• Biomolecules & Therapeutics
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• v.23 no.2
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• pp.128-133
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• 2015

Although coffee is known to have antioxidant, anti-inflammatory, and antitumor properties, there have been few reports about the effect and mechanism of coffee compounds in colorectal cancer. Heat shock proteins (HSPs) are molecular chaperones that prevent cell death. Their expression is significantly elevated in many tumors and is accompanied by increased cell proliferation, metastasis and poor response to chemotherapy. In this study, we investigated the cytotoxicity of four bioactive compounds in coffee, namely, caffeine, caffeic acid, chlorogenic acid, and kahweol, in HT-29 human colon adenocarcinoma cells. Only kahweol showed significant cytotoxicity. Specifically, kahweol increased the expression of caspase-3, a pro-apoptotic factor, and decreased the expression of anti-apoptotic factors, such as Bcl-2 and phosphorylated Akt. In addition, kahweol significantly attenuated the expression of HSP70. Inhibition of HSP70 activity with triptolide increased kahweol-induced cytotoxicity. In contrast, overexpression of HSP70 significantly reduced kahweol-induced cell death. Taken together, these results demonstrate that kahweol inhibits colorectal tumor cell growth by promoting apoptosis and suppressing HSP70 expression.

• Journal of Korean Medicine Rehabilitation
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• v.19 no.2
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• pp.89-102
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• 2009

Objectives : This study was carried out to understand the immunity responses and anti-oxidation effect of the Gamidaeganghwal-tang(GDT) on rheumatoid arthritis by using the THP-1 cells and the serum of CIA mice. Methods : For this purpose, GDT was orally administerd to mice with rheumatoid arthritis induced by collagen II. To investigate the immunity responses, value of cytokine and gene expression in the THP-1 cell, levels of cytokines in the serum of CIA(collagen type II induced arthritis) mice, number of immunocyte in PBMC of CIA mice were measured. Then, anti-oxidant activity, scavenging activity on DHHP(2,2-diphenyl-1-picrylhydrazyl) free radical and SOD(Superoxide dismutae)-like activity of GDT was observed. Results : 1. The levels of IL-$1{\beta}$, IL-6, IL-8, MCP-1 at 100, $50{\mu}g/m{\ell}$ of GDT were significantly reduced in the THP-1 cell. 2. The levels of TNF-${\alpha}$, COX-2 mRNA expression at 100, $50{\mu}g/m{\ell}$ of GDT and IL-$1{\beta}$, IL-6 at $100{\mu}g/m{\ell}$ of GDT were significantly reduced in the THP-1 cell line. 3. The levels of IL-6, TNF-${\alpha}$ and IL-$1{\beta}$ were significantly reduced in the serum of CIA mice. 4. The absolute number of CD3+, CD4+ and CD8+ cells were significantly induced, CD3+/CD69+, CD3+/CD49+, CD19+, B220+/CD23+ cells were significantly reduced in PBMC. 5. Scavenging activity on DPPH free radical and SOD-like activity were significantly induced in a concentration dependent manner. Conclusions : Taking all these observations, GDT considered to be effective in treating rheumatoid arthritis. Therefore we have to survey continuously in looking for the effective substance and mechanism in the future.

• Korean Journal of Pharmacognosy
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• v.53 no.3
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• pp.153-161
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• 2022

Cotoneaster mongolicus Pojark. (CM), in the family Rosaceae is an endemic plant to the Mongolian region (its name: Moнroл чapraй). In Mongolia, Cotoneaster species as a crude drug is mainly used for inflammatory diseases, diarrhea, and stomach indigestion. In this study, we evaluated the gastro-protective activity underlying mechanism of CM. For in vivo experiments, mice were divided into 5 groups; normal mice (Normal), gastritis mice (Control), gastritis mice treated with sucralfate 10 mg/kg (SC), gastritis mice treated with CM 100 mg/kg (CML), gastritis mice treated with CM 200 mg/kg (CMH). Gastritis was provoked by HCl/ethanol (60% ethanol in 150 mM HCl). After oral administration of each drug, HCl/ethanol was orally administered 90 mins later to induce gastritis. CM alleviated the damage to the gastric mucosa caused. As a result of confirming the expression of protein in gastric tissue through western blot, CM significantly reduced the expression of NF-κB activated due to gastritis. Also, it significantly modulated the Nrf2-Keap1 pathway. These results indicate that CM not only inhibits the nuclear metastasis of NF-𝛋B but also modulates the Nrf2-Keap1 pathway to relieve inflammation of the gastric mucosa.

• Journal of Nutrition and Health
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• v.54 no.4
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• pp.412-421
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• 2021

Purpose: Thioacetamide (TAA) produces reactive oxygen species (ROS) in the liver, and the generated ROS induces liver injury through inflammatory reactions. The current study was undertaken to investigate the hepatoprotective effect of Artemisiae Capillaris Herba water extract (AC), imparted via its antioxidant activity, in an animal model of TAA-induced liver injury. Methods: Animal experiments were conducted in 5 groups: normal, control (TAA 200 mg/kg), SM (TAA 200 mg/kg + silymarin 100 mg/kg), ACL (TAA 200 mg/kg + AC 100 mg/kg), ACH (TAA 200 mg/kg + AC 200mg/kg). TAA (intraperitoneal) and treatment compounds (per oral) were administered for 3 days. Serum levels of ammonia concentration and myeloperoxidase (MPO) activity were subsequently measured. Liver tissues were subjected to western blot analysis for measuring the oxidative stress (NADPH oxidase), anti-oxidative activity (Nrf2, heme oxygenase-1 [HO-1], superoxide dismutase [SOD], catalase, and GPx-1/2), tissue inhibitors of metalloproteinase (TIMP)-1, and matrix metalloproteinases (MMPs) protein expressions. Results: Serum ammonia levels and MPO activity were significantly increased in the TAA-induced control group, whereas groups administered AC treatment showed markedly reduced levels. Western blot analysis revealed significantly increased NOX2 and p22^phox expressions, (oxidative stress-related factors) in the TAA-induced control group. These levels were determined to be significantly decreased after AC exposure. Moreover, antioxidant-related factors including Nrf2, HO-1, SOD, catalase, and GPx-1/2 were significantly decreased in the control group and increased in the AC treated groups. In addition, MMP expressions were significantly suppressed in the AC treatment group due to increased levels of TIMP-1. Conclusion: Taken together, these data indicate that exposure to AC reduces the oxidative stress by inhibiting the expression of NADPH oxidase (NOX2 and p22^phox) through the Nrf2 signaling pathway. We therefore propose the potential of AC for the prevention and treatment of TAA-induced liver injury.

• Journal of Applied Biological Chemistry
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• v.62 no.2
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• pp.187-193
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• 2019

The newly bred Picnic apple was extracted using water and ethanol for extracting solvent. Each water and ethanol extract showed relatively high phenolic compound of 3.69 and 5.55 mg/g. Each water and ethanol extract of Picnic apple showed 1,1-diphenyl-2-picrylhydrazyl of 88.10 and 88.07%, 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) of 98.79 and 97.25%, antioxidant protection factor of 2.07 and 2.00 PF and thiobarbituric acid reactive substances showed anti-oxidation effect of 9.69 and 19.83% all at $100{\mu}g/mL$ phenolics concentration. Therefore extract of Picnic apple can be considered as anti-oxidant for anti-aging. The anti-inflammatory effect (hyaluronidase inhibition) of extract of Picnic apple were 4.62% with water extract and 4.39% with ethanol extract both at $200{\mu}g/mL$ phenolics concentration. Both water and ethanol extract showed low ${\alpha}$-amylase inhibition effect but each showed 67.37 and 79.16% of ${\alpha}$-glucosidase inhibition effect at $200{\mu}g/mL$ phenolics concentration. In anti-wrinkle effect, water extract showed each 23.70 and 66.29% in elastase inhibition and collagenase inhibition and ethanol extract showed 64.83 and 65.70% each. These result show high potential for functional food and cosmetic source. Picnic apple was identified to have various functions of anti-oxidation, anti-inflammation, anti-wrinkle effect, and anti-diabetic effect. Therefore, Picnic apple is qualified as a source for new functional cosmetics and functional foods.

• Reproductive and Developmental Biology
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• v.38 no.3
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• pp.115-121
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• 2014

Humulus japonicus is an ornamental plant in the Cannabaceae family. Although the mode of action of Humulus japonicus is not fully understood, a strong relationship was observed between anti-inflammatory and anticancer in some types of cells. Recent studies also have shown that Humulus japonicus possesses anti-inflammatory activities and may significantly improve antioxidant potential in Raw 264.7 macrophage cells. Thus, the aim of this study was evaluated the effect of Humulus japonicus extract on sperm motility and subsequent preimplantation developmental competence of the bovine embryos. After in vitro maturation, the oocytes with sperms were exposed in in vitro fertilization (IVF) medium supplemented with Humulus japonicus extract (0.01, 0.05, $0.1{\mu}g/mL$, respectively) for 1 day. In our results, exposure of IVF medium to Humulus japonicus extract did not affect sperm motility and percentage of penetrated oocytes but ROS intensity was significantly decreased by $0.01{\mu}g/mL$ compared with other groups (p< 0.05). Moreover, treatment with $0.01{\mu}g/mL$ of Humulus japonicus extract was higher the frequency of blastocyst formation than the any other groups (p<0.05). Otherwise, treatment with $0.01{\mu}g/mL$ of Humulus japonicus extract not increased the total cell number but reduced apoptotic-positive nuclei number. In conclusion, our results indicate that supplementation of Humulus japonicus extract in IVF medium may have important implications for improving early embryonic development in bovine embryos.

• Journal of Life Science
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• v.30 no.11
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• pp.965-972
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• 2020

Sambucus sieboldiana var. miquelii (Nakai) Hara is distributed in Korea, China, and Japan, and has been used as an anti-rheumatic in folk medicine in oriental countries. The present study aims to investigate the potential use of this species in health functional foods, cosmetics, and food preservatives. Methanol extracts of leaves and branches from this plant were prepared to quantitatively analyze the total phenol and flavonoid contents, and to investigate the antioxidative and enzyme inhibitory activities, and the inhibition of nitric oxide (NO) production activity. The results showed that the total polyphenol and flavonoid contents of the crude extract were 1.52±0.1 mg/g and 1.73±0.1 mg/g, respectively. S. sieboldiana polyphenols exhibited potent scavenging activity shown by 2, 2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and 2, 2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation assay. The crude extract also exhibited significant α-glucosidase and tyrosinase inhibitory activity with IC₅₀ values of 183.5 ㎍/ml and 323.9 ㎍/ ml, respectively. Additionally, the crude extract exhibited strong anti-inflammatory activity determined through the nitric oxide inhibition assay in a dose-dependent manner with an IC₅₀ value of 36.7 ㎍/ml and no cytotoxic effect on the macrophages. Therefore, we demonstrated that the leaves and branches of S. sieboldiana extract possess antioxidant, anti-diabetic, depigmentation potential, and NO production inhibitory activities. According to recent research, S. sieboldiana has great potential as a source of the bioactive compound which could be used as food, cosmetics, and pharmaceutical agents.

• Journal of Nutrition and Health
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• v.55 no.1
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• pp.36-46
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• 2022

Purpose: Quercetin is a polyphenolic flavonoid abundant in many fruits and vegetables. It has potential health-beneficial properties, such as antioxidant, anti-obesity, anti-cancer, anti-diabetic and anti-inflammatory effects. The purpose of this study was to investigate whether the lipid metabolism improvement effect of quercetin affected the regulation of AMP-activated protein kinase (AMPK) activity and microRNA (miR)-21 expression in the liver of mice fed a high-cholesterol diet. Methods: Male C57BL/6J mice were fed with normal diet, quercetin-free diet and diets containing 0.05% or 0.1% quercetin for six weeks. Hypercholesterolemia was induced by adding 1% cholesterol and 0.5% cholic acid to all diets. Serum and liver triglyceride (TG), and total cholesterol (TC) concentrations were analyzed using a commercial enzymatic colorimetric kit. AMPK activity was quantified using an AMPK kinase assay kit. The levels of miR-21 and genes involved in lipid metabolism were measured by real-time quantitative polymerase chain reaction. Results: Supplementation of quercetin reduced serum and hepatic TG and TC levels without changing body weight and food intake. Dietary quercetin significantly inhibited the mRNA levels of hepatic sterol-regulatory element binding protein-1c, acetyl-CoA carboxylase 1 and fatty acid synthesis, which are involved in hepatic lipogenesis. Dietary quercetin enhanced AMPK activity and suppressed miR-21 expression, promoting hepatic lipid accumulation. Conclusion: These results suggest that the lipid-lowering effect of quercetin on the serum and liver of mice may be partially mediated by the regulation of lipogenic gene expression, AMPK activity and miR-21 expression in the liver of mice fed a high-cholesterol diet.

• Journal of the Korean Society of Food Science and Nutrition
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• v.42 no.3
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• pp.369-377
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• 2013

In order to increase the utilization of sweet potato leaves and stalks as much as roots, it is necessary to study their beneficial potential. In this study, the antioxidant, antiallergic and anti-inflammatory effects of sweet potato leaves and stalks were evaluated by measuring total polyphenol and flavonoid contents, DPPH radical scavenging effects, the reducing power and inhibition effects on xanthine oxidase (XO), 5-lipoxygenase (LOX), and cyclo-oxygenase (COX)-2 activities. Blanched sweet potato leaves (SL), raw whole purple stalks (ST) and peeled stalks (PST) were freeze-dried and extracted with 95% ethanol. Total polyphenol content was highest in SL (11.03 mg/g), followed by ST (0.87 mg/g), and PST (0.37 mg/g). Total flavonoid content was highest for SL (9.01 mg/g), followed by ST (0.50 mg/g) and PST (0.25 mg/g). The $IC_{50}$ for DPPH radical scavenging effects was highest for SL ($43.6{\mu}g/mL$), followed by ST ($308.4{\mu}g/mL$) and PST ($1,631.3{\mu}g/mL$). The reducing power was highest for SL ($59.72{\mu}g$ ascorbic acid eq./mL), followed by ST ($12.56{\mu}g$ ascorbic acid eq./mL) and PST ($2.18{\mu}g$ ascorbic acid eq./mL) with $1,000{\mu}g/mL$ of ethanol extract. The inhibition rate on XO activity was highest for SL (13.06%), followed by ST (5.05%) and PST (0.0%) at $250{\mu}g/mL$ extract treatment. The inhibition rate on COX-2 activity was highest for SL (55.34%), followed by ST (2.18%) and PST (0.0%) at $250{\mu}g/mL$ extract treatment. The inhibition rate on 5-LOX activity was highest for SL (91.16%), followed by ST (33.38%) and PST (14.93%) at $50{\mu}g/mL$ treatment. Taken together, sweet potato leaves showed high antioxidative, anti-allergic and anti-inflammatory activities, especially with very strong inhibition effects on 5-LOX activity. These beneficial effects of sweet potato leaves might be mainly caused by the high content of polyphenols and flavonoids.

• Journal of the Korean Society of Food Science and Nutrition
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• v.45 no.5
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• pp.664-670
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• 2016

Cheonggukjang (CKJ) is a Korean traditional food made of fermented soybeans. In comparison to normal intake of soybeans, Cheonggukjang has high digestibility with bioactive, antioxidant substances, and thrombolytic enzymes. Recent studies have reported anti-oxidant, anti-cancer, anti-inflammatory, anti-obesity activities as well as inhibitory activities against osteoporosis for CKJ. In this study, we identified the effects of CKJ on osteoblast differentiation by increasing the polyglutamic acid (PGA) content of CKJ. Alkaline phosphatase (ALP) activity and mineralization significantly increased in response to treatment with both natural CKJ (CKJ A) and PGA-increased CKJ (CKJ B). However, CKJ B exhibited higher ALP activity and mineralization than CKJ A. Real-time reverse transcription PCR demonstrated that mRNA expression of osteoblastic-associated genes such as type I collagen, alkaline phosphatase, osteocalcin, and osteopontin in C2C12 cells was significantly up-regulated by CKJ A or B treatment. These results indicate that treatment with CKJ has an anabolic effect on bone by increasing osteoblastic differentiation and ALP activity. Increasing PGA content in CKJ had a greater effect than CKJ A on up-regulation of osteoblastic gene expression in osteoblast cells.