BIOCHEMICAL PHARMACOLOGY
·
2021
·
IF 5.858
Shisong Jing,Li Wang,Tiedong Wang,Lianghai Fan,Lin Chen,Hua Xiang,Yan Shi,Dacheng Wang
Methicillin-resistant Staphylococcus aureus is one of the leading causes of community and nosocomial infections, which has created the urgent need for innovative anti-infective agents to control MRSA-associated infections. A conserved serine protease , caseinolytic peptidase P (ClpP) in Staphylococcus aureus is highly associated with pathogenicity and has been claimed to be a novel antimicrobial target. We aim to search suitable inhibitors of ClpP to attenuate the virulence of MRSA and combat their infections in vivo . Over 500 natural compounds were pre-screened via fluorescence resonance energy transfer using the Suc-LY-AMC substrate. The binding of myricetin to ClpP was determined and the mechanism of action was elucidated by thermal shift assay, surface plasmon resonance , and molecular dynamics simulations. The therapeutic effects of myricetin on S. aureus infection were further investigated using a S. aureus -induced pneumonia model. We revealed that myricetin could effectively block the activity of ClpP without disturbing the growth of the bacteria and the Gln-47 and Met-31 residues were necessary for myricetin binding to ClpP. Importantly, myricetin attenuated the pathogenicity of S. aureus in vivo , while improving the efficacy of the traditional antibiotic oxacillin against MRSA infection and protecting mice from fatal lung infections caused by MRSA. These findings indicate that myricetin has the potential to be applied in the pharmaceutical industry as a promising therapeutic agent.
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF IMMUNOPATHOLOGY AND PHARMACOLOGY
·
2025
·
IF 2.6
Jie-Fang Gao,Tong-Xuan Li,Guo-Qiang Zhang
The skin serves as the primary defensive barrier of the human body against external stimuli and damage. Keratinocytes, which are the predominant cell type in the human epidermis, undergo a differentiation process that is crucial for the formation of the skin barrier. Myricetin, a dietary flavonoid present in various fruits and vegetables, is known to play a significant role in maintaining intestinal barrier function; however, its impact on the skin barrier remains inadequately understood. Consequently, this study investigates the effects of myricetin on the differentiation of epidermal keratinocytes and the integrity of the skin barrier. Differentiation of primary mouse keratinocytes was induced using 1.8 mM CaCl2. tudy demonstrated that myricetin effectively suppresses cell proliferation and induces both cell cycle arrest and calcium ion (Ca2+) influx, without influencing apoptosis. Concurrently, myricetin enhances the expression of differentiation markers, including K10, TGase1, Filaggrin, and Involucrin, and facilitates the formation of tight junctions. Upon examining the underlying mechanisms, we discovered that myricetin activates the TRPV4 channel, and the promotion of keratinocyte differentiation by myricetin is contingent upon the activation of this channel. In summary, these findings suggested that myricetin could promote keratinocytes differentiation and have well-established skin barrier protective function.
研究领域:
细胞生物学
·
皮肤病学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
·
2020
·Vol. 394
·期 1
·165-175
·
IF 2.05
Xu Haibo,Qi Qian,Yan Xixin
Myricetin belongs to the flavonoid family which is derived from plant source. It is well-known for the anti-inflammatory and anti-oxidative properties yet the clinical use of myricetin awaits further discovery. Acute lung injury (ALI) is commonly caused by sepsis which leads to enormous burden with high morbidity and mortality. In this study, a murine sepsis model was constructed by cecal ligation and puncture (CLP). The indicated dose of myricetin (100 mg/kg) was further administrated intragastrically. The survival rate test indicated that myricetin significantly improved the vitality of CLP-operated mice. The pathological changes in morphology, biomarkers of inflammatory response, oxidative stress response, and mitochondrial damage were further detected. Myricetin showed significant inhibitory effects on these changes in CLP-induced mice. Furthermore, expression levels of transcription factor Nrf2 and heme oxygenase-1 (HO-1) along with DNA binding activity of Nrf2 were analyzed by western blot and EMSA, indicating that myricetin positively regulates the Nrf2/HO-1 pathway in CLP-induced sepsis mice. Murine sepsis models with knockdown of Nrf2 and control were further established and suggested that myricetin might exert protective effects on sepsis lung injury in dependent with Nrf2. Our study provides novel mechanisms for the protective effect of myricetin in sepsis-associated acute lung injury.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2023
·
IF 5.6
Hui-Wen Yang,Yan Lan,An Li,Han Wu,Zi-Wei Song,Ai-Ling Wan,Yue Wang,Shi-Bao Li,Shuai Ji,Zhong-Cheng Wang,Xin-Yu Wu,Ting Lan
Background: Ovarian cancer (OC) is the second most common gynecological malignancy and has a high mortality rate. The current chemotherapeutic drugs have the disadvantages of drug resistance and side effects. Myricetin, a kind of natural compound, has the advantages of easy extraction, low price, and fewer side effects. Multiple studies have demonstrated the anti-cancer properties of myricetin. However, its impact on OC is still unknown and needs further investigation. Therefore, this study aimed to elucidate the mechanism by which myricetin suppresses transforming growth factor-β (TGF-β) -induced epithelial-to-mesenchymal transition (EMT) in OC through in vivo and in vitro experiments. Methods: In vitro experiments were conducted to evaluate the effects of myricetin on cell proliferation and apoptosis using CCK8 assay, plate clonal formation assay, and flow cytometry. Western blot was employed to evaluate the expression levels of caspase-3, PARP, and the MAPK/ERK and PI3K/AKT signaling pathways. Wound healing, transwell, western blot and immunofluorescence assay were used to detect TGF-β-induced cell migration, invasion, EMT and the levels of Smad3, MAPK/ERK, PI3K/AKT signaling pathways. Additionally, a mouse xenograft model was established to verify the effects of myricetin on OC in vivo . Results: Myricetin inhibited OC proliferation through MAPK/ERK and PI3K/AKT signaling pathways. Flow cytometry and western blot analyses demonstrated that myricetin promoted apoptosis by increasing the expression of cleaved-PARP and cleaved-caspase-3 and the ratio of Bax/Bcl-2 in OC. Furthermore, myricetin suppressed the TGF-β-induced migration and invasion by transwell and wound healing assays. Mechanistically, western blot indicated that myricetin reversed TGF-β-induced metastasis through Smad3, MAPK/ERK and PI3K/AKT signaling pathway. In vivo , myricetin significantly repressed OC progression and liver and lung metastasis. Conclusion: Myricetin exhibited inhibitory effects on OC progression and metastasis both in vivo and in vitro . And it also reversed TGF-β-induced EMT through the classical and non-classical Smad signaling pathways.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ELECTROCHIMICA ACTA
·
2026
·
IF 5.8
Ruipeng Hao,Fangyuan He,Xuwen Gao,Wenbo Lu,Sumin Bian,Hugo Vankelecom,Chenzhong Li
Myricetin is a naturally occurring flavonoid found in various fruits and medicinal plants, possessing significant antioxidant and pharmacological activities. Accurate determination of myricetin is crucial for food quality control and pharmaceutical analysis. In this work, we synthesized a hierarchical composite consisting of cobalt-based Prussian blue analogue grown on Ni-MOF nanosheets supported on nickel foam (Co-PBA@Ni-MOF/NF) and employed it as a sensitive electrochemical sensor for myricetin detection. The composite combines the high conductivity and large surface area of Ni-MOF with the uniform catalytic sites of Co-PBA, significantly enhancing the electrocatalytic oxidation of myricetin. The as-prepared myricetin electrochemical sensor exhibited a wide linear range of 0–500 μM, a low detection limit of 0.168 μM, and high sensitivity of 1126 μA·mM⁻ 1 ·cm⁻ 2 . Furthermore, this sensor demonstrated excellent selectivity, stability, and reproducibility. Importantly, the sensor was successfully applied for the quantitative detection of myricetin in juice samples, achieving a satisfactory recovery rate of 98.15%–101.37%, demonstrating its practical utility for myricetin detection in real food samples.
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Xiaoman Yang,Yun Huang,Xiaoju Liang,Haibo Tan,Zhongyu Zhou,Xinxin Feng,Xiaoyi Chai,Ling Yuan,Ying Wang,Yongqing Li
This study lays a foundation for trimethylated flavonoid biosynthesis. • Two novel flavonoid OMTs with 3′,4′,5′- O -trimethylation were identified and characterized. • Key residue driving trimethylation was identified and verified. • Trimethylation enhanced the antibacterial activity of myricetin. Flavonoids are plant specialized metabolites widely distributed in plants with many health benefits. O -methyltransferases (OMTs) are pivotal in plant specialized metabolism by producing methylated derivatives with enhanced biological activity. In this study, we identified two novel flavonoid OMTs, GiOMT4 and GiOMT9, from Glycyrrhiza inflata , a medicinal licorice species commonly used in Chinese medicine. These enzymes could catalyze myricetin and dihydromyricetin to produce 3′,4′,5′- O -trimethyl derivatives in a reaction. Structural modeling and site-directed mutagenesis identified Trp193 as critical residue determining the specificity of trimethylation of GiOMT4. Notably, trimethylation markedly enhanced the antibacterial activity of flavonoids against Gram-positive bacteria, including Methicillin-Resistant Staphylococcus aureus and Vancomycin-Resistant Enterococcus . Furthermore, trimethyl dihydromyricetin was identified as a novel compound with unexplored pharmacological potential. Collectively, this study expands the enzymatic repertoire of licorice OMTs, provides new insights into the structure-function relationships underling multiple methylations, and establishes a foundation or sustainable biocatalytic production of highly bioactive methylated flavonoids in G. inflata and related species.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2022
·
IF 7.419
Zhiqi Zhao,Yizhang Chen,Xiaoqiong Li,Liying Zhu,Xin Wang,Li Li,Haibiao Sun,Xiaoqiang Han,Jinjun Li
To verify the role of myricetin in alleviating the symptoms of type 2 diabetes and regulating the intestinal flora, we established a type 2 diabetes mouse model. After being fed a high-fat and high-sugar diet for six weeks, mice were intraperitoneally injected with streptozotocin (80 mg/kg body weight [BW]) 2–3 times. Type 2 diabetes mice were randomly divided into type 2 diabetes control (T2DM) and myricetin intervention groups. Water and food intake, fasting blood glucose (FBG), and BW were monitored weekly. After six weeks of myricetin administration, superoxide dismutase (SOD) levels and blood lipid content were measured. Furthermore, 16S rRNA sequencing was used to detect the gut microbiota composition. FBG and blood lipid levels of T2DM mice were significantly reduced upon myricetin treatment, while SOD levels were increased. Myricetin improved polydipsia, polyphagia, polyuria, and weight loss in T2DM mice. In addition, the signature type 2 diabetes microflora was established by analyzing the microflora structure of healthy mice, type 2 diabetes mice, and mice treated with myricetin. Results showed that type 2 diabetes disrupted the mice intestinal flora, and myricetin intervention normalized the intestinal flora. In conclusion, our results indicate that myricetin alleviates type 2 diabetes in mice and regulates the intestinal microflora.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2019
·Vol. 24
·期 20
·3747
·
IF 3.06
Weiyu Yang,Ling Guo,Fenfen Li,Xin Liu,Shaoping Nie,Mingyong Xie,Danfei Huang
Myricetin (Myr) is a phytochemical with many functional properties. However, its hydrophobicity, low bioavailability, and stability limit its application. In this study, octadecanoate oat β-glucan (OGE) was synthesized and gained recognition as a self-assembled micelle forming a polymer with a critical micelle concentration (CMC) of 59.4 μg/mL. The Myr-loaded OGE micelle was then prepared and characterized by dynamic light scattering (DLS), transmission electron microscope (TEM), X-ray diffractometer (XRD), and Fourier-transform infrared spectroscopy (FT-IR) spectra. The water solubility of Myr was greatly enhanced by forming the Myr/OGE inclusion complex. Consequently, compared to free Myr, the retention of Myr in Myr-loaded OGE micelle was effectively increased during the intestinal digestion phase, and its antioxidant activity was also improved. Overall, our findings demonstrated the potential applications of OGE polymer for the development of prospective micelle in health food, cosmetics, and pharmaceutical fields because they can aid in the delivery of hydrophobic functional compounds like Myr.Keywords:phytochemicals;myricetin;amphiphilicity;micelle;self-assembly
✓ 已验证
产品关联
DOI
PubMed
高影响因子
APPLIED SURFACE SCIENCE
·
2019
·
IF 5.155
Palanivel Sathishkumar,Zhaofa Li,Bingru Huang,Xin Guo,Qiuqiang Zhan,Chaoyang Wang,Feng Long Gu
In this study, flavonoid myricetin-mediated gold nanoparticles (Myr-AuNPs) were synthesized and their molecular interactions were evaluated through a combined experimental and theoretical study. The physicochemical properties of the synthesized Myr-AuNPs were characterized using TEM , FT-IR, and XRD analysis. The average particle size of the Myr-AuNPs was found to be 6 nm with spherical in shape. FT-IR results indicated that the hydroxyl groups of myricetin interacts with Au 3+ ions during the nanoparticles formation. Consequently, density functional theory (DFT) was used to evaluate the possible molecular interactions of myricetin hydroxyl groups with Au 3+ ions. Interestingly, the DFT results confirmed that the 5′-hydroxyl group of ring B in myricetin was more suitable and highly stable to interact with Au 3+ ions during the nanoparticles formation in aqueous medium. Further, this study emphasized that the synthesized Myr-AuNPs exhibits excellent pH, temperature, and storage stability. In addition to this, biocompatibility study recommended that Myr-AuNPs is safe for therapeutic applications. This is the first detailed report on the molecular interaction between the hydroxyl groups of myricetin and Au 3+ ions during the nanoparticle formation.
✓ 已验证
产品关联
DOI
高影响因子
PHARMACOLOGICAL RESEARCH
·
2017
·
IF 4.48
Yuchao Sun,Mengqiao Lian,Yuan Lin,Bin Xu,Yanli Li,Jin Wen,Dapeng Chen,Ming Xu,Marwan Almoiliqy,Li Wang
Intestinal ischemia reperfusion (I/R) may cause inflammation-, oxidative stress-, and apoptosis-related tissue injuries and facilitate bacterial infection, leading to multiple organ failure. Myricetin , a flavonoid , is found to have diverse biological effects including anti-inflammatory, anti-oxidative, and anti-bacterial effects. Based on our pre-experiment, we proposed that myricetin pretreatment (25, 50 mg/kg) could ameliorate intestinal I/R injury and myricetin-induced modulation on MKK7/JNK signal pathway might play a key role in the amelioration. The present study was designed to verify the proposal by using both rat intestinal I/R model in vivo and hypoxia/reoxygenation (H/R)-injured intestinal epithelial cell line (IEC-6 cells) model in vitro. The results confirmed our proposal. Myricetin selectively ameliorated I/R- and H/R-induced injuries in vivo and in vitro respectively without significantly affecting the corresponding normal controls. Myricetin significantly alleviated I/R-induced rat intestinal injury by reducing the generation of pro-inflammatory cytokines including TNF-α, IL-1β, and IL-6 and by reducing MPO activity. Myricetin significantly reduced oxidative stress through decreasing MDA level and increasing the levels of SOD and GSH in the intestinal tissues compared with I/R control rats. Myricetin significantly decreased apoptosis by selectively down-regulating the expression of p-MKK7 and p-JNK without affecting MKK7 and JNK, inhibiting Bax, caspase-3 protein expression, and up-regulating Bcl-2 protein expression in I/R-injured jejunum of rats. In vitro study indicated that MKK7 siRNA transfection significantly decreased both MKK7 and p-MKK7 and other apoptosis-related proteins, partially simulating myricetin-induced anti-apoptotic effects. MKK7 siRNA transfection + myricetin could not further decrease MKK7, p-MKK7, and other apoptosis-related proteins, suggesting that inhibition of MKK7/JNK pathway plays a key role in myricetin-induced protection against intestinal I/R. MKK7 overexpression by cDNA transfection abrogated myricetin-reduced apoptosis-related protein expression, confirming that the MKK7/JNK signal pathway is the key target for myricetin-induced amelioration. The present study indicated that pretreatment of myricetin induced selective protection against intestinal I/R injury without significantly affecting corresponding normal controls and p-MKK7 was the key target, suggesting that myricetin is worth further translational studies.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2016
·
IF 3.773
Yashu Yao,Mengxin Xia,Huizhen Wang,Guowen Li,Hongyi Shen,Guang Ji,Qianchao Meng,Yan Xie
A novel nanogel/gel based on chitosan (CS) for the oral delivery of myricetin (Myr) was developed and evaluated comprehensively. The particle size of the obtained Myr-loaded CS/β-glycerol phosphate (β-GP) nanogels was in the range of 100–300 nm. The rheological tests showed that the sol-gel transition happened when the nanogels were exposed to physiological temperatures, and 3D network structures of the gelatinized nanogels (gels) were confirmed by Scanning Electron Microscopy. Myr was released from CS/β-GP nanogel/gel in acidic buffers via a Fickian mechanism, and this release was simultaneously accompanied by swelling and erosion. Moreover, the nanogel/gel exhibited no cytotoxicity by MTT assay, and the oral bioavailability of Myr in rats was improved with an accelerated absorption rate after Myr was loaded into CS/β-GP nanogel/gel. In summary, all of the above showed that CS/β-GP nanogel/gel was an excellent system for orally delivering Myr.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2016
·
IF 4.052
Cen Zhang,Guowen Zhang,Yijing Liao,Deming Gong
Myricetin, a plant-derived flavonol, was found to inhibit the formation of uric acid in a mixed-type manner with IC 50 value of (8.66 ± 0.03) × 10 −6 mol L −1 and more potently inhibit the generation of superoxide anion (O 2 − ) catalysed by xanthine oxidase (XOD) with IC 50 value of (4.55 ± 0.02) × 10 −6 mol L −1 . Inhibiting O 2 − generation by myricetin may be attributed to the reduced form of XOD with a substantially higher reduction potential for FADH /FADH 2 couple. Moreover, molecular docking verified that myricetin bound to the site around isoalloxazine ring in the flavin adenine dinucleotide (FAD) domain to block the diffusion of O 2 − out of the FAD site, resulting in the transfer of another electron from FADH 2 to O 2 − to form hydrogen peroxide. This study has provided new insight into the role of myricetin in inhibiting XOD catalysis, which may be beneficial to improve myricetin’s potential application in functional foods.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）