• Proceedings of the PSK Conference
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• 2003.10b
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• pp.112.2-112.2
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• 2003

CYP1 enzymes, CYP1A1, CYP1A2 and CYP1B1, are known to bioactivate procarcinogens particularly polyaromatic compounds. Flavonoids are a class of natural compounds that are present in edible plants. Structurally, these compounds are polyphenols with two aromatic rings (A, B) and a heterocycyclic ring (C). We observed the differential inhibition of 5,7-dihydroxyflavones which are different in numbers of B-ring-OH, to the activity of ethoxyresorufin O-deethylase (EROD) in human hepatic microsomes with the IC50 values, ie, 0.57 mM, 1.28 mM, and 3.62 mM, chrysin, apigenin, and Luteolin, respectively. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.192.2-192.2
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• 2003

Apigenin-7-O-${\beta}$-D-glucoside, chrysoeriol, and luteolin were isolated from the aqueous ethanolic extract of Zostera marina L. leaves as the scavengers of reactive oxygen species (ROS) with the SC$\_$50/ values of 0.18 mM, 0.68 mM, and 0.18 mM against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 0.04 mM, 0.03 mM, and 0.01 mM against superoxide radicals in the xanthine/xanthine oxidase system, respectively. The luteolin suppressed the expression of matrix metalloproteinase-1 (MMP-1) up to 44% at 4.0 ${\mu}$M. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.200.1-200.1
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• 2003

Cephalotaxus koreana Nakai is an endemic species in Korea. The EtOH extract of leaf and branch from the plant showed potent antitumor activity in Teruhiro's method. The tumor volume inhibition ratio value is 25.2% with 20mg/kg in the BDF1 mouse injected LLC cell. We isolated one flavone, sciadopitysin (1), two flavone O-glycosides, quercetin 3-O-${\beta}$-D-glucuronide 6"-ethyl ester (2), apigenin 7-neohesperidoside (3) in comparison with literatures data. Compounds 1-3 showed stronger antitumor activity than Taxol used as positive control. The inhibition ratio values of compounds 1-3 is 34.9, 31.6, 34.0%, respectively, and Taxol is 27.0 % compared with control group.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.255.1-255.1
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• 2002

We investigated the anti-proliferative effects of lxeris sonchifolia H. (godulbaegi) root extracts. luteolin(3'. 4', 5. 7-Q-glucoside and 3'. 4', 5, 7-tetrahydoxyflavone) and apigenin (3', 4'. 5. 7-O-gluconic acid) on HepG2 (p53 wild type) cells. Hep3B (p53 null) cells, and Chang liver cells. In MTT assay 3', 4'.5. 7-tetrahydoxyflavone showed the most efficient anti-proliferative effects on these three cell lines. However, there was no significant anti-proliferative effect on Chang liver cell line in MTT results. (omitted)

• Journal of the Korean Chemical Society
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• v.67 no.3
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• pp.181-190
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• 2023

Melanoma is a malignant skin tumor caused by damage to melanocytes that can spread to other organs. Hence, various studies have been conducted on preventing the spread of melanoma. Flavonoid-structured substances such as apigenin and galanzin are effective therapeutic agents for inhibiting the proliferation and metastasis of melanoma. In this study, luteolin, quercetin, and their respective derivatives were synthesized. These compounds inhibited cell proliferation of B16 melanoma cells. These results confirmed that the derivatives of quercetin and luteolin may be useful as therapeutic agents to prevent melanoma metastasis.

• Korean Journal of Food Science and Technology
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• v.37 no.2
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• pp.183-188
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• 2005

Effects of co-solvent polarity, citric acid, pressure, temperature, run time, and co-solvent ratio on extraction of major flavonoids from Lonicera Flos were investigated using supercritical fluid $CO_{2}(SF-CO_{2})$. HPLC analysis revealed addition of pure methanol resulted in low extraction yield of major flavonoids, luteoloin (Lu), Quercetin (Qu), Apigenin (Ap). Under same condition, as co-solvent polarity increased, yields of major flavonoids increased gradually, At optimum co-solvent extraction condirion of 60% aqueous methanol (10%, v/v), yields of Lu, Qu, and Ap were 42.09, 28.18, and 3.49 mg/100 g, respectively. Addition of citric acid to 60% aqueous methanol gave higher, with addition of 1% citrie acid resulting in highest yields of 63.2 (Lu), 39.35 (Qu), and 5.79 (Ap) mg/100 g. Optimum extraction conditions of major flavonoids were 200 bar, $50^{\circ}C$, 60 min, and $CO_{2}$-methanol-water(20: 1.8: 1.2).

• Journal of the Korean Society of Food Science and Nutrition
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• v.32 no.4
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• pp.501-505
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• 2003

In order to use as a new functional food material, chemical components of propolis and its extracts were surveyed. The contents of crude fat, nitrogen free extract, crude protein, ash and crude fiber in propolis were 86.41%, 7.32%, 2.71%, 1.05% and 0.20%, respectively. The mineral contents were in the order of Na (120.40 mg%), Ca (115.40 mg%), K (105.87 mg%) and Ca were higher in water extract than alcohol extract. Free sugars were composed of sucrose 152 mg%, glucose 114 mg% and fructose 6 mg%. The major amino acids of propolis were lysine 395.29 mg%, cystine 267.66 mg% and glutamic acid 248.14 mg%, respectively. Eight fatty acids in propolis were identified and the major fatty acids were oleic acid (51.89%), myristic acid (20.86%) and palmitic acid (20.28%). Myricetin, quercetin, apigenin and kaempferol were shown as major flavonols and total flavonol contents were higher in 50% ethanol extract than any other extracts. Major Polyphenol compounds in four kinds of extracts were gallic acid, chlorogenic acid, catechin, epigallocatechin gallate, epicatechin and epicatechin gallate.

• 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.22-39
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• 2003

Biological activity of phenolic compounds in seeds and leaves of safflower (Carthamu tinctorius L.) were evaluated using several in vitro and in vivo assays. Six phenolic constituents were isolated from the seeds and identified as N-feruloylserotonia, N- (p-coumaroyl)serotonin, matairesinol, 8′-hydroxyarctigenin, acacetin 7-O-$\beta$-D-glucoside (tilianine) and acacetin. Six phenolic compounds exhibited considerable antioxidative activity, and especially two serotonins showed potent DPPH radical scavenging activity and antiperoxidative activity against rat liver microsomal lipid peroxidation induced by the hydroxyl radical generated via a Fenton-type reaction. Additionally, six phenolic compounds possessed comparable cytotoxicity against three cancer cells, Hela cell, MCF-7 and HepG2 cell, and particularly acacetin and its glycosides had the most potent cytotoxicity. Moreover, we found that feeding safflower seeds attenuated bone loss, and lowered levels of plasma and liver lipids in ovariectomized rats. Serotonins, lignans and flavones stimulated proliferation of the osteoblast-like cells in a dose-dependent manner (10$^{-15}$ ~10$^{-6}$ M), as potently as E$_2$ (17$\beta$-estradiol). Particularly, serotonins were mainly responsible for bone-protecting and lipid lowering effects in ovariectomized rats. Meanwhile, eight flavonoids, including a novel quercetin-7-O-(6"-O-acetyl)-$\beta$-D-glucopyranoside and seven kown flavonoids, luteolin quercetin, luteolin 7-O-$\beta$-D-glucopyranoside, luteolin-7-O-(6"-O-acetyl)-$\beta$-D-gluco-pyranoside, quercetin 7-O- -glucopyranoside, acacetin 7-O-$\beta$-D-glucuronide and apigenin-6-C-$\beta$-D-glucopyranosyl-8-C-$\beta$-D-glucopyranoside were first isolated and identified from safflower leaf. Among these flavonoids, luteolin-acetyl-glucoside and $\beta$quercetin- acetyl-glucoside showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin, quercetin and their corresponding glycosides also exhibited strong antioxidative activity, while acacetin glucuronide and apigenin-6, 8-di-C-glucoside were relatively less active. Finally, changes in phenolic compositions were also determined by HPLC in the safflower seed and leaf during growth stages and roasting process to produce standardized supplement powerds. These results suggest that phenolic compounds in the roasted safflower seed and leaf may be useful as potential sources of therapeutic agents against several pathological disorders such as carcinogenesis, atherosclerosis and osteoporosis.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.2
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• pp.235-240
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• 2004

In order to develop new anti-photoaging agents from marine natural products, Zostera marina L. was selected for its antioxidative activity and inhibition of matrix metalloproteinase-1 (MMP-1) expression. Three compounds (compounds 1, 2, and 3) were isolated from the extract, and they were identified as apigenin-7-O-${\beta}$-D-glucoside (1), chrysoeriol (2), and luteolin (3). These compounds have SC$\_$50/ values of 0.18 mM, 0.68 mM, and 0.01 mM against l,l-dipheny1-2-picrylhydrazyl radical and 0.04mM, 0.03mM, and 0.01mM against the superoxide radical in the xanthine/xanthine oxidase system, respectively. Compound 3 suppressed the expression of MMP-1 by up to 44% at 35.0${\mu}$M and inhibited the production of interleukin 6, which is known as a cytokine that induces MMP-1 expression. In addition, the wrinkle improvement effect of the formulation with Z. marina extract was measured. As a result, remarkable reduction was found in the fine wrinkle and skin roughness after application of the cream with 3.0% this extract for 8 weeks. In conclusion, the isolated compounds from Z. marina extract were good antioxidant and suppressor of MMP-1 expression and the formulation with the extract diminished the skin wrinkle. Therefore, the extract can be used as a new anti-aging agent for application in cosmetic.

• Archives of Pharmacal Research
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• v.29 no.8
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• pp.633-644
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• 2006

In last couple of decades the use of natural compounds like flavonoids as chemopreventive agents has gained much attention. Our current study focuses on identifying chemopreventive flavonoids and their mechanism of action on human prostate cancer cells. Human prostate cancer cells (PC3), stably transfected with activator protein 1 (AP-1) luciferase reporter gene were treated with four main classes of flavonoids namely flavonols, flavones, flavonones, and isoflavones. The maximum AP-1 luciferase induction of about 3 fold over control was observed with $20\;{\mu}M$ concentrations of quercetin, chrysin and genistein and $50\;{\mu}M$ concentration of kaempferol. At higher concentrations, most of the flavonoids demonstrated inhibition of AP-1 activity. The MTS assay for cell viability at 24 h showed that even at a very high concentration $(500\;{\mu}M)$, cell death was minimal for most of the flavonoids. To determine the role of MAPK pathway in the induction of AP-1 by flavonoids, Western blot of phospho MAPK proteins was performed. Four out of the eight flavonoids namely kaempferol, apigenin, genistein and naringenin were used for the Western Blot analysis. Induction of phospho-JNK and phospho-ERK activity was observed after two hour incubation of PC3-AP1 cells with flavonoids. However no induction of phospho-p38 activity was observed. Furthermore, pretreating the cells with specific inhibitors of JNK reduced the AP-1 luciferase activity that was induced by genistein while pretreatment with MEK inhibitor reduced the AP-1 luciferase activity induced by kaempferol. The pharmacological inhibitors did not affect the AP-1 luciferase activity induced by apigenin and naringenin. These results suggest the possible involvement of JNK pathway in genistein induced AP-1 activity while the ERK pathway seems to play an important role in kaempferol induced AP-1 activity.