Hyperoside Inhibits High-Glucose-Induced Vascular Inflammation In Vitro and In Vivo

Ku, Sae‐Kwang; Kwak, Soyoung; Kwon, O-Jun; Bae, Jong‐Sup

doi:10.1007/s10753-014-9863-8

Cited by 69 publications

(39 citation statements)

References 47 publications

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“…[37] and Hypericum perforatum ,[38] that exerts a wide variety of biological activities, including antioxidant[39], antihyperglycemic[40], anticancer[41], anti-inflammatory[42, 43], and cardiovascular protective effects[44, 45]. However, the underlying molecular mechanisms remain largely elusive.…”

Section: Discussionmentioning

confidence: 99%

Induction of Nur77 by hyperoside inhibits vascular smooth muscle cell proliferation and neointimal formation

Huo

Chen

et al. 2014

Biochemical Pharmacology

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Nur77 is an orphan nuclear receptor that belongs to the nuclear receptor 4A (NR4A) subfamily, which has been implicated in a variety of biological events, such as cell apoptosis, proliferation, inflammation, and metabolism. Activation of Nur77 has recently been shown to be beneficial for the treatment of cardiovascular and metabolic diseases. The purpose of this study is to identify novel natural Nur77 activators and investigate their roles in preventing vascular diseases. By measuring Nur77 expression using quantitative RT-PCR, we screened active ingredients extracted from Chinese herb medicines with beneficial cardiovascular effects. Hyperoside (quercetin 3-D-galactoside) was identified as one of the potent activators for inducing Nur77 expression and activating its transcriptional activity in vascular smooth muscle cells (VSMCs). We demonstrated that hyperoside, in a time and dose dependent manner, markedly increased the expression of Nur77 in rat VSMCs, with an EC50 of ∼0.83μM. Mechanistically, we found that hyperoside significantly increased the phosphorylation of ERK1/2 MAP kinase and its downstream target cAMP response element-binding protein (CREB), both of which contributed to the hyperoside-induced Nur77 expression in rat VSMCs. Moreover, through activation of Nur77 receptor, hyperoside markedly inhibited both vascular smooth muscle cell proliferation in vitro and the carotid artery ligation–induced neointimal formation in vivo. These findings demonstrate that hyperoside is a potent natural activator of Nur77 receptor, which can be potentially used for prevention and treatment of occlusive vascular diseases.

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Section: Discussionmentioning

confidence: 99%

Induction of Nur77 by hyperoside inhibits vascular smooth muscle cell proliferation and neointimal formation

Huo

Chen

et al. 2014

Biochemical Pharmacology

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“…The extract of L. dentata possess cytotoxic and pro-apoptotic properties assessed against human breast adenocarcinoma (MCF-7) cell lines using the MTT assay (Ali et al 2014). Ku et al (2014) evaluated antioxidant, antihyperglycemic, anti-cancer, anti-inflammatory, and anti-coagulant activities of hyperoside, an active compound from the genera of Crataegus and Hypericum. Venskutonis et al (2010) reported that the extract of G. macrorrhizum possesses strong antioxidant properties.…”

Section: Antiproliferative Propertiesmentioning

confidence: 99%

Antibacterial, antioxidant and anti-proliferative properties and zinc content of five south Portugal herbs

Nunes

Paśko

Tyszka-Czochara

et al. 2016

Pharmaceutical Biology

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Context: Crataegus monogyna L. (Rosaceae) (CM), Equisetum telmateia L. (Equisataceae) (ET), Geranium purpureum Vil. (Geraniaceae) (GP), Mentha suaveolens Ehrh. (Lamiaceae) (MS), and Lavandula stoechas L. spp. luisieri (Lamiaceae) (LS) are all medicinal. Objective: To evaluate the antioxidant, antiproliferative and antimicrobial activities of plant extracts and quantify individual phenolics and zinc. Material and methods: Aerial part extracts were prepared with water (W), ethanol (E) and an 80% mixture (80EW). Antioxidant activity was measured with TAA, FRAP and RP methods. Phenolics were quantified with a HPLC. Zinc was quantified using voltammetry. Antibacterial activity (after 48 h) was tested using Enterococcus faecalis, Bacillus cereus, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Listeria monocytogenes. Antiproliferative activity (after 24 h) was tested using HEP G2 cells and fibroblasts. Results: Solvents influenced results; the best were E and 80EW. GP had the highest antioxidant activity (TAA and FRAP of 536.90 mg AAE/g dw and 783.48 mg TE/g dw, respectively). CM had the highest zinc concentration (37.21 mg/kg) and phenolic variety, with neochlorogenic acid as the most abundant (92.91 mg/100 g dw). LS was rich in rosmarinic acid (301.71 mg/100 g dw). GP and LS inhibited the most microorganisms: B. cereus, E. coli and S. aureus. GP also inhibited E. faecalis. CM had the lowest MIC: 5830 lg/mL. The antibacterial activity is explained by the phenolics present. LS and CM showed the most significant anti-proliferative activity, which is explained by their zinc content. Conclusion: The most promising plants for further studies are CM, LS and GP.ARTICLE HISTORY

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“…Hyperoside is a flavonol glycoside mainly found in plants of the genera Hypericum and Crataegus [29] . Pharmacological investigations have demonstrated that hyperoside has anti-oxidant [30] , anti-cancer [31] and anti-inflammatory activities [32][33][34] . This compound exerts anti-inflammatory effects by suppressing the production of proinflammatory cytokines through inhibiting the activation of the NF-κB signaling pathway in human endothelial cells [33] .…”

Section: Introductionmentioning

confidence: 99%

Hyperoside exerts anti-inflammatory and anti-arthritic effects in LPS-stimulated human fibroblast-like synoviocytes in vitro and in mice with collagen-induced arthritis

Jin¹,

Yan

Wang

et al. 2016

Acta Pharmacol Sin

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Aim: Hyperoside is a flavonol glycoside mainly found in plants of the genera Hypericum and Crataegus, which has shown anti-oxidant, anti-cancer and anti-inflammatory activities. In this study, we investigated the effects of hyperoside on human rheumatoid fibroblastlike synoviocytes (FLSs) in vitro and on mouse collagen-induced arthritis (CIA) in vivo. Methods: FLSs were isolated from primary synovial tissues obtained from rheumatoid arthritis (RA) patients and exposed to LPS (1 µg/mL). Cell viability and proliferation were measured with MTT and BrdU assay. Cell migration was assessed using wound-healing assay and Transwell assay. DNA binding of NF-κB was measured using a TransAM-NFkappaB kit. The localization of p65 subunit was detected with immunocytochemistry. CIA was induced in mice by primary immunization with Bovine Type II collagen (CII) emulsified in CFA, followed by a booster injection 3 weeks later. The arthritic mice were treated with hyperoside (25, 50 mg·kg -1 ·d -1, ip) for 3 weeks, and the joint tissues were harvested for histological analysis. Results: Hyperoside (10, 50, 100 µmol/L) dose-dependently inhibited LPS-induced proliferation and migration of human RA FLSs in vitro. Furthermore, hyperoside decreased LPS-stimulated production of TNF-α, IL-6, IL-1 and MMP-9 in the cells. Moreover, hyperoside inhibited LPS-induced phosphorylation of p65 and IκBα, and suppressed LPS-induced nuclear translocation of p65 and DNA biding of NF-κB in the cells. Three-week administration of hyperoside significantly decreased the clinical scores, and alleviated synovial hyperplasia, inflammatory cell infiltration and cartilage damage in mice with CIA. Conclusion: Hyperoside inhibits LPS-induced proliferation, migration and inflammatory responses in human RA FLSs in vitro by suppressing activation of the NF-κB signaling pathway, which contributes to the therapeutic effects observed in mice with CIA.

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Hyperoside Inhibits High-Glucose-Induced Vascular Inflammation In Vitro and In Vivo

Cited by 69 publications

References 47 publications

Induction of Nur77 by hyperoside inhibits vascular smooth muscle cell proliferation and neointimal formation

Induction of Nur77 by hyperoside inhibits vascular smooth muscle cell proliferation and neointimal formation

Antibacterial, antioxidant and anti-proliferative properties and zinc content of five south Portugal herbs

Hyperoside exerts anti-inflammatory and anti-arthritic effects in LPS-stimulated human fibroblast-like synoviocytes in vitro and in mice with collagen-induced arthritis

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