• Journal of Plant Biology
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• v.35 no.4
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• pp.409-414
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• 1992

Effect of quercetin, a kind of natural plant flavonoids, on auxin-induced ethylene production in barley coleoptiles was studied. Auxin-induced ethylene production was apparently stimulated by quercetin. This stimulatory effect of quercetin appeared after 4 h of incubation period. Ethylene production was stimulated 200% over the control after 8 h of incubation by $3{\times}10^{-5}\;M$ quercetin. The quercetin effect was most prominent at $10^{-4}\;M$ of IAA. Ethylene production induced by the synthetic auxin, 2,4-D and NAA, was not significantly affected by quercetin. Also ACC-based ethylene production was unaffected by the flavonoid. In an effort to elucidate mechanisms of quercetin action on auxin-induced ethylene production, the effect of quercetin on 1M metabolism was studied. Data obtained from these experiments indicate that quercetin treatment resulted in about 90% inhibition of IAA oxidase activity. IAA ($3{\times}10^{-5}\;M$) conjugation was found to be not affected by quercetin. This results suggest that the stimulatory effect of quercetin on auxin-induced ethylene production may be due to the fact that quercetin inhibits 1M oxidase activity, thus increasing the free IAA level.

• Mass Spectrometry Letters
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• v.7 no.3
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• pp.79-83
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• 2016

We prepared solid dispersion formulations of quercetin to enhance its solubility and dissolution rate. Various quercetin-loaded solid dispersion were tested with quercetin, poloxamer 407, and carrier such as hydroxypropyl methyl cellulose (HPMC), polyethylene glycol 8000 (PEG 8000), and polyvinylpyrrolidone K40 (PVP K40) using solvent evaporation and freeze drying methods in terms of both the aqueous solubility and the dissolution rates of quercetin. The solubility of quercetin as its solid dispersion formulations was markedly improved compared with that of quercetin powder. Especially, highest solubility of quercetin was observed when HPMC was used as a carrier. The cumulative dissolution of quercetin within 360 min from solid dispersion composed of quercetin, poloxamer 407, and HPMC was 8.8-fold higher than the dissolution of pure quercetin. The results of powder X-ray diffraction (XRD) and scanning electron microscope (SEM) indicated that quercetin transformed from a crystalline to an amorphous form through the solid dispersion formulation process. These results suggest that the solid dispersion formulation of quercetin with poloxamer 407 and HPMC could be a promising option for enhancing the solubility and dissolution rate of quercetin.

• Biomolecules & Therapeutics
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• v.24 no.4
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• pp.410-417
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• 2016

Quercetin is a flavonoid usually found in fruits and vegetables. Aside from its antioxidative effects, quercetin, like other flavonoids, has a various neuropharmacological actions. Quercetin-3-O-rhamnoside (Rham1), quercetin-3-O-rutinoside (Rutin), and quercetin-3-(2(G)-rhamnosylrutinoside (Rham2) are mono-, di-, and tri-glycosylated forms of quercetin, respectively. In a previous study, we showed that quercetin can enhance ${\alpha}7$ nicotinic acetylcholine receptor (${\alpha}7$ nAChR)-mediated ion currents. However, the role of the carbohydrates attached to quercetin in the regulation of ${\alpha}7$ nAChR channel activity has not been determined. In the present study, we investigated the effects of quercetin glycosides on the acetylcholine induced peak inward current ($I_{ACh}$) in Xenopus oocytes expressing the ${\alpha}7$ nAChR. $I_{ACh}$ was measured with a two-electrode voltage clamp technique. In oocytes injected with ${\alpha}7$ nAChR copy RNA, quercetin enhanced $I_{ACh}$, whereas quercetin glycosides inhibited $I_{ACh}$. Quercetin glycosides mediated an inhibition of $I_{ACh}$, which increased when they were pre-applied and the inhibitory effects were concentration dependent. The order of $I_{ACh}$ inhibition by quercetin glycosides was Rutin${\geq}$Rham1>Rham2. Quercetin glycosides-mediated $I_{ACh}$ enhancement was not affected by ACh concentration and appeared voltage-independent. Furthermore, quercetin-mediated $I_{ACh}$ inhibition can be attenuated when quercetin is co-applied with Rham1 and Rutin, indicating that quercetin glycosides could interfere with quercetin-mediated ${\alpha}7$ nAChR regulation and that the number of carbohydrates in the quercetin glycoside plays a key role in the interruption of quercetin action. These results show that quercetin and quercetin glycosides regulate the ${\alpha}7$ nAChR in a differential manner.

• Korean Journal of Food Science and Technology
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• v.37 no.1
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• pp.90-94
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• 2005

Absorption, metabolism, and tissue concentrations of quercetin were examined and compared in mice and rats after oral administration of quercetin at 50 or 100 mg/kg. Quercetin was absorbed quickly in mice and reached maximum plasma concentration in I hr post-administration, and declined sharply after 4 hr. Plasma concentration of isorhamnetin, a major metabolite, also increased sharply, indicating rapid metabolic conversion, but elevated level was maintained longer than that of quercetin. Quercetin and isorhamnetin were found predominantly in glucuronide/sulfate-conjugate forms in both mice and rats. Tissue concentrations of quercetin and isorhamnetin in mice and rats were in the order of liver>kidney>spleen>plasma both 1 and 6 hr postadministration. These results show that quercetin is absorbed in mice after oral feeding and quickly metabolized into isorhamnetin as demonstrated in humans and other animal species. The results also can be used to explain various pharmacological activities reported in mouse models.

• Journal of Food Hygiene and Safety
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• v.11 no.2
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• pp.115-121
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• 1996

In order to compare the suppressive effect of quercetin and several its glycosides, such as quercitrin (quercetin-3-rhamnoside), isoquercitrin (quercetin-3-glucoside), hyperin (quercetin-3-galactoside) and tutin (quercetin-3-rhamnosyl glucoside), on the genotoxicity by N-methyl-N-nitrosourea(MNU), in vitro sister chromatid exchange(SCE) test using mouse spleen lymphocytes and in vivo micronucleus test using mouse peripheral blood were performed. MNU-induced SCEs in vitro were not decreased by the simultaneous treatment of test compounds. Among them, quercetin and hyperin showed significant suppressive effects at high dose(10-5M). On the other hand, MNU-induced micronucleated reticulocytes(MNRETS) in vivo were significantly decreased with good dose-dependent manner in all compound tested. However, there were not significant differences between quercetin aglycone and its glycosides in the suppressive aglycone and its glycosides may act as an antigenotoxic agent in vivo and may be useful as a chemopreventive agent of alkylating agent.

• Horticulture, Environment, and Biotechnology : HEB
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• v.59 no.6
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• pp.909-917
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• 2018

Quercetin and its glycoside derivatives were identified and quantified using high-performance liquid chromatograph (HPLC) and liquid chromatograph/mass spectrometer/mass spectrometer (LC/MS/MS) in the leaves, flowers, and fruits of 22 Malus genotypes. In all genotypes, small amounts of quercetin aglycone were present, with water-soluble glycoside forms were the most abundant in different Malus plant tissues, including quercetin-3-galactoside, quercetin-3-rutinoside, quercetin-3-glucoside, quercetin-3-xyloside, quercetin-3-arabinoside, and quercetin-3-rhamnoside. Among these six quercetin glycosides, quercetin-3-galactoside was the common form in Malus plants, except in the leaves and flowers of M. ceracifolia and M. magdeburgensis, and in the fruits of M. micromalus 'Haihong Fruit', where there was a higher concentration of quercetin3-glucoside. Among the different tissues tested, leaves contained the highest concentration of quercetin and its glycosides, while fruits contained the lowest concentrations of these compounds. Among the genotypes we analyzed, no specific genotype consistently contained the highest concentration of quercetin and its glycoside derivatives. M. domestica 'Honeycrisp' had the highest total compound concentration (approximately $1600mg\;kg^{-1}$), whereas M. hupehensis contained the lowest in its fruits. In contrast, the concentration of total quercetin and its glycosides was more than $5000mg\;kg^{-1}$ in the leaves of eight genotypes and greater than $2500mg\;kg^{-1}$ in the flowers of seven species. In general, the concentration of quercetin and its glycoside derivatives depended on the species and tissue type. These results may provide useful information for the evaluation and selection of edible Malus fruits and the materials for quercetin glycoside extraction.

• Journal of Food Hygiene and Safety
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• v.33 no.4
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• pp.289-295
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• 2018

The aim of this study was to develop and validate an analytical method for determining the presence of wogonin, quercetin, and quercetin-3-O-glucuronide in extracts of Nelumbo nucifera, Morus alba L., and Raphanus sativus mixtures. We evaluated the specificity, linearity, precision, accuracy, limit of detection (LOD), and limit of quantification (LOQ) of analytical methods for wogonin, quercetin, and quercetin-3-O-glucuronide using high performance liquid chromatography. Our result showed that the correlation coefficients of the calibration curve for wogonin, quercetin, and quercetin-3-O-glucuronide were 0.9999. The LOD for wogonin, quercetin, and quercetin-3-O-glucuronide ranged from 0.09 to 0.16 and those for the LOQ ranged from 0.26 to $0.48{\mu}g/mL$. The inter-day and intra-day precision values of wogonin, quercetin, and quercetin-3-O-glucuronide ranged from 0.74 to 1.87 and from 0.28 to 1.12%, respectively. The inter-day and intra-day accuracies were 99.96~115.88% and 99.73~114.81%, respectively. Therefore, the analytical method was validated for the detection of wogonin, quercetin, and quercetin-3-O-glucuronide in extracts of Nelumbo nucifera, Morus alba L., and Raphanus sativus mixtures.

• The Korean Journal of Pharmacology
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• v.27 no.1
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• pp.69-80
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• 1991

Inhibitory effects of quercetin and rutin on lipid peroxidation of microsomes caused by iron(II) were investigated with respect to the scavenging action for oxygen radicals produced during oxidation of iron and the chelating action for iron. Lipid peroxidation by $Fe^{2+}$ alone was markedly inhibited by quercetin or rutin in a dose dependent fashion. Lipid peroxidation by ascorbate or NADPH in the presence of $Fe^{2+}$ was almost completely inhibited by both quercetin and rutin. The peroxidative action of $Fe^{2+}$ was inhibited by SOD and DABCO and slightly inhibited by catalase, DMSO and mannitol. Quercetin and rutin inhibited oxidation of $Fe^{2+}$ which is responsible for DETAPAC and they showed a significant initial chelating effect. Quercetin and rutin effectively inhibited lipid peroxidation by $H_{2}O_{2}$ and decomposed $H_{2}O_{2}$. Both $OH{\cdot}$ production in the presence of $Fe^{2+}$ and $^1O_2$ production by U.V. irradiation were inhibited by quercetin and rutin. Lipid peroxidations by $Cd^{2+},\;Cu^{2+},\;Ni^{2+},\;Pb^{2+}$ and $Zn^{2+}$ were almost completely inhibited by quercetin. Quercetin and rutin significantly prevented the loss of sulfhydryl groups by $Fe^{2+}$. These results suggest that inhibitory effects of quercetin and rutin on the peroxidative action of $Fe^{2+}$ in the presence or absence of ascorbate and NADPH may be attributable to their scavenging action on reactive oxygen species and chelating action on iron.

• Journal of the Korean Institute of Oriental Medical Informatics
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• v.21 no.1
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• pp.14-22
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• 2015

Flavonoids show diverse bioactivities, such as anti-oxidant, anti-cancer, anti-allergic, anti-inflammatory, and anti-viral. Quercetin is one of the flavonoids present in a wide range of plants, especially onions and consumed all over the world. Recently, it is known that quercetin induces mitochondrial biogenesis in vivo and in vitro. However, detail mechanism of these actions remains unknown. We investigated quercetin's effects on mitochondrial biogenesis in HepG2 cells, and determined the mechanisms involved. We found that quercetin treatment induced the expression of mitochondrial biogenesis activators, $PGC-1{\alpha}$, NRF-1, TFAM, and mitochondrial proteins, cytochorome c and complex IV (COXIV). Moreover, amount of mitochondrial DNA was also increased by quercetin. Quercetin has been known to induce heme oxygenase (HO)-1 in several types of cells. Here, we found quercetin induces HO-1, and inhibition of HO-1 or CO, which is product of HO-1, decreased quercetin-induced mitochondrial biogenesis such as induction of $PGC-1{\alpha}$, NRF-1, TFAM, cytochorome c, COXIV, and mitochondrial DNA. These findings imply that quercetin can increase mitochondrial biogenesis via HO-1/CO system. High glucose results in dysfunction of mitochondria biogenesis. In the present study, 25 mM glucose decreased mitochondrial biogenesis and this damage was restored by quercetin. Conversely, inhibition of HO-1 or CO inhibited quercetin-induced mitochondrial biogenesis rescue. These results suggest that quercetin enhances mitochondrial biogenesis via HO-1/CO system and hence, can rescue mitochondria from damage by high glucose.

• Proceedings of the Korean Society of Postharvest Science and Technology of Agricultural Products Conference
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• 2003.04a
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• pp.106-107
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• 2003

양파는 세계적으로 가장 많이 사용하는 약용식물이며 식품에도 많이 이용되어왔다. 기존의 많은 연구들은 양파에는 많은 양의 quercetin이 함유되어 있다고 보고하였으며, quercetin은 주로 와인, 차, 양파, 사과와 같은 식품이나 과일이나 채소에 존재한다고 알려져 왔다. 그러나 과거에는 quercetin은 돌연변이성이 있으며, 종양의 크기를 증가시키는 원인으로 알려져 왔으나 최근에는 quercetin은 식품으로 섭취하였을 때, antithrombotic, antiallergic, antiviral과 antiinflammatory 효과를 갖는다고 보고되었다. 최근에는 자연적인 항암제로써 잠재성을 갖고 있다고 보고하고 있다. 이번 연구에서 onion을 4부위 (skin, outward, middle, core)로 분리 후 각각의 부위별 quercetin의 함량을 비교분석 하였다. 각각의 부위는 동결건조 후 HPLC를 사용하여 374 nm에서 $C_{18}$ coloum을 가지고 분석하였다. 그 결과 각각부위별 quercetin의 함량은 skin, outward, middle, core에서 8.41 mg/g, 1.34 mg/g, 0.47 mg/g, 0.18 mg/g로 측정되었다. 결국 중심에서 밖으로 갈수록 quercetin의 함량이 증가하는 것이 판명되었으며 특히, skin에서 quercetin의 함량은 가식부위와 비교하였을 때 가장 높은 것으로 나타났다.