Effects of myricetin on glucose tolerance after a single-dose injection. Wistar rats were administered liraglutide or myricetin after a period of food withdrawal. Glucose (2 g/kg body weight) was administered 30 min before each time point (0–48 h). A) The effect of a single dose of the myricetin (250 mg/kg body weight by oral) and liraglutide (100 mg/kg body weight) on glucose regulation in Wistar rats. B) The dosage-efficacy of myricetin 12 h after administration. The administration of myricetin maintained the blood glucose concentration at normal levels for 8 h after a single-dose treatment, suggesting it might possess a half-life similar to that of liraglutide (11.3 h).  

Effects of myricetin on glucose tolerance after a single-dose injection. Wistar rats were administered liraglutide or myricetin after a period of food withdrawal. Glucose (2 g/kg body weight) was administered 30 min before each time point (0–48 h). A) The effect of a single dose of the myricetin (250 mg/kg body weight by oral) and liraglutide (100 mg/kg body weight) on glucose regulation in Wistar rats. B) The dosage-efficacy of myricetin 12 h after administration. The administration of myricetin maintained the blood glucose concentration at normal levels for 8 h after a single-dose treatment, suggesting it might possess a half-life similar to that of liraglutide (11.3 h).  

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... This finding also suggests, in this case, that a fine treatment of the outer shell sample is desirable to optimize an exhaustive recovery of these compounds, which can exert a massive protective action that goes well beyond the much-claimed antioxidant activity. Long-term oral administration of myricetin demonstrated glycoregulatory activity [69], and isorhamnetin was found to reduce diabetes-related disorders by decreasing glucose levels, improving oxidative status, relieving inflammation, and modulating lipid metabolism and adipocyte differentiation [70]. Furthermore, quercetin has been investigated for treating metabolic diseases, including diabetes, hyperlipidemia, and nonalcoholic fatty liver disease [71]. ...
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Nowadays, chestnut by-products are gaining a lot of interest as a low-cost raw material, exploitable for developing added-value products. This is in line with suitable chestnut by-products’ management, aimed at reducing the environmental impact, thus improving the chestnut industry’s competitiveness and economic sustainability. In this context, with the aim of valorizing local cultivars of European chestnuts (Castanea sativa Mill.), our attention focused on the Verdole cultivar, which has been characterized by using the UPOV guidelines for its distinctness, homogeneity, and stability. After harvesting, Verdole chestnuts were properly dissected to collect the outer and inner shells, and episperm. Each chestnut part, previously crushed, shredded, and passed through diverse sieves, underwent ultrasound-assisted extraction. The extracts obtained were evaluated for their total phenolic, flavonoid, and tannin content. The antiradical capacity by DPPH and ABTS assays, and the Fe(III) reducing power, were also evaluated. Although all the samples showed dose-dependent antioxidant efficacy, plant matrix size strongly impacted on extraction efficiency. LC-HRMS-based metabolic profiling highlighted the occurrence of different polyphenol subclasses, whose quantitative ratio varied among the chestnut parts investigated. The outer shell was more chemically rich than inner shell and episperm, according to its pronounced antioxidant activity. The polyphenol diversity of Verdole by-products is a resource not intended for disposal, appliable in the nutraceutical sector, thus realizing a new scenario in processing chestnut waste.
... Myricetin (3,3',4',5,5',7-hexahydroxyflavone, Fig. 1), is a widespread naturally occurring flavonoid, which can be found in lots of berries, fruits, vegetables and herbal medicines [1]. Myricetin has multiple biological activities, such as antioxidant, anti-diabetic, anti-inflammatory, anticarcinogenic and anti-proliferative effects [2][3][4][5][6][7][8][9][10][11][12][13][14][15]. In previous study, myricetin were also reported which could treat and prevent colitis and the risk of colitis-associated colorectal cancer (CAC) [16]. ...
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Myricetin is a common plant-derived flavonoid and exhibits a wide range of activities. However, myricetin also exhibits substantial limitations, such as its poor water-solubility and low stability in body when it was administrated orally. To solve these problems, a series of myricetin derivatives with different disaccharide groups were designed, synthesized and evaluated their hypoglycemic activities. All synthesized compounds displayed significant α-glucosidase inhibitory activity in comparison with acarbose in vitro, which indicated that myricetin derivatives with different disaccharide groups had good hypoglycemic activity and could be further developed as hypoglycemic drugs.
... Myricetin (3,3',4',5,5',7-hexahydroxy avone, Fig. 1), is a widespread naturally occurring avonoid, which can be found in lots of berries, fruits, vegetables and herbal medicines [1]. Myricetin has multiple biological activities, such as antioxidant, anti-diabetic, anti-in ammatory, anti-carcinogenic and antiproliferative effects [2][3][4][5][6][7][8][9][10][11][12][13][14][15]. In previous study, myricetin were also reported which could treat and prevent colitis and the risk of colitis-associated colorectal cancer (CAC) [16]. ...
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Myricetin is a common plant-derived flavonoid and exhibits a wide range of activities. However, myricetin also exhibits substantial limitations, such as its poor water-solubility and low stability in body when it was administrated by oral. To solve these problems, a series of myricetin derivatives with different disaccharide groups were designed, synthesized and evaluated their hypoglycemic activities. All synthesized compounds displayed significant α-glucosidase inhibitory activity in comparison with acarbose in vitro , which indicated that myricetin derivatives with different disaccharide groups had good hypoglycemic activity and could be further developed as hypoglycemic drugs.
... (Pan X. et al., 2017). Consistent with the previous studies, we identified five myricetin and their derivatives in JHK [myricetin, myricetin-3-O-(6 -malony) glucoside, myricetin-3-O-arabinoside, myricetin-3-O-galactoside, myricetin-3-Oglucoside], which were active constituents to inhibit platelet aggregation (Survay et al., 2011) having anti-inflammatory, anticancer activities (Feng et al., 2015), and as natural B GPCR agonist or α-glucosidase inhibitor for type 2 diabetes treatment (Kang et al., 2015;Li et al., 2017). We found that myricetin-3-O-arabinoside was unique in the flowers of the JHK. ...
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Hibiseu manihot L. (Jinhuakui, JHK), also known as a garden landscape plant, is widely cultivated as a landscape plant having pharmacological effects due to its high flavonoids content. Although flavonoids were the main active pharmaceutical ingredients in JHK, little information was obtained about the content, composition, and accumulation pattern of flavonoids in different tissues. Most studies only identified a few kinds of flavonoids in JHK limited by separation and identification problems. Therefore, combined metabolome and transcriptome analysis was performed to explore the accumulation patterns and biosynthesis mechanisms of flavonoids in JHK. In this study, we identified 160 flavonoids in 15 samples of JHK (flower, leaf, root, stem, and seeds) by using LC-MS/MS. Consistent with the total flavonoid content determination, these flavonoids were significantly accumulated in flowers, followed by leaves, stems, roots, and seeds. Among them, certain flavonoids, with high content, were also identified for the first time in JHK, such as tricetin, catechin, hesperidin, ncyanidin-3-O-sambubioside, astragalin, procyanidin B2/B3/C1, apigenin-5-O-glucoside, etc. Different tissues underwent significantly reprogramming of their transcriptomes and metabolites changes in JHK, particularly in the flavonoid, flavone, and flavonol biosynthesis pathways. We conducted a correlation analysis between RNA-seq and LC-MS/MS to identify the key genes and related flavonoids compounds, rebuild the gene-metabolites regulatory subnetworks, and then identified 15 key genes highly related to flavonoids accumulation in JHK. These key genes might play a fine regulatory role in flavonoids biosynthesis by affecting the gene expression level in different organs of JHK. Our results could be helpful for the improvement of the market/industrial utilization value of different parts of JHK, to pave the way for the regulatory mechanism research of flavonoids biosynthesis, and provide insight for studying the production quality improvement of JHK.
... The essential mechanism of myricetin for improving insulin sensitivity might be the amelioration of impaired signaling intermediates downstream of insulin receptors through enhancing the secretion of β-endorphin (BER), which in turn leads to the activation of peripheral µ-opioid receptors [6]. Additionally, myricetin has been identified as an agonist of glucagon-like peptide 1 (GLP-1) receptor using receptor knock-out mice [7]. However, myricetin also increased GLP-1 due to inhibition of degrading enzyme dipeptidyl peptidase-4 (DPP-4) at a higher dose in rats [3]. ...
... Myricetin has many beneficial effects, which include potential antimicrobial, antioxidant, immunomodulatory and cardioprotective activity, and so on [19]. Myricetin could activate GLP-1 receptor expressions in the GLP-1 receptor-knockout model [7]. Our results indicated that myricetin dose-dependently increased the GLP-1 receptor expression in PC-12 cells. ...
... Recently, myricetin has been demonstrated to inhibit DPP-4 and enhance the GLP-1 levels in type-2 diabetic rats [3]. The increase of the GLP-1 receptors induced by myricetin was markedly higher in diabetic rats administered with 20 mg/kg orally compared with that in the group, who treated with myricetin at the dose of 1 mg/kg) [7]. Moreover, myricetin at a high dose (20 mg/kg) improved the antioxidant enzyme activities and lowered the lipid peroxidation, although it was described as irrespective of its ability to restore the GLP-1 levels [3]. ...
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Myricetin is a common plant-derived flavonoid, considered an agonist of glucagon-like peptide 1 (GLP-1) receptor. It improves glycemic control and helps reduce body weight in diabetic subjects. The potential mechanisms of action of myricetin in this context might be enhancing the secretion of β-endorphin (BER) to activate peripheral μ-opioid receptors. Moreover, adropin is a nutritionally regulated peptide hormone, which regulates energy metabolism, and plays a role in ameliorating diabetes. Because their mechanisms of insulin sensitivity are closely related, we hypothesized that myricetin may interact with adropin and plasma BER. The present study investigated the glucose-lowering effect of acute and chronic treatments of myricetin in type-1 diabetic rats. Plasma BER and adropin levels were determined by enzyme-linked immunosorbent assay (ELISA). The secretion of BER was measured in rats who received adrenalectomy. The changes in adropin gene (Enho) or mRNA level of GLP-1 receptor were measured using qPCR analysis. The results showed that myricetin dose-dependently increased plasma BER and adropin levels like the reduction of hyperglycemia after bolus injection as acute treatment. In addition, these effects of myricetin were inhibited by the antagonist of GLP-1 receptor. Moreover, in HepG2 cell line, myricetin induced GLP-1 receptor activation, which modulated the expression of adropin. In diabetic rats, the plasma adropin increased by myricetin is mainly through endogenous β-endorphin after activation of GLP-1 receptor via bolus injection as acute treatment. Additionally, chronic treatment with myricetin increased adropin secretion in diabetic rats. In conclusion, our results provide a new finding that activation of opioid μ-receptor in the liver may enhance circulating adropin in animals.
... Dietary flavonoids could promote the delays of gastric emptying and increased satiety, which prevented the excessive consumption of glucose/fructose intake. Metabolites of flavonoids such as the gut-produced SCFA regulated the secretion of GLP-1, suggesting that flavonoids may be a promising option for the prevention and treatment of T2DM (Li et al., 2017). Many studies indicated that flavonoids inhibited glucose uptake in gut cells (CaCO-2 cells) through inhibiting glucose transporters such as SGLT1 and GLUT2 (Castro-Acosta et al., 2017; Kerimi et al., 2019;Rymenan et al., 2018). ...
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Type 2 diabetes mellitus (T2DM) is a common endocrine and progressive metabolic disorder disease, which seriously threatens peoples' lives and health. Due to the high cost of clinical treatments and obvious side effects, looking for effective bioactive ingredients in the diet is an important strategy to prevent or even reduce the risk of diabetes. Epidemiological studies have suggested that dietary flavonoids have a potential antidiabetic effect, but the underlying mechanism remains unclear. Accumulating evidences indicates that gut microbiota has become an important target of dietary interventions. It plays essential roles in the digestion and absorption of flavonoids and affects the occurrence and progression of T2DM. This review systematically summarized the progress of dietary flavonoids targeting gut microbiota to ameliorate T2DM and analyzed possible molecular mechanisms. It suggests that flavonoids may prevent T2DM for healthy people and ameliorate health situations for T2DM patients. In addition, microbiota-based nutrition aims to provide personalized nutritional guidance to alter an individual's microbiota and further improve response to dietary flavonoids, which will benefit to achieve a more effective diet for the prevention and management of T2DM.
... Wistar rats revealed its' glucoregulatory activity. 44 Li et al 45 have proved Myricetin as an active anticancer compound with pharmacological effects on tamoxifen and its metabolites. Rosmarinic acid pharmacokinetic properties are a good recommendation for oral prescription as it has a low acute toxicity value. ...
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Introduction: Epidermal growth factor receptor (EGFR) is a transmembrane protein that belongs to the ErbB/HER-family of tyrosine kinase receptors. Somatic mutations and overexpression of EGFR have been reported to play a vital role in cancer cell development and progression, including cell proliferation, differentiation, angiogenesis, apoptosis, and metastatic spread. Hence, EGFR is an important therapeutic target for the treatment of various types of epithelial cancers. Somatic mutations have led to resistance to clinically approved synthetic EGFR inhibitors. Furthermore, synthetic EGFR inhibitors have been associated with several side effects. Thus, there is a need to develop novel EGFR inhibitors with an acceptable biosafety profile and high efficacy. Methods: Herein, we employed structural bioinformatics and theoretical chemistry techniques via molecular docking, molecular mechanics generalized Born surface area (MM-GBSA) calculation, density functional theory analysis (DFT), and pharmacokinetic study to identify novel EGFR inhibitors. Results: The stringent molecular docking and MM-GBSA calculations identified MET 793, LYS 745, PHE 723, ASP 855, ARG 411, and THR 854 as principal amino acid residues for EGFR-ligands interactions. Furthermore, Colocasia affinis Schott compounds exhibited higher binding energy and more stable interactions than the reference compound (gefitinib). DFT analysis also ascertains better bioactivity and chemical reactivity of C. affinis Schott with favorable intramolecular charge transfer between electron-donor and electron acceptor groups. The pharmacokinetic profile of C. affinis Schott bioactive compounds satisfies Lipinski's rule of five assessment. Conclusion: Collectively, C. affinis Schott compounds demonstrated higher inhibitory potentials against EGFR and better pharmacological properties when compared with gefitinib. C. affinis Schott compounds are therefore suggested as promising therapeutic EGFR inhibitors for cancer treatment.
... Myricetin is a natural product that is extracted from the leaves of Myrica rubra [82] and has the potential to be a small-molecule GLP-1R agonist that can be administered orally. Li et al. [83] showed that myricetin had insulinotropic effects in Wistar rats and also stimulated cAMP accumulation and insulin secretion in INS-1 cells. However, myricetin failed to lower blood glucose in GLP-1RKO mice, which strongly confirmed that myricetin was a GLP-1R agonist [83]. ...
... Li et al. [83] showed that myricetin had insulinotropic effects in Wistar rats and also stimulated cAMP accumulation and insulin secretion in INS-1 cells. However, myricetin failed to lower blood glucose in GLP-1RKO mice, which strongly confirmed that myricetin was a GLP-1R agonist [83]. Despite these initial studies, the molecular mechanisms by which myricetin interacts with the GLP-1R as well as its effects on downstream signaling pathways need to be further elucidated in order to better optimize myricetin for clinical use as a new therapy for T2DM. ...
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Glucagon-like peptide-1 (GLP-1) receptor-based therapies have been developed and extensively applied in clinical practice. GLP-1 plays an important role in improving glycemic homeostasis by stimulating insulin biosynthesis and secretion, suppressing glucagon activity, delaying gastric emptying, and reducing appetite and food ingestion. Furthermore, GLP-1 has positive effects on β-cell function by promoting β-cell proliferation and neogenesis while simultaneously reducing apoptosis. Here, we summarize possible mechanisms of action of GLP-1 upon pancreatic islets as well as describe phytochemicals that modulate pancreatic islet β cell function through glucagon-like peptide-1-related mechanisms. Together, this information provides potential lead compound candidates against diabetes that function as GLP-1 receptor-based pharmacotherapy.
... Liao et al. (2017) Enhanced the insulin sensitivity via lowering glucose level Li et al. (2017) Suppressed the α-amylase and α-glucosidase activities Meng et al. (2016) Prevented from momentous increment in urea, plasma glucose, uric acid, urinary albumin, blood urea nitrogen, glucose−6-phosphatase, glycosylated hemoglobin, glycogen phosphorylase, hexokinase, glycogen synthase, and glycogen with insulin signaling molecule expression and fructose−1,6-bisphosphatase Normalized the insulin signaling molecule expression like PKB (protein kinase B), IRS−1 (insulin receptor−1), IRS−2 (insulin receptor−2), GLUT−2 (glucose transporter−2) and GLUT−4 (glucose transporter−4) Kandasamy and Ashokkumar (2014b) (Continues) ...
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This is an open access article under the terms of the Creat ive Commo ns Attri bution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. Abstract Myricetin is a critical nutritive component of diet providing immunological protection and beneficial for maintaining good health. It is found in fruits, vegetables, tea, and wine. The families Myricaceae, Polygonaceae, Primulaceae, Pinaceae, and Anacardiaceae are the richest sources of myricetin. Different researchers explored the therapeutic potential of this valuable constituent such as anticancer, antidiabetic, antiobesity, cardiovascular protection, osteoporosis protection, anti-inflammatory, and hepatoprotective. In addition to these, the compound has been tested for cancer and diabetic mellitus during clinical trials. Health benefits of myricetin are related to its impact on different cell processes, such as apoptosis, glycolysis, cell cycle, energy balance, lipid level, serum protein concentrations, and osteoclastogenesis. This review explored the potential health benefits of myricetin with a specific emphasis on its mechanism of action, considering the most updated and novel findings in the field.
... Liao et al. (2017) Enhanced the insulin sensitivity via lowering glucose level Li et al. (2017) Suppressed the α-amylase and α-glucosidase activities Meng et al. (2016) Prevented from momentous increment in urea, plasma glucose, uric acid, urinary albumin, blood urea nitrogen, glucose−6-phosphatase, glycosylated hemoglobin, glycogen phosphorylase, hexokinase, glycogen synthase, and glycogen with insulin signaling molecule expression and fructose−1,6-bisphosphatase Normalized the insulin signaling molecule expression like PKB (protein kinase B), IRS−1 (insulin receptor−1), IRS−2 (insulin receptor−2), GLUT−2 (glucose transporter−2) and GLUT−4 (glucose transporter−4) Kandasamy and Ashokkumar (2014b) (Continues) ...