• Title/Summary/Keyword: Quercetin

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In vitro Modulation of Proliferation and Melanization of B16/F10 Melanoma Cells by Quercetin (Quercetin이 B16/F10 멜라닌세포의 중식 및 멜라닌화에 미치는 영향)

  • 천현자;백승화;우원홍;황상구;김춘관;김춘관
    • YAKHAK HOEJI
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    • v.46 no.1
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    • pp.75-80
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    • 2002
  • Quercetin is one of the bioflavonoid compounds and has multiple biological effects such as antioxidant and effective anti-inflammatory agent. Melanin has an important role in protecting human skin from the damaging effects of ultra-violet W) radiation. We studied the effect of quercetin on proliferation of B16/F10 melanoma cells. After 48h treatment of cells with quercetin, the cells exhibited a dose-dependent inhibition in their proliferation without apoptosis. Therefore, the decrease in cell numbers may be due to cell growth arrest, not due to cell death by cytotoxicity. We also investigated the effect of quercetin on melanogenesis of this cells. B16/F10 melanoma cells were grown for 48h in the presence of 0.01~50$\mu\textrm{g}$/ml quercetin and the total melanin contents were measured. Quercetin stimulated melanization of the cells in low concentrations (0.01~20$\mu\textrm{g}$/ml), whereas it inhibited melanization in high concentrations (30~50$\mu\textrm{g}$/ml). It was observed that quercetin differently regulates melanogenesis of B16/F10 melanoma cells dependent on its concentrations.

Antigenotoxicity and Action Mechanism of Quercetin and its Glycosides against Oxidative DNA Damage (Oxidative DNA 손상에 대한 Quercetin 및 그 배당체들의 유전독성억제효과와 작용기전)

  • 김수희;허문영
    • Environmental Mutagens and Carcinogens
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    • v.19 no.2
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    • pp.116-121
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    • 1999
  • Quercetin and its glycosides showed a strong free radical scavenging effect to DPPH radical generation. However, there were not big differences between quercetin aglycone and glycosides under experimental condition of this study. On the other hand, quercetin had pro-oxidant effect in bleomycin-dependent DNA assay. Quercetin aglycone and its glycosides, quercitrin inhibited $H_2$$O_2$- induced DNA damage in CHL cells. They also have an anticlastogenicity toward DNA breakage agent by radical generation like bleomycin. These results indicate that quercetin aglycone and its glycosides are capable of protecting the free radical generation induced by reactive oxygen species like $H_2$$O_2$. The mechanism of inhibition in hydrogen peroxide-induced genotoxicity may be due to their free radical scavenging properties. Therefore, quercetin aglycone and its glycosides may be useful chemopreventive agents by protecting of free radical generation which are involved in carcinogenesis and aging. However, quercetin and its glycosides must also carefully examined for pro-oxidant properties before being proposed for use in vivo.

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Quercetin Directly Interacts with Vitamin D Receptor (VDR): Structural Implication of VDR Activation by Quercetin

  • Lee, Ki-Young;Choi, Hye-Seung;Choi, Ho-Sung;Chung, Ka Young;Lee, Bong-Jin;Maeng, Han-Joo;Seo, Min-Duk
    • Biomolecules & Therapeutics
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    • v.24 no.2
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    • pp.191-198
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    • 2016
  • The vitamin D receptor (VDR) is a member of the nuclear receptor (NR) superfamily. The VDR binds to active vitamin $D_3$ metabolites, which stimulates downstream transduction signaling involved in various physiological activities such as calcium homeostasis, bone mineralization, and cell differentiation. Quercetin is a widely distributed flavonoid in nature that is known to enhance transactivation of VDR target genes. However, the detailed molecular mechanism underlying VDR activation by quercetin is not well understood. We first demonstrated the interaction between quercetin and the VDR at the molecular level by using fluorescence quenching and saturation transfer difference (STD) NMR experiments. The dissociation constant ($K_d$) of quercetin and the VDR was $21.15{\pm}4.31{\mu}M$, and the mapping of quercetin subsites for VDR binding was performed using STD-NMR. The binding mode of quercetin was investigated by a docking study combined with molecular dynamics (MD) simulation. Quercetin might serve as a scaffold for the development of VDR modulators with selective biological activities.

Development of Separating Techniques on Quercetin-Related Substances in Onion(Allium cepa L.) 1. Contents and Stability of Quercetin-Related Substances in Onion (양파의 Quercetin 관련 물질의 분리 기술 개발 1. 양파의 Quercetin 관련 물질의 함량과 안정성)

  • 강성구;김용두;현규환;김영환;송보현;신수철;박양균
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.27 no.4
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    • pp.682-686
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    • 1998
  • To use onion(Allium cepa L.) residue as raw materials of food products, contents and stability of quercetin-related substance in onion were investigated. The amount of quercetin-related substance of onion was richer in the inedible portion(317.99mg%) than the edible protion(4.10mg%). Total quercetin-related substances of juice and residue from fresh onions were 2.26mg% and 1.57mg%, respectively, but they were changed to 1.50mg% and 2.96mg% by heating at 8$0^{\circ}C$ for 10min. Quercetin was found to be stable at 20$0^{\circ}C$ for 60 min, but it was unstable to light. When it was illuminated with 30W, the content was decreased and reached to 80~85% of the original content after 48 hours. Quercetin was not affected by pH, but quercitrin and rutin were unstable below pH 5.

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Autophagy Inhibition Promotes Quercetin Induced Apoptosis in MG-63 Human Osteosarcoma cells

  • Park, Sung-Jin;Yu, Su-Bin;Kim, Yong-Ho;Kim, In-Ryoung;Park, Hae-Ryoun;Park, Bong-Soo
    • International Journal of Oral Biology
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    • v.40 no.2
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    • pp.85-91
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    • 2015
  • Quercetin is a natural flavonoid phytochemical that is extracted from various plants. Having an advantages due to its varied biological properties, such as anti-inflammatory, anti-viral, anti-oxidant, and anti-cancer effects, quercetin is used to treat many diseases. Recently, it has been reported that autophagy inhibition may play a key role in anti-cancer therapy. Therefore, in this study, we investigated the molecular mechanisms and anti-cancer effects of quercetin in human osteosarcoma cells via autophagy inhibition. We ascertained that quercetin inhibited cell proliferation and induced cell death, these process is demonstrated that apoptosis via the mitochondrial pathway and the caspase cascade. Quercetin also induced autophagy which was inhibited by 3-MA, autophagy inhibitor and the blockade of autophagy promoted the quercetin-induced apoptosis, confirming that autophagy is a pro-survival process. Thus, these findings demonstrate that quercetin is an effective anti-cancer agent, and the combination of quercetin and an autophagy inhibitor should enhance the effect of anti-cancer therapy.

Optimum Concentration of the Cd(II)-Quercetin Complexation Reaction (Quercetin의 카드뮴 착물반응에 대한 최적농도)

  • Lee, Jeong-Ho;Shin, Sun-Woo;Baek, Seung-Hwa
    • YAKHAK HOEJI
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    • v.53 no.5
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    • pp.235-240
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    • 2009
  • The interaction of cadmium (II) ion with quercetin was investigated in aqueous solution at different pH. The quercetin/cadmium stochiometries for cadmium (II) binding have been determined by UV-vis spectrophotometric method. The complexation of Cd(II) ion with 54.72 ${\mu}M$ quercetin (A=1.00793) was formed in 0.2 M $NH_3-0.2$ M $NH_4Cl$ (pH 8.0) buffer solution. 1:1 Cd(II)-complex had a maximum absorbance and showed the bathochromic shift of the long-wavelength band of the UV-vis spectra in the alkaline pH when interacted with quercetin in buffer solution. These results suggest that Cd(II)-quercetin complex has the optimal condition of chelation in basic buffer solution.

Anxiolytic Effects of Quercetin: Involvement of GABAergic System (Quercetin의 항불안 효과: GABA 신경계를 중심으로)

  • Jung, Ji Wook;Lee, Seungheon
    • Journal of Life Science
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    • v.24 no.3
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    • pp.290-296
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    • 2014
  • The present experiment investigated putative anxiolytic-like effects of quercetin using an elevated plus-maze (EPM) and hole-board apparatus test in mice. Quercetin is a flavonoid widely distributed in nature. Quercetin (1.25, 2.5, 5, or 10 mg/kg) was orally administered to ICR mice 1 h before a behavioral evaluation in the EPM. Control mice were treated with an equal volume of vehicle, and positive control mice were treated with buspirone (2 mg/kg, i.p.). The mice administered quercetin (5 mg/kg) spent a significantly longer percentage of time in the open arms of the EPM and their percentage of entries into the open arms was significantly increased compared to the vehicle-treated controls (p<0.05). The anxiolytic-like activities of quercetin were antagonized by trans-4-aminocrotonic acid (a $GABA_{A-{\rho}}$ agonist, 20 mg/kg) but not by flumazenil (a $GABA_A$ antagonist, 10 mg/kg) or WAY-100635 (a $5-HT_{1A}$ antagonist, 0.3 mg/kg). Moreover, there were no changes in the locomotor activity or myorelaxant effects in any group compared with the vehicle-treated controls. In the hole-board apparatus test, the number of head-dips increased significantly in the single treatment with quercetin (5 mg/kg) group compared to the vehicle-treated controls (p<0.05). These findings suggest that quercetin can promote anxiolytic-like activity, mediated by the GABAergic nervous system, in mice.

Quercetin Inhibits Inflammation Responses via MAPKs and NF-κB Signaling Pathways in LPS-stimulated RAW264.7 Cells (마우스 대식세포 RAW264.7 세포에서 MAPK와 NF-κB 경로를 통한 quercetin의 염증 반응 저해 활성)

  • Woo Young, Won;Jeong Tae, Kim;Keun Ho, Kim;Ji Young, Hwang;Chung-Wook, Chung;Jong Sik, Kim
    • Journal of Life Science
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    • v.32 no.11
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    • pp.899-907
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    • 2022
  • Quercetin is one of bio-flavonoids which are abundant in fruits and vegetables and has been reported to have various pharmacological potentials such as anti-oxidation, anti-inflammation, anti-cancer, and anti-virus effects. In the present study, the anti-inflammatory effects and its working molecular mecha- nism of quercetin were investigated in mouse macrophage RAW264.7 cells. Quercetin significantly inhibited nitric oxide (NO) production in a dose-dependent manner without affecting cell viability and decreased inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression in LPS-stimulated RAW264.7 cells. In addition, quercetin decreased phosphorylation of p38, JNK, and ERK, and inhibited phosphorylation of NF-κB p65 protein and its inhibitor IκBα indicating that quercetin has the anti-inflammatory effects via regulation of MAPKs and NF-κB signaling pathway. We also detected expression changes of four kinds of pro-inflammatory cytokine genes (CSF2, IL-1β, IL-6, and TNF-α) with quantitative real-time PCR. The results showed that quercetin decreased the expression of four pro-inflammatory genes in LPS-stimulated RAW264.7 cells. Overall, our results showed that quercetin effectively suppressed inflammation responses induced by LPS in RAW264.7 cells via regulating MAPK and NF-κB pathway and down-regulating the expression of pro-inflammatory cytokine genes.

Effect of Dietary Supplementation of Quercetin on Oxidative Stability of Chicken Thigh (Quercetin의 급여가 육계 다리육의 산화 안정성에 미치는 영향)

  • Jang, Ae-Ra;Park, Jung-Eun;Kim, Sang-Ho;Chae, Hyun-Seok;Ham, Jun-Sang;Oh, Mi-Hwa;Kim, Hyoun-Wook;Seol, Kuk-Hwan;Cho, Soo-Hyun;Kim, Dong-Hun
    • Korean Journal of Poultry Science
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    • v.37 no.4
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    • pp.405-413
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    • 2010
  • This study was carried out to determine the effect of dietary supplementation of quercetin and methoxylated quercetin extracted from onions on oxidation of chicken thigh during cold storage. For 35 days, 1-day-old 320 broiler chicks (Ross) were divided into 8 groups and supplemented the diet; basal diet only (T1), T1 with antibiotics (T2), vitamin E 20 IU (T3), vitamin E 200 IU (T4), quercetin 20 ppm (T5), quercetin 200 ppm (T6), methoxylated quercetin 20 ppm (T7), methoxylated quercetin 200 ppm (T8). After slaughtering the broilers, thigh meats were collected and analyzed the oxidation stability during storage at $4^{\circ}C$ for 7 days. Volatile basic nitrogen (VBN) was ranged from 10.98~15.37 mg% until day 3 and quercetin 20 ppm (T5) significantly reduced (p<0.05) the VBN value of thigh as much as antibiotics treatment group (T2). The supplementation of quercetin at a 200 ppm level significantly reduced 2-thiobarbituric acid reactive substances value when compared with the control. Supplementation of 20 ppm quercetin also affected fatty acid composition of chicken thigh and resulted in increase of C18:1w9 and decrease of C18:2w6 on day 3. In microbes of chicken thigh during storage, supplementation of 20 ppm quercetin significantly reduced total microbes compare to control on day 7 (p<0.05). There was no effect on the number of coliforms in thigh with quercetin diet. From these results, the dietary supplementation of 20 ppm of quercetin may have effects on enhancing oxidation stability.

Effect of Quercetin in the UV-Irradiated Human Keratinocyte HaCaT Cells and A Model of Its Binding To p38 MAPK

  • Jnawali, Hum Nath;Lee, Eunjung;Shin, Areum;Park, Young Guen;Kim, Yangmee
    • Bulletin of the Korean Chemical Society
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    • v.35 no.9
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    • pp.2787-2790
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    • 2014
  • Quercetin is a major dietary flavonoid found in onions, apples, tea, and red wine, and potentially has beneficial effects on disease prevention. We carried out this study to investigate the effect of quercetin on UVB-induced matrix metalloproteinase-1 (MMP-1) expression in human keratinocyte HaCaT cells and to further understand the mechanisms of its action. The anti-inflammatory activity of quercetin was investigated and quercetin significantly suppressed the NO production in LPS-stimulated RAW264.7 mouse macrophages. Post treatment of quercetin decreased UV irradiation-induced phosphorylation of JNK, p38 MAPK, and ERK by 91%, 21%, and 17%, respectively. MMP-1 is mainly responsible for the degradation of dermal collagen during the aging process of human skin and quercetin suppressed the UVB-induced MMP-1 by 94%. Binding studies revealed that quercetin binds to p38 with high binding affinity ($1.85{\times}10^6M^{-1}$). The binding model showed that the 4'-hydroxy groups of the B-ring of quercetin participated in hydrogen bonding interactions with the side chains of Lys53, Glu71, and Asp168 and the 5-hydroxy group of the A-ring formed a hydrogen bond with the backbone amide of Met109. The major finding of this study shows that quercetin inhibits phosphorylation of JNK, p38 MAPK, and ERK pathway leading to the prevention of MMP-1 expression in human keratinocyte HaCaT cells. Therefore, our findings suggested the potentials of quercetin as a skin anti-photoaging agent.