• Title/Summary/Keyword: ${\alpha}_i$-properties

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TI-I-174, a Synthetic Chalcone Derivative, Suppresses Nitric Oxide Production in Murine Macrophages via Heme Oxygenase-1 Induction and Inhibition of AP-1

  • Kim, Mi Jin;Kadayat, Taraman;Kim, Da Eun;Lee, Eung-Seok;Park, Pil-Hoon
    • Biomolecules & Therapeutics
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    • v.22 no.5
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    • pp.390-399
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    • 2014
  • Chalcones (1,3-diaryl-2-propen-1-ones), a flavonoid subfamily, are widely known for their anti-inflammatory properties. Propenone moiety in chalcones is known to play an important role in generating biological responses by chalcones. In the present study, we synthesized chalcone derivatives structurally modified in propenone moiety and examined inhibitory effect on nitric oxide (NO) production and its potential mechanisms. Among the chalcone derivatives used for this study, TI-I-174 (3-(2-Hydroxyphenyl)-1-(thiophen-3-yl)prop-2-en-1-one) most potently inhibited lipopolysaccharide (LPS)-stimulated nitrite production in RAW 264.7 macrophages. TI-I-174 treatment also markedly inhibited inducible nitric oxide synthase (iNOS) expression. However, TI-I-174 did not significantly affect production of IL-6, cyclooxygenase-2 (COX-2) and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), implying that TI-I-174 inhibits production of inflammatory mediators in a selective manner. Treatment of macrophages with TI-I-174 significantly inhibited transcriptional activity of activator protein-1 (AP-1) as determined by luciferase reporter gene assay, whereas nuclear factor-${\kappa}B$ (NF-${\kappa}B$) activity was not affected by TI-I-1744. In addition, TI-I-174 significantly inhibited activation of c-Jun-N-Terminal kinase (JNK) without affecting ERK1/2 and p38MAPK, indicating that down-regulation of iNOS gene expression by TI-I-174 is mainly attributed by blockade of JNK/AP-1 activation. We also demonstrated that TI-I-174 treatment led to an increase in heme oxygenase-1 (HO-1) expression both at mRNA and protein level. Transfection of siRNA targeting HO-1 reversed TI-I-174-mediated inhibition of nitrite production. Taken together, these results indicate that TI-I-174 suppresses NO production in LPS-stimulated RAW 264.7 macrophages via induction of HO-1 and blockade of AP-1 activation.

Magnetic Properties of $\alpha$-Fe Based Nd-Fe-B Nanocrystalline with High Remanence (고잔류자화 $\alpha$-Fe기 Nd-Fe-B 초미세결정립 합금의 자기특성)

  • 조용수;김윤배;박우식;김창석;김택기
    • Journal of the Korean Magnetics Society
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    • v.5 no.1
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    • pp.38-41
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    • 1995
  • The effects of Nb and Cu additives as will as substitutional Co into $Nd_{4}Fe_{85.5}B_{10.5}$ melt-spun alloy were studied aiming for finding a $\alpha$-Fe based Nd-Fe-B composite alloys with high energy product. The addition of Nb and Cu to $Nd_{4}Fe_{85.5}B_{10.5}$ decreased the average grain size and increased the coercivity up to 207kA/m(2.6kOe), Further-more, the substitution of Co for Fe in $Nd_{4}Fe_{82}B_{10}Nb_{3}Cu_{1}$ alloy resulted in the decrease of the average grain size (<20nm) and improved the hard magnetic properties. The remanence, coercivity and energy product of optimally annealed $Nd_{4}Fe_{74}Co_{8}B_{10}Nb_{3}Cu_{1}$ alloy were 1.345, 219kA/m(2.75kOe) and $95.5kJ/m^{3}$(12MGOe), respectively.

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The Search of fig Pheromonal Odorants for Biostimulation Control System Technologies: I. Ligand Based Molecular Shape Similarity of 5$\alpha$-androst-16-en-3-one Analogous and Their Physicochemical Parameters (생물학적 자극 통제 수단으로서 활용하기 위한 돼지 페로몬성 냄새 물질의 탐색: I. 5$\alpha$-androst-16-en-3-one 유사체들의 리간드에 기초한 분자 유사성과 물리화학 파라미터)

  • 성낙도;김철호;진동일;박창식
    • Reproductive and Developmental Biology
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    • v.28 no.1
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    • pp.45-52
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    • 2004
  • To search a new porcine pheromonal odorants, this research for biostimulation and role of pheromone was augmented by means of "control system technologies" to offer a potentially useful and practical way to improve reproductive efficiency in livestock species. Therefore the 13 physicochemical parameters such as similarity indice (S), hydrophobicity (logP) and van der Waals molecule volume (MV) etc. of 54 steroid analogues, which are analogous of substrate molecules, 5$\alpha$-androst-16-en-3-one (P1) and 5$\alpha$-androst-16-en-3-ol (P2) of lipocalin as receptor of pig pheromones were calculated and discussed. The physicochemical properties of these steroid analogues were mainly followed by steric dissimilar of A and D ring in steroid nucleus. And we found that from correlation with S values and MV constants of molecules, the more MV constants are small, the more S values tend to approach 1. Based on this results, the S-values of 4-androsten-3,17-dione (P1-1) and 5 $\alpha$ -androstan-3-one (P2-1) were 1.0, respectively. The two compounds of them were chosen because they showed the same value each other at a side of hydrophobicity, molar refractivity and molecular volume. It is expected that the new two compounds will be able to substitute for P1 and P2, porcine pheromonal odorants.

Eryngium foetidum Suppresses Inflammatory Mediators Produced by Macrophages

  • Mekhora, Chusana;Muangnoi, Channarong;Chingsuwanrote, Pimjai;Dawilai, Suwitcha;Svasti, Saovaros;Chasri, Kaimuk;Tuntipopipat, Siriporn
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.2
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    • pp.653-664
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    • 2012
  • Objective: This study assessed anti-inflammatory and antioxidant activities of $E.$ $foetidum$ leaf extract on LPS-activated murine macrophages. Methods: RAW264.7 cells were pretreated with or without $E.$ $foetidum$ extract for 1 h prior to incubation with LPS for 24 h. Anti-inflammatory activity was evaluated with reference to iNOS, COX-2, TNF-${\alpha}$ and IL-6 gene expression. In addition, NO and intracellular ROS generation were determined by Griess method and fluorescence intensity and activation of MAPKs and $I{\kappa}B$ by Western blotting. Results: Prior treatment with $E.$ $foetidum$ leaf extract inhibited elevation of IL-6, TNF-${\alpha}$, iNOS and COX-2, together with their cognate mRNAs in a dose-dependent manner. NO and intracellular ROS contents were similarly reduced. These effects were due to inhibition of LPS-induced phosphorylation of JNK and p38 as well as $I{\kappa}B$. $E.$ $foetidum$ ethanol extract were shown to contain lutein, ${\beta}$-carotene, chlorogenic acid, kaempferol and caffeic acid, compounds known to exert these bioactive properties. Conclusions: $E.$ $foetidum$ leaf extract possesses suppressive effects against pro-inflammatory mediators. Thus, $E.$ $foetidum$ has a high potential to be used as a food supplement to reduce risk of cancer associated with inflammation.

Microstructural evolution and mechanical properties of $Al_{71.6}Ge_{28.4}$ eutectic alloy ($Al_{71.6}Ge_{28.4}$ 공정합금의 미세구조 및 기계적 성질의 평가)

  • Park, Jin-Man;Yook, Wan;Kim, Do-Hyang
    • Journal of Korea Foundry Society
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    • v.27 no.4
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    • pp.167-172
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    • 2007
  • In the present study, the microstructural evolution and mechanical properties of $Al_{71.6}Ge_{28.4}$ eutectic alloy have been investigated. Stable (fcc ${\alpha}$-Al and diamond cubic ${\beta}$-Ge) and various metastable crystalline (monoclinic, rhombohedral) phases were produced by competitive phase selection during non-equilibrium processing methods i.e. melt spinning and injection casting. The as-injection casted samples containing metastable-equilibrium eutectic (${\alpha}$-Al + monoclinic) structure showed much higher strength than samples with equilibrium eutectic (${\alpha}-Al+{\beta}-Ge$) structure but plasticity disappointingly diminished. In order to endow the enhanced ductility without significant strength drop, the alloys was heat-treated at transition temperature from metastable phase to stable phase. The annealed specimen displayed the phase transformed microstructural evolution and enhanced macroscopic plasticity.

A new extended alpha power transformed family of distributions: properties, characterizations and an application to a data set in the insurance sciences

  • Ahmad, Zubair;Mahmoudi, Eisa;Hamedani, G.G.
    • Communications for Statistical Applications and Methods
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    • v.28 no.1
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    • pp.1-19
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    • 2021
  • Heavy tailed distributions are useful for modeling actuarial and financial risk management problems. Actuaries often search for finding distributions that provide the best fit to heavy tailed data sets. In the present work, we introduce a new class of heavy tailed distributions of a special sub-model of the proposed family, called a new extended alpha power transformed Weibull distribution, useful for modeling heavy tailed data sets. Mathematical properties along with certain characterizations of the proposed distribution are presented. Maximum likelihood estimates of the model parameters are obtained. A simulation study is provided to evaluate the performance of the maximum likelihood estimators. Actuarial measures such as Value at Risk and Tail Value at Risk are also calculated. Further, a simulation study based on the actuarial measures is done. Finally, an application of the proposed model to a heavy tailed data set is presented. The proposed distribution is compared with some well-known (i) two-parameter models, (ii) three-parameter models and (iii) four-parameter models.

Mangiferin isolated from the rhizome of Anemarrhena asphodeloides inhibits the LPS-induced nitric oxide and prostagladin $E_2$ via the $NF-{\kappa}B$ inactivation in inflammatory macrophages

  • Shin, Ji-Sun;Noh, Young-Su;Kim, Dong-Hyun;Cho, Young-Wuk;Lee, Kyung-Tae
    • Natural Product Sciences
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    • v.14 no.3
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    • pp.206-213
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    • 2008
  • This study was designed to investigate the anti-inflammatory effects of mangiferin isolated from the rhizome of Anemarrhena asphodeloides, a natural polyphenol, on lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. Mangiferin dose-dependently inhibited LPS-induced nitric oxide (NO) and prostaglandin $E_2\;(PGE_2)$ productions in RAW 264.7 macrophages and peritoneal macrophages isolated from C57BL/6 mice. Consistent with these data, mangiferin suppressed the LPS-induced expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) at the protein and mRNA levels in a concentration-dependent manner, as determined by Western blotting and RT-PCR, respectively. In addition, the release of tumor necrosis $factor-{\alpha}$($TNF-{\alpha}$) and interleukin-6 (IL-6), and the mRNA expression levels of these cytokines were reduced by mangiferin in a dose-dependent manner. Moreover, mangiferin effectively inhibited the transcriptional activation of nuclear factor-kappa B $(NF-{\kappa}B)$. These results suggest that the anti-inflammatory properties of mangiferin are caused by iNOS, COX-2, $TNF-{\alpha}$, and IL-6 down-regulation due to $(NF-{\kappa}B)$ inhibition in RAW 264.7 macrophages.

Effects of the Essential Oil Components from Ligusticum chuanxiong on Proinflammatory Mediators of RAW264.7 Macrophage Cells

  • Lim, Hye-Rim;Shin, Seung-Won
    • Natural Product Sciences
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    • v.16 no.4
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    • pp.259-264
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    • 2010
  • The essential oil fraction was obtained from the underground parts o of Ligusticum chuanxiong (Umbelliferae) by steam distillation, and its main components, Z-ligustilide and butylidene phthalide, were isolated by column chromatography. Its essential oil fraction and the isolated main components were examined for effects on their anti-inflammatory properties in RAW 264.7 macrophage cells to develop a new natural anti-inflammatory drug. The results showed that the L. chuanxiong essential oil fraction and its main components, Z-ligustilide and butylidene phthalide, inhibited the production of nitric oxide significantly in lipopolysaccharide (LPS)-treated RAW 264.7 cells. LPS-induced interleukin-$1{\beta}$ (IL-$1{\beta}$), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-$\alpha$) production was also decreased in a dose-dependent manner. In addition, western blot analysis revealed that the L. chuanxiong essential oil fraction and also its main components, Z-ligustilide, and butylidene phthalide reduced the expression levels of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS).

Influence of Roller Speed on Magnetic Properties and Structures of α-Fe/Nd2Fe14B Nanocomposite Magnets Prepared by Melt-spinning

  • Pei, Wenli;Lian, Fazeng;Fu, Meng;Zhou, Guiqin;Takahashi, M.
    • Journal of Magnetics
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    • v.9 no.4
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    • pp.101-104
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    • 2004
  • The crystallization behaviours of nanocomposite made by a function of quenching rate (roller speed) were studied. The results showed that there was one step c$\mathbb{r}$ystallization process for the alloy quenched at roller speed of 32 m/s, which could be shown as, Am (amorphouse) + ${\alpha}-Fe/Nd_2Fe_{14}B$ ${\rightarrow}$ ${\alpha}-Fe/Nd_2Fe_{14}B$ . For the alloy quenched at roller speed of 40 m/s, there was steps crystallization process taking place at different temperatures, which could be shown as, Am ${\rightarrow}$ ${\alpha}-Fe/Nd_2Fe_{23}B_3+Nd_2Fe_{14}B+Am`$ ${\rightarrow}$ ${\alpha}-Fe/Nd_2Fe_{14}B$. The presence of transition phase ($Nd_2Fe_{23}B_3$) was harmful to get fine and uniform grain size during crystallization process. Uniform microstructures and high magnetic properties could be attained for the as-quenched alloy containing less amorphous phase and no presence of transition phase during annealing treatment. For the alloy prepared at roller speed of 32 m/s, the following properties were obtained, $B_r= 0.904 T,_iH_c = 801 kA/m, (BH)_{max} = 122 kJ/m^3 and M_r/M_s = 0.6$.

Enzymatic Studies on the α-Galactosidases from Soybean and Aspergillus niger (대두(大豆) 및 Aspergillus niger α-galactosidase의 효소학적(酵素學的) 연구(硏究))

  • Keum, Jong-Hwa;Oh, Man-Jin
    • Korean Journal of Agricultural Science
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    • v.18 no.1
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    • pp.49-73
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    • 1991
  • To elucidate enzymatic properties of $\alpha$-galactosidases (EC3, 2, 1, 22) from germinated soybean and Aspergillus niger changes in the enzyme activities and oligosaccharide contents during germination of soybean were determined and $\alpha$-galactosidases from germinated soybean and wheat bran culture of Aspergillus niger were purified by ammonium sulfate fractionation, ion exchange chromatography and gel filtration. Their chemical and enzymatic properties were investigated and the results obtained were summarized as follows : 1. $\alpha$-Galactosidase activity of soybean was maximized when it was germinated at $25^{\circ}C$ for 120 hours. And raffinose and stachyose in soybean were decomposed completely after 96 hours and 120 hours of germination, respectively. 2. The highest level of $\alpha$-Galactosidase activity was obtained when Aspergillus niger was grown on wheat bran medium at $30^{\circ}C$ for 96 hours. 3. Soybean $\alpha$-galactosidase was purified by 6.6 fold by ammonium slufate fractionation, ion exchange chromatography on DEAE-Cellulose and Sephadex A-50., and gel filtration on Sephadex G-150. Its specific activity was 825 units/mg protein and the yield was 2.5% of the total activity of crude extracts. 4. Aspergillus niger $\alpha$-galactosidase was purified by 23.7 fold. Its specific activity was 1,229 units/mg protein and the yield was 14% of the total activity of wheat bran culture. 5. The purified $\alpha$-galactosidases of soybean and Aspergillus niger were found to be homogeneous by polyacrylamide gel electrophoresis and by HPLC. 6. Chemical properties of the purified $\alpha$-galactosidases were : 1) The soybean $\alpha$-galactosidase was monomeric and its molecular weight was estimated to be 30,000 by SDS-PAGE whereas the Aspergillus niger $\alpha$-galactosidase was a tetrameric glycoprotein which consisted of identical subunits with molecular weight of 28,000 each.

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