• Korean Journal of Medicinal Crop Science
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• v.18 no.6
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• pp.409-415
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• 2010

In this study, the bioactivities of ethanol (EELS) and water extract (WELS) from the leaf of Lythrum salicaria L. were investigated. In the anti-cancer activity, the growths of both human prostate cancer (DU145) and human colonic carcinoma cell (HT29) were inhibited up 60% by adding 10 mg/$m{\ell}$ of EELS. Anti-inflammatory activity of EELS and WELS have been evaluated on lipopolysaccharide (LPS) induced release of nitric oxide (NO) by the macrophage RAW 264.7 cells. EELS and WELS inhibited inflammatory by 57.3 and 46.9% in 10 mg/$m{\ell}$, respectively. In the anti-oxidative activity, $IC_{50}$ of DPPH radical scavenging activity was respectively 60.71 and $92.90\;{\mu}g/m{\ell}$ by EELS and WELS. In the anti-diabetic activity, $IC_{50}$ of ${\alpha}$-amylase inhibitory activity of EELS and WELS were respectively 5,250 and $5,020\;{\mu}g/m{\ell}$. $IC_{50}$ of ${\alpha}$-glucosidase inhibitory activity was 7.96 and $68.41\;{\mu}g/m{\ell}$ by EELS and WELS. In the anti-obesity, $IC_{50}$ of lipase inhibitory activity was 880 and $9,840\;{\mu}g/m{\ell}$ by EELS and WELS. Finally, EELS and WELS exhibited anti-oxidative, anti-inflammatory, anti-diabetic activity and anti-obesity. It suggests that Lythrum salicaria L. could be potentially used as a resource of bioactive materials for health functional foods.

• The Journal of Korean Medicine
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• v.30 no.1
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• pp.51-63
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• 2009

Objectives: Peroxynitrite ($ONOO^-$), superoxide anion radical (${\cdot}{O_2}^-$ and nitric oxide (NO) are cytotoxic because they can oxidize several cellular components such as proteins, lipids and DNA. They have been implicated in the aging processes, and age-related diseases such as Alzheimer's disease, rheumatoid arthritis, cancer, diabetes, obesity and atherosclerosis. The aim of this study was to investigate the $ONOO^-$, NO, ${\cdot}{O_2}^-$ scavenging and NF-${\kappa}B$ related anti-inflammatory activities of Sotosaja-hwan in ob/ob mice. Methods: Mice were grouped and treated for 5 weeks as follows. Both the normal lean (C57/BL6J black mice) and control obese (ob/ob mice) groups have received standard chow. The experimental groups were fed with a diet of chow supplemented with 30 and 90 mg Sotosaja-hwan per 1 kg of body weight for 14 days. For this study, the fluorescent probes, namely 2',7'-dichlorodihydrofluorescein diacetate (DCFDA), 4,5-diaminofluorescein (DAF-2) and dihydrorhodamine 123 (DHR 123) were used. Western blotting was performed using anti-phospho-$I{\kappa}B$-${\alpha}$, anti-IKK-${\alpha}$, anti-NF-${\kappa}B$ (p50, p65), anti-COX-2, anti-iNOS, anti-YCAM-1 and anti-MMP-9 antibodies, respectively. Results: Sotosaja-hwan inhibited the generation of $ONOO^-$, NO and ${\cdot}{O_2}^-$ in the lipopolysaccharide (LPS)-treated mouse kidney postmitochondrial fraction in vitro. The generation of $ONOO^-$, NO, ${\cdot}{O_2}^-$ and PGE2 were inhibited in the Sotosaja-hwan-administered ob/ob mice groups. The GSH/GSSG ratio was decreased in the ob/ob mice, whereas the ratio was improved in the Sotosaja-hwan-administered groups. Sotosaja-hwan inhibited the protein expression levels of phospho-$I{\kappa}B$-${\alpha}$, IKK-${\alpha}$, NF-${\kappa}B$ (p50, p65), COX-2, iNOS, YCAM-1 and MMP-9 genes. Conclusions: These results suggest that Sotosaja-hwan is an effective $ONOO^-$, ${\cdot}{O_2}^-$ and NO scavenger and has NF-kB related anti-inflammatory activity in ob/ob mice. Therefore, Sotosaja-hwan might be a potential therapeutic drug against the inflammation process and inflammation-related diseases.

• The Korean Journal of Physiology and Pharmacology
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• v.19 no.3
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• pp.219-228
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• 2015

Excessive microglial activation and subsequent neuroinflammation lead to synaptic loss and dysfunction as well as neuronal cell death, which are involved in the pathogenesis and progression of several neurodegenerative diseases. Thus, the regulation of microglial activation has been evaluated as effective therapeutic strategies. Although dieckol (DEK), one of the phlorotannins isolated from marine brown alga Ecklonia cava, has been previously reported to inhibit microglial activation, the molecular mechanism is still unclear. Therefore, we investigated here molecular mechanism of DEK via extracellular signal-regulated kinase (ERK), Akt and nicotinamide adenine dinuclelotide phosphate (NADPH) oxidase-mediated pathways. In addition, the neuroprotective mechanism of DEK was investigated in microglia-mediated neurotoxicity models such as neuron-microglia co-culture and microglial conditioned media system. Our results demonstrated that treatment of anti-oxidant DEK potently suppressed phosphorylation of ERK in lipopolysaccharide (LPS, $1{\mu}g/ml$)-stimulated BV-2 microglia. In addition, DEK markedly attenuated Akt phosphorylation and increased expression of $gp91^{phox}$, which is the catalytic component of NADPH oxidase complex responsible for microglial reactive oxygen species (ROS) generation. Finally, DEK significantly attenuated neuronal cell death that is induced by treatment of microglial conditioned media containing neurotoxic secretary molecules. These neuroprotective effects of DEK were also confirmed in a neuron-microglia co-culture system using enhanced green fluorescent protein (EGFP)-transfected B35 neuroblastoma cell line. Taken together, these results suggest that DEK suppresses excessive microglial activation and microglia-mediated neuronal cell death via downregulation of ERK, Akt and NADPH oxidase-mediated pathways.

• Journal of the Korean Society of Food Science and Nutrition
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• v.34 no.8
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• pp.1188-1194
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• 2005

This study was conducted to investigate effects of fructans (chicory inulin, fructooligosaccharide and chicory inulin oligosaccharide) on blood glucose, activities of disaccharidases in small bowel and kidneys, and splenocyte proliferation in streptozotocin-induced diabetic mice. Sixty ICR male mice were divided into one normal group and four diabetic groups. Diabetes was induced by injecting streptozotocin after 2 weeks of experimental diets feeding. Experimental diets based on AIN93G diet were control diet, 6$ \%$ fructooligosaccharide (FOS) diet, 6$\%$ chicory inulin oligosaccharide (CIOS) diet, 6$\%$ chicory inulin (Cl) diet, and given for 25 days after streptozotocin injection. Plasma glucose was lower in Diabetic-Cl group as compared to Diabetic-control group. Plasma insulin level was not different among diabetic groups. Specific activities of jejunal maltase and sucrase in diabetic groups were about double as that of Normal group. Jejunal maltase activity and plasma glucose were positively correlated (r=0.643). However, specific activity of renal maltase in diabetic groups was not significantly different as compared to Normal group. Stimulation index of splenocyte proliferation by lipopolysaccharide (LPS) was significantly increased in Diabetic-CIOS as compared to Diabetic-control. Stimulation index of splenocyte proliferation by Concanavalin A (ConA) tended to be higher in Diabetic-CIOS group. Concentrations of interleukin-2 and interferon- $\gamma$ secreted from splenocytes induced by ConA were not significantly different among all groups. In conclusion, fructans may be effective for lowering plasma glucose, possibly by lowering disaccharidase activity and for increasing immune responses in diabetic con-ditions, where their effects can be different depending on degree of polymerization.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.04a
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• pp.3-3
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• 2018

For centuries, Panax ginseng Meyer (Korean ginseng) has been widely used as a medicinal herb in Korea, China, and Japan. Ginsenosides are a class of triterpene saponins and recognized as the bioactive components in Korean ginseng. Ginsenosides, which can be classified broadly as protopanaxadiols (PPD), protopanaxatriols (PPT), and oleanolic acids, have been shown to flaunt a vast array of pharmacological activities such as immune-modulatory, anti-inflammatory, anti-tumor, anti-diabetic, and antioxidant effects. In recent years, a number of ginseng and ginsenoside researches have increasingly gained wide attention owing to its unique pharmacological properties. Although good efficacies of ginsenosides have been reported, lack of target specific delivery into tumor sites, low solubility, and low bioavailability due to modifications in gastro-intestinal environments limit their biomedical application in clinical trials. As a result to this major challenge, nanotechnology and drug delivery techniques play a significant role to solve this problematic issue. Thus, we reported the preparation of poly-ethylene glycol (PEG) and glycol chitosan (GC) functionalized to ginsenoside (Compound K and PPD) conjugates via hydrolysable ester bonds with improved aqueous solubility and pH-dependent drug release. In vitro cytotoxicity assays revealed that PEG-CK, and PPD-CK conjugates exhibited lower cytotoxicity compared to bare CK and PPD in HT29 cells. However, GC-CK conjugates exhibited higher and similar cytotoxicity in HT29 and HepG2 cells. Furthermore, GC-CK-treated RAW264.7 cells did not exhibit significant cell death at higher concentration of treatment which supports the biocompatibility of the polymer conjugates. They also inhibited nitric oxide production in lipopolysaccharide (LPS)-induced RAW64.7 cells. In addition to polymer-ginsenoside conjugates, silver (AgNps) and gold nanoparticles (AuNps) have been successfully synthesized by green chemistry using different m. The biosynthesized nanoparticles demonstrated antimicrobial efficacy, anticancer, anti-inflammatory, antioxidant activity, biofilm inhibition, and anticoagulant effect. Special interest on the effective delivery methods of ginsenoside to treatment sites is the focus of metal nanoparticle research.In short, nano-sizing of ginsenoside results in an increased water solubility and bioavailability. The use of nano-sized ginsenoside and P. ginseng mediated metallic nanoparticles is expected to be effective on medical platform against various diseases in the future.

• Animal cells and systems
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• v.14 no.4
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• pp.275-282
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• 2010

Chunghyul-dan (CHD) is a combinatorial drug known to exert anti-inflammatory effects in endothelial cells. In this study, we employed global transcriptional profiling using cDNA microarrays to identify molecular mechanisms responsible for the anti-inflammatory activity of CHD in endothelial cells. An analysis of the microarray data revealed that transcript levels of monocyte chemotactic protein-1 (MCP-1), vascular cell-adhesion molecule-1 (VCAM-1) and activated leukocyte cell-adhesion molecule were dramatically altered in CHD-treated endothelial cells. These changes in gene expression were confirmed by RT-PCR, Western blotting and ELISA. Chronic CHD treatment also appeared to decrease MCP-1 secretion, probably as a result of decreased MCP-1 expression. In addition, we determined that chronic CHD treatment inhibited lipopolysaccharide-stimulated adhesion of THP-1 leukocytes to endothelial cells. The inhibitory effect of CHD on LPS-stimulated adhesion resulted from downregulation of VCAM-1 expression. Transmigration of THP-1 leukocytes through endothelial cells was also inhibited by chronic CHD treatment. In conclusion, CHD controls a variety of inflammatory activities by regulating MCP-1 and VCAM-1 gene expression.

• Food Science and Preservation
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• v.24 no.8
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• pp.1122-1128
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• 2017

Pumpkin has long been used as traditional health materials in oriental medicine, pharmacy, medicine, and food industries in many countries. In this study, the water extract and two active components from tendril of young C. moschata Duch. were investigated on inflammation inhibitory activity. The water extract of young C. moschata Duch. showed high cell viability over 95% and it decreased the production of interlukin 6 (IL-6) and tumor necrosis factor (TNF-${\alpha}$) in the capacity of mouse bone marrow-derived macrophages (BMDM) upon lipopolysaccharide (LPS) stimulation. Also, isolated fraction (B4) suppressed the secretion of IL-6 and TNF-${\alpha}$. Among the domestically cultivated pumpkins, B4 fraction contained in the tendril part of them and it comprised of the order of tendril from Cucurbita pepo var. cylindrica, old of C. moschata Duch., and young of C. moschata Duch. These results suggest that water extracts of C. moschata Duch. and purified active compound, rutin, show anti-inflammation activity by suppression of the secretion of IL-6 and TNF-${\alpha}$. It can be applicable as pharmaceutical materials.

• Journal of Periodontal and Implant Science
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• v.36 no.2
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• pp.361-373
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• 2006

치주질환의 진행이 나이에 의해 영향을 받는다는 사실은 알려져 있으나 노화에 따른 치주조직 세포의 기능적인 변화에 관한 사실은 많이 알려져 있지 않다. 노화에 따른 세포의 노화가 치주질환의 진행에 어떠한 여향을 끼치는가를 아는 것은 중요하다. 염증 상태에서 nitric oxide (NO)는 조직 파괴에 관여하는 인자로 작용하여 치주질환의 진행에 관여하는 것으로 알려져 있다. 따라서 이 연구는 사람의 치은에서 배양된 치은섬유아세포를 이용하여 세포의 노화에 따른 NO와 이의 합성효소인 inducible nitric oxide synthase (iNOS)의 발현을 알아봄으로써 세포의 노화가 치주질환의 진행에 끼치는 영향에 대해 알아보고자 하였다. 10세의 환자와 55세의 환자에서 각각 채취한 치은에서 배양된 세포와 10세의 환자에서 채취한 세포를 계속적인 계대배양을 통해 얻은 실험실 상 노화된 세포를 포함하여 총 3 종류의 치은섬유세포를 실험에 이용하였다. Hot phenol-water extraction을 통해 추출된 Porphyromonas, gingivalis ATCC 33277 lipopolysaccharide (LPS)와 재조합 $IFN-{\gamma}$ 를 세포에 적용시켜 Griess assay를 통해 조건화된 배지에서 NO를 측정하였다. 20세와 55세의 환자에서 채취된 치은 조직과 총 3 종류의 배양된 세포에 NOS-II 항체를 적용시켜 iNOS 단백질 발현을 관찰하였다. Total RNA를 추출하여 RT-PCR를 통해 iNOS mRNA의 발현을 분석하였다. 치은섬유아세포에서 NO는 자발적으로 발생되었고, 이러한 발현은 젊은 세포보다 노화된 세포에서 강하였다. P, gingivalis LPS와 제조합 $IFN-{\gamma}$는 치은섬유아세포에서 NO의 발현을 증가시켰고, 이러한 발현은 젊은 세포보다 노화된 세포에서 강하였다. 면역조직화학 염색에서 iNOS 단백질은 젊은 사람과 노화된 사람의 치은 조직 모두에서 치은섬유아세포와 상피의 기저층 세포와 염증세포에서 발현되었으나 노화에 따른 발현의 차이를 구별할 수는 없었다. 세포의 면역염색에서 iNOS 단백질은 노화된 세포에서 강하게 발현되었고 이러한 발현은 LPS와 $IFN-{\gamma}$ 에 의해 강화되었다. LPS와 $INF-{\gamma}$ 의 조건이 주어지지 않은 상태에서 iNOS mRNA는 젊은 세포에서보다 노화된 세포에서 강하게 발현되었다. 이러한 결과를 통해 세포의 노화가 NO와 iNOS 발현을 증가시킴으로서 치주질환의 진행에 영향을 끼칠 수 있음을 시사하였다.

• Food Science and Preservation
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• v.23 no.7
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• pp.1026-1032
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• 2016

Citrus platymamma hort. ex Tanaka is widely used in traditional Korean medicine because of its medicinal benefits including an anti-inflammatory effect. This study aimed to evaluate changes in the flavonoid content and anti-inflammatory activities of C. platymamma during its harvest period. Fruit peel samples were obtained between September 2015 and February 2016. The results indicate that C. platymamma peel extract (CPE) was an effective inhibitor of lipopolysaccharide (LPS)-induced NO production in RAW264.7 cells. The inhibitory effects of CPE at $100{\mu}g/mL$ concentration included dose-dependent decreases in the expression of iNOS and COX-2 proteins. In addition, CPE decreased the expression of pro-inflammatory cytokines TNF-${\alpha}$, IL-$1{\beta}$, and IL-6. The highest anti-inflammatory activity and flavonoid content were observed in CPE of C. platymamma peel harvested during the immature fruit period in September. Further, to assess the suitability of CPE for cosmetic use, we performed MTT assays using HaCaT keratinocytes and observed that CPE did not exhibit any cytotoxicity. To test the potential application of CPE as a cosmetic material, we also performed primary skin irritation tests on normal skin of 30 volunteers and no adverse reactions were observed. The results of this study indicate that CPE may be considered as an anti-inflammatory candidate for inclusion in cosmetic materials.

• Journal of Life Science
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• v.22 no.9
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• pp.1137-1144
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• 2012

Inflammation is a host defense mechanism that is activated in response to harmful substances or pathogens. However, an excessive inflammatory response is a problem in itself. Macrophages secrete inflammatory mediators such as nitric oxide (NO) or cytokines through various pathways such as the nuclear factor kappa B (NF-${\kappa}B$)-activated pathway after recognizing pathogen-like lipopolysaccharides (LPSs). In this study, anti-inflammatory effects of Eupatorium chinensis var. simplicifolium (EUC) extracts were investigated using LPS-stimulated RAW 264.7 macrophages. The EUC root extract significantly reduced NO production, inducible nitric oxide synthase (iNOS) expression, and cyclooxygenase-2 expression in a concentration-dependent manner. In addition, the EUC root extract reduced phosphorylation of mitogen-activated protein kinases and protein kinase B, which is upstream of NF-${\kappa}B$. The EUC root extract also reduced the degradation of inhibitory kappa B. These results indicate that EUC root extract exerts anti-inflammatory effects, which are mediated by inhibition of iNOS expression and the NF-${\kappa}B$ pathway.