• Title/Summary/Keyword: inhibiting activity

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Anti-platelet effects of Artesunate through Regulation of Cyclic Nucleotide on Collagen-induced Human Platelets

  • Dong-Ha Lee
    • Biomedical Science Letters
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    • v.29 no.1
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    • pp.41-47
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    • 2023
  • Discovery of new substance that can regulate platelet aggregation or suppress aggregation will aid in the prevention and treatment of cardiovascular diseases. Artesunate is a compound from plant roots of Artemisia or Scopolia, and its effects have shown to be promising in areas of anticancer and Alzheimer's disease. However, the role and mechanisms by which artesunate affects the aggregation of platelets, and the formation of a thrombus are currently not understood. This study examined the ways artesunate affects platelets activation and thrombus formation induced by collagen. As a result, cAMP and cGMP production were increased significantly by artesunate relative to the doses, as well as phosphorylated VASP and IP3R, substrates to cAMP-dependent kinase and cGMP-dependent kinase, in a significant manner. The Ca2+ normally mobilized from the dense tubular system was inhibited due to IP3R, phosphorylation from artesunate, and phosphorylated VASP aided in inhibiting platelet activity via αIIb/β3 platelet membrane inactivation and inhibiting fibrinogen binding. Finally, artesunate inhibited thrombin-induced thrombus formation. Therefore, we suggest that artesunate has importance with cardiovascular diseases stemming from the abnormal platelets activation and thrombus formation by acting as an effective prophylactic and therapeutic agent.

Polarization Behavior and Corrosion Inhibition of Copper in Acidic Chloride Solution Containing Benzotriazole

  • Sang Hee Suh;Youngjoon Suh
    • Corrosion Science and Technology
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    • v.22 no.3
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    • pp.137-152
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    • 2023
  • Polarization behavior and corrosion inhibition of copper in acidic chloride solutions containing benzotriazole were studied. Pourbaix diagrams constructed for copper in NaCl solutions with different BTAH concentrations were used to understand the polarization behavior. Open circuit potential (OCP) depended not only on chloride concentration, but also on whether a CuBTA layer was formed on the copper surface. Only when the (pH, OCP) was located well in the CuBTA region of the Pourbaix diagram, a stable corrosion inhibiting CuBTA layer was formed, which was confirmed by X-ray Photoelectron Spectroscopy (XPS) and a long-term corrosion test. The OCP for the CuBTA layer decreased logarithmically with increasing [Cl-] activity in the solution. A minimum BTAH concentration required to form a CuBTA layer for a given NaCl concentration and pH were determined from the Pourbaix diagram. It was found that 320 ppm BTAH solution could be used to form a corrosion-inhibiting CuBTA layer inside the corrosion pit in the sprinkler copper tube, successfully reducing water leakage rate of copper tubes. These experimental results could be used to estimate water chemistry inside a corrosion pit.

Polygonatum sibiricum component liquiritigenin restrains breast cancer cell invasion and migration by inhibiting HSP90 and chaperone-mediated autophagy

  • Suli Xu;Zhao Ma;Lihua Xing;Weiqing Cheng
    • The Korean Journal of Physiology and Pharmacology
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    • v.28 no.4
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    • pp.379-387
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    • 2024
  • Breast cancer (BC) is most commonly diagnosed worldwide. Liquiritigenin is a flavonoid found in various species of the Glycyrrhiza genus, showing anti-tumor activity. This article was to explore the influences of liquiritigenin on the biological behaviors of BC cells and its underlying mechanism. BC cells were treated with liquiritigenin alone or transfected with oe-HSP90 before liquiritigenin treatment. RT-qPCR and Western blotting were employed to examine the levels of HSP90, Snail, E-cadherin, HSC70, and LAMP-2A. Cell viability, proliferation, migration, and invasion were evaluated by performing MTT, colony formation, scratch, and Transwell assays, respectively. Liquiritigenin treatment reduced HSP90 and Snail levels and enhanced E-cadherin expression as well as inhibiting the proliferation, migration, and invasion of BC cells. Moreover, liquiritigenin treatment decreased the expression of HSC70 and LAMP-2A, proteins related to chaperone-mediated autophagy (CMA). HSP90 overexpression promoted the CMA, invasion, and migration of BC cells under liquiritigenin treatment. Liquiritigenin inhibits HSP90-mediated CMA, thereby suppressing BC cell growth.

Role of $Na^+\;-K^+$ Pump on Endothelium-dependent Relaxation

  • Sung, Sang-Hyun;Roh, Joon-Ryang;Park, Tae-Sic;Suh, Suk-Hyo;Hwang, Sang-Ik;Kim, Ki-Whan
    • The Korean Journal of Physiology
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    • v.27 no.2
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    • pp.199-207
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    • 1993
  • To study the underlying mechanism through which the endothelium-dependent relaxation is inhibited by blocking the $Na^+\;-K^+$ pump, the effects of $Na^+\;-K^+$ pump blockade on the release of EDRF and its relaxing activity were examined, using organ bath study, bioassay technique, and cGMP measurement. Endothelium-dependent relaxation was attenuated by blocking the $Na^+\;-K^+$ pump in the vascular ring with intact endothelium. In bioassay experiment EDRF release was decreased with the blockade of the $Na^+\;-K^+$ pump in the EDRF donor strip. Endothelium-dependent increase of cGMP level was suppressed by inhibiting the $Na^+\;-K^+$ pump in the test strips. The magnitude of relaxation of test strip which was induced by the perfusate that had passed through the EDRF donor strip was decreased with the blockade of the $Na^+\;-K^+$ pump in the test strip. Therefore, it could be suggested that the attenuation of endothelium-dependent relaxation caused by inhibiting $Na^+\;-K^+$ pump activity is due to both the decreased release of EDRF from endothelial cells and the decreased sensitivity of the smooth muscle cells to EDRF.

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Bowman-Birk type proteinase inhibitors from soybean : Isolation and partial characterization (대두 Bowman-Birk형 proteinase inhibitor들의 분리 및 성질)

  • Choi, Ki-Bong;Kim, Su-Il
    • Applied Biological Chemistry
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    • v.33 no.4
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    • pp.287-292
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    • 1990
  • Eight(I through VII) of Bowman-Birk proteinase inhibitor have been isolated from soybean with DEAE-Sephadex A-50. Inhibitor VII was a typical BBTI, showing high cysteine content(17%/mole) ud low trypsin to chymotrypsin inhibiting activity(TIA/CIA= 1.0) with the independent reactive site to each enzyme. Dissociation constant of trypsin-BBTI and chymotrypsin-BBTl complexes were $9.17{\times}10^{-9}M$ and $5.14{\times}10^{-8}M$, respectively. Inhibitor Vll was extremely heat stable. Six hours heat treatment at $100^{\circ}C$ caused only 50% decrease in it's original inhibiting activity. Except inhibitor III,6 other isoinhibitors differed from a typical BBTI in TIA/CIA, values, ranging from 3 to 29.

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Effects of Bojeongjeongcheon-tang on Cytokines and Immunoglobulin E in B Cells (보정정천탕의 Cytokine 및 IgE에 대한 조절효과)

  • 권혁성;정주호;김성훈;정승기
    • The Journal of Korean Medicine
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    • v.25 no.2
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    • pp.51-66
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    • 2004
  • Objectives : To evaluate experimentally the clinical effect of Bojeongjeongcheon-tang, we observed the cytokines ($IL-1{\beta}$/TEX>, IL-4, IL-5, IL-6, IL-10, TNF-{\alpha},{\;}TGF-{\beta},{\;}IFN-{\gamma}$) and what effect they have on IgE in B cells of a rat. Methods : First of all, we extracted the spleens of healthy Balb/c mice and separated B cells from them. These B cells were cultured with anti-CD40 mAb (500 ng/ml), rmIL-4 (500 U/ml), Bojeongjeongcheon-tang (100 ug/ml, 10 ug/ml, 1 ug/ml). We used rmiL-10 (50 ng/ml) as a control group. Furthermore, we analyzed the expression of IgE, CD23, CD69 and the coherence of HRF in B cells using a flow cytometer. We also analyzed the cytokine gene expression in B cells by reverse transcriptase-PCR. We also measured B cells proliferation using the Liquid Scintillation Counter. Results : In this study, the Bojeongjeongcheon-tang treated group showed a tendency to decrease depending on the density compared with the control group in the expression of IgE+, CD23+, CD69, HRF. All of the Bojeongjeongcheon-tang treated group showed inhibitory effects with $IL-1{\beta}$, IL-4, IL-5 and proliferating effects with IL-6, IL-10, and $IFN-{\gamma}$ on cytokines transcript expression depending on the density. Meanwhile, $TNF-{\alpha}$ increased in all density. In IgE production, there was inhibitory effect on Bojeongjeongcheon-tang (both 100 ug/ml and 10 ug/ml) of significance (p < 0.01, p < 0.05). Also in B cell proliferation, the result revealed an inhibitory effect of Bojeongjeongcheon-tang (both 100 ug/ml and 10 ug/ml), of significance (p < 0.001, p < 0.01). Conclusions : This study shows that Bojeongjeongcheon-tang has an inhibitory effect on the production and activity of B cells. Also it inhibited CD23, IL-4 activity and IgE production and activation. It is obvious that Bojeongjeongcheon-tang treats asthma by inhibiting the production of histamine and HRF, IL-5 and proliferating IL-10. Also Bojeongjeongcheon-tang has some preventive effects on bronchial change by inhibiting $TGF-{\beta}$, which stimulates the bronchial transformation.

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Curcumin Analogue A501 induces G2/M Arrest and Apoptosis in Non-small Cell Lung Cancer Cells

  • Xia, Yi-Qun;Wei, Xiao-Yan;Li, Wu-Lan;Kanchana, Karvannan;Xu, Chao-Chao;Chen, Da-Hui;Chou, Pei-Hong;Jin, Rong;Wu, Jian-Zhang;Liang, Guang
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.16
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    • pp.6893-6898
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    • 2014
  • Curcumin and its analogues have been reported to exert anti-cancer activity against a variety of tumors. Here, we reported A501, a new curcumin analogue. The effect of A501 on cell viability was detected by MTT assay, the result showed that A501 had a better inhibiting effect on the four non-small cell lung cancer (NSCLC) cells than that of curcumin. Moreover, Colony forming experiment showed A501 significant restrained cell proliferation. Flow cytometry displayed A501 can cause G2/M arrest and induce apoptosis. Western blotting showed that A501 decreased the expression of cyclinB1, cdc-2, bcl-2, while increased the expression of p53, cleaved caspase-3 and bax. In conclusion, curcumin analogues A501 played antitumor activity by inhibiting cell proliferation and inducing apoptosis of NSCLC cells. And it was likely to be a promising starting point for the development of curcumin-based anticancer drugs.

Black soybean anthocyanins attenuate inflammatory responses by suppressing reactive oxygen species production and mitogen activated protein kinases signaling in lipopolysaccharide-stimulated macrophages

  • Kim, Jin Nam;Han, Sung Nim;Ha, Tae Joung;Kim, Hye-Kyeong
    • Nutrition Research and Practice
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    • v.11 no.5
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    • pp.357-364
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    • 2017
  • BACKGROUND/OBJECTIVES: Oxidative stress is closely related with inflammation and development of many diseases. Black soybean seed coat contains high amount of anthocyanins, which are well-known for free radical scavenging activities. This study investigated inflammatory response and action mechanism of black soybean anthocyanins with regard to antioxidant activity in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. MATERIALS/METHODS: RAW 264.7 cells were treated with anthocyanins extracted from black soybean seed coats in a concentration range of 12.5 to $100{\mu}g/mL$. The production of reactive oxygen species (ROS), secretion of pro-inflammatory mediators and cytokines, and the signaling in the mitogen activated protein kinases (MAPKs) pathway were examined. RESULTS: Black soybean anthocyanins significantly decreased LPS-stimulated production of ROS, inflammatory mediators such as nitric oxide (NO) and prostaglandin $E_2$, and pro-inflammatory cytokines, including tumor necrosis factor ${\alpha}$ and interleukin-6, in a dose-dependent manner without cytotoxicity (P < 0.001). Black soybean anthocyanins downregulated the expression of inducible NO synthase and cyclooxygenase-2 in LPS-stimulated RAW 264.7 cells (P < 0.001). Moreover, black soybean anthocyanins inhibited LPS-induced phosphorylation of MAPKs, including extracellular signal-regulated kinase, c-Jun N-terminal kinase, and p38 (P < 0.001). CONCLUSION: These results suggest that black soybean anthocyanins exert anti-inflammatory activity by inhibiting ROS generation and subsequent MAPKs signaling, thereby inhibiting inflammatory responses.

Study of Mori Fructus and Dried Mori Fructus Extracts on the Antioxidant Effect and the Inhibitory Effect on Adipocyte Differentiation (상심자와 건조상심자 추출물의 항산화 효과 및 전지방세포 분화억제 효과에 관한 연구)

  • Kim, Hyung-Gu;Wang, Jing-Hua;Lim, Dong-Woo;Chae, Hee-Sung;Chin, Young-Won;Choi, Han-Seok;Kim, Hojun
    • Journal of Korean Medicine Rehabilitation
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    • v.24 no.4
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    • pp.1-13
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    • 2014
  • Objectives This study was to investigate the antioxidative capacity, antiobesity effect and anti-diabetes effects of Mori Fructus and dried Mori Fructus in Raw 264.7 cells and 3T3-L1 cells. Methods 3 different types of Mori Fructus extracts (water 100%, ethanol 30%, ethanol 100%) were used in this study. And 3 different types of dried Mori Fructus extracts (water 100%, ethanol 30%, ethanol 100%) were used in this study. Total polyphenol compund, total favonoid compound, DPPH radical scavenging, ROS activity, NO, cell proliferation were measured in the experiment. Expressions of adipogenic transcription factors including $C/EBP-{\alpha}$, $C/EBP-{\beta}$, $PPAR-{\alpha}$, $PPAR-{\gamma}$, $AMPK-{\alpha}$ were analyzed by Real time PCR. Results Mori Fructus extracts measurements are higher than dried Mori Fructus extracts measurements at Total flavonoid compound and total flavonoid compound. Mori Fructus extracts measurements are lower than dried Mori Fructus extracts measurements at DPPH radical scavenging, ROS activity, NO. In RT-PCR analysis, there is a tendency that dried Mori Fructus extracts inhibit the expression of $C/EBP-{\alpha}$, $C/EBP-{\beta}$ genes. In RT-PCR analysis, there is a tendency that dried Mori Fructus extracts promote the expression of $PPAR-{\alpha}$, $PPAR-{\gamma}$, $AMPK-{\alpha}$ genes. Conclusions Mori Fructus is effective on inhibiting the oxidation and dried Mori Fructus is effective on inhibiting the obesity and diabetes.

Conditioned Media of ASC-17D Sertoli Cells Induce G1-Growth Arrest of DU145 Human Prostate Cancer Cells

  • Kang, Hyeog;Kang, Sang-Wook;Choi, Sang-Hyun;Lee, Kwang-Ho;Chun, Boe-Gwun;Min, Bon-Hong
    • BMB Reports
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    • v.31 no.5
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    • pp.508-514
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    • 1998
  • We studied the effects of ASC-17D rat Sertoli cell-conditioned media (rSCCM) on the proliferation of the DU145 prostate cancer cells. rSCCM was prepared from ASC-17D cells cultured in DMEM/F-12 serum-free media at a nonpermissive temperature of $40^{\circ}C$, which is the condition for the high expression of c1usterin. We found that rSCCM could inhibit the proliferation of DU145 cells by arresting the cell cycle in the G1 phase in a dose-dependent manner. This growth arresting activity was abolished by boiling rSCCM for 5 min. The G1 growth-inhibiting activity of rSCCM was also detected in other prostate-originated cancer cells examined (i.e., LNCaP and PC-3) but not in other cells (ASC-17D, HepG2, SK-N-SH, and NIH3T3). Western blot analysis of partially purified growth inhibiting fractions with the clusterin antibody showed that the cytostatic factor in rSCCM was not c1usterin. This cytostatic factor was semi purified by DEAE-Sepharose, ammonium sulfate precipitation, and Phenyl-Sepharose column chromatography, and was estimated to have a molecular weight of 88 kDa by Sephacryl S-300 gel filtration.

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