• Title/Summary/Keyword: Flavonoids

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Anticancer and Antimutagenic Activities after Simulated Digestion of Ethanol Extracts from White, Red and Yellow Onions

  • Shon, Mi-Yae;Park, Seok-Kyu
    • Preventive Nutrition and Food Science
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    • v.11 no.4
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    • pp.278-284
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    • 2006
  • The beneficial effects of digested onion extracts have been assessed by antimutagenic and anticancer activities by Ames test and SRB test. The total phenolic acids and flavonoids in onion extracts were determined. Red and yellow onions contain more phenolic acids and flavonoids than those in the white onion. Digested, extracts showed antimutagenic activity and anticancer activity, and it appears that the antimutagenic activity of digested extracts of onion against mutagens and anticancer activities were related to their phenols and flavonoids contents. Moreover, the extracts inhibited the proliferation of four human tumorigenic cell lines such as HT-29 (colon), MCF-7 (breast), DU-145 (prostate) and HepG2 (liver), in a dose-dependent manner. Phenolic acids and flavonoids caused oxidative damage to the cancer cell lines and induced apoptosis. Generally, red onion extracts showed effective antimutagenic and anticancer activity, and the digested red onion extracts elicited stronger antimutagenic activity than those of the onion extracts without digestion.

Flavonoids analysis about mulberry fruit of Korean mulberry cultivar, 'Daeshim'

  • Ju, Wan-Taek;Kwon, O-Chul;Kim, Yong-Soon;Kim, Hyun-Bok;Sung, Gyoo-Byung;Kim, Jong-gil
    • International Journal of Industrial Entomology
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    • v.37 no.2
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    • pp.43-48
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    • 2018
  • Mulberry fruit is a new income product in Korea sericulture due to the increase of fruit consumption. However, flavonoids of Korean mulberry cultivar for fruit production did not reported yet. In this study, the typical mulberry cultivar, 'Daeshim' was analyzed using ultrahigh performance liquid chromatography coupled with diode array detection and quadrupole time-of-flight mass spectrometry (UPLC-DAD-QTOF/MS) technique for flavonoids analysis. Nine flavonoids were isolated and analyzed from Daeshim using UPLC-DAD-QTOF/MS chromatogram. According to quantitative analysis, rutin (66.1 mg/100g DW) and quercetin 3-O-(6"-O-malonyl) glucoside (26.7 mg/100g DW) were abundant in mulberry fruit. Our results might be used as basic information for mulberry consumption.

Flavonoids: Broad Spectrum Agents on Chronic Inflammation

  • Lim, Hyun;Heo, Moon Young;Kim, Hyun Pyo
    • Biomolecules & Therapeutics
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    • v.27 no.3
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    • pp.241-253
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    • 2019
  • Flavonoids are major plant constituents with numerous biological/pharmacological actions both in vitro and in vivo. Of these actions, their anti-inflammatory action is prominent. They can regulate transcription of many proinflammatory genes such as cyclooxygenase-2/inducible nitric oxide synthase and many cytokines/chemokines. Recent studies have demonstrated that certain flavonoid derivatives can affect pathways of inflammasome activation and autophagy. Certain flavonoids can also accelerate the resolution phase of inflammation, leading to avoiding chronic inflammatory stimuli. All these pharmacological actions with newly emerging activities render flavonoids to be potential therapeutics for chronic inflammatory disorders including arthritic inflammation, meta-inflammation, and inflammaging. Recent findings of flavonoids are summarized and future perspectives are presented in this review.

Flavonoids as Novel Therapeutic Agents Against Chikungunya Virus Capsid Protein: A Molecular Docking Approach

  • E. Vadivel;Gundeep Ekka;J. Fermin Angelo Selvin
    • Journal of the Korean Chemical Society
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    • v.67 no.4
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    • pp.226-235
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    • 2023
  • Chikungunya fever has a high morbidity rate in humans and is caused by chikungunya virus. There are no treatments available until now for this particular viral disease. The present study was carried out by selecting 19 flavonoids, which are available naturally in fruits, vegetables, tea, red wine and medicinal plants. The molecular docking of selected 19 flavonoids was carried out against the Chikungunya virus capsid protein using the Autodock4.2 software. Binding affinity analysis based on the Intermolecular interactions such as Hydrogen bonding and hydrophobic interactions and drug-likeness properties for all the 19 flavonoids have been carried out and it is found that the top four molecules are Chrysin, Fisetin, Naringenin and Biochanin A as they fit to the chikungunya protein and have binding energy of -8.09, -8.01, -7.6, and 7.3 kcal/mol respectively. This result opens up the possibility of applying these compounds in the inhibition of chikungunya viral protein.

Effects of Naturally Occurring Flavonoids on Inflammatory Responses and Their Action Mechanisms

  • Kim, Hyun-Pyo;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik
    • Natural Product Sciences
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    • v.6 no.4
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    • pp.170-178
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    • 2000
  • Flavonoids are natural polyphenolic compounds widely distributed in plant kingdom. Although many flavonoids were found to show anti-inflammatory activity in vitro and in vivo, the potency of anti-inflammatory activity was not enough for a clinical trial. Thus, a search for finding potential flavonoid molecules is continuing. In this review, in vivo anti-inflammatory activity of various flavonoid derivatives is summarized mainly based on the results obtained in authors' laboratories. Among them, several biflavonoids such as amentoflavone and ginkgetin were found to possess anti-inflammatory activity on animal models of acute/chronic inflammation comparable to nonsteroidal and steroidal anti-inflammatory drugs currently used. In respect of their action mechanisms, the effects on arachidonic acid metabolism and nitric oxide production were described. Some flavonoids directly inhibit cyclooxygenase and/or lipoxygenase. Biflavones such as ochnaflavone and ginkgetin are inhibitors of phospholipase $A_2$. In recent studies, certain flavonoids were also found to suppress cyclooxygenase-2 and inducible nitric oxide synthase expression induced by inflammatory stimuli. Therefore, it is suggested that anti-inflammatory activity of the certain flavonoids (mainly flavones, flavonols and biflavonoids) may be mediated by direct inhibition of arachidonic acid metabolizing enzymes as well as suppression of the enzyme expression involved in inflammatory responses.

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Anti-Inflammatory Effect of Quercetagetin, an Active Component of Immature Citrus unshiu, in HaCaT Human Keratinocytes

  • Kang, Gyeoung-Jin;Han, Sang-Chul;Ock, Jong-Woo;Kang, Hee-Kyoung;Yoo, Eun-Sook
    • Biomolecules & Therapeutics
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    • v.21 no.2
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    • pp.138-145
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    • 2013
  • Citrus fruit contain various flavonoids that have multiple biological activities. However, the content of these flavonoids are changed during maturation and immature Citrus is known to contain larger amounts than mature. Chemokines are significant mediators for cell migration, while thymus and activation-regulated chemokine (TARC/CCL17) and macrophage-derived chemokine (MDC/CCL22) are well known as the typical inflammatory chemokines in atopic dermatitis (AD), a pruritic and chronic inflammatory skin disease. We reported recently that the EtOH extract of immature Citrus unshiu inhibits TARC and MDC production. Therefore, we investigated the activity of flavonoids contained in immature Citrus on TARC and MDC levels. As a result, among the various flavonoids, quercetagetin has stronger inhibitory effects on the protein and mRNA expression of TARC and MDC than other flavonoids. Quercetagetin particularly has better activity on TARC and MDC level than quercetin. In HPLC analysis, the standard peak of quercetagetin matches the peaks of extract of immature C. unshiu. This suggests that quercetagetin is an anti-inflammatory component in immature C. unshiu.

Antioxidative Flavonoids from Leaves of Carthamus tinctorius

  • Lee, Jun-Young;Chang, Eun-Ju;Kim, Hyo-Jin;Park, Jun-Hong;Choi, Sang-Won
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.313-319
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    • 2002
  • A total of eight flavonoids (1-8), including a novel $quercetin-7-o-(6"-o-acetyl)-{\beta}-D-glucopyranoside$ (6) and seven known flavonoids, luteolin (1), quercetin (2), luteolin $7-o-{\beta}-D-glucopyranoside$ (3), $luteolin-7-o-(6"-Ο-acetyl)-{\beta}-D-glucopyranoside$ (4) quercetin $7-o-{\beta}-D-glucopyranoside$ (5), acacetin 7-o-{\beta}-D-glucuronide (7) and apigenin-6-C-{\beta}-D-glucopyrano $syl-8-C-{\beta}-D-glucopyranoside$ (8), have been isolated from the leaves of the safflower (Carthamus tinctorius L.) and identified on the basis of spectroscopic and chemical studies. The antioxidative activity of these flavonoids was evaluated against 2-deoxyribose degradation and rat liver microsomal lipid peroxidation induced by hydroxyl radicals generated via a Fenton-type reaction. Among these flavonoids, luteolin-acetyl-glucoside (4) and quercetin-acetyl-glucoside (6) showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin (1), quercetin (2), and their corresponding glycosides (3 & 5) also exhibited strong antioxidative activity, while acacetin glucuronide (7) and apigenin-6,8-di-C-glucoside (8) were relatively less active.

Inhibitory effects of flavonoids on TNF-α-induced IL-8 gene expression in HEK 293 cells

  • Lee, Soo-Hyoung;Kim, Young-Jin;Kwon, Sang-Hoon;Lee, Young-Hee;Choi, Soo-Young;Park, Jin-Seu;Kwon, Hyung-Joo
    • BMB Reports
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    • v.42 no.5
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    • pp.265-270
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    • 2009
  • Due to their multiple biological activities, flavonoids have gained attention as potentially useful therapeutics for a variety of diseases including cancer, cardiovascular diseases, and autoimmune diseases. In this study, we demonstrated that several flavonoids, including kaempferol, quercetin, fisetin, and chrysin block TNF-$\alpha$ induced IL-8 promoter activation and gene expression in HEK 293 cells. In addition, phosphorylation and degradation of $I{\kappa}B{\alpha}$ and translocation of NF-${\kappa}B$ p65 were inhibited by these flavonoids in TNF-$\alpha$-stimulated HEK 293 cells. Furthermore, generation of reactive oxygen species (ROS) in response to TNF-$\alpha$ was reduced by the flavonoids. Moreover, although pretreatment with fisetin, quercetin, or chrysin decreased cell viability, kaempferol did not. Taken together, these findings suggest that kaempferol would be useful for the treatment of TNF-$\alpha$-induced inflammatory diseases.

Quantitative Analysis of Flavonoids in the Unripe and Ripe Fruits and the Leaves of Four Korean Rubus species (한국산 4종 Rubus속 숙과, 미숙과 및 잎의 플라보노이드 함량 분석)

  • Kim, Min-Young;Choi, Moo-Young;Nam, Jung-Hwan;Park, Hee-Juhn
    • Korean Journal of Pharmacognosy
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    • v.39 no.2
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    • pp.123-126
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    • 2008
  • The five flavonoids, isoqueritrin, juglanin, astragalin and 2-O-trans-p-coumaroyl astragalin were quantitatively analyzed in the leaves, unripe- and ripe fruits of four Korean Rubus species including Rubus crataegifolius, R. pungens var. oldhami, R. parvifolius, and R. coreanus belonging to the Rosaceae family. The HPLC analysis demonstrated that flavonoids are more abundant in the leaves than in the fruits. In the four Rubus species, ripe fruits generally contained similar or more amount of flavonoids than in unripe fruits. In particular, the quantity levels of total flavonoid (49.81${\pm}$0.50 mg/g) and isoquercitrin (35.08${\pm}$0.37 mg/g) were highest in the leaf of R. crataegifolius. In addition, the content of the flavonoids were quite low in the unripe fruits of R. coreanus that is most widely used as Rubi Fructus.

Prosuction of Cytokine and NO by RAW 264.7 Macrophages and PBMC In Vitro Incubation with Flavonoids

  • Lyu, Su-Yun;Park, Won-Bong
    • Archives of Pharmacal Research
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    • v.28 no.5
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    • pp.573-581
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    • 2005
  • Flavonoids, a group of low molecular weight phenylbenzopyrones, have various pharmacological properties including antioxidant activity, anticancer, and immunomodulatory effects. In the present study, lipopolysaccharide (LPS) and phorbol 12-myristate 13-acetate/phytohemagglutinin (PMA/PHA) were used as stimulants for RAW 264.7 macrophages and human peripheral blood mononuclear cell (hPBMC), and tumor necrosis factor (TNF)-${\alpha}$ and interleukin (IL)-2 productions were measured. In addition, flavonoids were examined for their effects on LPS-induced NO production in RAW 264.7 macrophages. The results showed that all compounds were not strongly cytotoxic at the tested concentrations on hPBMC and RAW 264.7 macrophages. On immunomodulatory properties, catechin, epigallocatechin (EGC), naringenin, and fisetin repressed NO production and TNF-${\alpha}$ secretion. Furthermore, catechin, epigallocatechin gallate (EGCG), epicatechin (EC), luteolin, chrysin, quercetin, and galangin increased IL-2 secretion while EGC, apigenin, and fisetin inhibited the secretion. These results indicated that flavonoids have the capacity to modulate the immune response and have a potential anti-inflammatory activity. There was no obvious structure-activity relationship regard to the chemical composition of the flavonoids and their cell biological effects.