• Title/Summary/Keyword: ED-H

Search Result 299, Processing Time 0.036 seconds

Antihypertensive activity of KR-31081, an orally active nonpeptide AT1 receptor antagonist (안지오텐신 수용체 리간드 KR-31081의 생체 내 활성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of the Korea Academia-Industrial cooperation Society
    • /
    • v.10 no.11
    • /
    • pp.3473-3479
    • /
    • 2009
  • The pharmacological profile of KR-31081, a newly synthesized AT1 receptor antagonist, was evaluated in pithed rats, conscious renal hypertensive rats (RHRs) and conscious furosemide-treated beagle dogs. In pithed rats, KR-31081 (i.v.) induced a non-parallel right shift in the dose-pressor response curve to angiotensin II (ID50: 0.05 mg/kg) with a dose-dependent reduction in the maximum responses; this antagonistic effect was about 40 times more potent than losartan (ID50: 1.74 mg/kg) which showed competitive antagonism. KR-31081 did not alter the responses induced by other agonists such as norepinephrine and vasopressin. In RHRs, orally given KR-31081 produced a dose-dependent and long-lasting (>24 h) antihypertensive effect with a higher potency to losartan (ED20: 0.30 and 3.36 mg/kg, respectively). In furosemide-treated dogs, orally given KR-31081 produced a dose-dependent and long-lasting (>8h) antihypertensive effect with a rapid onset of action (time to Emax: 1-1.5 h) and 20-fold greater potency than losartan (ED20: 0.41 and 8.13 mg/kg, respectively). These results suggest that KR-31081 is a potent, orally active AT1 receptor antagonist useful for the research and diagnostic tools as an added exploratory potential.

Nutrient composition and in vitro fermentability of corn grain and stover harvested at different periods in Goesan, a mountainous area

  • Nogoy, Kim Margarette;Zhang, Yan;Lee, Ye Hyun;Li, Xiang Zi;Seong, Hyun A;Choi, Seong Ho
    • Journal of Animal Science and Technology
    • /
    • v.61 no.1
    • /
    • pp.18-27
    • /
    • 2019
  • With South Korea's limited capability of feed production because of its relatively small cultivable area, the country is pushed to depend on foreign feed imports despite the immensely fluctuating price of corn. Hence, intensive efforts to increase the total cultivable area in Korea like extending of farming to mountainous area is being practiced. Corn was planted in Goesan County, a mountainous area in the country. Grain and stover were harvested separately in three harvest periods: early-harvest (Aug 8), mid-harvest (Aug 18), and late-harvest (Aug 28). The nutrient composition such as dry matter (DM), crude protein (CP), crude fat (EE), organic matter (OM), neutral detergent fiber (NDF), acid detergent fiber (ADF), and non-fibrous carbohydrates (NFC) was determined after harvest. Effective degradability (ED) of the major nutrients (DM, NDF, ADF, and CP) were measured through in vitro fermentation of rumen fluid from Hanwoo (Korean cattle). pH, ammonia-N concentration, volatile fatty acid (VFA) concentration, and gas production were periodically measured at 0, 3, 6, 12, 24, 48, and 72 h. Corn grain showed higher nutrient content and ED than stover. It also had higher gas production but its pH, ammonia-N, and total VFA concentration were lower than corn stover. The best nutrient composition of corn grain was observed in early-harvest (high CP, EE, NDF, OM, NFC, and low ADF). Early-harvest of corn grain also had high effective degradability of dry matter (EDDM), effective degradability of neutral detergent fiber (EDNDF), effective degradability of acid detergent fiber (EDADF), and total VFA concentration. On the other hand, the best nutrient composition of stover was observed in mid-harvest (high DM, CP, NDF, and low ADF). EDDM, EDNDF, and EDADF were pronounced in early-harvest and mid-harvest of stover but the latter showed high total VFA concentration. Hence, early and mid-harvested corn stover and grain in a mountainous area preserved their nutrients, which led to the effective degradation of major nutrients and high VFA production.

Ginsenosides Attenuate Formalin-Induced Pains Through Spinal and Supraspinal Sites

  • Yoon, So-Rah;Park, Seok;Jung, Se-Yeon;Kim, Seok-Chang;Ko, Sung-Ryong;Nam, Ki-Yeul;Nah, Seung-Yeol
    • Journal of Ginseng Research
    • /
    • v.24 no.3
    • /
    • pp.143-147
    • /
    • 2000
  • In previous studies we have demonstrated that several individual ginsenosides such as Rc, Rd, Re and Ri relieves formalin-induced pain following systemic treatment. But it is unknown where these single ginsenosides induce antinociception. We investigated the antinoiceptive effect of four individual ginsenosides on formalin-induced pain after intrathecal (i.t.), intracereventricular (i.c.v.), or subcutaneous (s.c.) administration using mice. We found that ginsenoside Rc, Rd, and Re except Rf attenuated both acute and tonic phase of pain. Ginsenoside Rf attenuated only tonic phase of pain after i.t. administration. The ED$\_$50/ was 1.0 (0.55∼l.75 mg/kg) for Rc, 1.15 (0.6∼2.25 mg/kg) for Rd, and 8.9 (3.9∼20.5 mg/kg) for Re in acute phase of pain. The ED$\_$50/ was 0.3 (0.1∼0.85 mg/kg) for Rc, 0.6 (0.35∼l.1 mg/kg) for Rd, 2.45 (1.25∼4.65 mg/kg) for Re, and 1.9 (1.5∼4.25 mg/kg) for Rf in tonic phase of pain. We also found that ginsenoside Rc, Rd, Re, and Rf after i.c.v. administration attenuated both acute and tonic phase of pain. The ED5o for acute phase of pain was 0.9 (0.55∼l.4mg/kg) for Rc, 0.9 (0.45∼1.7 mg/kg) for Rd, 0.93 (0.5∼l .75 mg/kg) for Re, and 1.85 (0.95∼3.5 mg/kg) for Rf. The ED$\_$50/ for tonic phase of pain was 0.7 (0.45∼1.05 mg/kg) for Rc,1.25 (0.7∼2.2 mg/kg) for Rd, 0.85 (0.45∼1.6 mg/kg) for Re, and 0.8 (0.4∼1.45 mg/kg) for Rf. Thus, the order of the analgesic potency was Rc$\geq$Rd>Re>Rf in both i.t. and i.c.v. administration routes. However, s.c. pretreatment of four ginsenosides did not reduce formalin-induced pain. These results suggest that analgesic effect of ginsenosides is achieved through spinal or supraspinal site(s) in formalin test.

  • PDF

FIELD RR LYRAE 변광성의 특성: 공간분포 및 증원소함량 분포

  • Jeon, Yeong-Beom;Lee, Si-U
    • Publications of The Korean Astronomical Society
    • /
    • v.7 no.1
    • /
    • pp.207-229
    • /
    • 1992
  • 우리 은하계내 field RR Lyrae 변광성의 관측자료(GCVS 4th ed. )의 특성과 이들의 공간분포 및 증원소함량 분포를 조사하였다 이들의 공간분포에서 scale height 가 H = 0.6 kpc 인 원반(thick)형과 H = 2.2 kpc 인 헬로형의 두 성분으로 나타난다. 그리고 증원소함량의 은하중심거리와 은하정면거리에 따른 변화율은 각각 d[Fe/H]/dr = $-0.013\;{\sim}\;-0.020\;/kpc$ ($r\;{\le}\;20\;kpc$), d[Fe/H]/d|Z| = -0.034 /kpc ($|Z|\;{\le}\;10\;kpc$) 이다. 이러한 공간분포와 증원소함량의 기울기 변화는 구상성단의 경우와 비슷하게 이증진화모형을 나타낸다. 그러나 증원소함랑의 빈도분포로 보아 field RR Lyrae 변광성이 모두 구상성단에서 기원되었다고 보기는 어렵다.

  • PDF

Endoplasmic Reticulum (ER) Stress and Apoptosis in Parthenogenetic Porcine Embryos following Different Combination of Activation Methods

  • Park, Hye-Bin;Park, Yeo-Reum;Lee, Hwa-Yeon;Bae, Hyo-Kyung;Lee, Seunghyung;Park, Choon-Keun;Yang, Boo-Keun;Cheong, Hee-Tae
    • Journal of Embryo Transfer
    • /
    • v.32 no.1
    • /
    • pp.25-31
    • /
    • 2017
  • This study was conducted to investigate the effect of activation method on the endoplasmic reticulum (ER) stress induction, apoptosis and in vitro development of porcine parthenogenetic embryos. Porcine in vitro matured oocytes were activated by four activation methods; 1) electric stimulus (ES) (E), 2) $ES+10{\mu}M$ Ca-ionophore (A23187) treatment (EC), 3) ES+2 mM 6-dimethylaminopurine (6-DMAP) treatment (ED), or 4) ES+A23187 and 6-DMAP treatments (ECD). Parthenogenetic embryos were sampled to analyze x-box binding protein 1 (Xbp1) mRNA, ER stress-associated genes and apoptosis genes at 3 h after ES and the 1-cell and blastocyst stages. In the EC group, the band intensity of spliced Xbp1 (Xbp1s) mRNA was higher than those of the other groups at the 3 h and 1-cell stage, and higher than that of the E group at the blastocyst stage. Four ER stress-associated genes were expressed at the highest level in the EC group and weakly expressed in the ED group at 3 h after activation. However, most of the genes were highly expressed at the 1-cell and blastocyst stages with some variation in the EC and ECD groups. Expression of Bcl-2-associated X protein (Bax) and caspase-3 mRNA was significantly higher in the EC group than in the other groups at all development stages. The developmental rates to the blastocyst stage were higher in the ED and ECD groups than in the E and EC groups. These results suggest that the intracellular ER stress of parthenogenetic porcine embryos is affected by the activation method and subsequently lead to the apoptosis of embryos.

Quality Characteristics of Sulgidduk Containing Added Red Ginseng Powder (홍삼분말을 첨가한 설기떡의 품질특성)

  • Shin, Seung-Mee;Jung, Jung-Suk;Han, Myung-Ryun;Kim, Ae-Jung;Kim, Young-Ho
    • Korean journal of food and cookery science
    • /
    • v.25 no.5
    • /
    • pp.586-592
    • /
    • 2009
  • Sulgidduk samples containing 2, 4, and 8% red ginseng powder and a control[ED highlight - consider specifying what the control was, if 0%, then change to Sulgidduk samples containing 0(control), 2, 4 and 8%] were examined for moisture content, color, gelatinization properties, textural characteristics, and sensory qualities to determine the optimal ratio of red ginseng powder in the formulation. The moisture contents among the samples did not differ significantly. Specifically, they ranged from 39.64 to 40.69%, and increased as the red ginseng powder content increased. Additionally, the lightness decreased and the yellowness and redness increased as the red ginseng powder content increased. Evaluation of the gelatinization properties revealed that the, peak viscosity(P), hold viscosity(H), final viscosity(F), setback, and time to peak viscosity decreased with increasing red ginseng powder content, but the breakdown and temperature to peak viscosity did not differ significantly among samples[ED highlight - please ensure my changes are correct]. The hardness and adhesiveness decreased with increasing red ginseng powder content, as did the cohesiveness, gumminess, and chewiness; however, the springiness did not differ significantly among samples. Sulgidduk containing 4% red ginseng received the highest scores for flavor, taste, texture and overallquality. Based on the above results of the sensory and texture analyses, Sulgidduk containing 4% red ginseng had the highest quality[ED highlight - please ensure my changes are correct].

Synthesis of 8-Alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-ones and Evaluation of their Anticonvulsant Properties

  • Sun, Xian-Yu;Jin, Yun-Zhe;Li, Fu-Nan;Li, Gao;Chai, Kyu-Yun;Quan, Zhe-Shan
    • Archives of Pharmacal Research
    • /
    • v.29 no.12
    • /
    • pp.1080-1085
    • /
    • 2006
  • A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3-a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4]triazole[4, 3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having $ED_{50}$ values of 17.17 mg/kg and 24.55 mg/kg and protective index ($PI=TD_{50}/ED_{50}$) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having $ED_{50}$ values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.

Human Blastocysts;The Correlation Between Embryo Microscopical Assessments and Their Cell Number (인간 배반포기 배의 현미경적 분류와 세포수의 상관관계에 관한 연구)

  • Kim, E.Y.;Uhm, S.J.;Kim, M.K.;Yoon, S.H.;Park, S.P.;Chung, K.S.;Lim, J.H.
    • Clinical and Experimental Reproductive Medicine
    • /
    • v.23 no.3
    • /
    • pp.319-326
    • /
    • 1996
  • The objective of this study was to investigate correlation between the morphology by microscopic assessments of surplus blastocysts produced in human IVF program and their cell number obtained by differential labelling method. For these experiments, 76 surplus human blastocysts were obtained from 36 patients on day 5 after IVF, the embryos were classified to early (ErB), early expanding (EEB), middle expanding (MEB), expanded blastocyst (EdB) according to their blastocoel expansion and zona thickness. When the ovum size and zona thickness of the classified blastocysts were measured using micrometer, although the embryos were produced in the same culture condition, there were significant variances in ovum size ($148.8 217.6{\mu}m$) and zona thickness ($1.2-14.4{\mu}m$). Total blastomere cell number counted after hoechst staining was increased by two to three fold during the transition period from ErB ($39.1{\pm}3.6$) to EdB ($(89.6{\pm}3.3)$) stage on day 5 after IVF. ICM ($11.9{\pm}1.8-22.2{\pm}4.3$) and TE ($24.5{\pm}3.6-70.0{\pm}7.7$) cell numbers using differential labelling were also showed the increased pattern according to the developmental level. Especially, EdB which showed poor ICM morphologically also indicated the low ICM cell number after differential labelling. This demonstrated that there is good correlation between the morphological assessment and the cell number. The count of ICM and TE nuclei using differential labelling can be used as an important criterion, if it is accompanied with morphological assessments, in selecting the better embryos for improving the pregnancy rates in human blastocyst transfer program.

  • PDF

REGULARIZED ELSENSTELN SERIES ON METAPLECTIC GROUPS

  • Park, Young-Ho
    • Communications of the Korean Mathematical Society
    • /
    • v.9 no.4
    • /
    • pp.783-796
    • /
    • 1994
  • Let V be a vector space of dimension m over Q, and let (, ) be a non-degenerate bilinear form on V. Let r be the Witt index of V, and let $V = V' + V_0 + V"$ be the Witt decomposition, where $V_0$ is anisotropic and V', V" are paired non-singularly. Let H = O(m-r, r) be the isometry group of V, (, ), viewed as an algebraic group over Q. Let G = Sp(n) be the symplectic group of rank n defined over Q.ed over Q.

  • PDF

5-Arylidene-2(5H)-furanone Derivatives: Synthesis and Structure-Activity Relationship toward Cytotoxicity

  • Bang, Seong-Cheol;Kim, Yong;Yun, Mi-Young;Kim, Dong-Hee;Ahn, Byung-Zun
    • Proceedings of the PSK Conference
    • /
    • 2002.10a
    • /
    • pp.343.2-343.2
    • /
    • 2002
  • Ranunculin (RAN). isolated from Ranunculaceae. exhibited significant cytotoxic activity against KB and Bel-7402 cells with ED$_{50}$ values of 0.21 and 0.35).${\mu}4M respectively. Under physiological condition. the ranunculin was deglycosylated to be protoanemonin. an active form containing ${\alpha}{\beta}$-unsaturated ketone moiety. which successively dimerized to be anemonin inactive form. (omitted)

  • PDF