• Title/Summary/Keyword: Inhibiting rate

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Herbicidal Activity of Rotation Crop Residues on Weeds and Selectivity to Crops (윤작작물 잔류물의 제초활성 및 작물에 대한 선택성)

  • Uddin, Md. Romij;Pyon, Jong-Yeong
    • Korean Journal of Agricultural Science
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    • v.37 no.1
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    • pp.1-6
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    • 2010
  • Allelopathic activity of rotation crop residues to common weeds and selectivity of crops were studied for developing an alternative weed control strategy in upland organic farming. All rotation crop residues with various ratios suppressed weed growth, but the growth of crop species stimulated a little when those were grown with the mixture of rotation crop residues except a few crop species. Among the rotation crop residues used in this study hairy vetch was the most effective, followed by Chinese milkvetch, barley and rye in suppression of weed growth. The 90:10 (crop:soil, v/v) treatments incorporation rate of crop residues such as hairy vetch and Chinese milkvetch suppressed completely the growth of all weed species tested in this study. The effect of crop residues on suppression of weed growth reduced to 90% when the incorporation rates decreased to 60% [60:40 (crop:soil, v/v). It was noticed that broadleaf weed species were more susceptible to rotation crop residues than grass weed species. In the influence of crop residues on the crop growth, no growth inhibition was found in red pepper, lettuce and perllia at any incorporation rates, but tomato, cucumber and corn were slightly inhibited in a few cases at their highest incorporation levels. This study demonstrated that rotation crop residues especially hairy vetch and Chinese milkvetch have high herbicidal effects against weeds without inhibiting the growth of crop species.

The Relationshin between ACE Inhibitory Activity and Degradations of Sulfur Containing Materials in Dolsan Leaf Mustard Juice

  • Yoo Eun-Jeong;Choi Myeong-Rak;Lim Hyun-Soo
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.9 no.5
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    • pp.400-404
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    • 2004
  • This Study was tarried out to investigate the relationship ACE inhibitory activity and degradations of sulfur containing materials in Dolsan leaf mustard juice (DLMJ). The changes of sulfur containing materials which were treated with autolysis, myrosinase, ascorbate and papain were studied, as well as the changes of ACE inhibitory activity in DLMJ. At $37^{\circ}C$, sulfur contain-ing materials by autolysis decreased most rapidly from $0.43\%$ to $0.13\%$ in the second day. Conversely. ACE inhibitory activity increased most from $66\%$ to $87\%$. in the second day at $37^{\circ}C$. As myrosinase concentrations increased more, sulfur containing materials in DLMJ decreased more. The ACE inhibitory activities at 0, 0.5, 1, 2, and 4 Units of myrosinase for 240 min later were 70, 74, 75, 82, and $85\%$, respectively. At 1 mM ascorbate. concentrations of Sulfur containing materials in DLMJ decreased more significantly on the second day than on the other days. At 1 mM ascorbate for 6 days, ACE Inhibitory activity reached a maximum of about $92\%$. And, an increase of papain concentration was noted in accordance with a decreased sulfur containing materials. The maximum rate of AEC inhibitory activity at control, 3, 6, and 12 Units of papains treatments was shown as 70, 70, 75, and $78\%$ at 60 min, respectively. These results suggested that the degradation of sulfur containing materials led to the increase of ACE inhibitory activity. Consequently, it was suggested that ACE inhibiting was significantly related to the degradatives of sulfur containing materials.

Stability Improvement of Esomeprazole Magnesium Dihydrate Enteric-Coated Tablet by Adding Alkalizing Agents (에스오메프라졸 마그네슘 이수화물을 함유하는 장용성 제제의 안정성 개선)

  • Cho, Young Ho;Jeon, Hyo Bin;Lee, Jong-Hwa;Lee, Gye Won
    • KSBB Journal
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    • v.32 no.2
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    • pp.108-116
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    • 2017
  • Omeprazole, a benzimidazole derivative, suppresses gastric acid secretion by inhibiting $H^+/K^+$ ATPase in gastric parietals cells, and by reducing $H^+$ concentration. To improve stability of esomeprazole magnesium dihydrate (ESMD), enteric-coated preperation was composed of core tablet, subcoating and enteric coating layer. We were evaluated in vitro dissolution characteristics between test and reference ESMD preparation and stability. We could prepare enteric-coated formulation of ESMD by controlling disintegrating agent and coating ratio which could rapidly dissolved in neutral or alkali medium. The formulation D5 with crospovidone of 1.25% and coating ratio of 16.25% had a similar dissolution behavior compare to reference preparation. Difference factor ($f_1$) and similarity factor ($f_2$) were 0~15 and 50~100 and there was no significant difference in bioequivalence between formulations. The content and dissolution rate of formulation D5 were $96.54{\pm}0.21$ and $78.56{\pm}0.87%$ without change of color in accelerated condition ($40^{\circ}C$, RH 75%, high density polyethylene (HDPE) container) for 6 months. This study concluded that our enteric coated preparation of ESMD could be an useful method to improve stability of unstable drug without direct contact with coating material.

Physalin D inhibits RANKL-induced osteoclastogenesis and bone loss via regulating calcium signaling

  • Ding, Ning;Lu, Yanzhu;Cui, Hanmin;Ma, Qinyu;Qiu, Dongxia;Wei, Xueting;Dou, Ce;Cao, Ning
    • BMB Reports
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    • v.53 no.3
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    • pp.154-159
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    • 2020
  • We investigated the effects of physalin A, B, D, and F on osteoclastogenesis induced by receptor activator of nuclear factor κB ligand (RANKL). The biological functions of different physalins were first predicted using an in silico bioinformatic tool (BATMAN-TCM). Afterwards, we tested cell viability and cell apoptosis rate to analyze the cytotoxicity of different physalins. We analyzed the inhibitory effects of physalins on RANKL-induced osteoclastogenesis from mouse bone-marrow macrophages (BMMs) using a tartrate-resistant acid phosphatase (TRAP) stain. We found that physalin D has the best selectivity index (SI) among all analyzed physalins. We then confirmed the inhibitory effects of physalin D on osteoclast maturation and function by immunostaining of F-actin and a pit-formation assay. On the molecular level, physalin D attenuated RANKL-evoked intracellular calcium ([Ca(2+)](i)) oscillation by inhibiting phosphorylation of phospholipase Cγ2 (PLCγ2) and thus blocked the downstream activation of Ca2+/calmodulin-dependent protein kinases (CaMK)IV and cAMP-responsive element-binding protein (CREB). An animal study showed that physalin D treatment rescues bone microarchitecture, prevents bone loss, and restores bone strength in a model of rapid bone loss induced by soluble RANKL. Taken together, these results suggest that physalin D inhibits RANKL-induced osteoclastogenesis and bone loss via suppressing the PLCγ2-CaMK-CREB pathway.

FADD Phosphorylation Modulates Blood Glucose Levels by Decreasing the Expression of InsulinDegrading Enzyme

  • Lin, Yan;Liu, Jia;Chen, Jia;Yao, Chun;Yang, Yunwen;Wang, Jie;Zhuang, Hongqin;Hua, Zi-Chun
    • Molecules and Cells
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    • v.43 no.4
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    • pp.373-383
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    • 2020
  • Our previous study revealed a novel role of Fas-associated death domain-containing protein (FADD) in islet development and insulin secretion. Insulin-degrading enzyme (IDE) is a zinc metalloprotease that selectively degrades biologically important substrates associated with type 2 diabetes (T2DM). The current study was designed to investigate the effect of FADD phosphorylation on IDE. We found that the mRNA and protein levels of IDE were significantly downregulated in FADD-D mouse livers compared with control mice. Quantitative real-time polymerase chain reaction analysis showed that FADD regulates the expression of IDE at the transcriptional level without affecting the stability of the mRNA in HepG2 cells. Following treatment with cycloheximide, the IDE protein degradation rate was found to be increased in both FADD-D primary hepatocytes and FADD-knockdown HepG2 cells. Additionally, IDE expression levels were reduced in insulin-stimulated primary hepatocytes from FADD-D mice compared to those from control mice. Moreover, FADD phosphorylation promotes nuclear translocation of FoxO1, thus inhibiting the transcriptional activity of the IDE promoter. Together, these findings imply a novel role of FADD in the reduction of protein stability and expression levels of IDE.

A Novel All-trans Retinoid Acid Derivative N-(3-trifluoromethyl-phenyl)-Retinamide Inhibits Lung Adenocarcinoma A549 Cell Migration through Down-regulating Expression of Myosin Light Chain Kinase

  • Fan, Ting-Ting;Cheng, Ying;Wang, Yin-Feng;Gui, Shu-Yu;Chen, Fei-Hu;Zhou, Qing;Wang, Yuan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.18
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    • pp.7687-7692
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    • 2014
  • Aim: To observe the effects of a novel all-trans retinoid acid (ATRA) derivative, N-(3-trifluoromethyl-phenyl)-retinamide (ATPR), on lung adenocarcinoma A549 cells and to explore the potential mechanism of ATPR inhibiting of A549 cell migration. Materials and Methods: The cytotoxicity of ATRA and ATPR on A549 cells was assessed using MTT assay. Wound healing assays were used to analyze the influences of ATRA, ATPR, ML-7 (a highly selective inhibitor of myosin light chain kinase (MLCK)), PMA (an activator of MAPKs) and PD98059 (a selective inhibitor of ERK1/2) on the migration of A549 cells. Expression of MLCK and phosphorylation of myosin light chain (MLC) were assessed by Western blotting. Results: ATRA and ATPR inhibited the proliferation of A549 cells in a dose- and time-dependent manner, and the effect of ATPR was much more remarkable compared with ATRA. Relative migration rate and migration distance of A549 cells both decreased significantly after treatment with ATPR or ML-7. The effect on cell migration of PD98059 combining ATPR treatment was more notable than that of ATPR alone. Moreover, compared with control groups, the expression levels of MLCK and phosphorylated MLC in A549 cells were both clearly reduced in ATRA and ATPR groups. Conclusions: ATPR could suppress the migration and invasion of A549 cells, and the mechanism might be concerned with down-regulating the expression of MLCK in the ERK-MAPK signaling pathway, pointing to therapeutic prospects in lung cancer.

Ca2+-ATPase and cAMP-mediated Anti-Apoptotic Effects of Acanthopanax senticosus Extracts on Ischemia/Reperfusion Liver Damages

  • Xie, Guang-Hua;Jeong, Jae-Hun;Choi, Sun Eun;Jeong, Seung Il;Park, Kwang-Hyun
    • Korean Journal of Plant Resources
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    • v.30 no.6
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    • pp.647-653
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    • 2017
  • Hepatic ischemia-reperfusion injury (HIRI) is linked with high mortality rate. Several agents have been developed so far to reduce the risk of HIRI. In this study, we investigated the effects of Acanthopanax senticosus extract (AS) on hepatic ischemia-reperfusion. To explore the protective effects of A. senticosus extract injection (ASI) on hepatic ischemia-reperfusion injury rats animal model were used. After the development of HIRI by using clamping method rats were then randomly divided into five groups. Different doses of AS were administered in HIRI rat model. The level of ALT, AST, and MDA content in serum were detected in sham and HIRI groups. The activity of SOD, MPO and $Ca^{2+}-ATPase$, content of MDA, and cAMP in hepatic tissue were also measured. Expression of Bcl-2 and Bax protein were detected by immunohistochemical staining method. Compared with sham group, ASI has the protective effect on the HIRI model in rats. Blood levels of ALT, AST, SOD, MPO, and MDA were significantly lower in ASI group compared with HIRI. Indeed SOD and $Ca^{2+}-ATPase$ activities, MDA content, and cAMP level were improved in ASI group. Furthermore, Bcl-2 and Bax protein were improved in ASI group compared with only HIRI group. These results suggest that AS may provide potential ameliorative therapy by inhibiting the damage signaling mechanism in hepatic ischemia/reperfusion injury model.

Induced Ovulation by using Human Chorionic Gonadotropin and Gonadotropin-Releasing Hormone Analogue plus Pimozide in Yellow Puffer, Takifugu obscurus (인간의 태반성 성선자극호르몬 또는 성선자극호르몬-방출호르몬 유도체와 Pimozide에 의한 황복의 배란유도)

  • Jang, Seon-Il
    • Journal of Aquaculture
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    • v.9 no.1
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    • pp.3-10
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    • 1996
  • Ovulation of maturing female yellow puffer, Takifugu obscrus, was induced by using single injection of human chorionic gonadotropin (HCG) or gonadotropin releasing hormone-analogue (GnRH-A) $des-Gly^{10}[D-Ala^6]$ GnRH-ethylamide plus pimozide. The response was evaluated using the fertilization and embryo-formation rate after insemination and the gonadotropin (GTH) level in blood plasma using radioimmunoassay. In the fertilization and embryo-formation, maximal effects were recorded by using 1,000 IU/kg HCG or $10\;{mu}g/kg$ GnRH-A plus 5 mg/kr pimozide. Pimozide (1, 5 mg/kg) or GnRH-A treatment alone was not effective in elevation of GTH level, however combinations of these treatments were particularly effective. Injection of dopamine blocked the rapid elevation of plasma GTH levels of blood. These data suggest that yellow puffer secrete GnRH and gonadotropin-releasing-inhibiting factor during the spawning or the other period.

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Effects of Water-Soluble Polysaccharides from Tott on Lipid Absorption and Animal Body Weight (톳 유래 수용성 다당류의 Lipase 저해활성과 지질 및 체중변화에 미치는 영향)

  • Baek, Gu;Goo, Bon Geun;Ahn, Byung Jae;Park, Jae Kweon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.42 no.4
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    • pp.556-562
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    • 2013
  • We examined the anti-obesity effects of water-soluble polysaccharides (WSP-A) extracted from the seaweed Hijikia fusiforme (Tott in Korean). The extracted alginate-like polysaccharide (verified by FT-IR and HPAEC-PAD analysis) was examined in a lipase inhibition assay and animal experiments. WSP-A inhibited lipase up to 30%, with over 80% of the initial activity retained until the 1 hour reaction in vitro. There was a 30% loss in the rate of weight gain in rats fed a high-fat diet. WSP-A therefore seems to serve as a healthy weight loss agent by inhibiting lipases, thus preventing the absorption of fat in the body.

Targeting of COX-2 Expression by Recombinant Adenovirus shRNA Attenuates the Malignant Biological Behavior of Breast Cancer Cells

  • Tu, Bo;Ma, Ting-Ting;Peng, Xiao-Qiong;Wang, Qin;Yang, Hong;Huang, Xiao-Ling
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.20
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    • pp.8829-8836
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    • 2014
  • Background: Cyclooxygenase-2 (COX-2), considered to have tumor-promoting potential, is highly expressed in a variety of tumors, including breast cancer. Since the functions and action mechanisms of COX-2 in breast cancer have not been fully elucidated, in the present study, the effects of target inhibiting COX-2 with recombinant adenovirus Ad-COX-2-shRNA on malignant biological behavior were investigated in representative cell lines. Materials and Methods: Breast cancer MDA-MB-231 and MCF-7 cells were transfected with Ad-COX-2-shRNA and COX-2 expression was tested by RT-PCR and Western blotting. Changes in proliferation, apoptosis and invasion of breast cancer cells were detected with various assays including MTT, colony forming, flowcytometry and Transwell invasion tests. The expression of related proteins involved in the cell cycle, apoptosis, invasion and signaling pathways was assessed by Western blotting. Results: COX-2 expression was significantly reduced in both breast cancer cell lines infected with Ad-COX-2-shRNA, with obvious inhibition of proliferation, colony forming rate, G2/M phase passage and invasion, as well as induction of apoptosis, in MDA-MB-231 and MCF-7 cells, respectively. At the same time, proteins related to the cell cycle, anti-apoptosis and invasion were significantly downregulated. In addition, c-myc expression and phosphorylation activation of Wnt/${\beta}$-catenin and p38MAPK pathways were reduced by the Ad-COX-2-shRNA. Conclusions: COX-2 expression is associated with proliferation, apoptosis and invasion of breast cancer cells, and its mechanisms of action involve regulating expression of c-myc through the p38MAPK and Wnt/${\beta}$-catenin pathways.