TROPICAL JOURNAL OF PHARMACEUTICAL RESEARCH
·
2014
·Vol. 13
·期 11
·1791-1796
·
IF 0.495
H Nan,H Ma,R Zhang,R Zhan
Purpose: To improve the hydrophilic property of myricetin by complexing it with hydroxypropyl-β- cyclodextrin (HP-β-CD)Methods: The complexes of myricetin and HP-β-CD were prepared in both water and ethanol. The physicochemical properties of the complex were investigated by ultraviolet-visible spectrometry (UV), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and x-ray diffractometry (XRD).Results: The content of myricetin in the complex prepared in ethanol (3.71 %) was higher than that prepared in water (1.43 %). Characterization studies indicate that myricetin in the complex was molecularly dispersed in HP-β-CD matrix.Conclusion: Ethanol is the better solvent to prepare the complex of myricetin and hydroxypropyl-β- cyclodextrin. Myricetin and HP-β-CD in the complex are combined by non-covalent bond, and thus did not form a new compound.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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
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CARBOHYDRATE POLYMERS
·
2014
·
IF 3.916
Yashu Yao,Yan Xie,Chao Hong,Guowen Li,Hongyi Shen,Guang Ji
Myricetin shows low oral bioavailability (<10%) in rats due to poor aqueous solubility, though it has various pharmacological activities. Complexation with cyclodextrins (CDs) is a potent pharmaceutical method to enhance the bioavailability of poorly soluble compounds. The myricetin/HP-β-CD inclusion complex was prepared and confirmed by DSC, PXRD, and SEM. Here, the inclusion mode is described in detail with regard to structural and energetic aspects using a phase solubility diagram and 1 H NMR, NOESY, and FT-IR spectra. The water solubility and dissolution rate of myricetin were greatly enhanced by forming the myricetin/HP-β-CD inclusion complex. Consequently, the oral bioavailability of the myricetin/HP-β-CD inclusion complex in rats was effectively increased 9.4-fold over free myricetin, and its antioxidant activity was also improved. The present study provides useful information for the potential application of complexation with myricetin, a naturally occurring hydrophobic phenolic compound in herbal medicine.
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NUTRITION RESEARCH
·
2015
·
IF 2.472
Qian Wang,Shuang-ting Wang,Xin Yang,Pan-pan You,Wen Zhang
Myricetin (MyR), a naturally occurring flavonol widely distributed in fruits, vegetables, and medicinal plants , has anticancer, anti-inflammatory, antihyperlipidaemic , and antiobesity activities. In the present study, we hypothesized that the antiobesity property of MyR is mediated via suppression of differentiation of preadipocytes into adipocytes and promotion of lipolysis of mature adipocytes, which effectively decrease the intracellular triglyceride concentration of adipocytes. Accordingly, the aim of this work was to investigate the effects of MyR on adipocyte differentiation and lipolysis in differentiated 3 T3-L1 adipocytes. Our results showed that MyR inhibited differentiation of 3 T3-L1 preadipocytes in a concentration-dependent manner. Myricetin downregulated the mRNA and protein levels of CCAAT/enhancer-binding protein α and peroxisome proliferator-activated receptor γ , both of which are major adipogenic transcription factors. Furthermore, the mRNA levels of other adipogenesis-related transcription factors, namely, CCAAT/enhancer-binding protein β , sterin regulatory element binding protein 1-c, peroxisome proliferator-activated receptor γ coactivator–1, adipocyte protein 2 , lipoprotein lipase and glucose transporter 4 , were also reduced by MyR treatment. Moreover, MyR significantly inhibited the phosphorylation of extracellular signal–regulated kinase, Jun N-terminal kinase, and p38 during the differentiation process. On the other hand, MyR induced a dose-dependent increase in glycerol release in fully differentiated adipocytes, indicating its stimulatory effect on adipocyte lipolysis. Furthermore, MyR downregulated mRNA level of perilipin A and enhanced the phosphorylation level of extracellular signal–regulated kinase, Jun N-terminal kinase, and p38 during lipolysis. Taken together, these findings indicate that MyR exerts antiobesity activity in adipocytes.
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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.
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