• Title/Summary/Keyword: Ligand effect

Search Result 427, Processing Time 0.03 seconds

Bone Cell Response to Neurotransmitters and Mechanical Loading (신경전달물질 및 물리적 자극에 대한 뼈 세포의 반응)

  • Kwag, J.H.;Kim, B.G.;Kim, K.H.;Kim, C.H.
    • Journal of Biomedical Engineering Research
    • /
    • v.30 no.1
    • /
    • pp.89-93
    • /
    • 2009
  • Bone remodeling is a continuous process of skeletal renewal during which bone formation is tightly coupled to bone resorption. Mechanical loading is an important regulator of bone formation and resorption. In recent studies, neurotransmitters such as vasoactive intestinal peptide (VIP) were found to be present inside bone tissue and have been suggested to potentially regulate bone remodeling. In this study, our objective was to use a pre-established in vitro oscillatory fluid flow-induced shear stress mechanical loading system to quantify the effect of VIP on bone resorptive activity and investigate its combined effect with mechanical loading. VIP decreased osteoclastogenesis significantly decreased RANKL/OPG mRNA ration by approximately 90%. Combined VIP and mechanical loading further decreased RANKL/OPG ratio to approximately 95%. These results suggest that VIP present in bone tissue may synergistically act with mechanical loading to regulate bone remodeling via suppression of bone resorptive activities.

Effects of Gardeniae Jasminoides on RANKL-induced Osteoclastogenesis and Bone Resorption (치자 추출물이 RANKL 유도 파골세포 형성 및 골 흡수에 미치는 영향)

  • Choi, You-kyung;Hwang, Gwi-seo
    • The Journal of Internal Korean Medicine
    • /
    • v.38 no.6
    • /
    • pp.1035-1048
    • /
    • 2017
  • Objectives: This study was performed to investigate the effects of Gardenia jasminoides extract (GJ) on osteoclast differentiation and bone resorption in vitro. Methods: To investigate the effect of GJ on osteoclast differentiation, the mouse leukemic myeloid cell line RAW 264.7 was stimulated by RANKL (receptor activator of nuclear factor kB ligand). Osteoclast differentiation was measured by counting TRAP (+) MNC in the presence of RANKL. To elucidate the mechanism of the inhibitory effect of GJ on osteoclast differentiation, gene expression of TRAP, Cathepsin K, MMP-9, NFATc1, c-Fos, MITF, DC-STAMP, CTR, OC-STAMP and Atp6v0d2 was measured using reverse transcription-PCR (RT-PCR). Bone resorption was measured using the bone pit formation assay. Results: GJ decreased the number of TRAP (+) MNCs in the presence of RANKL. GJ inhibited the expression of cathepsin K, MMP-9, TRAP, MITF, NFATc1, c-Fos, iNON, OC-STAMP, Atp6v0d2, and DC-STAMP in the osteoclast, and inhibited bone pit formation in vitro. Conclusions: The results suggest that GJ has inhibitory effects on bone resorption resulting from inhibition of osteoclast differentiation and gene expression.

The Search of Pig Pheromonal Odorants for Biostimulation Control System Technologies: Synthesis of $N^1$-allyl-$N^2$-(tetrahydrofuran-2-ylmethyl)oxalamide Molecule and Induction Effect of Pig Estrus (생물학적 자극 통제 수단으로 활용하기 위한 돼지 페르몬 성 냄새 물질의 탐색: $N^1$-allyl-$N^2$-(tetrahydrofuran-2-ylmethyl)oxalamide 분자의 합성과 돼지의 발정 유도효과)

  • Park, Chang-Sik;Song, Suck-Oh;Lim, Jae-Sam;Soung, Min-Gyu;Sung, Nack-Do
    • Reproductive and Developmental Biology
    • /
    • v.33 no.1
    • /
    • pp.1-5
    • /
    • 2009
  • To search a new pig pheromonal odorant, the $N^1$-allyl-$N^2$-(tetrahydrofuran-Z-ylmethyl)oxalamide molecule predicted by ligand based approach and molecular docking method was synthesized by nucleophilic addition-elimination reaction ($Ad_{NU-E}$) between N-allyloxalamic acid ethylester and tetrahydrofurlmethylamine. According to the evaluation results for efficiency of pig estrus control, the synthesized pig pheromonal $N^1$-allyl-$N^2$-(tetrahydrofuran-2-ylmethyl)oxalamide molecule advanced the estrus by 11.3 days (p<0.05) compared with the non-pheromone group. And from these results, it is predicted that the synthesized pig pheromonal compound will be able to increase the reproduction efficiency of pig.

Chlorine Effect on Thermal Aging Behaviors of BR and CR Composites

  • Choi, Sung-Seen;Kim, Jong-Chul
    • Bulletin of the Korean Chemical Society
    • /
    • v.31 no.9
    • /
    • pp.2613-2617
    • /
    • 2010
  • Chloroprene is a chlorine substituent of 1,3-butadiene. Butadiene rubber (BR) and chloroprene rubber (CR) composites were thermally aged at 60, 70, 80, and $90^{\circ}C$ for 2 - 185 days in a convection oven and changes of the crosslink densities by the accelerated thermal aging were investigated. The crosslink densities increased as the aging time elapsed and as the aging temperature became higher. Degrees of the crosslink density changes of the BR composite were on the whole larger than those of the CR one except the short-term thermal aging at 60 and $70^{\circ}C$. The crosslink densities abnormally increased after themal aging at high temperatures for a long time. Activation energies for the crosslink density changes of the rubber composites tended to increase with increase of the aging time and the variation showed a local minimum. The activation energies of the CR composite were lower than those of the BR one. The experimental results were explained with a role of ligand of chlorine atom of CR in a zinc complex, steric hindrance by chlorine atom of CR, and oxidation of rubber chain.

Ubiquitination of p53 is Involved in Troglitazone Induced Apoptosis in Cervical Cancer Cells

  • Chen, Hui-Min;Zhang, Ding-Guo;Wu, Jin-Xiz;Pei, Dong-Sheng;Zheng, Jun-Nian
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.15 no.5
    • /
    • pp.2313-2318
    • /
    • 2014
  • Peroxisome proliferator-activated receptor gamma (PPAR-${\gamma}$), a ligand-dependent nuclear transcription factor, has been found to widely exist in tumor tissues and plays an important role in affecting tumor cell growth. In this study, we investigated the effect of PPAR-${\gamma}$ on aspects of the cervical cancer malignant phenotype, such as cell proliferation and apoptosis. Cell growth assay, Western blotting, Annexin V and flow cytometry analysis consistently showed that treatment with troglitazone (TGZ, a PPAR-${\gamma}$ agonist) led to dose-dependent inhibition of cervical cancer cell growth through apoptosis, whereas T0070907 (another PPAR-${\gamma}$ antagonist) had no effect on Hela cell proliferation and apoptosis. Furthermore, we also detected the protein expression of p53, p21 and Mdm2 to explain the underlying mechanism of PPAR-${\gamma}$ on cellular apoptosis. Our work, finally, demonstrated the existence of the TGZ-PPAR-${\gamma}$-p53 signaling pathway to be a critical regulator of cell apoptosis. These results suggested that PPAR-${\gamma}$ may be a potential therapeutic target for cervical cancer.

Effect of TGF-${\beta}1$ on Osteoclast Differentiation

  • Park, Su-Jin;Ko, Jea-Seung;Kim, Hyun-Man
    • International Journal of Oral Biology
    • /
    • v.30 no.4
    • /
    • pp.135-141
    • /
    • 2005
  • Although it has been known that TGF-${\beta}1$ acts as a crucial cofactor in osteoclast differentiation, its mode of action is still unclear. In the present study, we studied the effect of TGF-${\beta}1$ on the differentiation of osteoclast depending on the developmental stages. Murine bone marrow cells were induced to differentiate into mature osteoclasts in the presence of receptor activator of NF-${\kappa}B$ ligand (RANKL) and macrophage colony stimulating factor (M-CSF). In the early stage of the differentiation TRAP(-) mononuclear precursor cells were obtained from nonadherent M-CSF dependent bone marrow cells, which further differentiated into mature osteoclasts. TGF-${\beta}1$ stimulated osteoclast differentiation, which was stronger when cells were stimulated by TGF-${\beta}1$ in the early stage than the later differentiation. TGF-${\beta}1$ increased the expression of RANK and synergistically stimulated RANKL-induced activation of NF-${\kappa}B$ MAP kinase in TRAP(-) mononuclear precursor cells. These results suggest that activation of osteoclast differentiation by TGF-${\beta}1$ may be ascribed to the both increased expression and activation of RANK in the osteoclast differentiation, especially in the early stage of differentiation.

Research Trend of Metal-Organic Frameworks for Magnetic Refrigeration Materials Application (자기 냉동 재료 응용을 위한 MOF의 연구 동향)

  • Kim, Suhwan;Son, Kwanghyo;Oh, Hyunchul
    • Korean Journal of Materials Research
    • /
    • v.30 no.3
    • /
    • pp.136-141
    • /
    • 2020
  • The magnetocaloric effect (MCE), which is the reversible temperature change of magnetic materials due to an applied magnetic field, occurs largely in the vicinity of the magnetic phase transition temperature. This phenomenon can be used to induce magnetic refrigeration, a viable, energy-efficient solid-state cooling technology. Recently, Metal-organic frameworks (MOFs), due to their structural diversity of tunable crystalline pore structure and chemical functionality, have been studied as good candidates for magnetic refrigeration materials in the cryogenic region. In cryogenic cooling applications, MCE using MOF can have great potential, and is even considered comparable to conventional lanthanum alloys and magnetic nanoparticles. Owing to the presence of large internal pores, however, MOF also exhibits the drawback of low magnetic density. To overcome this problem, therefore, recent reports in literature that achieve high magnetic entropy change using a dense structure formation and ligand tuning are introduced.

Modulatory Effect of Diethylstilbestrol on CD29-Mediated Cell-cell Adhesion in Monocytic U937 Cells (Diethylstilbestrol의 단핵구의 세포간 유착과정 조절효과)

  • Kim, Byung-Hun;Cho, Jae-Youl
    • YAKHAK HOEJI
    • /
    • v.52 no.2
    • /
    • pp.111-116
    • /
    • 2008
  • Diethylstilbestrol (DESB) is a synthetic estrogen not only that routinely prescribed, but also that known to be a teratogen. In this study, we found a novel pharmacological feature that DESB is able to positively modulate CD29 $({\beta}1-integrin)$ function. Thus, DESB up-regulated homotypic cell-cell adhesion of monocytic U937 cells mediated by CD29. However, DESB did not increase the surface level of CD29 and its binding activity to ligand (fibronectin), according to flow cytometric analysis and cell-fibronectin adhesion assay. Instead, the DESB-mediated up-regulation of cell-cell adhesion was blocked by several signaling enzyme inhibitors. Treatment of U0126 [an extracellular signal-regulated kinase (ERK) inhibitor], SB20358 (a p38 inhibitor) or Rp-8-pCPT-cGMP (a protein kinase G inhibitor) clearly inhibited DESB-mediated up-regulation of cell-cell adhesion induced by CD29. However, estrogen receptor antagonist ICI 182,780 failed to abrogate DESB effect. Therefore, our data suggest that DESB may up-regulate CD29-mediated cell-cell adhesion via modulating intracellular signaling enzymes such as ERK, PKG, and p38, independent of estrogen receptor function.

14N Mines Pulsed-ENDOR of Proximal Histidine and Heme of Aquometmyoglobin and Fluormetmyoglobin

  • Lee, Hong-In
    • Bulletin of the Korean Chemical Society
    • /
    • v.23 no.12
    • /
    • pp.1769-1772
    • /
    • 2002
  • Previous $^{19}F\;and\;^{1,2}H$ electron-nuclear double resonance (ENDOR) study of fluorometmyoglobin (MbF) in frozen-solution state provided sensitive tools sensing subtle structural changes of the heme that are not obtainable from X-ray. [Fann et al., J. Am. Chem. Soc. 1995, 117, 6019] Because of the intrinsic inhomogeneouse EPR line broadening effect of MbF in frozen-solution state, detection of the intrinsic inhomogeneouse EPR line broadening effect of MbF in frozen-solution state, detection of the electronic and geometrical changes of the heme ring itself and the proximal histidine by using $^{14}N$ CW ENDOR was interfered. In the present study, hyperfine-sensitive $^{14}N$ Mims ENDOR technique of pulsed-EPR was employed to probe the changes. With two different $\tau$ values of 128 and 196 ns, $^{14}N$ ENDOR signals of the heme and proximal histidine were completely resolved at $g'_{II}(=g_e=2)$. This study present that X-band $^{14}N$ Mims ENDOR sequence can sensitively detect the small changes of the spin densities and p orbital populations of the proximal and the heme nitrogens, caused by ligand and pH variation of the distal site.

A Chromo- and Fluoroionophoric Thiaoxaaza-Macrocycle Functionalized with Nitrobenzofurazan Exhibiting Mercury(II) Selectivity

  • Lee, Ji-Eun;Lee, Shim-Sung;Choi, Kyu-Seong
    • Bulletin of the Korean Chemical Society
    • /
    • v.31 no.12
    • /
    • pp.3707-3710
    • /
    • 2010
  • A chromo/fluorogenic $NO_2S_2$-macrocycle L functionalized with nitrobenzofurazan unit as a dual-signaling probe was synthesized and structurally characterized by single crystal X-ray analysis. In a cation-induced color change experiment, L exhibited excellent $Hg^{2+}$ ion selectivity by showing the color change from orange-red to yellow. However, this hypochromic shift by $Hg^{2+}$ was observed for the weaker coordinating anion system such as ${NO_3}^-$ and ${ClO_4}^-$ ions. The observed anion effect is due to the strong coordination of anions inhibits the bond formation between $Hg^{2+}$ and the macrocyclic tert-N atom, which is sensitive to induce the color change. In the fluorometric experiment, L showed chelate-enhanced fluorescence change effect only with $Hg^{2+}$ ion, together with a change from yellow to green emission. The sensing ability for $Hg^{2+}$ with the proposed chemosensor L is due to the stable complexation with 1:1 stoichiometry (metal-to-ligand).