• 제목/요약/키워드: rK1-3

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Diosgenin 유도체 합성과 진통 및 항고지혈 효과 (Synthetic Derivatives of Diosgenin and Their Antinociceptive and Antihypercholesterolemic Effects)

  • 김학순;마은숙
    • 약학회지
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    • 제51권1호
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    • pp.56-62
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    • 2007
  • Twelve epoxy and hydroxydiosgenin derivatives (DI-1${\sim}$DI-12) were synthesized from diosgenin (25(R)-5-spirosten-3${\beta}$-ol). Diosgenin was epoxidized with m-chloroperoxybenzoic acid (mCPBA) to oxidize 25(R)-4${\alpha}$,5${\alpha}$-epoxyspirostane (DI-1). Diosgenin was reacted with DDQ to form 25(R)-1,4,6-spirostatrien-3-one (DI-2), which was treated with 30% H$_2$O$_2$ to give 25(R)-1${\alpha}$,2${\alpha}$-epoxy-4,6-spirostadien-3-one (DI-3) and treated with mCPBA to form 25(R)-6${\alpha}$,7${\alpha}$-epoxy-1,4-spirostadien-3-one (DI-7), respectively. DI-3 was reduced with NaBH$_4$ to afford 25(R) -1${\alpha}$,2 ${\alpha}$-epoxy-4,6-spirostadien-3${\beta}$-ol(DI-4) and reacted with Li metal in absolute ethanol to form 25(R)-2-ethoxy-1,4,6-spirostatrien-3-one (DI-5). DI-7 was reduced with NaBH$_4$ to produce 25(R)-3${\beta}$,7${\alpha}$-dihydroxy-4-spirostene (DI-8) and treated with Li metal in liquid ammonia to produce 25(R)-7${\alpha}$-hydroxy-4-spirosten-3-one (DI-9). DI-2 was reduced with NaBH$_4$ to form 25(R) -4,6-spirestadien-3${\beta}$-ol(DI-10), which was stirred with 30% H$_2$O$_2$ to synthesize 25(R)-4,6-spirostadien-3-one (DI-11) and reacted with mCPBA to give 25(R)-4${\beta}$,5${\beta}$ -epoxy-6-spirosten-3${\beta}$-ol (DI-12), respectively. The antinociceptive effects of synthesiz ed compounds were measured by hot plate method and compound DI-7 signifcantly exhibited antinociceptive effect. DI-2 decreased the serum triglyceride and total cholesterol levels in poloxamer P-407 injected rat.

Separation performances of a nanofiltration membrane for chlorides, nitrates and sulfates aqueous solutions

  • Wang, Da-Xin;Su, Meng;Wang, Xiao-Lin
    • 한국막학회:학술대회논문집
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    • 한국막학회 2004년도 Proceedings of the second conference of aseanian membrane society
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    • pp.155-160
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    • 2004
  • Permeation experiments of a commercial nanofiltration membrane (nominated as ESNA 1) were carried out with aqueous solutions of various single salts, that is, five chlorides (NH$_4$Cl, NaCl, KCl, MgCl$_2$ and $CaCl_2$), three nitrates $(NaNo_3,\;Mg(No_3)_2\;and\;Ca(NO_3)_2)\;and\;three\;sulfates\;((NH_4)_2SO_4,\;Na_2SO_4\;and\;MgSO_4)$. The experimental results showed that (1) the permeate volume flux of the ESNA 1 membrane increased and decreased with the growth of the applied pressure and the feed concentration of salts, respectively. The real rejection of ESNA 1 membrane to most single salts increased with the growth of the permeate volume flux. (2) The reflection coefficients of ESNA 1 membrane to chlorides, nitrates and sulfates are 0.97, 0.96 and 0.99, respectively. The solute permeability of most salts except for magnesium and calcium salts increased with the growth of feed concentration. (3) The sequence of the rejections of ESNA 1 membrane to anions is $R({SO_4}^{2-})>R(CI)>R(NO_3)$ at the same feed concentration. While the sequence of the rejections to cations is cataloged into two cases: $R(Na^+)>R(K^+)>R(Mg^{2+})>R(Ca^{2+})$ at the concentration of 10 mol/$m^3$ and $R(Mg^{2+})>R(Ca^{2+})>R(Na^+)>R(K^+)$ at the concentration of 100 mol/$m^3$. The separation capability of a NF membrane is usually affected by the electrostatic effect and the steric-hindrance effect. In this case, the electrostatic effect is the major factor at low concentration and the steric-hindrance effect is the major factor at high concentration. Both the specific sorption and the hydration also reasonably influenced the separation performance of NF membrane to salts.

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MicroRNA expression profiling during the suckling-to-weaning transition in pigs

  • Jang, Hyun Jun;Lee, Sang In
    • Journal of Animal Science and Technology
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    • 제63권4호
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    • pp.854-863
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    • 2021
  • Weaning induces physiological changes in intestinal development that affect pigs' growth performance and susceptibility to disease. As a posttranscriptional regulator, microRNAs (miRNAs) regulate cellular homeostasis during intestinal development. We performed small RNA expression profiling in the small intestine of piglets before weaning (BW), 1 week after weaning (1W), and 2 weeks after weaning (2W) to identify weaning-associated differentially expressed miRNAs. We identified 38 differentially expressed miRNAs with varying expression levels among BW, 1W, and 2W. Then, we classified expression patterns of the identified miRNAs into four types. ssc-miR-196a and ssc-miR-451 represent pattern 1, which had an increased expression at 1W and a decreased expression at 2W. ssc-miR-499-5p represents pattern 2, which had an increased expression at 1W and a stable expression at 2W. ssc-miR-7135-3p and ssc-miR-144 represent pattern 3, which had a stable expression at 1W and a decreased expression at 2W. Eleven miRNAs (ssc-miR-542-3p, ssc-miR-214, ssc-miR-758, ssc-miR-4331, ssc-miR-105-1, ssc-miR-1285, ssc-miR-10a-5p, ssc-miR-4332, ssc-miR-503, ssc-miR-6782-3p, and ssc-miR-424-5p) represent pattern 4, which had a decreased expression at 1W and a stable expression at 2W. Moreover, we identified 133 candidate targets for miR-196a using a target prediction database. Gene ontology and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses revealed that the target genes were associated with 19 biological processes, 4 cellular components, 8 molecular functions, and 7 KEGG pathways, including anterior/posterior pattern specification as well as the cancer, PI3K-Akt, MAPK, GnRH, and neurotrophin signaling pathways. These findings suggest that miRNAs regulate the development of the small intestine during the weaning process in piglets by anterior/posterior pattern specification as well as the cancer, PI3K-Akt, MAPK, GnRH, and neurotrophin signaling pathways.

CHOW GROUPS OF COMPLETE REGULAR LOCAL RINGS III

  • Lee, Si-Chang
    • 대한수학회논문집
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    • 제17권2호
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    • pp.221-227
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    • 2002
  • In this paper we will show that the followings ; (1) Let R be a regular local ring of dimension n. Then $A_{n-2}$(R) = 0. (2) Let R be a regular local ring of dimension n and I be an ideal in R of height 3 such that R/I is a Gorenstein ring. Then [I] = 0 in $A_{n-3}$(R). (3) Let R = V[[ $X_1$, $X_2$, …, $X_{5}$ ]]/(p+ $X_1$$^{t1}$ + $X_2$$^{t2}$ + $X_3$$^{t3}$ + $X_4$$^2$+ $X_{5}$ $^2$/), where p $\neq$2, $t_1$, $t_2$, $t_3$ are arbitrary positive integers and V is a complete discrete valuation ring with (p) = mv. Assume that R/m is algebraically closed. Then all the Chow group for R is 0 except the last Chow group.group.oup.

감마선 조사에 의한 수도의 단간 및 조숙돌연변이체 I. 변이체의 출현빈도 및 변이분포 (Short Culm and Early Maturing Mutants Induced by Gamma Irradiation in Rice I . Mutation Rate and Variability)

  • 이영일;신인철;홍병희
    • 한국작물학회지
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    • 제34권4호
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    • pp.378-383
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    • 1989
  • 수도 재배품종의 단점형질을 수양코자 상풍벼와 섬진벼 종자에 ${\gamma}$-선을 20kR로 조사하여 단간 및 조숙돌연변이 계통을 선발하는 과정에서 얻은 결과를 요약하면 다음과 같다. 1. 품종간에 변이출현율은 섬진벼보다 상풍벼에서 높게 나타났으며 조신선량간에는 두 품종 모두 20kR보다 25kR 조신구에서 높게 나타났다. 2. M$_2$세대에서 단간 조숙 및 유성변이체의 출현율은 상풍벼 20kR와 25kR에서 각각 1.10%와 1.47%, 섬진벼 20kR와 25kR에서 0.51%와 1.25%이었다. 3. M$_3$ 세대에서 단간돌연변이 계통중 상풍벼와 섬진벼의 두 품종 모두 25kR 조신구에서 모품종에 비해 각각 간장이 57%와 40%RK지 단축된 단간변이계통을 선발할 수 있었고, 모품종에 비해 10%정도 단축된 계통이 많이 출현하였다. 4. M$_3$세대에서 출수기의 변이분포는 비교적 넓었고 상풍벼와 섬진벼에서 모품종보다 출수기가 각각 30일과 20일 빠른 조숙돌연변이 계통을 선발할 수 있었고 모품종에 비해 7일 정도 단축된 계통의 출현은 많았다.

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Beagle Dog에서 cis-Malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II)(SKI 2053R)의 아급성독성시험에 관한 연구 (Subacute toxicity of cis-Malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II)(SKI 2053R) in Beagle Dogs)

  • 이영순;강경선;신동진;조재진;김형욱;김배환;임윤규
    • Toxicological Research
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    • 제8권2호
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    • pp.235-253
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    • 1992
  • A subacute toxicity study of cis-Malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II)(SKI 2053R) was carried out to obtain information on its toxicological profiles, and to determine the maximum tolerated dose in beagle dogs. Four groups of beagle dogs (2M and 2F per group, 0,0.5,1.0,2.0mg/kg/day)were given 15 i.v. injections of SKI 2053R. In order to compare the toxic effects of SKI 2053R with those of cisplatin, one group was treated with cisplatin(0.7mg/kg/day)according to the same treatment schedule. The dosing schedule was divided into 3 courses of 5 consecutive days with 23-day dose-free intervals between each course. After completion of the treatments, remaining dogs were necropsied under established guidelines. Three of four dogs in the high dose group and one of four dogs in the middle dose group treated with SKI 2053R died of hypovolemic shock secondary to hemorrhagic and ulcerative enterocolitis. No toxicity-related mortality occurred in the low dose group of SKI 2053R. No survivor was observed in the group of cisplatin. Clinical signs including vomiting, diarrhea, anorexia and loss body weight were apparent in dogs given either cisplatin or high and middle doses of SKI 2053R. Severe thrombocytopenia and leukocytopenia were observed in the high dose group of SKI 2053R and cisplatin-treatment group, while toxicities as bone marrow suppression were reversible. The significant elevation of serum ALP values in group of SKI 2053R(2.0 mg/kg/day and 1.0mg/kg/day) and cisplatin(0.7mg/kg/day)was observed. Slight proteinuria waa observed in high and middle dose level groups of SKI 2053R. In histopathological examinations, pathological alterations of liver, kidney and spleen were noted dose-dependantly in dogs treated with SKI 2053R, and there was no overt sign of toxicity in low dose group of SKI 2053R. Compared to SKI 2053R, more severe durg-related toxicities occurred in dogs treated with cisplatin. It waw estimated that maximum tolerated dose of SKI 2053R in this treatment schedule was 0.5~0.7mg/kg/day. In conclusion, overall toxic potential of SKI 2053R was approximately 3 times lower than that of cisplatin with respect of lethality.

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MicroRNA-766-3p Inhibits Tumour Progression by Targeting Wnt3a in Hepatocellular Carcinoma

  • You, Yu;Que, Keting;Zhou, Yun;Zhang, Zhen;Zhao, Xiaoping;Gong, Jianpin;Liu, Zuojin
    • Molecules and Cells
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    • 제41권9호
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    • pp.830-841
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    • 2018
  • Recent studies have indicated that microRNAs (miRNAs) play an important role in hepatocellular carcinoma (HCC) progression. In this study, we showed that miR-766-3p was decreased in approximately 72% of HCC tissues and cell lines, and its low expression level was significantly correlated with tumour size, TNM stage, metastasis, and poor prognosis in HCC. Ectopic miR-766-3p expression inhibited HCC cell proliferation, colony formation, migration and invasion. In addition, we showed that miR-766-3p repressed Wnt3a expression. A luciferase reporter assay revealed that Wnt3a was a direct target of miR-766-3p, and an inverse correlation between miR-766-3p and Wnt3a expression was observed. Moreover, Wnt3a up-regulation reversed the effects of miR766-3p on HCC progression. In addition, our study showed that miR-766-3p up-regulation decreased the nuclear ${\beta}-catenin$ level and expression of Wnt targets (TCF1 and Survivin) and reduced the level of MAP protein regulator of cytokinesis 1 (PRC1). However, these effects of miR-766-3p were reversed by Wnt3a up-regulation. In addition, PRC1 upregulation increased the nuclear ${\beta}-catenin$ level and protein expression of TCF1 and Survivin. iCRT3, which disrupts the ${\beta}-catenin-TCF4$ interaction, repressed the TCF1, Survivin and PRC1 protein levels. Taken together, our results suggest that miR-766-3p down-regulation promotes HCC cell progression, probably by targeting the Wnt3a/PRC1 pathway, and miR-766-3p may serve as a potential therapeutic target in HCC.

Isolation and Development of Quantification Method for Cyanidin-3-Glucoside and Cyanidin-3-Rutinoside in Mulberry Fruit by High-Performance Countercurrent Chromatography and High-Performance Liquid Chromatography

  • Choi, Soo-Jung;Jeon, Heejin;Lee, Chang Uk;Yoon, Shin Hee;Bae, Soo Kyung;Chin, Young-Won;Yoon, Kee Dong
    • Natural Product Sciences
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    • 제21권1호
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    • pp.20-24
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    • 2015
  • Cyanidin-3-glucoside (C3G) and cyanidin-3-rutinoside (C3R) were isolated by high-performance countercurrent chromatography (HPCCC) using a two-phase solvent system composed of tert-butyl methyl ether/n-butanol/acetonitrile/water/trifluoroacetic acid (1 : 3 : 1 : 5 : 0.01, v/v) to give pure C3G (34.1 mg) and C3R (14.3 mg) from 1.5 g crude mulberry fruit extract. Using the pure C3G and C3R, a reliable high-performance liquid chromatography (HPLC) method was developed and validated to determine the C3G and C3R contents in mulberry fruit. C3G and C3R were separated simultaneously using an Eclipse XDB-C18 column ($4.6{\times}250mm$ I.D., $5{\mu}m$) coupled with a photodiode array detector (PDA). The gradient elution of the mobile phase consisting of acetonitrile (0.5% formic acid) and water (0.5% formic acid) was applied (1.0 mL/min), and the detection wavelength was 520 nm. The calibration curves of C3G and C3R showed good linearity (both with $r^2=0.9996$) in the concentration range $15.625-500{\mu}g/mL$, and the relative standard deviations (RSD%) of intra- and inter-day variability were in the ranges 2.1 - 8.2% and 4.1 - 17.1%, respectively. The accuracies were ranged 96.5 - 102.6% for C3G and C3R, respectively. The developed HPLC method was used to determine the contents of C3G and C3R in newly harvested mulberry from eight different provinces of Korea.

On the Subsemigroups of a Finite Cyclic Semigroup

  • Dobbs, David Earl;Latham, Brett Kathleen
    • Kyungpook Mathematical Journal
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    • 제54권4호
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    • pp.607-617
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    • 2014
  • Let S = C(r,m), the finite cyclic semigroup with index r and period m. Each subsemigroup of S is cyclic if and only if either r = 1; r = 2; or r = 3 with m odd. For $r{\neq}1$, the maximum value of the minimum number of elements in a (minimal) generating set of a subsemigroup of S is 1 if r = 3 and m is odd; 2 if r = 3 and m is even; (r-1)/2 if r is odd and unequal to 3; and r/2 if r is even. The number of cyclic subsemigroups of S is $r-1+{\tau}(m)$. Formulas are also given for the number of 2-generated subsemigroups of S and the total number of subsemigroups of S. The minimal generating sets of subsemigroups of S are characterized, and the problem of counting them is analyzed.