• Journal of Applied Biological Chemistry
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• v.66
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• pp.122-127
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• 2023

Cardiovascular disease (CVD) is increasingly increasing as the main cause of death worldwide, and activation of platelet in vascular damage is one of the important causes of CVD. In recent, there is a growing interest in anti-thrombotic materials through platelet suppression, and efforts are being made to reduce side effects by using natural bioactive compounds. Known as one of the Flavonoids, hydroxygenkwanin (HGK) is a purified substance in Daphne Genkwa, which is known to have antibacterial, anti-inflammatory and anti-cancer effects, and has been reported to serve as an inhibitor of tissue factor that prevents thrombosis, but its anti-platelet effects and the action mechanisms is not known. In this study, we confirmed that the effects of HGK on the collagen-induced human platelets activation. HGK suppressed phosphorylation of PI3K/AKT and mitogen-activated protein kinases during platelet signaling, and reduced granule secretion in platelets such as ATP and serotonin. In addition, HGK inhibited the phosphorylation of cPLA₂ and strongly undermined the production of TXA₂, which is a powerful aggregation amplifier. As a result, the platelet aggregation derived by Collagen, a cohesive induced substance, was strongly suppressed by HGK to an IC₅₀ of 86.36 µM. Therefore, HGK might be worth the antithrombotic substance that inhibits the activation and aggregation of human platelets that occur through blood vessel damage.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.503-511
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• 2023

The aim of this study was to investigate in vitro antioxidant activities of defatted Camellia japonica L. seeds (DCJS). The DCJS were extracted using ethanol and then fractionated with butanol (BuOH), ethyl acetate (EtOAc), chloroform, and hexane. To evaluate antioxidant activity of extract and fractions from DCJS, we investigated free radical scavenging activities such as 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS⁺), hydroxyl radical (^•OH), and superoxide anion (O₂^-) radicals. The five extract and fractions of DCJS dose-dependently increased DPPH, ABTS⁺ and O₂^- radical scavenging activities. The BuOH fraction of DCJS showed the highest free radical scavenging activities among other extract and fractions. The contents of total polyphenol and flavonoid in BuOH fraction of DCJS were 23.26 mg GAE/g and 32.39 mg QE/g, respectively. The polyphenol and flavonoids contents of BuOH fraction has highest than other extract and fractions. In addition, BuOH and EtOAc fraction of DCJS contained 102.37 and 165.05 ㎍/g of camelliaside B, respectively. Therefore, DCJS has higher antioxidant activity and may be useful as a natural antioxidant material.

• Journal of Life Science
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• v.24 no.11
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• pp.1157-1167
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• 2014

In order to compare the anti-inflammatory effects of five selected cereal grains-proso millet, hwanggeumchal sorghum, foxtail millet, barnyard millet, and adlay-the inhibitory activities of 80% ethanol (EtOH) extracts obtained from the individual grains on lipopolysaccharide (LPS)-induced nitric oxide (NO) generation were investigated in RAW264.7 cells. The EtOH extract of barnyard millet (Echinochloa crus-galli var. frumentacea) grains exhibited more potent anti-inflammatory activity than that of the other grains. When the EtOH extract of barnyard millet grains was sequentially fractionated with n-hexane, methylene chloride (MC), ethyl acetate (EtOAc), and n-butanol, the majority of the anti-inflammatory activity was detected in the MC fraction, followed by the EtOAc fraction. Pretreatment with the MC fraction caused downregulation of the expression levels of iNOS- and COX-2-specific transcripts and proteins, as well as proinflammatory cytokine gene transcripts (IL-$1{\beta}$, IL-6, and TNF-${\alpha}$) in LPS-stimulated RAW264.7 cells. Additionally, the MC fraction could suppress not only the LPS-induced nuclear translocation of cytosolic NF-kB, but also the LPS-induced activation of MAPKs, such as ERK, JNK, and p38MAPK. Further analysis of the MC fraction by HPLC identified kaempferol, biochanin A, and formononetin as the major phenolic components. Both kaempferol and biochanin A, but not formononetin, could exert anti-inflammatory effect at the same concentrations as those of the MC fraction. Consequently, these results indicate that kaempferol and biochanin A are among the most effective anti-inflammatory phenolic components in barnyard millet grains. This finding suggests that barnyard millet grains and the MC extract enriched in kaempferol and biochanin A could be beneficial functional food sources that have an anti-inflammatory effect.

• Food Science and Preservation
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• v.15 no.6
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• pp.891-896
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• 2008

Total phenolics and flavonoids, and the antioxidant capacity of plum cultivar wines (Prunus salicina L. cv. Soldam and P. salicina L. cv. Formosa) were determined using spectrophotometric methods. The total phenolic and flavanoid contents of Soldam wine were $478.4\;{\pm}\;5.6\;mg$ GAE and $202.4\;{\pm}\;7.5\;mg$ CE per L,respectively, and in Formosa wine were $200.6\;{\pm}\;7.5\;mg$ GAE and $64.4\;{\pm}\;6.8\;mg$ CE per L, respectively. Neutral and acidic phenolics in Soldam wine were extracted with ethyl acetate and 0.01 N HCl, respectively. In the 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging assay, neutral phenolics (64.5 EDA%) had $3{\sim}4$ times higher antioxidant activity than acidic phenolics (21.5 EDA%) and other related phenolic compounds such as chlorogenic acid (15.5 EDA%) and quercetin (24.6 EDA%) at a concentration of $100\;{\mu}g/mL$. The antiviral activities of neutral and acidic phenolics in Soldam wine were investigated in vitro using a virus-induced cytopathic effect (CPE) inhibition assay. Results showed that neutral and acidic phenolics at concentrations of $100\;{\mu}g/mL$ inhibited porcine epidemic diarrhea virus (PEDV) replication at rates of 78.12% and 58.37%, respectively. The inhibition rate of 10 g/mL neutral phenolics (69.42%) was higher than that of ribavirin as an antiviral reagent (57.86%). At concentrations of $100\;{\mu}g/mL$ or less, neutral and acidic phenolics of Soldam wine had no cytotoxic effect against vero cells.

• Journal of Nutrition and Health
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• v.47 no.6
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• pp.394-402
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• 2014

Purpose: Dendropanax morifera Leveille (DML) exhibits diverse biological and pharmacological activities, including anti-oxidative effect, anti-cancer activity, hepatoprotection, immunological stimulation, and bone regeneration. As part of the identification for novel functions of DML, we investigated the therapeutic effects of DML on diabetes induced by streptozotocine (STZ) treatment. Methods: First, the four extracts including the water extract of leaf (DLW), the ethanol extract of leaf (DLE), the water extract of stem (DSW), and the ethanol extract of stem (DSE) were collected from the leaf and stem of DML using a hot water and ethanol solvent. Alterations in body weight, glucose concentration, insulin level, and pancreatic islet structure were investigated in diabetic mice after treatment with extracts of DML for 2 weeks. Results: Among four extracts, the highest level of total polyphenols and total flavonoids was detected in DLW, while the lowest level of these was measured in DSE. The radical scavenging activity was also higher in DLW than in the other three extracts at the concentration of $25-100{\mu}g/mL$, although this activity was maintained at a constant level in all groups at the concentration of $500{\mu}g/mL$. Based on the results of anti-oxidant activity, DLW and DLE were selected for examination of anti-diabetic effects in a diabetes model. Body weight was gradually decreased in all STZ treated groups compared with the No treated group. However, four STZ/DML treated groups maintained a high level of body weight during 7-14 days, while the STZ/vehicle treated group showed a gradual decrease of body weight during the same period. Also, a significant decrease or increase in the concentration of glucose and insulin in the blood of the diabetes model was detected in a subset of groups, although the highest increase was detected in the STZ/DLE-200 treated group. In addition, the histological structure of pancreatic islet was significantly recovered after treatment with DLW and DLE. Conclusion: These results suggest that DLW and DLE may contribute to attenuation of clinical symptoms of diabetes as well as prevent the destruction of pancreatic ${\beta}$-cells in STZ-induced diabetes mice.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.10
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• pp.1439-1449
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• 2015

Prunus persica Flos (PPF) were investigated for their antioxidant and anti-inflammatory activities to find a natural functional food resource preventing degenerative diseases associated with excessive oxidative stress and chronic inflammation. PPF was extracted using ethanol (EtOH) and then sequentially fractioned by hexane (Hx), dichloromethane (DM), ethyl acetate (EA), n-butanol (BtOH), and water (DW). Contents of total phenolics and flavonoids, as well as 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activities were measured. Anti-inflammatory effects in terms of nitric oxide (NO), prostaglandin (PG) E2, and pro-inflammatory cytokines such as interleukin (IL)-6 and tumor necrosis factor (TNF)-${\alpha}$ production were also measured using LPS-treated RAW 264.7 macrophages. EtOH extract showed relatively high antioxidant activity with high total phenolic (78.1 mg tannic acid/g) and flavonoid contents (55.3 mg rutin/g). EA fraction contained the highest total phenolic and flavonoid contents (394.6 mg tannic acid/g, 253.7 mg rutin/g), followed by BtOH (128.3 mg tannic acid/g, 93.1 mg rutin/g). EA and BtOH fractions and EtOH extract showed higher DPPH radical and ABTS radical scavenging activities than the others (P<0.05). In LPS-treated RAW 264.7 macrophages, EtOH extract ($200{\mu}g/mL$) showed significantly reduced (P<0.05) NO, PGE2, and TNF-${\alpha}$ production levels to 38.5%, 32.3%, and 48.9% of the control, respectively, as well as reduced iNOS and COX-2 protein expression. DM fraction ($50{\mu}g/mL$) showed significantly reduced (P<0.05) NO, PGE2, IL-6, and TNF-${\alpha}$ production levels to 43.5%, 13.3%, 38.7%, and 41.3% of the control, respectively, and EA fraction ($50{\mu}g/mL$) showed significantly reduced NO, PGE2, IL-6, and TNF-${\alpha}$ production levels to 44.8%, 22.4%, 45.7%, and 62.0% of the control, respectively. Taken together, EtOH extract of PPF showed potent antioxidant and anti-inflammatory activities, and EA and BtOH fractions showed comparatively stronger antioxidant activities while DM and EA fractions showed stronger anti-inflammatory activities. It can be concluded that EtOH extract of PPF and its fractions are good candidates as natural resources for the development of anti-oxidative and anti-inflammatory functional food products.

• Food Science and Preservation
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• v.22 no.2
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• pp.275-280
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• 2015

Among the naturally occurring antioxidants, polyphenols are widely distributed in various fruits, vegetables, wines, juices, and plant-based dietary sources and divided into several subclasses that included phenolic acid, flavonoids, stilbenes, and lignans. As part of our continuing search for bioactive food ingredients, the antioxidant and ${\alpha}$-glucosidase inhibitory activities of the aqueous ethanolic extract from the aerial parts of Ainsliaea acerifolia were investigated in vitro. The antioxidant properties were evaluated via radical scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) ($ABTS^+$) radicals. In addition, the anti-diabetic effect of A. acerifolia extracts was tested via ${\alpha}$-glucosidase inhibitory assay. Furthermore, the total phenolic contents were determined using a spectrophotometric method. All the tested samples showed dose-dependent radical scavenging and ${\alpha}$-glucosidase inhibitory activities. In particularly, the ${\alpha}$-glucosidase inhibitory and radical scavenging properties of the ethyl acetate (EtOAc)-soluble portion from the aerial parts of the A. acerifolia were higher than those of the other solvent-soluble portions. These results suggest that A. acerifolia could be considered a new potential source of natural antioxidants and antidiabetic ingredients. More systematic investigation of the aerial parts of A. acerifolia will be performed for the further development of anti-oxidative and antidiabetic drugs.

• Journal of Life Science
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• v.28 no.9
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• pp.1048-1055
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• 2018

In the current study, comparisons of Oenothera Biennis seed extracts with water, ethanol, methanol, and 70% ethanol in their total polyphenolics contents, anti-oxidant, anti-neurotoxicity, anti-cancer, and immune-modulatory activities were investigated. Compared with other extracts, those concentrations of total phenolics and flavonoids were the highest in MeOH extract (31.90 mg GAE/g and 20.66 mg QE/g). The radical scavenging and reducing power activities were dose-dependently increased by treatment of O. Biennis seed water, EtOH, MeOH, and 70% EtOH extracts. Furthermore, pretreatment of water, EtOH, and MeOH extracts significantly reduced glutamate-induced cytotoxicity in HT22 hipocampal neuron cells. In the case of cancer cells, MeOH extracts showed lower $IC_{50}$ values in HepG2 ($74.21{\mu}g/ml$), A549 ($188.24{\mu}g/ml$), MCF-7 ($186.42{\mu}g/ml$), and B16 ($101.80{\mu}g/ml$) than other extracts, where those water ($101.96{\mu}g/ml$) and EtOH ($788.39{\mu}g/ml$) extracts showed the lowest $IC_{50}$ activity in HT-29 and PC-3 cells, respectively. O. Biennis seed extracts did not show any cytotoxicity in RAW 264.7 macrophages at the concentration of $1-10{\mu}g/ml$, whereas 70% EtOH extract dose-dependently enhanced nitric oxide (NO) production in RAW 264.7 cells. Overall, we evaluated that various bioactive potentials of O. Biennis seed extracts which would relate with phenolic compounds abundance, thus these can be useful to future developments as functional food ingredients and natural medicines.

• Applied Chemistry for Engineering
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• v.28 no.4
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• pp.479-484
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• 2017

In this study, antioxidative activities and cellular protective effects of 70% ethanol extracts and fractions from lavender were evaluated. The scavenging activity ($FSC_{50}$) of free radical (1,1-phenyl-2-picrylhydrazyl, DPPH) was 46.6, 45.5 and $477.5{\mu}g/mL$ in the 70% ethanol extract, ethyl acetate fraction and aglycone fraction, respectively. The reactive oxygen species scavenging activities (${OSC_{50}$) of 70% ethanol extract, ethyl acetate fraction and aglycone fraction were 8.1, 3.3 and $17.6{\mu}g/mL$, respectively, and they showed lower antioxidative activity than that of using L-ascorbic acid ($1.5{\mu}g/mL$). However, the aglycone fraction showed higher photohemolysis protective effect than that of using the 70% ethanol extract and ethyl acetate fraction. At $50{\mu}M$ concentration, the cellular protective effect (${\tau}_{50}$) of 70% ethanol extract, ethyl acetate fraction and aglycone fraction from lavender was 70.6, 87.2 and 165.2 min, respectively. In particular, the lavender aglycone fraction showed 3.8 times higher cellular protective effect than that of (+)-${\alpha}$-tocopherol. The lavender fractional components including luteolin 7-O-glucuronide, vitextin, rosmarinic acid, luteolin, and apigenin were identified using TLC and LC-MS. However, the lavender aglycone fraction did not show any significant increase in flavonoids (luteolin and apigenin) compared to that of the ethyl acetate fraction. In conclusion, it is suggested that lavender may be applied as an antioxidant material in cosmetic industries.

• Journal of Nutrition and Health
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• v.53 no.2
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• pp.121-128
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• 2020

Purpose: The Rubus coreanus fruit (RF) is an important traditional medicinal herb having antioxidant, anti-inflammatory, and immunoregulatory properties. These activities are known to change dramatically, depending on maturity of the RF. It is presumed that change of functional components, such as flavonoids, tannins, phenolic acids, triterpenoids and organic acids in RF, affect the various bioactivities. This study aimed to confirm changes in the anti-melanogenic effects of RF based on maturity, and to identify the bioactive compounds responsible. Methods: The cell viability of mature RF (MRF) and immature RF (IRF) extracts was investigated using B16F10 cells. To compare the anti-melanogenic effect of MRF and IRF extracts, we first assessed the melanin content. High-performance liquid chromatography analysis was performed to evaluate changes in the level of ellagic acid according to maturity of the RF. In addition, tyrosinase inhibitory activity of both extracts was examined. Results: MRF and IRF extracts (50-200 ㎍/mL) do not affect the cell viability of B16F10 melanoma cells. IRF extract more effectively inhibited melanin synthesis than MRF extract. The content of ellagic acid in IRF extract was higher than that obtained in MRF extract. Furthermore, greater inhibition of tyrosinase activity was observed after exposure to IRF extract than MRF extract. A positive correlation was determined between ellagic acid content and tyrosinase inhibitory activity, and a negative correlation was obtained between ellagic acid content and melanin content. Taken together, our results indicate that ellagic acid is one of the major bioactive compounds of RF that imparts a whitening effect. Conclusion: Our results indicate that ellagic acid in MRF and IRF extracts affect the anti-melanogenesis effect through inhibition of tyrosinase activity. Therefore, the ellagic acid rich IRF has greater potential for application as a natural and functional cosmetic material.