• 한방안이비인후피부과학회지
• /
• 제31권3호
• /
• pp.39-49
• /
• 2018

Objectives : This study is designed to clarify whitening, anti-inflammatory effect of fractions extracted from the mixture of Phaseolus radiatus L. and ethanol. Methods : In this experiment, we were intended to reveal whitening, anti-inflammatory effect of fractions extracted from the mixture of Phaseolus radiatus L. and ethanol. The whitening activity was confirmed by UV blocking activity, tyrosinase inhibiting activity, and melanin formation inhibiting activity. Anti-inflammatory activity is confirmed by measurement of cytotoxicity level by MTT assay and measurement of Cytokine expression, which is the main mediator of inflammation reaction. Results : As a results, overall activity was high in the ethyl acetate fraction. Tyrosinase inhibitory activity was less than 20% at all concentrations, but the activity to inhibit melanin self-production was higher than that of ethyl acetate fraction at $32.19{\pm}2.79%$ at $100{\mu}g/m{\ell}$. And ethyl acetate fraction had a relatively high UV blocking activity. In the anti-inflammatory test, the concentration-dependent activity was shown, and the chloroform and ethyl acetate fractions showed significant NO production inhibitory activity. Cytokine expression was superior to that of the final stage of B cell differentiation, and cell viability was over 80% except for the chloroform fraction at the concentration of $200{\mu}g/m{\ell}$. Conclusions : The results of this experiment confirmed the whitening effect and anti-inflammatory effect of Phaseolus radiatus L.'s extracts and fractions and report the possibility of application as external medicine.

• Journal of Gastric Cancer
• /
• 제11권1호
• /
• pp.16-22
• /
• 2011

Purpose: Eupatilin is an antioxidative flavone and a phytopharmaceutical derived from Artemisia asiatica. It has been reported to possess anti-tumor activity in some types of cancer including gastric cancer. Eupatilin may modulate the angiogenesis pathway which is part of anti-inflammatory effect demonstrated in gastric mucosal injury models. Here we investigated the anti-tumor effects of eupatilin on gastric cancer cells and elucidated the potential underlying mechanism whereby eupatilin suppresses angiogenesis and tumor growth. Materials and Methods: The impact of eupatilin on the expression of angiogenesis pathway proteins was assessed using western blots in MKN45 cells. Using a chromatin immunoprecipitation assay, we tested whether eupatilin affects the recruitment of signal transducer and activator of transcription 3 (STAT3), aryl hydrocarbon receptor nuclear translocator (ARNT) and hypoxia-inducible factor-$1{\alpha}$ (HIF-$1{\alpha}$) to the human VEGF promoter. To investigate the effect of eupatilin on vasculogenesis, tube formation assays were conducted using human umbilical vein endothelial cells (HUVECs). The effect of eupatilin on tumor suppression in mouse xenografts was assessed. Results: Eupatilin significantly reduced VEGF, ARNT and STAT3 expression prominently under hypoxic conditions. The recruitment of STAT3, ARNT and HIF-$1{\alpha}$ to the VEGF promoter was inhibited by eupatilin treatment. HUVECs produced much foreshortened and severely broken tubes with eupatilin treatment. In addition, eupatilin effectively reduced tumor growth in a mouse xenograft model. Conclusions: Our results indicate that eupatilin inhibits angiogenesis in gastric cancer cells by blocking STAT3 and VEGF expression, suggesting its therapeutic potential in the treatment of gastric cancer.

• 약학회지
• /
• 제39권2호
• /
• pp.153-160
• /
• 1995

Receptor binding study was carried out as an in vitro assay to test the anti-ulcer effect for newly synthesized test compounds(IY-80843 and IY-80845) which were reported to have a strong anti-secretory effect in Shay-ligated rats. The histamine H$_{2}$-receptor fraction was prepared from the membranes of the isolated gastric glands in guinea pigs and $^{3}$H-cimetidine was used as a radioligand. The binding of $^{3}$H-cimetidine to the membranes of the isolated gastric glands was found to be time dependent, saturable and confined to a single population of binding sites with $K_{D}$ value of 0.13$\pm$0.03 $\mu{M}$ and B$_{max}$ value of 52.5$\pm$1.5 pmol/mg. From the competition experiments, both IY-80843 and IY-80845 were shown to have a strong blocking effect against binding of $^{3}$H-cimetidine to the histamine H$_{2}$-receptor. The IC$_{50}$, Ki, and Hill coefficient(nH) values for IY-80843 were 0.18$\pm$0.02 $\mu{M}$, 0.16$\pm$0.02 $\mu{M}$, and 0.97$\pm$0.15, respectively and those values for IY-80845 were 0.27$\pm$0.02 $\mu{M}$, 0.24$\pm$0.02 $\mu{M}$, and 0.82$\pm$0.13, respectively. The results demonstrated that the blocking effects of IY-80843 and IY-80845 were 7 and 5 times stronger than that of cimetidine, respectively. Therefore, the newly synthesized compounds, IY-80843 and IY-80845, appeared to be the highly potent competitive inhibitors of histamine on the H$_{2}$-receptor.

• 정보처리학회논문지A
• /
• 제8A권4호
• /
• pp.385-390
• /
• 2001

본 논문에서는 시스템 해킹 시에 가장 많이 사용되는 버퍼 오버플로우 공격의 기법을 소개하고 운영체제 커널 수준에서 막을 수 있는 대응 기법을 소개한다. 보안 운영체제 시스템이란 리눅스 커널에 접근제어, 사용자 인증, 감사 추적, 해킹 대응 등과 같은 보안 기능을 추가 구현하여 시스템에서 발생 가능한 해킹을 방지하고 차단하는 시스템을 말한다. 본 논문에서는 보안 운영체제 시스템에서 제공하는 해킹 대응 기술 중의 하나로 버퍼 오버플로우 공격을 막을 수 있는 커널 내 구현 내용을 설명한다.

• BMB Reports
• /
• 제49권4호
• /
• pp.232-237
• /
• 2016

Mulberry tree twigs (Ramulus mori) contain large amounts of oxyresveratrols and have traditionally been used as herbal medicines because of their anti-inflammatory properties. However, the signaling mechanism by which R. mori exerts its anti-inflammatory action remains to be elucidated. In this study, we observed that R. mori ethanol extracts (RME) exerted an inhibitory effect on the lipopolysaccharide (LPS)-induced production of the pro-inflammatory cytokine interleukin-6 (IL-6) in Raw264.7 macrophage cells. Additionally, RME inhibited IL-6 production by blocking the leukotriene B₄ receptor-2 (BLT2)-dependent-NADPH oxidase 1 (NOX1)-reactive oxygen species (ROS) cascade, leading to anti-inflammatory activity. Finally, RME suppressed the production of the BLT2 ligands LTB4 and 12(S)-HETE by inhibiting the p38 kinase-cytosolic phospholipase A₂-5-/12-lipoxygenase cascade in LPS-stimulated Raw264.7 cells. Overall, our results suggest that RME inhibits the 'BLT2 ligand-BLT2'-linked autocrine inflammatory axis, and that this BLT2-linked cascade is one of the targets of the anti-inflammatory action of R. mori.

• Biomolecules & Therapeutics
• /
• 제24권4호
• /
• pp.402-409
• /
• 2016

It has been found that 4-isopropyl-2,6-bis(1-phenylethyl)phenol (KTH-13), a novel compound isolated from Cordyceps bassiana, is able to suppress tumor cell proliferation by inducing apoptosis. To mass-produce this compound, we established a total synthesis method. Using those conditions, we further synthesized various analogs with structural similarity to KTH-13. In this study, we aimed to test their anti-cancer activity by measuring anti-proliferative and pro-apoptotic activities. Of 8 compounds tested, 4-methyl-2,6-bis(1-phenylethyl)phenol (KTH-13-Me) exhibited the strongest anti-proliferative activity toward MDA-MB 231 cells. KTH-13-Me also similarly suppressed the survival of various cancer cell lines, including C6 glioma, HCT-15, and LoVo cells. Treatment of KTH-13-Me induced several apoptotic signs in C6 glioma cells, such as morphological changes, induction of apoptotic bodies, and nuclear fragmentation and chromatin condensation. Concordantly, early-apoptotic cells were also identified by staining with FITC-Annexin V/PI. Moreover, KTH-13-Me highly enhanced the activation of caspase-3 and caspase-9, and decreased the protein level of Bcl-2. In addition, the phosphorylation levels of Src and STAT3 were diminished in KTH-13-Me-treated C6 cells. Therefore, these results suggest that KTH-13-Me can be developed as a novel anti-cancer drug capable of blocking proliferation, inducing apoptosis, and blocking cell survival signaling in cancer cells.

• 한국임상수의학회지
• /
• 제18권4호
• /
• pp.418-423
• /
• 2001

각막상피의 창상치유에 중요한 역할을 하는 것으로 알려진 Nerve Growth Factor(NGF)의 내인성 변화와 국소적 투여효과를 알아보았다. 6마리의 Beagle 을 사용하여 비교군인 오른쪽 눈에만 6mm의 기계적인 각막 창상을 만들었고 왼쪽 눈은 대조군으로 사용하였다. 눈물은 수술후 1주일동안 매일, 각막 상피는 수술중 그리고 수술후 7일에 각각 채취하여 NGF 농도를 enzyme-linked immunosorbent assay (ELISA)를 사용하여 측정하였다. 2차 실험으로, 16마리의 Bealgle을 사용하여 오른쪽 눈에 위와 동일한 창상을 만든 후, 창상 부위가 회복될 때까지 recombinant human (rh) NGF (n=4), murine NGF (n=6) 그리고 anti-NGF blocking antibody (n=6)를 6시간마다 점안하였으며, 왼쪽 눈은 bovine serum albumin (BSA)를 점안하여 대조군으로 사용하였다. 창상 면적은 NIH image software를 이용하여 분석하였다. 대조군에 비하여, 비교군의 눈물내 NGF는 치유초기에 현저하게 증가하였으며, 각막 상피의 NGF도 유의적인 증가를 보였다. 그러나 rh NGF, murine NGF, anti-NGF blocking antibody처치군과 BSA처치군 간에는 각막창상 치유에 유의적인 차이가 인정되지 않았다. 각막창상후, rh NGF 혹은 murine NGF의 추가적인 국소점안은 정상개의 각막상피 치유에 효과가 없었으나, 창상후 초기 치유기동안 눈물과 손상받은 각막상피에서 내인성 NGF의 급격한 보상성 증가로 미루어 NGF는 각막 상피의 창상치유에 중요한 역할을 하는 것으로 사료된다.

• IMMUNE NETWORK
• /
• 제3권3호
• /
• pp.176-181
• /
• 2003

Background: The molecular basis of follicular dendritic cells (FDC)-germinal center (GC) B cell interaction is largely unknown, although this cellular interaction is thought to be important for the whole process of GC B cell differentiation. Methods: Using FDC-like cells, HK, and highly purified GC B cells, we attempted to identify the molecules that play critical roles in the interactions between FDC and B cells. GC B cells were co-cultured with HK cells and soluble CD154 in the presence or absence of various function-blocking monoclonal antibodies to examine their effect on GC B cell binding to HK cells and B cell proliferation. Results: Anti-CD11a and anti-CD54 antibodies inhibited GC B cell binding to HK cells while anti-CD49d and anti-CD106 antibodies did not. GC B cell proliferation was not impaired by the disruption of GC B cell-HK cell adherence. Conclusion: Our results suggest that CD11a/CD18-CD54 interactions play an important roles in the initial binding of GC B cells to FDC and diffusible growth factors from FDC may be responsible the massive proliferation of GC B cells.

• Journal of Microbiology and Biotechnology
• /
• 제18권8호
• /
• pp.1423-1426
• /
• 2008

Nuruk, which is a natural inoculator and source of amylolytic enzymes, is used in Korean traditional rice wine. A methanol extract of nuruk (NE) attenuated lipopolysaccharide (LPS)-induced nitrite and interleukin (IL)-6 in RAW 264.7 cells. Both the n-hexane and water fractions from NE (MEH and MW, respectively) inhibited the production of nitrite and IL-6 in RAW 264.7 cells. MEH and MW also inhibited the LPS-induced inducible nitric oxide synthase expression. Further, and MEH protected against the LPS-induced activation of p38 mitogen-activated protein kinase. Together, these results indicate that nuruk may contribute to the anti-inflammatory and cancer-preventive effects of Korean traditional rice wine.

• Environmental Analysis Health and Toxicology
• /
• 제24권1호
• /
• pp.63-70
• /
• 2009

Naringenin, major one of the citrus flavonoids, have been identified that exert antioxidative, anticancer effects. The present study investigated the effects of naringenin on tumor invasion and matrix metalloproteinases(MMPs) activities. Naringenin inhibited cell invasion of HT-1080 fibrosarcoma cells in a dose-dependent manner. The activities of MMP-2 and MMP-9 were inhibited by naringenin as demonstrated by gelatin zymography assay. Furthermore, the amounts of MMP-2, MMP-9, and MT1-MMP mRNA were analyzed in the cells. MMP-2, MMP-9, and MT1-MMP mRNA expression were suppressed by naringenin with time and dose-dependent. These results demonstrate that anti-metastatic activities of naringenin resulted from blocking of invasion of the HT-1080 cells. Taken together, the results of this studies provide evidence that naringenin possess an anti-metastatic activity.