• Toxicological Research
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• v.29 no.4
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• pp.229-234
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• 2013

Phytoestrogens exist in edible compounds commonly found in fruits or plants. For long times, phytoestrogens have been used for therapeutic treatments against human diseases, and they can be promising ingredients for future pharmacological industries. Kaempferol is a yellow compound found in grapes, broccoli and yellow fruits, which is one of flavonoid as phytoestrogens. Kaempferol has been suggested to have an antioxidant and anti-inflammatory effect. In past decades, many studies have been performed to examine anti-toxicological role(s) of kaempferol against human cancers. It has been shown that kaempferol may be involved in the regulations of cell cycle, metastasis, angiogenesis and apoptosis in various cancer cell types. Among them, there have been a few of the studies to examine a relationship between kaempferol and apoptosis. Thus, in this review, we highlight the effect(s) of kaempferol on the regulation of apoptosis in diverse cancer cell models. This could be a forecast in regard to use of kaempferol as promising treatment against human diseases.

• Biomolecules & Therapeutics
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• v.21 no.4
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• pp.258-263
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• 2013

We demonstrate herein that silibinin, a polyphenolic flavonoid compound isolated from milk thistle (Silybum marianum), inhibits LPS-induced activation of macrophages and production of nitric oxide (NO) in RAW 264.7 cells. Western blot analysis showed silibinin inhibits iNOS gene expression. RT-PCR showed that silibinin inhibits iNOS, TNF-${\alpha}$, and $IL1{\beta}$. We also showed that silibinin strongly inhibits p38 MAPK phosphorylation, whereas the ERK1/2 and JNK pathways are not inhibited. The p38 MAPK inhibitor abrogated the LPS-induced nitrite production, whereas the MEK-1 inhibitor did not affect the nitrite production. A molecular modeling study proposed a binding pose for silibinin targeting the ATP binding site of p38 MAPK (1OUK). Collectively, this series of experiments indicates that silibinin inhibits macrophage activation by blocking p38 MAPK signaling.

• Korean Journal of Pharmacognosy
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• v.25 no.1
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• pp.11-19
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• 1994

Gleditsia japonica var. koraiensis NAKAI(Leguminosae) is commonly distributed in Korea and has been used as a folk medicine in the treatment of bronchitis, neoplasm and blennorrhgia in the Orient. The aqueous acetone extract of the leaves of G. japonica was subjected to a combination of Sephadex LH-20, Cosmosil $75C_{18}-OPN$, TSK-gel Toyopearl HW 40F, Avicel cellulose, and MCI-gel CHP 20P chromatographies with various solvent systems. Twelve compounds were isolated and confirmed to be vitexin(1), isovitexin(2), orientin(3), isoorientin(4), 4-caffeoyl quinic acid(5), 5-caffeoyl quinic acid(6), 3, 5-dicaffeoyl quinic acid(7), 4, 5-dicaffeoyl quinic acid(8), caffeic acid(9), quercetin(10), isoquercitrin(11) and luteolin-7-O-glucoside(12), on the basis of chemical and spectroscopic evidences.

• YAKHAK HOEJI
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• v.55 no.3
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• pp.251-259
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• 2011

Cigarette smoke condensate (CSC) is known to be carcinogenic compound. CSC contains many organic compounds such as polycyclic aromatic hydrocarbons (PAHs), and heterocyclic amine compounds (HCAs). Reactive oxygen species (ROS) are also generated and induce oxidative DNA damage during the metabolism of CSC. The rat microsome mediated and DNA repair enzyme treated comet assays together with conventional comet assay were performed to evaluate the mechanisms of CSC genotoxicity. The organic extract of CSC induced oxidative and microsome mediated DNA damage. Vitamin C as a model antioxidant reduced DNA damage in endonuclease III treated comet assay. One of flavonoid, galangin as a CYP1A1 inhibitor, reduced DNA damage in the presence of S-9 mixture. The ethanol extracts of the mixed vegetables (BV) or the mixed fruits (BF) showed potent inhibitory effects against CSC induced DNA damage with oxidative DNA lesions and in the prescence of S-9 mixture. These results indicate that BV and BF could prevent CSC-induced cellular DNA damage by inhibiting oxidative stress and suppressing cytochrome P450 in mammalian cells.

• Journal of Applied Biological Chemistry
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• v.61 no.3
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• pp.227-232
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• 2018

Simultaneous determination of three methoxyflavones, namely, cirsimarin (1), hispidulin (2), and cirsimaritin (3) in selected Korean thistles was performed via reversed-phase high performance liquid chromatography system. Compound 1 was present in all the thistle species examined, whereas 2 and 3 were only detected in Cirsium japonicum and C. japonicum var. maackii (CJM). The concentration of compounds 1-3 in CJM varied according to the time of harvest. Plants collected in the spring (CJMS) and fall (CJMF) had the highest contents of 3 and 1, respectively. A lower content of 2 was observed in CJMF than in CJMS. This indicates that seasonal variation affects the flavonoid content of CJM. The results of this study show that CJM is an excellent source of compounds 1-3 and it can potentially be cultivated for industrial and pharmaceutical applications involving these compounds.

• YAKHAK HOEJI
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• v.54 no.1
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• pp.22-26
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• 2010

We studied the antimicrobial activities of five compounds isolated from the stems of Vitis coignetiae Pulliat and the seeds of Perilla frutescens (L.) Britton. Based on spectroscopic evidence, compounds 1 to 5 were characterized as resveratrol, $\varepsilon$-viniferin, ampelopsin E, apigenin, and luteolin, respectively. The antimicrobial activities against Gram-positive (Staphylococcus aureus) and -negative (Pseudomonas aeruginosa) bacteria and a fungus (Candida albicans) were investigated using the disc diffusion and broth dilution methods. C. albicans was not inhibited by the five compounds. Compounds 2 and 5 had significant anti-microbial activity against S. aureus, and the 50% inhibitory concentration ($IC_{50}$) of compound 2 against S. aureus was 7.2 ${\mu}M$. Compounds 4 and 5 significantly inhibited P. aeruginosa and the minimum inhibitory concentration (MIC) of compounds 2 and 5 was 0.07 and 2.0 ${\mu}M$, respectively. Compounds 2, 4, and 5 had strong anti-microbial activity against S. aureus and P. aeruginosa.

• Molecules and Cells
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• v.22 no.3
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• pp.291-299
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• 2006

Vitexin, a natural flavonoid compound identified as apigenin-8-C-${\beta}$-D-glucopyranoside, has been reported to exhibit antioxidative and anti-inflammatory properties. In this study, we investigated its effect on hypoxiainducible factor-$1{\alpha}$ (HIF-$1{\alpha}$) in rat pheochromacytoma (PC12), human osteosarcoma (HOS) and human hepatoma (HepG2) cells. Vitexin inhibited HIF-$1{\alpha}$ in PC12 cells, but not in HOS or HepG2 cells. In addition, it diminished the mRNA levels of hypoxia-inducible genes such as vascular endothelial growth factor (VEGF), smad3, aldolase A, enolase 1, and collagen type III in the PC12 cells. We found that vitexin inhibited the migration of PC12 cells as well as their invasion rates, and it also inhibited tube formation by human umbilical vein endothelium cells (HUVECs). Interestingly, vitexin inhibited the hypoxia-induced activation of c-jun N-terminal kinase (JNK), but not of extracellular-signal regulated protein kinase (ERK), implying that it acts in part via the JNK pathway. Overall, these results suggest the potential use of vitexin as a treatment for diseases such as cancer.

• Journal of Microbiology and Biotechnology
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• v.31 no.4
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• pp.630-636
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• 2021

Glabridin, a compound of the flavonoid, has shown outstanding skin-whitening and anti-aging properties, but its water insolubility limits its wide application. Therefore, glabridin liposome (GL) has been developed to improve its poor bioavailability, while there are few studies to evaluate its amelioration of UVB- induced photoaging. This study is performed to investigate the amelioration of GL against UVB- induced cutaneous photoaging. The prepared GL has a spheroidal morphology with an average diameter of 200 nm. The GL shows lower cytotoxicity than glabridin, but it has a more effective role in inhibition of melanin. Moreover, the application of GL can effectively relieve UV radiation induced erythema and leathery skin, associated with the down-regulated expression of inflammatory cytokines (TNF-α, IL-6 and IL-10). Taken together, these results demonstrate that GL has potentials as topical therapeutic agents against UVB radiation induced skin damage through inhibiting inflammation.

• Microbiology and Biotechnology Letters
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• v.49 no.2
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• pp.201-209
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• 2021

Agarwood (Aquilaria spp) has high economic value. However, essential oil production from agarwood is a time-consuming process. Additionally, agarwood leaves have not been utilized even though they contain various bioactive ingredients. In this study, agarwood leaves were fermented using Lactobacillus plantarum ATCC 8014 with or without Stevia (4, 8, and 12%; v/v). The fermented fluid was mixed with maltodextrin (15%; w/v) and subjected to spray drying (inlet temperature, 120℃; outlet temperature, 65-70℃). The contents of polyphenols, polysaccharides, saponins, and flavonoids and the viability of L. plantarum were determined. Fermentation enhanced the levels of bioactive compounds. The contents of polyphenol (69.19 ± 4.05 mg GAE/g of sample), polysaccharide (20.75 ± 0.98 mg GE/g of sample), saponin (305.23 ± 4.21 mg OAE/g of sample), and flavonoid (7.86 ± 0.72 mg QE/g of sample), and the viability of L. plantarum (8.72 ± 0.17 log CFU/ml) were markedly upregulated in the samples containing Stevia (12%; v/v). This indicated that the supplementation of Stevia during fermentation decreases the fermentation time (9 h), upregulates bioactive compound production in agarwood leaves, enhances microencapsulation during spray drying, and increases the viability of L. plantarum under simulated gastric digestion conditions.

• Journal of Microbiology and Biotechnology
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• v.32 no.4
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• pp.397-404
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• 2022

Natural killer (NK) cell activity is more attenuated in hepatocellular carcinoma (HCC) patients than normal. Hypoxic-inducible factor (HIF)-1α is highly expressed in tumors to maintain their metabolism in a hypoxic environment. The expression of HIF-1α in cancers can lead to cell growth, proliferation, invasion/metastasis and immune escape. Although apigenin, a flavonoid, is known to have various biological activities, it has not been demonstrated in NK cell immune activity in HCC cells. In this study, NK-92 cells were directly cocultured with HCC SK-Hep1 cells for 24 h to evaluate NK cell activity in HCC cells or HCC cells expressing HIF-1α by apigenin. NK cell cytotoxicity to HCC cells expressing HIF-1α was significantly increased, and NK cell-activating receptors, NKG2D, NKp30 and NKp44 were highly expressed. The activating effect of apigenin on NK cells substantially induced apoptosis in HCC cells expressing HIF-1α through high expression of CD95L on the surface of NK-92 cells. Moreover, apigenin excellently inhibited the level of TGF-β1 in a coculture of NK cells and HCC cells. In conclusion, apigenin seems to be a good compound that increases NK cell cytotoxicity to HCC cells by controlling HIF-1α expression.