• Title/Summary/Keyword: Pi-b

Search Result 823, Processing Time 0.023 seconds

In vivo Pharmacokinetics, Activation of MAPK Signaling and Induction of Phase II/III Drug Metabolizing Enzymes/Transporters by Cancer Chemopreventive Compound BHA in the Mice

  • Hu, Rong;Shen, Guoxiang;Yerramilli, Usha Rao;Lin, Wen;Xu, Changjiang;Nair, Sujit;Kong, Ah-Ng Tony
    • Archives of Pharmacal Research
    • /
    • v.29 no.10
    • /
    • pp.911-920
    • /
    • 2006
  • Phenolic antioxidant butylated hydroxyanisole (BHA) is a commonly used food preservative with broad biological activities, including protection against chemical-induced carcinogenesis, acute toxicity of chemicals, modulation of macromolecule synthesis and immune response, induction of phase II detoxifying enzymes, as well as its undesirable potential tumor-promoting activities. Understanding the molecular basis underlying these diverse biological actions of BHA is thus of great importance. Here we studied the pharmacokinetics, activation of signaling kinases and induction of phase II/III drug metabolizing enzymes/transporter gene expression by BHA in the mice. The peak plasma concentration of BHA achieved in our current study after oral administration of 200 mg/kg BHA was around $10\;{\mu}M$. This in vivo concentration might offer some insights for the many in vitro cell culture studies on signal transduction and induction of phase II genes using similar concentrations. The oral bioavailability (F) of BHA was about 43% in the mice. In the mouse liver, BHA induced the expression of phase II genes including NQO-1, HO-1, ${\gamma}-GCS$, GST-pi and UGT 1A6, as well as some of the phase III transporter genes, such as MRP1 and Slco1b2. In addition, BHA activated distinct mitogen-activated protein kinases (MAPKs), c-Jun N-terminal kinase (JNK), extracellular signal-regulated protein kinase (ERK), as well as p38, suggesting that the MAPK pathways may play an important role in early signaling events leading to the regulation of gene expression including phase II drug metabolizing and some phase III drug transporter genes. This is the first study to demonstrate the in vivo pharmacokinetics of BHA, the in vivo activation of MAPK signaling proteins, as well as the in vivo induction of Phase II/III drug metabolizing enzymes/transporters in the mouse livers.

Relationships between osteoporosis, alveolar bone density and periodontal disease in postmenopausal women (골다공증과 악골의 골밀도 및 치주 질환과의 상관 관계)

  • Han, E.Y.;Rhyu, I.C.;Lee, Y.M.;Ku, Y.;Han, S.B.;Choi, S.M.;Shin, J.Y.;Yang, S.M.;Chung, C.P.
    • Journal of Periodontal and Implant Science
    • /
    • v.31 no.3
    • /
    • pp.565-571
    • /
    • 2001
  • The purpose of this study is to determine if a relationship exists among osteoporosis, alveolar bone density and periodontal disease in postmenopausal osteoporotic women and postmenopausal healthy women. Twenty-two women were evaluated for this study. They were attending the postmenopausal clinic, Seoul National University Hospital and generally healthy except osteoporosis. They had experienced menopause not less than one year when we began to examine them. Bone densities of lumbar area(L2-L4) was determined by DEXA(LUNAR-expert Co,. U.S.A). We diagnosed osteoporosis when T-score was below -2.5 and healthy state when T-score was over -1. Osteoporotic(10 female), not hormone-treated group and healthy control group(12 female) were asked for their age, menopausal age, menopausal period and the number of remaining teeth and examined clinically for plaque index(PI), gingival index(GI), clinical attachment loss(CAL) on their 6 Ramfjord index teeth. Intraoral radiographs were taken in maxillary anterior zone. All films were equally exposed and developed. Each films was digitized and analysed using image processing software, Scion image. Alveolar bone regions of interest were selected and Intensity of each pixel was quantized in the array ranging from 0(white) to 255(black). The two groups were comparable with respect age, menopausal age, menopausal period and number of remaining teeth. The osteoporotic women had significantly lower alveolar bone density than controls in maxilla. But no significant difference was found with respect clinical attachment loss, plaque index and gingival index. Supported by the Ministry of Public Health and Welfare, Korea (HMP-00-CH-10-0009).

  • PDF

Experimental and numerical investigations on remaining strengths of damaged parabolic steel tubular arches

  • Huang, Yonghui;Liu, Airong;Pi, Yong-Lin;Bradford, Mark A.;Fu, Jiyang
    • Steel and Composite Structures
    • /
    • v.34 no.1
    • /
    • pp.1-15
    • /
    • 2020
  • This paper presents experimental and numerical studies on effects of local damages on the in-plane elastic-plastic buckling and strength of a fixed parabolic steel tubular arch under a vertical load distributed uniformly over its span, which have not been reported in the literature hitherto. The in-plane structural behaviour and strength of ten specimens with different local damages are investigated experimentally. A finite element (FE) model for damaged steel tubular arches is established and is validated by the test results. The FE model is then used to conduct parametric studies on effects of the damage location, depth and length on the strength of steel arches. The experimental results and FE parametric studies show that effects of damages at the arch end on the strength of the arch are more significant than those of damages at other locations of the arch, and that effects of the damage depth on the strength of arches are most significant among those of the damage length. It is also found that the failure modes of a damaged steel tubular arch are much related to its initial geometric imperfections. The experimental results and extensive FE results show that when the effective cross-section considering local damages is used in calculating the modified slenderness of arches, the column bucking curve b in GB50017 or Eurocode3 can be used for assessing the remaining in-plane strength of locally damaged parabolic steel tubular arches under uniform compression. Furthermore, a useful interaction equation for assessing the remaining in-plane strength of damaged steel tubular arches that are subjected to the combined bending and axial compression is also proposed based on the validated FE models. It is shown that the proposed interaction equation can provide lower bound assessments for the remaining strength of damaged arches under in-plane general loading.

Study on DNA Content and Ki-67 Antibody Expression by Means of Image Analyzer for the Benign and Malignant Lesions of the Larynx (후두 편평상피의 전암성 및 악성병변에서 화상분석기를 이용한 DNA 배수성검사와 Ki-67 항체 양성세포의 분석에 관한 연구)

  • 주형로;이선희;최종욱;김인선
    • Proceedings of the KOR-BRONCHOESO Conference
    • /
    • 1993.05a
    • /
    • pp.89-89
    • /
    • 1993
  • The laryngeal epithelial cell kinetics of 26 laryngeal lesions(invasive squamous cell carcinoma 14, epithelial hyperplasia 5, laryngeal nodule 7) were studied by immunehistochemical analysis with the monoclonal antibody Ki-67, which reacts with nuclear antigen in proliferating cells using paraffin embedded tissue. For DNA analysis, touch implint with fresh biopsy specimens were stained with feulgen and analyzed by image analyzer in 22 cases. 1) The proportion of Ki-67-positive cells were 32.65$\pm$ 11.59% in invasive squamous cell ca, 20.14$\pm$3.38% in epithelial hyperplasia lesion and 11.66$\pm$3.02% in laryngeal nodule. 2) DNA aneuploidy was found in 7 cases of 10(70%) invasive squamous cell carcinomas, 2 cases of 5(40%) epithelial hyperplasia lesions and all cases of laryngeal 3) Proliferation index(S phase+G2/M phase) show 23.42$\pm$11.33% in squamous cell carcinoma, 13.09$\pm$ 10.90% in epithelial hyperplasia lesion and 4.50$\pm$1.19% in laryngeal nodule. As the results, measuring the DNA content from touch imprint method together positivity of Ki-67 antibody from the microtissue during the laryngeal microscopic surgery, cell kinetics can be assessed as an effort of deciding the prognosis and provide a key to the management of precancerous lesions.

  • PDF

Theoretical Studies of the Gas-Phase Identity Nucleophilic Substitution Reactions of Cyclopentadienyl Halides

  • Lee, Ik-Choon;Li, Hong-Guang;Kim, Chang-Kon;Lee, Bon-Su;Kim, Chan-Kyung;Lee, Hai-Whang
    • Bulletin of the Korean Chemical Society
    • /
    • v.24 no.5
    • /
    • pp.583-592
    • /
    • 2003
  • The gas phase identity nucleophilic substitution reactions of halide anions (X = F, Cl, Br) with cyclopentadienyl halides (1) are investigated at the B3LYP/6-311+G**, MP2/6-311+G** and G2(+)MP2 levels involving five reaction pathways: σ-attack $S_N2$, β-$S_N$2'-syn, β-$S_N$2'-anti, γ-$S_N$2'-syn and γ-$S_N$2'-anti paths. In addition, the halide exchange reactions at the saturated analogue, cyclopentyl halides (2), and the monohapto circumambulatory halide rearrangements in 1 are also studied at the same three levels of theory. In the σ-attack $S_N2$ transition state for 1 weak positive charge develops in the ring with X = F while negative charge develops with X = Cl and Br leading to a higher energy barrier with X = F but to lower energy barriers with X = Cl and Br than for the corresponding reactions of 2. The π-attack β-$S_N$2' transition states are stabilized by the strong $n_C-{\pi}^{*}_{C=C}$ charge transfer interactions, whereas the π-attack γ-$S_N$2' transition states are stabilized by the strong $n_C-{\sigma}^{*}_{C-X}$ interactions. For all types of reaction paths, the energy barriers are lower with X = F than Cl and Br due to the greater bond energy gain in the partial C-X bond formation with X = F. The β-$S_N$2' paths are favored over the γ-$S_N$2' paths only with X = F and the reverse holds with X = Cl and Br. The σ-attack $S_N2$ reaction provides the lowest energy barrier with X = Cl and Br, but that with X = F is the highest energy barrier path. Activation energies for the circumambulatory rearrangement processes are much higher (by more than 18 kcal $mol^{-1}$) than those for the corresponding $S_N2$ reaction path. Overall the gas-phase halide exchanges are predicted to proceed by the σ-attack $S_N2$ path with X = Cl and Br but by the β-$S_N$2'-anti path with X = F. The barriers to the gas-phase halide exchanges increase in the order X = F < Br < Cl, which is the same as that found for the gas-phase identity methyl transfer reactions.

Surface properties on ion beam irradiated polycarbonate (이온주입에 의한 폴리카보네이트의 표면특성 조사)

  • Lee, Jae-Hyung;Yang, Dae-Jeong;Kil, Jae-Kyun;Kim, Bo-Young
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
    • /
    • 2003.11a
    • /
    • pp.31-35
    • /
    • 2003
  • 폴리카보네이트는 내열성과 투명성이 우수한데 비해 내후성이 좋지 않아 황변 및 물성이 저하되고, 내찰상성이 약하여 긁히기 쉬운데다 이물질에 의해 오염되기 쉬워 투명성이 저하되는 문제점이 있다. 이러한 단점을 극복하고, 사용하는 용도에 따라 요구되는 다양한 기능성을 부여하기 위하여 폴리카보네이트 표면에 기능성층을 형성시킴으로써 그 목적을 달성하고자 한다. 본 논문에서는 이온 주입기술을 이용하여, 폴리카보네이트 표면의 전기전도도 특성을 향상시키고, 피부암 및 백내장 등을 유발하는 유해한 자외선 (UV-A, UV-B)을 차단하려 한다. 표면전기전도도의 향상은 이물질로부터 오염되는 정도를 낮추며, 정전기를 방지할 수 있다. PC(Polycarbonate) 표면에 $N^+,\;Ar^+,\;Kr^+,\;Xe^+$ 이온을 에너지 20keV에서 50keV을 사용하여, 주입량 $5{\times}10^{15}\;{\sim}\7{\times}10^{16}\cm^2$ 로 조사하였다. 이온 주입된 PC의 표면을 두 접점 방법의 표면 저항 측정으로 표면전기전도도 특성을 알아보았고, 자외선차단 특성은 UV-Vis 로 분석하였다. 이들 전기적 광학적 특성간의 상관관계를 관찰하고, 이러한 특성을 나타내는 화학적 기능그룹들의 변화를 보기 위해 FTIR 분석법으로 관찰하였다. 이온조사량의 증가에 따라 표면저항은 $10^7{\Omega}/sq$까지 감소하여 표면전기특성을 증가시키며, 자외선 차단 특성은 UV-A를 95%까지 차단하여 인체에 유해한 자외선 차단에 유용함을 확인하였다. 이러한 특성은 PC 표면에 카본 네트워크 형성과 $\pi$전자들의 운동량을 증가시키는 구조로 고분자 사슬들의 결합구조 변형에 의한 것으로 생각된다.블을 가지고 파서를 설계하였다. 파서의 출력으로 AST가 생성되면 번역기는 AST를 탐색하면서 의미적으로 동등한 MSIL 코드를 생성하도록 시스템을 컴파일러 기법을 이용하여 모듈별로 구성하였다.적용하였다.n rate compared with conventional face recognition algorithms. 아니라 실내에서도 발생하고 있었다. 정량한 8개 화합물 각각과 총 휘발성 유기화합물의 스피어만 상관계수는 벤젠을 제외하고는 모두 유의하였다. 이중 톨루엔과 크실렌은 총 휘발성 유기화합물과 좋은 상관성 (톨루엔 0.76, 크실렌, 0.87)을 나타내었다. 이 연구는 톨루엔과 크실렌이 총 휘발성 유기화합물의 좋은 지표를 사용될 있고, 톨루엔, 에틸벤젠, 크실렌 등 많은 휘발성 유기화합물의 발생원은 실외뿐 아니라 실내에도 있음을 나타내고 있다.>10)의 $[^{18}F]F_2$를 얻었다. 결론: $^{18}O(p,n)^{18}F$ 핵반응을 이용하여 친전자성 방사성동위원소 $[^{18}F]F_2$를 생산하였다. 표적 챔버는 알루미늄으로 제작하였으며 본 연구에서 연구된 $[^{18}F]F_2$가스는 친핵성 치환반응으로 방사성동위원소를 도입하기 어려운 다양한 방사성의 약품개발에 유용하게 이용될 수 있을 것이다.었으나 움직임 보정 후 영상을 이용하여 비교한 경우, 결합능 변화가 선조체 영역에서 국한되어 나타나며 그 유의성이 움직임 보정 전에 비하여 낮음을 알 수 있었다. 결론: 뇌활성화 과제 수행시에 동반되는 피험자의 머리 움직임에 의하여 도파민 유리가 과대평가되었으며 이는 이 연구에서 제안한 영상정합을 이용한 움직임 보정기법에 의해서 개선되었다. 답이 없는 문제, 문제 만들기, 일반화가 가능한 문제 등으

  • PDF

Synthesis of Binuclear Bismacrocyclic Iron(II) Complex by the Aerobic Oxidation of Iron(II) Complex of 1,4,8,11-Tetraazacyclotetradecane

  • Myunghyun Paik Suh;Gee-Yeon Kong;Il-Soon Kim
    • Bulletin of the Korean Chemical Society
    • /
    • v.14 no.4
    • /
    • pp.439-444
    • /
    • 1993
  • The aerobic oxidation of the Fe(II) complex of 1,4,8,11-tetraazacyclotetradecane, [Fe(cyclam)$(CH_3CN)_2](ClO_4)_2$, in MeCN in the presence of a few drops of $HClO_4$ leads to low spin Fe(III) species [Fe(cyclam)$(CH_3CN)_2](ClO_4)_3$. The Fe(III) cyclam complex is further oxidized in the air in the presence of a trace of water to produce the deep green binuclear bismacrocyclic Fe(II) complex $[Fe_2(C_{20}H_{36}N_8)(CH_3CN)_4](ClO_4)_4{\cdot}2CH_3CN$. The Fe(II) ions of the complex are six-coordinated and the bismacrocyclic ligand is extensively unsaturated. $[Fe_2(C_{20}H_{36}N_8)(CH_3CN)_4](ClO_4)_4{\cdot}2CH_3CN$ crystallizes in the monoclinic space group $P2_1/n$ with a= 13.099 (1) ${\AA}$, b= 10.930 (1) ${\AA}$, c= 17.859 (1) ${\AA}$, ${\beta}$= 95.315 $(7)^{\circ}$, and Z= 2. The structure was solved by heavy atom methods and refined anisotropically to R values of R= 0.0633 and $R_w$= 0.0702 for 1819 observed reflections with F > $4{\sigma}$ (F) measured with Mo K${\alpha}$ radiation on a CAD-4 diffractometer. The two macrocyclic units are coupled through the bridgehead carbons of ${\beta}$-diimitie moieties by a double bond. The double bonds in each macrocycle unit are localized. The average bond distances of $Fe(II)-N_{imine}$, $Fe(II)-N_{amine}$, and $Fe(II)-N_{MeCN}$ are 1.890 (5), 2.001 (5), and 1.925 (6) ${\AA}$, respectively. The complex is diamagnetic, containing two low spin Fe(II) ions in the molecule. The complex shows extremely intense charge transfer band in the near infrared at 868 nm with ${\varepsilon}$= 25,000 $M^{-1}cm^{-1}$. The complex shows a one-electron oxidation wave at +0.83 volts and two one-electron reduction waves at -0.43 and-0.72 volts vs. Ag/AgCl reference electrode. The complex reacts with carbon monoxide in $MeNO_2$ to form carbonyl adducts, whose $v_{CO}$ value (2010 $cm^{-1}$) indicates the ${\pi}$-accepting property of the present bismacrocyclic ligand.

1,2-Dichloropropane (1,2-DCP)-Induced Angiogenesis in Dermatitis

  • Jin, Meiying;Hong, Youngeun;Lee, Hyunji;Tran, Quangdon;Cho, Hyeonjeong;Kim, Minhee;Kwon, So Hee;Kang, Nak Heon;Park, Jisoo;Park, Jongsun
    • Toxicological Research
    • /
    • v.35 no.4
    • /
    • pp.361-369
    • /
    • 2019
  • 1,2-Dichloropropane (1,2-DCP) has been used as an industrial solvent and a chemical intermediate, as well as in soil fumigants. Human exposure may occur during its production and industrial use. The target organs of 1,2-DCP are the eyes, respiratory system, liver, kidneys, central nervous system, and skin. Repeated or prolonged contact may cause skin sensitization. In this study, 1,2-DCP was dissolved in corn oil at 0, 2.73, 5.75, and 8.75 mL/kg. The skin of mice treated with 1,2-DCP was investigated using western blotting, hematoxylin and eosin staining, and immunohistochemistry. 1,2-DCP was applied to the dorsal skin and both ears of C57BL/6J mice. The thickness of ears and the epidermis increased significantly following treatment, and the appearance of blood vessels was observed in the dorsal skin. Additionally, the expression of vascular endothelial growth factor, which is tightly associated with neovascularization, increased significantly. The levels of protein kinase-B (PKB), phosphorylated PKB, mammalian target of rapamycin (mTOR), and phosphorylated mTOR, all of which are key components of the phosphoinositide 3-kinase/PKB/mTOR signaling pathway, were also enhanced. Taken together, 1,2-DCP induced angiogenesis in dermatitis through the PI3K/PKB/mTOR pathway in the skin.

Molecular physiological inhibitory effects of chloroacetanilide herbicide pretilachlor on marine dinoflagellate Prorocentrum minimum (해양 와편모조류 Prorocentrum minimum에 대한 아세트아닐라이드계 제초제 프레틸라클로르의 분자 생물학적 저해 효과)

  • Hansol Kim;Jang-Seu Ki
    • Korean Journal of Environmental Biology
    • /
    • v.39 no.4
    • /
    • pp.452-462
    • /
    • 2021
  • Pretilachlor (PRE) is a common acetanilide herbicide used worldwide. However, its effects on aquatic organisms, particularly marine photosynthetic life, are not sufficiently known. Herein, we evaluated the toxic effects of PRE by physiological and molecular parameters in the photosynthetic dinoflagellate Prorocentrum minimum. The cell density, pigment content, and photosynthetic parameters (Fv/Fm and PIABS) were considerably decreased with increased PRE exposure time and doses. In addition, photosynthesis-related genes, PmpsbA, PmpsaA, and PmatpB, were significantly upregulated when exposed to 1.0 mg L-1 of PRE for 24 h (p<0.001). In 72 h treatment, the relative gene expression was significantly increased (0.1 and 0.5 mg L-1; p<0.01). In contrast, PmrbcL was decreased or little changed compared to the controls. Reactive oxygen species (ROS) increased after 24 h exposure (p<0.001). However, the transcriptional fold-changes in glutathione S-transferase (GST) were significantly increased (0.5 and 1.0 mg L-1; p<0.001) at 72 h. These findings suggested that the PmGST might be involved in PRE detoxification in P. minimum. In addition, PRE may affect the photosystem function in phytoplankton similar to other acetanilides, causing severe damage or cell death.

In Vitro/In Vivo Development of Vitrified Immature Mouse Oocytes (초자화 동결된 생쥐 미성숙란의 체외/체내 발달)

  • Yi, B.K.;Kim, E.Y.;Nam, H.K.;Lee, K.S.;Yoon, S.H.;Park, S.P.;Lim, J.H.
    • Korean Journal of Animal Reproduction
    • /
    • v.23 no.2
    • /
    • pp.133-139
    • /
    • 1999
  • This study was carried out to investigate in vitro/in vivo development of vitrified-thawed immature mouse oocytes. Immature mouse oocytes were vitrified with EFS40 (40% ethylene glycol, 18% ficoll and 0.5 M sucrose). Thawed oocytes were matured for 16 hr in vitro. Matured oocytes with the first polar body were fertilized with the concentration of 1~2$\times$10$^{6}$ $m\ell$ of epididymal sperm. After fertilization, cleavage ($\geq$ 2-cell) and in vitro/in vivo development rates were examined. $\pi$ Ie results were summarized as follows: in vitro maturation rate of immature mouse oocytes in vitrified-thawed group was similar to that in exposed group (67.5%) and control (66.3%), but cleavage rate of vitrified-thawed oocytes (64.9 %) and blastocyst formation rate (59.0%) were significantly different compared to those of exposed group (83.7 and 74.7%) and control (90.7 and 83.7%) (p<0.05). However, when the blastocysts derived from immature mouse oocytes vitrified-thawed were transferred to pseudopregnant mouse, total implantation (31.3%) was slightly lower than that in control (40.8%), but live fetus formation rate (66.7%)was slightly higher than that in control (58.1%), there was not significantly different. Therefore, when the blastocyts produced in vitro were transferred into recipients, although the development in vitro of oocytes vitrified-thawed was decreased, live fetus formation rate was similar to that of control group. The present results indicate that immature mouse oocytes can be frozen successfully by vitrification with EFS40.

  • PDF