• Title/Summary/Keyword: KRICT

Search Result 419, Processing Time 0.027 seconds

Embryo lethality and teratogenicity of 2-Bromopropane in the Sprague-Dawley rat (Sprague-Dawley 랫드에서 2-Bromopropane의 배자치사 및 최기형성 효과)

  • Kim, Jong-Choon;Oh, Ki-Seok;Shin, Dong-Ho;Kim, Sung-Ho;Kim, Hyeon-Yeong;Yun, Hyo-In;Jiang, Cheng-Zhe;Heo, Jeong-Doo;Chung, Moon-Koo
    • Korean Journal of Veterinary Research
    • /
    • v.43 no.4
    • /
    • pp.657-666
    • /
    • 2003
  • The present study was undertaken to evaluate the potential adverse effects of 2-BP on pregnant dams and embryo-fetal development after maternal exposure during the gestational days (GD) 6 through 19 in Sprague-Dawley rats. The test chemical was administered subcutaneously to pregnant rats at dose levels of 0, 375, 750 and 1250 mg/kg/day. During the test period, clinical signs, mortality, body weights and food consumption were examined. All dams were subjected to caesarean section on GD 20 and their fetuses were examined for external, visceral and skeletal abnormalities. At above 750 mg/kg, toxic effects including signs of toxicity, suppressed body weight, decreased gravid uterine weight and reduced food intake were observed in pregnant dams. An increase in the fetal deaths, a decrease in the litter size, a reduction in the fetal body weight and an increase in the incidence of fetal morphological alterations were also found. There were no adverse effects on either pregnant dams or embryo-fetal development at a dose level of 375 mg/kg. These results suggest that a 14-day subcutaneous dose of 2-BP is embryolethal and teratogenic at above 750 mg/kg/day in pregnant rats. In the present experimental condition, the no-observed-adverse-effect level of 2-BP is considered to be 375 mg/kg/day for dams and embryo-fetuses, respectively.

Dimethyl Ether Formation Using a Zeolite Catalyst Impregnated with Ceria (세리아 첨가 제오라이트 촉매를 이용한 디메틸 에테르 합성)

  • Kim, Bo-Kyung;Koh, Jae-Cheon;Kim, Beom-Sik;Han, Myung-Wan
    • Korean Chemical Engineering Research
    • /
    • v.49 no.2
    • /
    • pp.155-160
    • /
    • 2011
  • Dimethyl ether draws an attention as a green fuel in recent years. In this study, we investigated dehydration of methanol to produce DME using solid-acid catalysts, a series of zeolite. We found that ceria took a role of promoting the reaction conversion as well as selectivity of DME formation as a cocatalyst to the zeolite catalyst. We varied Si/Al ratio and ceria percentage on the surface of the catalyst to get high performance catalyst. ZSM5-30 with 5 wt% ceria on the surface was found to have excellent DME selectivity and to be little influenced by water content in methanol feed. We proposed a reaction model and obtained kinetic parameters for the DME formation using the catalyst based on experimental results using a microreactor.

Antiviral activity of sertindole, raloxifene and ibutamoren against transcription and replication-competent Ebola virus-like particles

  • Yoon, Yi-Seul;Jang, Yejin;Hoenen, Thomas;Shin, Heegwon;Lee, Younghoon;Kim, Meehyein
    • BMB Reports
    • /
    • v.53 no.3
    • /
    • pp.166-171
    • /
    • 2020
  • A chemical library comprising 2,354 drug-like compounds was screened using a transcription and replication-competent viruslike particle (trVLP) system implementing the whole Ebola virus (EBOV) life cycle. Dose-dependent inhibition of Ebola trVLP replication was induced by 15 hit compounds, which primarily target different types of G protein-coupled receptors (GPCRs). Based on the chemical structure, the compounds were divided into three groups, diphenylmethane derivatives, promazine derivatives and chemicals with no conserved skeletons. The third group included sertindole, raloxifene, and ibutamoren showing prominent antiviral effects in cells. They downregulated the expression of viral proteins, including the VP40 matrix protein and the envelope glycoprotein. They also reduced the amount of EBOV-derived tetracistronic minigenome RNA incorporated into progeny trVLPs in the culture supernatant. Particularly, ibutamoren, which is a known agonist of growth hormone secretagogue receptor (GHSR), showed the most promising antiviral activity with a 50% effective concentration of 0.2 μM, a 50% cytotoxic concentration of 42.4 μM, and a selectivity index of 222.8. Here, we suggest a strategy for development of anti-EBOV therapeutics by adopting GHSR agonists as hit compounds.

Temperature-sensitive Liposomes Modified with Poly(N-isopropylacrylamide-co-acrylamide) (Poly(N-isopropylacrylamide-co-acrylamide)로 변형된 온도민감성 리포좀)

  • Hee Dong Han;Sung Soo Kim;Ho Suk Choi;Byung Cheol Shin
    • Journal of the Korean Chemical Society
    • /
    • v.47 no.3
    • /
    • pp.257-264
    • /
    • 2003
  • This study has investigated the temperature-sensitive liposomes, which release anticancer drug(doxorubicin) at the hyperthermia temperature$(~40^{\circ}C)$. The temperature-sensitive liposomes were modified with a copolymers of N-isopropylacrylamide(NIPAAm) and acrylamide(AAm), which exhibit a lower critical solution temperature (LCST) at the hyperthermia temperature. The release of doxorubicin from the modified liposomes was determined by measuring the fluorescence intensity with changing temperature and time. The release of doxorubicin from liposomes modified with poly(NIPAAm-co-AAm) copolymer was increased significantly, because poly(NIPAAm-co-AAm) could undergo the conformational transition in the narrow hyperthermia temperature region$(~40{\pm}2^{\circ}C)$. Moreover, we observed that doxorubicin released from liposomes within 5 minutes, and the size of modified liposomes was 120~170 nm. In this study, we have prepared temperature-sensitive liposomes which could be controlled by temperature. They can be applied in the field of a drug delivery system for tumor targeting by temperature control.

Toxicity Screening of Single Dose of Inorganic and Organic Arsenics on Hematological and Serum Biochemical Parameters in Male Cynomolgus Monkeys

  • Kim, Choong-Yong;Han, Kang-Hyun;Heo, Jeong-Doo;Han, Eui-Sik;Yum, Young-Na;Lee, Jin-Young;Park, Kyung-Su;Im, Ruth;Choi, Seong-Jin;Park, Jung-Duck
    • Toxicological Research
    • /
    • v.24 no.3
    • /
    • pp.219-225
    • /
    • 2008
  • A screening study of the acute toxicity of organic arsenics such as arsenobetaine and arsenocholine, a product of arsenic methylation metabolite, and inorganic arsenic was carried out to examine hematological and serum biochemical parameters in cynomolgus monkeys(Macaca fascicularis). We found soft and liquid feces, and vomiting in all treated groups with inorganic and organic arsenics. The monkeys in inorganic arsenic-treated group showed a significant increase in vomiting frequency compared with those in three organic arsenics-treated groups. These results suggest that inorganic arsenic might be more toxic than three other organic arsenics tested. The monkeys in inorganic arsenic-treated group showed a decrease in platelet and an increase in monocyte on day 4 and the monkeys in arsenocholine-treated group showed an increase in reticulocyte percentage on day 8. The monkeys in inorganic-treated group also showed decreases in AST and ALT values and the monkeys in arsenobetaine-treated group showed a decrease in AST value and an increase in T-CHO value. However, these hematological and biochemical changes were within the physiological ranges, showing that the single dose of inorganic and organic arsenics did not affect at least hematological and serum biochemical parameters. The present study of toxicity with single dose of arsenics provides valuable indicators for longer term study of toxicity of repeated doses of arsenics in primates.

Effects of Novel Potassium Channel Opener KR-30450 and its Metabolite KR-30818 on the Smooth, Muscle of the Guinea Pig

  • Jung, Yi-Sook;Moon, Chang-Hyun;Yoo, Sung-Eun;Shin, Hwa-Sup
    • Biomolecules & Therapeutics
    • /
    • v.4 no.4
    • /
    • pp.373-377
    • /
    • 1996
  • The effect of potassium channel openers, KR-30450, KR-30818 and lemakalim have been compared against several spasmogens in guinea pig bronchi. In guinea pig bronchi, KR-30450 had a greater relaxant effect than lemakalim and KR-30818 against tone induced by histamine $10^{-5}M$ ($EC_{50}$ $\mu$M: KR-30450, 0.108$\pm$0.077; KR-30818, 0.403$\pm$0.023; lemakalim, 0.968$\pm$0.036) and prostaglandin $F_{2\alpha} 3\times10^{-6} M$ ($EC_{50}$ $\mu$M: KR-30450, 0.018$\pm$0.001; KR-30818, 0.028$\pm$0.003; lemakalim, 0.138$\pm$0.019). Relaxant effect of KR-30450 and KR-30818 were significantly reduced by 20 min pretreatment of tissues with $10^[-6}$ M glibenclamide, a selective blocker of ATP-sensitive potassium channel. Against acetylcholine-induced tone in guinea pig bronchi, however, these compounds had little effect. In summary, KR-30450 and KR-30818 showed greater relaxant effect than lemakalim in guinea pig bronchi (KR-30450>KR-30818>lemakalim). These relaxant actions are suggested to be mediated at least in part by a mechanism which involves the opening of ATP-sensitive potassium channel.

  • PDF

Pervaporative Recovery of Bio-butanol through Dense- and Composite-type PDMS Membranes (PDMS막을 이용한 바이오 부탄올 분리정제와 투과증발 특성에 관한 연구)

  • Kim, Jeong-Hoon;Ryu, Bi-Ho;Chang, Bong-Jun;Kim, Woo-Nyon
    • Membrane Journal
    • /
    • v.19 no.2
    • /
    • pp.157-164
    • /
    • 2009
  • Bio-butanol recovery by pervaporation was performed with dense and composite polydimethylsiloxane (PDMS) membranes. The pervaporative behavior of the membranes was investigated as a function of operation temperature $(20{\sim}40^{\circ}C)$ and membrane thickness $(100{\sim}1{\mu}m)$ using a series of aqueous BtOH model solutions $(1{\sim}5wt%)$. With the increment of the BtOH concentration in feed, the Butanol concentration in permeate, pervaporation selectivity of Butanol over water and Butanol permeation flux increased. As the operating temperature of feed solutions increased, the BtOH concentration in permeate, pervaporation selectivity and permeation flux increased markedly. As the thickness of the PDMS membrane decreased, permeation flux increased but pervaporation selectivity decreased. These results were explained in terms of high solubility and low diffusion resistance of BtOH over water toward hydrophobic and rubbery PDMS membranes.

Physiology of Anthocyanin Accumulation in Corn Leaves Treated with Metsulfuron-methyl (Metsulfuron-methyl 처리에 의한 옥수수의 Anthocyanin 축적 생리에 관한 연구)

  • Park, E.Y.;Kim, J.S.;Cho, K.Y.;Pyon, J.Y.
    • Korean Journal of Weed Science
    • /
    • v.18 no.3
    • /
    • pp.246-256
    • /
    • 1998
  • The objective of this study was to investigate the cause of anthocyanin accumulation in the corn leaves treated with metsulfuron-methyl. The accumulation of anthocyanin and total sugar was increased with the time after metsulfuron-methyl application and with the greater herbicide concentration as well. The anthocyanin increase was alleviated by the combined treatment of DUMU or the tank-mixture treatment of metsulfuron-methyl, isoleucine and valine. Metsulfuron-methyl could not enhance the anthocyanin formation in the nonchlorophyllous tissue in which photosynthetic carbohydrate production was limited. Upon the exogenous supply of sucrose, however, the contents of anthocyanin was increased in the both chlorophyllous and nonchlorophyllous leaf segment of corn without the herbicide treatment. On the other hand, the herbicide itself did not influence Hill reaction in vitro and photosynthesis electron transport in vivo. The anthocyanin accumulation by metsulfitronmethyl did not occur in the corn mutants deficient in the structural gene of anthocyanin synthesis, but corns deficient in the regulatory gene had the anthocyanin accumulation only in R-r and r-r type. The above results suggest that the purple pigmentation in the corn leaves treated with metsulfuron-methyl is related to the accumulation of photosynthetic carbohydrate which can stimulate the. regulatory gene related to anthocyanin biosynthetic pathway.

  • PDF

Action Mechanism of S-23142 on the PPIX Biosynthesis System of Spinacia oleracea L. Chloroplast (엽록체내 Protoporphyrin IX(PPIX) 생합성계에서 S-23142의 작용기구)

  • Kim, T.J.;Kim, J.S.;Cho, K.Y.;Yoshida, S.
    • Korean Journal of Weed Science
    • /
    • v.14 no.1
    • /
    • pp.1-7
    • /
    • 1994
  • The effects of S-23142{N-(4-chloro-2-fluoro-5-propargyloxyphenyl)-3, 4, 5, 6-tetrahydrophtalimide}, on protoporphyrin IX(PPIX) biosynthesis in Spinacia oleracea L, leaf in vivo and in vitro condition were investigated by reversed-phase HPLC with fluorescence detector. The stroma and the membrane fraction of spinach chloroplast were isolated by osmotic regulation. The conversion of ${\delta}$-aminolevulinic acid(ALA) to PPIX occured more in the stroma than in the membrane fraction. It suggested that the enzymes that catalyse PPIX biosynthesis from ALA were localized in the stroma. Also, the synthesized PPIX content from ALA was completely inhibited by $10^{-8}M$ of S-23412 or $10^{-7}M$ of acifluorfen in the stroma but not in the membrane fractions. Therefore, these results suggested that the target site of S-23142 and acifluorfen may exist in the stroma fraction of spinach chloroplast.

  • PDF

Physiological Responses of Corn Plants to Chlorsulfuron and Imazaquin (Chlorsulfuron 과 Imazaquin에 대한 옥수수의 생리적 반응)

  • Kim, K.J.;Hwang, I.T.;Choi, J.S.;Cho, K.Y.;Pyon, J.Y.
    • Korean Journal of Weed Science
    • /
    • v.16 no.1
    • /
    • pp.64-71
    • /
    • 1996
  • This study was conducted to determine the physiological responses of corn plants to chlorsulfuron, CHL, (2-chloro-N-(((4-methoxy-6-methyl-1,3,5- triazin-2-yl)amino)carboxyl) benzenesulfonamide) and/or imazaquin, IMA, (2-(4,5-dihydro-4-methyl-4-(1-methyl)-5-oxo-1H-imidazol-2y1)-3-quinoline carboxylic acid). CHL inhibited the plant growth within 6h after treatment, whereas IMA inhibited the growth more slowly(i.e., 36h). CHL inhibited the cell division of the root tips rapidly, however, little effect was found with IMA treatment. Neither CHL nor IMA had effect on the cell elongation of the shoots. CHL inhibited acetolactate synthase(ALS) activity of the roots within 1h after treatment. Interaction between CHL and IMA in growth inhibition was found to be additive or synergistic with simultaneous or sequential treatment of the two herbicides, respectively. In addition, interaction between CHL and IMA in ALS inhibition was found to be additive when the two herbicides were treated simultaneously.

  • PDF