• Journal of Life Science
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• v.28 no.10
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• pp.1186-1192
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• 2018

The purpose of this study was to compare the effects of either aerobic exercise or polyphenols supplementation on mRNA expression of endoplasmic reticulum stress in skeletal muscle of high fat diet-induced obese mice. In the study, mice were divided into five groups: (1) NC (normal diet for 16 weeks as a control, n=10), (2) HC (high fat diet for 16 weeks as a control, n=10), (3) H-Re (high fat diet with resveratrol 25 mg/kg supplementation for 16 weeks, n=10), (4) H-Ch (high fat diet with chrysin 50 mg/kg supplementation for 16 weeks, n=10), and (5) HE (high fat diet with aerobic exercise for 16 weeks, n=10). Aerobic exercise was performed on a treadmill for 40~60 min/day at 10~14 m/min, 0% grade, four days/week for 16 weeks. Endoplasmic reticulum stress related genes were measured by real-time polymerase chain reaction. ATF6, PERK, $IRE1{\alpha}$, and BIP/GRP78 mRNA were significantly decreased in HE compared with those in HC (p<0.05). Also, ATF6, $IRE1{\alpha}$, and BIP/GRP78 mRNA were significantly decreased in H-Re compared with those in HC (p<0.05). ATF6 mRNA was significantly decreased in H-Ch compared with that in HC (p<0.05). These findings suggest that aerobic exercise, resveratrol, and chrysin supplementation changed ER stress markers. However, aerobic exercise was most effective on ameliorating the high fat diet induced ER stress markers. Thus, it seems that aerobic exercise might have a more positive effect on skeletal muscle endoplasmic reticulum stress compared with polyphenol supplementation in high fat diet-induced obese mice.

• Korean Journal of Food Science and Technology
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• v.34 no.4
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• pp.546-551
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• 2002

Nutritional composition and phenolic compounds of raw propolis collected from falseacacia (Robinia pseudoacacia L.) and chestnut tree (Castanea crenata), and their 70% ethanol extracts of propolis (EEP) were analyzed. Propolis had high crude lipid content, but no significant differences in general compositions in terms of collection area and plant origins. Mineral contents varied greatly depending on the plant origins, with falseacacia propolis showing the highest mineral content. Sixteen amino acids were analyzed, among which aspartic acid content was the highest at $328.4{\sim}410.6\;mg%$ and methionine the lowest at $0{\sim}21.1\;mg%$. Extraction yield for EEP was relatively high at $64.2{\sim}81.9%$, and total polyphenol and flavonoid contents were $13.9{\sim}23.7$ and $8.6{\sim}10.8%$, respectively. HPTLC and HPLC analysis on the phenolic compounds revealed the overall chromatographic patterns were almost equal, showing similar polyphenol compositions between the propolis. About 16 peaks were identified by HPLC analysis, among which 6 peaks of p-hydroxy benzoic acid, caffeic acid, ferulic acid, benzoic acid, cinnamic acid, and chrysin were identified.

• Korean Journal of Pharmacognosy
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• v.30 no.1
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• pp.34-39
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• 1999

To search for less toxic antiherpetic agents, the inhibitory effects of twelve kinds of flavonoids including chrysin, quercetin, quercitrin, rutin, fisetin, gossypin, kaempferol, morin, naringenin, naringin, hesperetin and hesperidin on the plaque formation of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in Vero cells were examined by plaque reduction assay in vitro. Some flavonoids tested in this study showed potent antiherpetic activity, reducing intracellular replication of herpes simplex viruses when Vero cell monolayers were infected and subsequently cultured in medium containing flavonoids. Naringenin showed the most potent antiviral activity against HSV-1 with selectivity index (SI) of 19.1 and hesperetin showed the most potent antiviral activity against HSV-2 with SI of 9.8. These results suggest that some flavonoids may be a potential therapeutic agent for the treatment and prevention of herpes simplex virus infections.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.128-128
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• 1995

To investigate the mechanism of the regulation of cytochrome P450IA1 gene expression, ethoxyresorufin deethylase(EROD) and benzo(a)pyrene hydroxylase in B6 mouse liver, in isolated perfused rat liver system. and in B6 mouse hepatocyte Hepa-I cells were examined. In C57BL/6N mouse, 3-methylcholan- throne( 3MC ) treatment have resulted in the stimulation of EROD activity based on fluorometry by 2.79 fold comparirng with that of control. Measurement of mRNA of cytochrome P450 was carried out by either nothern blot or dot blot analysis. Findings are similar to that of studies with enzymes. Furhtermore, when RTPCR method was applied to detect mRNA in Hepa I cell and liver tissues the results were more clear. Cytochrome P450IA1 upstream DNA containing CAT construct was transfected into Hepa-1 cells. After transfection of CAT construct, 3MC and flavonoids, such as, chrysin, hesperetin, kaempferol, morin, myricetin and aminoyrine were treated. 48 Hours after treatments, cells were harvested and assayed for CAT mRNA by RTPCR. 3MC treatment to hepa I cells transfected with trout P450IA1-CAT construct increased CAT mRNA by 2.81 fold when it was compared with that of control. This increase CAT mRNA was decreased by concomitantly treated flavonoids and aminopyrine. The level of CAT protein was 29.2-58.0% of 3MC stimulated CAT protein. Results of this study suggested that RTPCR seems to be a very good method to study regulation of gene expression in liver tissue or Hepa cells.

• Archives of Pharmacal Research
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• v.17 no.2
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• pp.71-75
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• 1994

The antimutagenic effects of 27 kinds of plant flavonoids on the mutagenicity of aflatoxin $B_1(AFB_1)$ and N-methyl-N'-nitro-N-nitrosoguanidine(MANG) in Salmonella typhimurium TA 100 were investigated. In the mixed applications of $AFB_1\;(1\;\mu{g/plate)}$ with the flavonoids $(300\;\mu{g/plate)}$ in the presence of a mammalian metabolic activation system (S9 mix), chrysin, apigenin, luteolin and its glucoside, kaempferol, fisetin, morin, naringenin, hesperetin, persicogenin, (+)-catechin and (-)epicatechin showed the antimutagenic effect against $AFB_1$ with more than 70% inhibition rate. A little or no antimutagenicities except flavone against MNNG $(0.5\;\mu{g/plate)}$ were observed. For the antimutagencity of the flavonoids on $AFB_1$, the flavonoid structure that contains the free 5, 7-hydroxyl gorup seemed to be essential. However, saturation of the 2, 3-double bond of elimination of the 4-keto group did not affect the activity.

• 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.

• Bulletin of the Korean Chemical Society
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• v.29 no.3
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• pp.590-594
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• 2008

The inclusion complexes of cyclodextrins (CDs) with flavones in aqueous solution were investigated by phase solubility measurements. The effect of b -cyclodextrin (b -CD), heptakis (2,6-di-O-methyl) b -cyclodextrin (DM-b -CD) and 2-hydroxypropyl-b -cyclodextrin (HP-b -CD) on the aqueous solubility of three flavones, namely, chrysin, apigenin and luteolin was investigated, respectively. Solubility enhancements of all flavones obtained with three CDs followed the rank order: HP-b -CD > DM-b -CD > b -CD, and besides, CDs show higher stability constant on luteolin than that on others flavones. 1H-nuclear magnetic resonance (NMR) spectroscopy and molecular modeling was used to help establish the model of interaction of the CDs with luteolin. NMR spectroscopic analysis suggested that A-C ring, and part of the B ring of luteolin display favorable interaction with the CDs, which was also confirmed by docking studies based on the molecular simulation. The observed augmentation of solubility of luteolin by three CDs was explained by the difference of electrostatic interaction of each complex, especially hydrogen bonding.

• Archives of Pharmacal Research
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• v.28 no.11
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• pp.1293-1301
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• 2005

Flavonoids, a group of low molecular weight phenylbenzopyrones, have various pharmacological properties including antioxidant, anticancer, bactericidal, and anti-inflammatory. We carried out anti-herpetic assays on 18 flavonoids in five classes and a virus-induced cytopathic effect (CPE) inhibitory assay, plaque reduction assay, and yield reduction assay were performed. When flavonoids were applied at various concentrations to Vero cells infected by HSV-1 and 2, most of the f1avonoids showed inhibitory effects on virus-induced CPE. Among the flavonoids, EC, ECG (flavanols), genistein (isoflavone), naringenin (flavanone), and quercetin (flavonol) showed a high level of CPE inhibitory activity. The antiviral activity of flavonoids were also examined by a plaque reduction assay. EC, ECG, galangin, and kaempferol showed a strong antiviral activity, and catechin, EGC, EGCG, naringenin, chrysin, baicalin, fisetin, myricetin, quercetin, and genistein showed moderate inhibitory effects against HSV-1. In these experiments, flavanols and flavonols appeared to be more active than flavones. Furthermore, treatment of Vero cells with ECG and galangin (which previously showed strong antiviral activities) before virus adsorption led to a slight enhancement of inhibition as determined by a yield reduction assay, indicating that an intracellular effect may also be involved.

• YAKHAK HOEJI
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• v.51 no.1
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• pp.68-74
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• 2007

Scutellaria Radix, the dried roots of Scutellaria baicalensis Georgi (Labiatae), has been used in oriental traditional medicine for treatment of fever urine disorder, diarrhea, inflammation. Present study was carried out for the gastroprotective effect of chrysin, baicalein, baicalin, wogonin from Scutellaria baicalensis. This reports evaluated antioxidant effect, antibacterial activity against Helicobacter pylori and HCI-ethanol-induced gastric lesion in rats and showed the significant effectiveness. It may be regarded that the antigastritic effects and antibacterial activity of baicalin, baicalein from Scutellaria baicalensis are originated from acid-neutralizing capacity, free radical scavenging effects and the antibacterial activity against Helicobacter pylori.

• YAKHAK HOEJI
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• v.34 no.5
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• pp.348-364
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• 1990

The activities of twenty-one flavonoids and their related compounds on the hypersensitivity reaction against various antigens were studied in vitro and in vivo. 1. Generally flavonoids inhibited significantly the homologous passive cutaneous anaphylaxis (PCA) induced by reaginic antibody as compared as anaphylaxis by compound 48/80-induced mast cell degranulation, and so more strongly active in the IgE-mediated anaphylaxis than non-IgE-mediated anaphylaxis. 2. Flavonids inhibited remarkably Arths reaction, hemolysin titer, delayed hypersensitivity, haemagglutinin titer, rosette forming cells and plague forming cells against sheep red blood cells, and so it exhibited that flavonoids inhibited type 2, 3 and 4 hypersensitivity. 3. Quercetin, kaempferol, hesperetin, disodium cromoglycate, malvin and baicalein were active dose-dependently in the all types of hypersensitivity. Fisetin, daidzein, morin, narigin, flavone, catechin, rutin, hesperidin, neophsperidin, apigenin and chrysin were significantly active in the various types of hypersensitivity, but apigenin, rutin and catechin were less active in the delayed hypersensitivity. Taxifolin was significantly active in PCA and histamine-induced anaphylaxis except other types of hypersensitivity. Rotenone and cyanin also inhibited all types of hypersensitivity, but they are toxic. 4. Based on these results from hypersensitivity, the following flavonoid structure-activity relationships became apparent. 1) Flavonoids with $C_{2-3}$ double bond in C-ring were more active than that of $C_{2-3}$ saturation. 2) Flavonoids with $C_4$ ketone group in C-ring were more active than abscence of them except catechin and malvin. 3) Flavonoids with benzene ring at positions 2 or 3 in C-ring exhibited same activities. 4) Flavonoids with opening of the C-ring does not abolish their activities. 5) The glycosylated flavonoids in position 3 or 7 was less active than their aglycone. 6) Flavonoids with the more hydroxy group in A and B-ring were more active. 7) Flavonoids with or without $C_3-OH$ did not change their activities.