• Archives of Pharmacal Research
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• v.22 no.2
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• pp.173-178
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• 1999

Remarks on polyphenolic compounds has been arisen since past few years. the flavonoids appears to be the important groups of compounds with their capability to inhibit DNA damage, lipid peroxidation, to quench free radicals and, at least, anticarcinogenic and antiproliferative effects. On the other hand, their mechanism of action is still unexplained. Apigenin and luteolin are the most wide-spread flavones and they exhibited to be useful in chemoprevention. UV spectrometric and DC polarographic studies on these two compounds have been carried out with regard to changing pH. The most significant changes were observed at basic pH. These results could aid to elucidation of their mechanism of action as pH is one of the important factors for bioprocesses passing in living organisms.

• Journal of Medicine and Life Science
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• v.15 no.1
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• pp.6-11
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• 2018

Previous studies have suggested that Citrus fruits might suppress the proliferation of various cancer cells. However, little is known about any specific ingredients in the extract of Citrus fruits to exert its anti-proliferative activity in cancer cells. The present study aimed to identify the active ingredients in Citrus fruits to suppress the proliferation of rat hepatocellular carcinoma cells. Among tested compounds, two polymethoxylated flavones (nobiletin and tangeritin) showed significant anti-proliferative activity whereas other compounds (synephrine, rutin, hesperidin) did not. Interestingly, nobiletin as well as tangeritin also decreased the protein amount of gluconeogenic enzymes, PEPCK and G6Pase. The possible involvement of gluconeogenic activity in the proliferation of hepatocellulacarcinoma cells are further to be investigated.

• Journal of Life Science
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• v.14 no.1
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• pp.1-7
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• 2004

The root of Stnchys Sieboldif MIQ was extracted three times with methanol and extract was found to contain 3.02% of polyphenols and 1.97% of flavonoids. DPPH radical scavenging method, ferric thiocyanate method, and nitrite scavenging ability method were employed to investigate the constituents of the extract and to measure their activity on antioxidation. The fraction extracted by ethylacetate showed higher anti oxidation value than that of $\alpha-tocopherol$, butylated hydroxyanisole (BHA), and butylated hydroxytoluene (BHT) at the same concentration. UV-VIS spectral data of the extract by ethylacetate that was isolated on a silica gel column proved adsorption maxima in the range of 280∼330 nm. The fraction ES-RS that has $\lambda_{max}(nm)$ of band 1, 325nm and band II, 289nm exhibitd the strongest activity on antioxidation. ES-R5 fraction showed similar pattern to flavones by the analysis of UV-VIS spectral data.

• Journal of Nutrition and Health
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• v.47 no.3
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• pp.176-185
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• 2014

Purpose: The purpose of this study was to investigate the relationship between dietary flavonoids intake and metabolic syndrome (MetS) in Korean women with polycystic ovary syndrome (PCOS). Methods: A total of 223 subjects (mean age; $27.3{\pm}4.2$ yrs, range; 17-38 yrs) were divided into the MetS group (n = 27) and non-MetS group (n = 196). Dietary intake data were assessed by 24-hour recall method for two non-consecutive days and the average of the two days was used to estimate the usual dietary intake. Dietary habits were assessed using the Mini Dietary Assessment (MDA) score. We analyzed the intakes of six flavonoid classes (anthocyanidins, flavan-3-ols, flavanones, flavones, flavonols, and iso-flavones) using a flavonoids database. Results: After adjustment for age, total energy intake, alcohol consumption, smoking, regular exercise, and oral contraceptive use, dietary flavonols intake was significantly lower in the MetS group ($5.1{\pm}2.4$ mg/d) than in the non-MetS group ($8.9{\pm}2.8$ mg/d) (p = 0.0472). Intakes of other flavonoids except for flavonols did not differ between the two groups. In MDA scores, significant differences were observed only for that related to daily consumption of fruit or fruit juice (p = 0.0180). A significant inverse relationship was observed between flavonols intake and the risk of MetS (4th vs. 1st quartile, OR = 0.11, 95% CI = 0.02-0.62, p for trend = 0.0131). Conclusion: These results suggest that higher intake of flavonols may be beneficial for MetS in PCOS women.

• 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.

• Journal of Applied Biological Chemistry
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• v.57 no.3
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• pp.211-218
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• 2014

Polymethoxyflavones (PMFs) are a group of polymethoxylated bioactive flavones with diverse biological activities, including anticancer, anti-inflammatory, antibacterial, and antiviral activities. PMFs are found from various plants such as orange, tangerine, and krachaidum. To establish the simple quantitative analytical methods for PMFs, chromatographic analysis was applied to the selected krachaidum foods because krachaidum contains diverse PMFs compared to other PMF-containing foods. Krachaidum is the rhizome of Kaempferia parviflora, and many commercial krachaidum products, such as tea, juice and wine, are commercially available and consumed as health functional foods in Asian countries. Apart from the claimed health promoting benefits, reliable quality assurance and legal guideline for the registration of these products are not available yet. Twelve PMFs were analyzed from the commercial krachaidum foods by GC-FID and HPLC-DAD. No single chromatographic method could not analyze 12 PMFs simultaneously. HPLC-DAD method was found more sensitive to detect PMFs. Based on our analysis data, we proposed 5,7-dimethoxyflaone and 5,7,4'-trimethoxyflavone as index components for the food products.

• Molecules and Cells
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• v.26 no.2
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• pp.171-174
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• 2008

Flavone (2-phenyl chromone) is a well-known plant flavonoid, but its bioactivity has been little explored. Treatment of Caenorhabditis elegans or C. brissage with flavones induced embryonic and larval lethality that was pronounced in early larval stages. This anti-nematodal effect was also observed in the pinewood nematode, B. xylophilus. $LD_{50}$ values were approximately $100{\mu}M$ for both B. xylophilus and C. elegans. Our results indicate that flavone is an active nematicidal compound that should be further investigated with the aim of developing a potent drug against B. xylophilus.

• Bulletin of the Korean Chemical Society
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• v.29 no.8
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• pp.1479-1484
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• 2008

Protein tyrosine phosphatase (PTP) 1B is the superfamily of PTPs and a negative regulator of multiple receptor tyrosine kinases (RTKs). Inhibition of protein tyrosine phosphatase 1B (PTP1B) has been proposed as a strategy for the treatment of type 2 diabetes and obesity. Recently, it has been reported that amentoflavone, a biflavonoid extracted from Selaginella tamariscina, inhibited PTP1B. In the present study, docking model between amentoflavone and PTP1B was determined using automated docking study. Based on this docking model and the interactions between the known inhibitors and PTP1B, we determined multiple pharmacophore maps which consisted of five features, two hydrogen bonding acceptors, two hydrogen bonding donors, and one lipophilic. Using receptor-oriented pharmacophore-based in silico screening, we searched the biflavonoid database including 40 naturally occurring biflavonoids. From these results, it can be proposed that two biflavonoids, sumaflavone and tetrahydroamentoflavone can be potent allosteric inhibitors, and the linkage at 5',8''-position of two flavones and a hydroxyl group at 4'-position are the critical factors for their allosteric inhibition. This study will be helpful to understand the mechanism of allosteric inhibition of PTP1B by biflavonoids and give insights to develop potent inhibitors of PTP1B.

• Journal of Microbiology and Biotechnology
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• v.17 no.3
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• pp.530-533
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• 2007

It has been well known that the use of Saccharomyces cerevisiae can cause fungemia in critically ill patients and flavone shows an antimicrobial effect on S. cerevisiae. Therefore, we have investigated the activities of thirteen flavone analogues on S. cerevisiae in our studies. Because flavonoids including flavones have antioxidative effects, we try to carry out the activity studies of flavone analogues in vitro and in vivo. In addition, the relationships between the structures of flavone analogues and their biological activities, such as antimicrobial and antioxidative effects, were elucidated using Comparative Molecular Field Analysis calculations. Of the flavone analogues tested here, 3,2'-dihydroxyflavone showed both good antimicrobial and antioxidative activities.

• Journal of Nutrition and Health
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• v.45 no.3
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• pp.283-292
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• 2012

Flavonoids have been hypothesized to reduce the risk of chronic diseases, but the lack of a flavonoid database hampered epidemiological studies addressing this issue in Korea. In this study, we developed a flavonoid database, based on a systematic review. A total of 1549 food items containing flavonoids were selected using the Korean Nutrient Database. Among them, flavonoid contents for only 649 food items were evaluated with analytical values and the remaining 900 items were replaced with adaptations or calculations from similar items. The developed flavonoid database covered 93.2% of fruits and fruit juices, 76.1% of vegetables, 98.4% of legumes and legume products, and 85.0% of all plant foods overall (1,549 items) as reported by the 24-hr dietary recall method regarding the 2008 Korean National Health and Nutrition Examination Survey. We found that this flavonoid database, overall, included 95.6% of all mainly consumed plant foods by Koreans. This flavonoid database is expected to be useful in regards to the correlation study of flavonoid intake and chronic diseases.