• Archives of Pharmacal Research
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• v.18 no.2
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• pp.65-68
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• 1995

The methanol extract from the whole parts of the flowers of Chrysanthemum boreals was found to exhibit a significant inhibition of a rat lens aldose reductase (RLAR) activity in vitro. Bioassay guided systematic fractionation of the methanol extract led to the isolation of four flavonoids which were identified as acacetin (1), apigenin (II), luteolin (III) and linarin (IV). Compounds I-III were demonstrated to exhibit a significant inhibition of RLAR. Luteolin (II) was found to be the most potent AR inhibitor with $IC_{50}$ value of $5{\times}10^{-7}M$.

• Archives of Pharmacal Research
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• v.29 no.7
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• pp.582-586
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• 2006

Due to consumer reluctance to take synthetic drugs for nematode infections and the appearance of resistance to anthelminthic drugs, new drugs from natural products must be developed. Caenorhabditis elegans is one of the freely living nematodes and serves as a good model system for screening anthelminthic drugs. In this study, thirteen flavonoid derivatives were tested for anthelminthic activity and the relationships between their activities and structures were investigated. The structural information combined with the data for the larval growth inhibition of C. elegans provided meaningful structural insights in the search for new anthelminthic drugs.

• Natural Product Sciences
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• v.26 no.4
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• pp.289-294
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• 2020

Eclipta prostrata is an annual herb, belonging to Asteraceae family, and has been traditionally used to improve immunity and treat hepatitis and bacterial disease in Korea. In this study, a new coumestan glucoside (1) along with ten known compounds (2 - 11) was isolated from E. prostrata. The chemical structures of isolates were elucidated to be wedelolactone-9-O-β-D-glucopyranoside (1), wedelolactone (2), demethylwedelolactone (3), apigenin (4), apigenin-7-sulfate (5), luteolin (6), luteolin-7-sulfate (7), luteolin-7-O-β-D-glucopyranoside (8), pratensein-7-O-β-D-glucopyranoside (9), 3,4-di-O-caffeoylquinic acid (10) and 3,5-di-O-caffeoylquinic acid (11) based on the spectroscopic evidence.

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.142.1-142.1
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• 2001

• Food Science and Biotechnology
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• v.17 no.6
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• pp.1361-1364
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• 2008

The inhibitory effects of naringenin, kaempherol, and apigenin on the production of cholesterol in HepG2 KCLB 88065 and MCF-7 KCLB 30022 cells were evaluated. In this study, quercetin was used as a reference reagent. After incubation for 3 days, fat-soluble contents of both cell types were extracted by using the Folch method and the cholesterol contents in both cultured cells were determined by high performance liquid chromatography. The concentration of cholesterol in untreated each tissue cells was $12.2{\pm}0.11$ and $8.83{\pm}0.12\;mg/g$ of lipid, respectively. The total concentration of each flavonoid was adjusted to 0, 35, or $350{\mu}M$ in the culture broth. As the results, the addition of 2% methanol and dimethyl sulfoxide (DMSO) to the media (control for flavonoid solvents) did not significantly affect cell growth; however, DMSO caused an increase in the production of cholesterol. Each flavonoid inhibited the production of cholesterol in both HepG2 and MCF-7 cells at the concentration of $35{\mu}M$ above. In addition, the inhibitory effect of kaempherol on the production of cholesterol in these cells was greater than the other flavonoids tested and HepG2 cells are more sensitive to flavonoids than MCF-7. From the results, the inhibitory effects of flavonoids on cholesterol production are different depending on the cell type.

• Natural Product Sciences
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• v.26 no.4
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• pp.326-333
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• 2020

The aerial parts of Eclipta prostrata is used as a traditional medicine and vegetable. In traditional folk medicine, it is used for treatment of hemorrhages, hepatic, disease, renal injuries, hair loss, tooth mobility, and viper bites. In this study, ten compounds (1 - 10) were isolated from the aerial parts of E. prostrata. A reliable high performance liquid chromatography equipped with photometric diode array detector (HPLC-PDA) method was developed to simultaneously quantitate 10 marker compounds [chlorogenic acid (1), paratensein 7-O-��-ᴅ-glucoside (2), quercetin 7-O-��-ᴅ-glucoside (3), luteolin 7-O-��-ᴅ-glucoside (4), apigenin 7-O-��-ᴅ-glucoside (5), apigenin 4'-O-��-ᴅ-glucoside (6), apigenin (7), luteolin (8), wedelolactone (9), and paratensein (10)]. In addition, compounds 5 and 6 showed considerable inhibitory effects against protein-tyrosine phosphatase 1B (PTP1B) enzyme. Moreover, compounds 6 - 8, and 10 exhibited potent α-glucosidase inhibitory effects with IC50 values of 24.5 ± 1.9, 33.0 ± 0.5, 45.5 ± 0.1, and 23.8 ± 1.0 µM, respectively. All compounds (1 - 10) showed considerable acetylcholinesterase (AChE) inhibitory effects with IC50 ranging from 30.1 to 75.2 µM.

• Journal of the Korean Society of Food Science and Nutrition
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• v.31 no.6
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• pp.1134-1141
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• 2002

Adhesion of leukocytes to the activated vascular endothelium and their subsequent recruitment/migration into the artery wall are key features in the pathogenesis of atherosclerosis and inflammatory diseases. These features have been mediated by cell adhesion molecules including vascular cell adhesion molecule-1 (VCAM-1) and in tracellular cell adhesion molecule-1 (ICAM-1). This study examined whether flavonoids inhibit the pro-inflammatory cytokine TNF-$\alpha$-induced monocyte adhesion via a modulation of the protein expression of VCAM-1 and ICAM-1 of human umbilical vein endothelial cells (HUVECs). TNF-$\alpha$ markedly increased the adhesion of THP-1 monocytes to endothelial cells and induced the expression of VCAM-1, ICAM-1 and E-selectin proteins in HUVECs. Micromolar concentrations of the flavones luteolin and apigenin and the flavonol quercetin near completely blocked the monocyte adhesion to the activated endothelial cells and the induction of these adhesion molecules. However, equimicromolar catechins of (-)epigallocatechin gallate and (+)catechin, the flavonol myr- icetin and the flavanones of naringin and hesperidin had no effect on TNF-$\alpha$-activated monocyte adhesion. (-)Epigallocatechin gallate, (+) catechin, and naringin did not attenuate the TNF-$\alpha$ induction of these adhesion molecules. Furthermore, culture with luteolin and apigenin strongly blocked the expression of TNF-$\alpha$-induced VCAM-1 mRNA and modestly attenuated ICAM-1 mRNA. Quercetin modestly decreased the TNF-$\alpha$-activated VCAM-1 and ICAM-1 mRNAs. These results demonstrate that flavonoids classified as flavones and flavonols may inhibit monocyte adhesion to the TNF-$\alpha$-activated endothelium, most likely due to a blockade of expression of functional adhesion molecules down-regulated at the transcriptional level, indicating a definite linkage between the chemical structure of flavonoids and the expression of cell adhesion molecules. Furthermore, the antiathero-genic feature of flavonoids appears to be independent of their antioxidant activity.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.2
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• pp.117-127
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• 2008

In this study, the antioxidative effects, inhibitory effects on elastase, and components of Cayratia japonica extracts were investigated. The free radical(1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activities($FSC_{50}$) of extract/fractions of Cayratia japonica were in the order: 50% ethanol extract(114.3 ${\mu}g/mL$)${\mu}g/mL$)${\mu}g/mL$). Reactive oxygen species(ROS) scavenging activities($OSC_{50}$) of some Cayratia japonica extracts in $Fe^{3+}-EDTA/H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The order of ROS scavenging activities were deglycosylated flavonoid aglycone fraction($OSC_{50},\;3.30{\mu}g/mL$)<50% ethanol extract(1.21 ${\mu}g/mL$)${\mu}g/mL$). Ethyl acetate fraction showed the most prominent scavenging activity. The protective effects of extract/fractions of Cayratia japonica on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The Cayratia japonica extracts suppressed photohemolysis in a concentration dependent manner($1{\sim}25{\mu}g/mL$), particularly deglycosylated flavonoid aglycone fraction exhibited the most prominent celluar protective effect(${\tau}_{50}$, 175.05min at 25 ${\mu}g/mL$). Aglycone fractions obtained from the deglycosylation reaction of ethyl acetate fraction among the Cayratia japonica extracts, showed 2 bands in TLC and 2 peaks in HPLC experiments(360 nm). Two components were identified as luteolin(composition ratio, 47.50%), apigenin(52.50). TLC chromatogram of ethyl acetate fraction of Cayratia japonica extract revealed 3 bands and HPLC chromatogram showed 4 peaks, which were identified as luteolin-7-O-${\beta}$-D-glucopyranoside(composition ratio, 11.14%), apigenin-7-O-${\beta}$-D-glucuronopyranoside(15.38%), luteolin(23.55%) and apigenin(49.92%) in the order of elution time. The inhibitory effect of aglycone fraction on elastase($IC_{50},\;70.5{\mu}g/mL$) was very high. These results indicate that extract/fractions of Cayratia japonica can function as antioxidants in biological systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS. And component analysis of Cayratia japonica extract and antioxidative effects could be applicable to new cosmetics.

• Korean Journal of Food Science and Technology
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• v.44 no.6
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• pp.750-758
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• 2012

This study investigated flavonoid, total phenol, total flavonoid content, antioxidant and antiproliferative activity on human breast cancer cells (MCF-7, MDA-MB-231). Four varieties of Korean green peppers (KP: kkuri pepper, PP: phut pepper, CP: cheongyang pepper, OP: ohi pepper) and one foreign green pepper (JP: jalapeno) were used. The contents of luteolin, quercetin and apigenin, which are abundant flavonoids in green pepper, were the highest in KP. Also, the contents of total phenol, and total flavonoids were the highest in KP, followed by CP, JP, PP, and OP (KP: total phenol $13.29{\pm}0.45$ mg GAE/g D.W., total flavonoid $7.02{\pm}0.13$ mg QE/g D.W. In DPPH ABTS radical-scavenging activity, KP showed the most potent antioxidant activity. In the result of viability in human breast cancer cells, KP had the highest antiproliferative effect. These results suggest that green peppers have significant antioxidant activity and can be a possible candidate for treatment of breast cancer.

• Applied Biological Chemistry
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• v.48 no.4
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• pp.418-420
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• 2005

In order to search for biologically active compounds from edible plant sources, the aerial parts of Sajabalssuk (Artemisia herba) were extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH and $H_2O$, successively. From the EtOAc fraction, four compounds were isolated through the repeated silica gel and ODS column chromatographies. From the results of physico-chemical data including NMR, MS and IR, the chemical structures of the compounds were determined as eupatilin (1), jaceosidin (2), apigenin (3) and eupafolin (4). Among them, compounds 3 and 4 were isolated for the first time from Sajabalssuk (Artemisia herba).