akt)-B-cell lymphoma (Bcl)-2/Bcl-xl pathway and suppressed SASP and its detrimental effects. Furthermore, fisetin combined with metformin therapy showed superior anti-aging effects on T2DM-related aortic aging compared to metformin monotherapy. In conclusion, chronic fisetin treatment alleviates T2DM-related aortic aging via clearing the SCs burden and abrogating the SASP factors. Fisetin combined with metformin therapy might be a potential therapeutic strategy for T2DM-related CVDs.
研究领域:
药理学
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心血管疾病
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分子生物学
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产品关联
DOI
PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2025
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IF 8
Yao Guo,Guangjie Shu,Ziyang Zhang,Xiaoshuang Hu,Huiru Huang,Wenxin Lu,Miaomiao Zhu,Bing Liu,Shenshen Zhang
Cholesterol homeostasis dysregulation is a primary risk factor for atherosclerosis (AS) development. Fisetin, a flavonoid compound, has shown promise in regulating cholesterol homeostasis by enhancing transintestinal cholesterol excretion (TICE). This study aimed to investigate the regulatory effects and underlying mechanisms of fisetin in AS. In this study, ApoE −/− mice fed a high-fat diet (HFD) were employed to investigate the effects of fisetin on the prevention of AS. Various methods, including biochemical analyses, histopathological staining, lipid deposition assessment, untargeted lipidomics analysis and RNA sequencing, were employed to explore the underlying mechanisms. The results showed that treatment with fisetin notably reduced lipid deposition in the aortic root of HFD-treated ApoE −/− mice and attenuated hepatic lipid deposition and histopathological changes. This was accompanied by decreased serum levels of total cholesterol, triglyceride and LDL cholesterol. Fisetin also effectively mitigated HFD-induced oxidative stress and inflammation in mice. Hepatic lipidomics revealed significant alterations in lipid content and composition following fisetin treatment, including reductions in lipids associated with AS risk, such as cholesteryl ester (ChE), phosphatidylcholines (PC), phosphatidylethanolamine (PE), lysophosphatidylcholine (LPC), cardiolipin (CL), phosphatidylinositol (PI), and TG. Additionally, phosphatidylserine (PS) levels were increased. RNA sequencing of livers revealed that fisetin affected genes related to cholesterol metabolism and bile acid biosynthesis, including cytochrome P450 ( Cyp ) family and Nr1h4 ( Fxr ). Molecular docking analysis suggested FXR may be a potential target of fisetin. In the liver, cholesterol can be either converted into bile acids or pumped out to bile ducts by ATP-binding cassette (ABC) transporters G5 (ABCG5) and G8 (ABCG8) for elimination. Fisetin treatment notably modulated the hepatic proteins related to cholesterol metabolism (HMGCR, PCSK9, LDLR, FXR, CYP27A1, CYP7A1, CYP8B1 and BSEP) and cholesterol excretion (ABCG5, ABCG8), maintaining cholesterol homeostasis. Additionally, fisetin increased the excretion of fecal neutral sterols, including cholesterol, dihydrocholesterol, and coprosterone. It also increased the expression of FXR, ABCG5, ABCG8, and LDLR, while decreasing NPC1L1 and PCSK9 levels in the jejunum, thereby stimulating the TICE pathway. These findings provide compelling evidence that fisetin reduces cholesterol levels and alleviates AS by stimulating FXR-mediated hepatic cholesterol metabolism and the TICE pathway. The findings suggest that fisetin-regulated cholesterol metabolism may represent a promising therapeutic strategy for the treatment of AS.
研究领域:
药理学
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心血管医学
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生物化学
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分子生物学
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营养科学
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产品关联
DOI
PubMed
高影响因子
Journal of Functional Foods
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2019
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IF 3.197
Ni Zeng,Guowen Zhang,Xing Hu,Junhui Pan,Deming Gong
Excessive activity of xanthine oxidase (XO) will promote the formation of uric acid and superoxide anion (O 2 − ), which may cause hyperuricemia and oxidative damage. Fisetin, a dietary flavonoid, was found to insert into flavin adenine dinucleotides (FAD) center of XO, which might hinder the diffusion of O 2 − out of the FAD site, leading to the significant decrease of uric acid formation. The promotion of reduced XO and the suppression of uric acid formation resulting from the inhibition of XO by fisetin led to a decrease in O 2 − radical. Hydrogen bonding and hydrophobic interactions facilitated the formation of fisetin–XO complex. The chemical modification of XO confirmed the results of molecular docking that three polar amino acid residues Gln, Arg and Lys played a crucial role in the binding process. Furthermore, the isobolographic analysis showed that the joint use of fisetin and allopurinol exhibited a synergistic inhibition on XO activity.
研究领域:
药理学
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生物化学
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分子生物学
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产品关联
DOI
高影响因子
Advanced Pharmaceutical Bulletin
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2016
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IF 0
Tingting Wang,Huajuan Lin,Qian Tu,Jingjing Liu,Xican Li
Purpose: The paper tries to assess the protective effect of fisetin against •OH-induced DNA damage, then to investigate the possible mechanism. Methods: The protective effect was evaluated based on the content of malondialdehyde (MDA). The possible mechanism was analyzed using various antioxidant methods in vitro, including •OH scavenging (deoxyribose degradation), •O 2 - scavenging (pyrogallol autoxidation), DPPH• scavenging, ABTS• + scavenging, and Cu 2+ -reducing power assays. Results: Fisetin increased dose-dependently its protective percentages against •OH-induced DNA damage (IC 50 value =1535.00±29.60 µM). It also increased its radical-scavenging percentages in a dose-dependent manner in various antioxidants assays. Its IC 50 values in •OH scavenging, •O2 - scavenging, DPPH• scavenging, ABTS• + scavenging, and Cu 2+ -reducing power assays, were 47.41±4.50 µM, 34.05±0.87 µM, 9.69±0.53 µM, 2.43±0.14 µM, and 1.49±0.16 µM, respectively. Conclusion: Fisetin can effectively protect DNA against •OH-induced oxidative damage possibly via reactive oxygen species (ROS) scavenging approach, which is assumed to be hydrogen atom (H•) and/or single electron (e) donation (HAT/SET) pathways. In the HAT pathway, the 3’,4’-dihydroxyl moiety in B ring of fisetin is thought to play an important role, because it can be ultimately oxidized to a stable ortho-benzoquinone form.
研究领域:
分子生物学
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药理学
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产品关联
DOI
PubMed
MACROMOLECULAR BIOSCIENCE
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2023
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IF 4.6
Chunru Wang,Yingjie Xiang,Wenjie Ma,Chuanlong Guo,Xiaochen Wu
Ulcerative colitis is a chronic inflammatory bowel disease with a high recurrence rate. Natural phytochemical compounds are increasingly being considered as preventative and supportive treatments for this condition. However, the poor water solubility and stability of many of these compounds limit their effectiveness in vivo. To address this issue, fisetin (FT), a natural phytochemical with poor solubility, was stabilized using silk sericin (SS) to create a composite (SS/FT). The therapeutic potential of the SS/FT on ulcerative colitis was extensively investigated, and the results showed that it effectively alleviated the body weight loss and colon length shortening induced by dextran sulfate sodium. Notably, SS/FT downregulated the immune response, decreased colonic histopathological lesions, and reduced the cGAS/STING signal activation. This suggests that SS/FT may offer a promising therapy for treating ulcerative colitis. This article is protected by copyright. All rights reserved
研究领域:
药理学
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炎症性肠病
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天然产物化学
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DOI
PubMed
高影响因子
RSC Advances
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2014
·Vol. 5
·期 10
·7433-7439
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IF 3.708
Xiaodan Liu,Xia Wu
In this work, in situ synthesized cetyltrimethyl ammonium bromide micelles-capped silver nanoparticles were used to sensitively and directly detect fisetin. Fisetin molecules solubilize in the Stern layer of cetyltrimethyl ammonium bromide micelles and mainly bind to the head group of the micelles by electrostatic interaction and hydrophobic effect. Silver nanoparticles also solubilize in cetyltrimethyl ammonium bromide micelles and form the micelles-capped silver nanoparticles. The suitable distances between fisetin molecules and silver nanoparticles for the fluorescence enhancement are provided by the micelles. The synergistic action of the solubilization and sensitization of micelles and metal-enhanced fluorescence of silver nanoparticles promote the fluorescence enhancement of the system. Under optimized conditions, the fluorescence intensity of the system exhibits a linear response with the concentrations of fisetin in the range from 5.0 × 10−8 mol L−1 to 7.0 × 10−6 mol L−1 and the detection limit (S/N = 3) is 1.5 × 10−9 mol L−1. Compared to the other methods, the developed method has higher sensitivity. Moreover, the method has been successfully used to detect fisetin in actual samples.
研究领域:
分析化学
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纳米技术
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药物分析
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产品关联
DOI
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2023
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IF 4.4
Wenli Shi,Wenxin Han,Yijing Liao,Jiaqi Wen,Guowen Zhang
The search for acetylcholinesterase (AChE) inhibitors produced by natural sources is of great significance for the prevention and therapy of Alzheimer's disease and has been widely concerned. In this study, fisetin, a flavonoid compound of plant origin, displayed a mixed inhibition mode on AChE (IC 50 = 8.88 ± 0.14 μM). Fluorescence spectra analysis revealed that fisetin statically quenched AChE fluorescence, and the ground state complex was formed by hydrogen bonds and hydrophobic interactions. Circular dichroism assays showed that fisetin induced AChE structure loosened with a decrease in α-helix structure (from 20.6 % to 19.5 %). Computer simulation exhibited that fisetin bound to both the peripheral anionic site (PAS) and the catalytic active site (CAS) and increased the stability of the AChE. Interestingly, the combination of fisetin and galantamine enhanced the binding affinity between AChE and galantamine and induced AChE structure further loosened, while the inhibition mode was still the mixed type. The heatmap analysis indicated that galantamine (0.2 μM) combined with fisetin (2.25 μM) had a significant synergy on AChE inhibition, probably because fisetin binding at the PAS-AChE induced conformation changes of the gorge and CAS, which enhanced galantamine binding affinity with CAS, and a further loose structure of AChE was induced by the mixture, so finally the interaction between the substrate and AChE was strongly affected. This work may offer a theoretical reference for the functional research of fisetin as a potential AChE inhibitor and an enhanced supplement for galantamine.
研究领域:
药理学
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神经科学
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植物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHYSICAL CHEMISTRY B
·
2026
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IF 3.2
Yongchun Tan,Cheng Wang,Ziyi Wang,Qin Yu,Han Pan,Xiya Peng,Jian Luo
Fisetin is widely employed as a natural fluorescent probe for sensing local environmental dynamics in micelles and membranes, owing to its large Stokes shift emission arising from excited-state intramolecular proton transfer (ESIPT) and the characteristic fluorescence of its anionic form. In contrast to the extensive studies on the ESIPT of neutral fisetin, the ESIPT processes in fisetin anions have received much less attention. In this work, we incorporated 3-hydroxyflavone and fisetin into two poly(vinyl alcohol) (PVA) films that were codoped with oxalic acid and dimethyl sulfoxide, respectively. Anionic 3-hydroxyflavone and fisetin species formed in the films, as evidenced by an increased absorption in the visible spectral region. Dual emission was achieved in the PVA films upon visible-light excitation, originating from the normal and ESIPT tautomer species of divalent fisetin anions. The ESIPT barrier heights for these anions, calculated using time-dependent density functional theory, are comparable to that of neutral fisetin. This study confirms the microbasicity of PVA films and provides fundamental insight into the ESIPT process of deprotonated fisetin, offering a clear basis for its application as a microenvironmental probe in soft matter systems.
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DOI
PubMed
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
·
2025
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IF 12.6
Deng Yu,Jiang Xinyu,Che Zhenzhen,Shang Yaqi,Hu Mengting,Wang Wentian,Yu Weixian,Yang Bai,Liu Xinchan
Periodontitis is a chronic inflammatory disease strongly linked to the sustained accumulation of reactive oxygen species (ROS). Eliminating excessive ROS and modulating the periodontal microenvironment to suppress inflammation represents a promising therapeutic approach for the treatment of periodontitis. Fisetin (FIS) is a naturally occurring flavonoid known for its strong antioxidant and anti-inflammatory effects. However, its poor water solubility and low bioavailability limit its therapeutic efficacy. Carbon dots (CDs), as an emerging nanomaterial, offer advantages such as simple synthesis, good biocompatibility, and low cost. To overcome the limitations of FIS, this study synthesized fisetin-derived carbon dots (FIS-CDs) via a hydrothermal method. The resulting FIS-CDs exhibits excellent water solubility, favorable biocompatibility, and demonstrates excellent ROS-scavenging capability without the need for further modification. In vitro FIS-CDs significantly reduced intracellular ROS levels, alleviate oxidative stress, maintain mitochondrial homeostasis, and suppress the generation of inflammatory cytokines. Furthermore, FIS-CDs exhibit excellent osteogenic potential. In vivo experiments confirmed that FIS-CDs markedly alleviated periodontal inflammation and oxidative damage, suppressed alveolar bone loss, and promoted regeneration of periodontal tissues. Mechanistically, FIS-CDs facilitate the activation of mitophagy by downregulating the SUMOylation of sirtuin 3 (SIRT3). This modulation contributes to the restoration of mitochondrial function, which in turn mitigates cellular injury and limits the secretion of inflammatory mediators. Collectively, these findings underscore the therapeutic promise of FIS-CDs as a safe and effective nanomaterial for periodontitis treatment and suggest a novel molecular target for future drug development. Graphical abstract
研究领域:
纳米医学
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牙科学
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分子生物学
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氧化应激与抗氧化
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炎症性疾病
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产品关联
DOI
PubMed
高影响因子
Foods
·
2024
·Vol. 13
·期 15
·2406
·
IF 4.7
Yan Sun,Xinghui Shen,Jiaqi Yang,Chen Tan
Fisetin has shown numerous health benefits, whereas its food application is constrained by water insolubility, poor stability, and low bioaccessibility. This work investigated the potential of hyaluronic acid (HA)-coated nanoliposomes for the encapsulation and delivery of fisetin. It was observed that HA can adsorb onto the liposomal membrane through hydrogen bonding and maintain the spherical shape of nanoliposomes. Fluorescence analysis suggested that the HA coating restricted the motion and freedom of phospholipid molecules in the headgroup region and reduced the interior micropolarity of the nanoliposomes but did not affect the fluidity of the hydrophobic core. These effects were more pronounced for the HA with a low molecular weight (35 kDa) and moderate concentration (0.4%). The HA coating improved the storage and thermal stability of the nanoliposomes, as well as the digestive stability and bioaccessibility of the encapsulated fisetin. These findings could guide the development of HA-coated nanoliposomes for the controlled delivery of hydrophobic bioactives such as fisetin in functional foods.
研究领域:
食品科学
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药物递送
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生物化学
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DOI
PubMed
高影响因子
Food Science & Nutrition
·
2025
·Vol. 13
·期 6
·e70309
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IF 3.8
Jiahui Gao,Yujia Song,Zanxiang Luo,Zejie Su,Chengshi Fu,Anran Gao,Jingxiu Zhao,Lie Liu,Xiangyun Teng,Jianhua Xu
Liver cancer (LC) is among the most prevalent malignant tumors in the digestive tract. The high incidence rate, high metastasis and recurrence rate, poor prognosis, and heterogeneity of liver cancer seriously threaten human health. It is very necessary to search for new drugs and new targets against liver cancer. Natural drugs have been proved to have good anti-tumor effects. Fisetin, a dietary flavonoid often found in fruits and vegetables, has multiple pharmacological functions such as anti-inflammation, anti-oxidation, immune regulation, and anti-tumor. Firstly, we found in vitro that fisetin could inhibit the proliferation, migration, and invasion of liver cancer cells. Bioinformatics analysis speculated that its anti-liver cancer mechanism might be related to the formation of neutrophil extracellular traps (NETs). Then, neutrophils were extracted from healthy volunteers, and it was found that fisetin might inhibit the formation of NETs through the AKT/ROS axis. Then, liver cancer cells were cultured in the medium containing NETs. We found that fisetin could weaken the proliferation, migration, and invasion of liver cancer cells induced by NETs. Finally, we found that fisetin could inhibit tumor growth in C57BL/6 mice. Fisetin could inhibit the recruitment of neutrophils and the level of NETs in tumor tissues. In conclusion, we found that fisetin could be used as a new NETs inhibitor and further clarified the anti-liver cancer effect of fisetin.
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DOI
PubMed
高影响因子
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