Imazethapyr 유도체의 제초활성에 미치는 3-(N-methyl-N-(X)-치환-phenylaminooxoacetyl) group의 영향

성낙도,김현재,장해성,김대황 충남대학교 생물공학연구소 1993 생물공학연구지 Vol.3 No.-

새로운 25종의 Imazethapyr 유도체, (2-(4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl)-3-(N-methyl-N-(X)치환 -phenylaminooxoacetyl)-5-methylpyridine)들을 합성하여 치환기(X) 변화에 따른 발아 전 후, 피(Echinochla crus-galli.)의 제초활성에 미치는 3-(N-methyl-N-(X)치환 -phenylaminoozoacetyl) group의 영향을 검토한 바, 발아 전보다 발아 후의 제초활성에 더 큰 영향을 미침을 알 수 있었다. 발아 후의 제초활성은 X-치환기의 전자밀게 효과와 입체상수(E_s)에 의존적이었으며 가장 큰 제초활성을 나타내는 화합물로는 bulky(E_s<O)하고 전자밀게 (б<O)가 치환된 화합물, 15(4-t-butyl group)와 20(3,5-dimethyl group)이었다. 그리고 높은 제초활성을 나타낼 것으로 예상되는 화합물의 조건들이 검토되었다. (1993년 9월 18일 접수, 1993년 9월 22일 수리). New twenty five Imazethapyr derivatives, [2-(4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl)-3-(N-methyl-N-X(sub.)-phenylaminooxoacetyl)-5-methylpyridine] were synthesized. and The quantitative structure activity relationships (QSARs) between their post-emergence herbicidal activity(pI_50) values in vivo against Barnyard grass (Echinochloa crus-galli) and physicochemical parameters of substituents(X) of 3-(N-methyl-N-X(sub.)-phenylaminoo-xoacetyl) group have been studied. From the basis on the findings, in case of post-emergence, the activities were dependent on the steric constant(E_s<θ)and electron donating (o<O) effect by subsitituents(X) of 3-(N-methyl-N-X(sub.)phenylaminooxacetyl) group. Therefore, The most effective compound, 15 (4-t-butyl group) and 20 (3,5-dimethyl group) were examined in this study. And the conditions on the compounds predicted to show higher herbicidal activity were also discussed.

토코페롤에서 유도된 기능성 화장품용의 새로운 계면 활성제

김영대 ( Y. D. Kim ),김창규 ( C. K. Kim ),이충남 ( C. N. Lee ),하병조 ( B. J. Ha ),이우영 ( W. Y. Lee ) 대한화장품학회 1992 대한화장품학회지 Vol.18 No.1

기능성 화장품을 위한 일련의 새롭고 독특한 비이온 계면활성제들을 생리활성물질인 a-Tocopherol과 에칠렌옥사이드의 반응에 의해서 제조하였다. 반응 생성물의 구조는 H¹-NMR, FT-IR, 원소분석, TLC를 통해 확인하였다. EP0에 대한 POV 와 CDV 연구에서 POE(n)TEs는 모두 토코페릴아세테이트와 유사한 항산화효과를 나타내었다. 그러나 POE(5)TE, POE(10)TE, P0E(18)TE의 광용혈에 대한 세포막보호효과는 Control에 비해 높은 결과를 나타내었다. POE(10)TE의 자외선흡수능은 Homosalate와 유사하게 나타났다. Primary Skin Irritation, Primary Eye Irritation 및 Acute Oral Toxicity 테스트결과 POE(n)TEs의 안전성이 입증되었다. P0E(n)TEs의 계면화학연구에서는 POE(10)TE가 가장낮은 CMC값을 나타내었고, POE(18)TE는 Maximum surface tension reduction과 최대 Foam volume을 보였다. 화장품의 실질적인 응용을 위한 테스트 결과 W/0유화에서는 POE(5>TE, 0/W유화에 서는 POE(10)TE 와 POE(12)TE, 분산에서는 POE(12)TE, 가용화에서는 P0E(18)TE, 겔화에서는 POE(50)TE가 우수하였는데, 이것은 POE(n)TEs의 구조적특성과 Liquid Crystal형성에 기인한 것으로 여겨진다. A new and unique class of nonionic surfactants was synthesized by reacting biological a-tocopherol with ethylene oxide for functional cosmetics. The structures were confirmed by Hl-UMR, FT-lR, TLC and elemental analysis. POV and conjugated diene value study for EPO showed POE(n)TE had antioxidative effect similar to tocopheryl acetate. Protective effect on cell membrane in photohemolysis of POE(5)TE, POE(10)TE and POE(18)TE were slightly lower than tocopherol but higher than nonoxynol-12, and POE(10)TE had UV absorption power comparable with tocopherol and homosalate. Biological activity of the hydrophobic group of the new surfactants make them unique and different from those of conventional nonionic surfactants. Systematic safety evaluations of POE(n)TEs on the skin and eye proved that they are as safe as tocopherol. The results of physicochemical study showed POE(10)TE had the lowest CMC value, POE(18)TE had the maximum surface tension reduction and the highest foam volume and POE(n)TEs had various HLB values by the degree of ethoxylation. The test results of technological and practical applications of these surfactants for cosmetics showed some POE(n)TEs were superior to conventional surfactants. POE(5)TE in W/O emulsions, POE(10)TE and POE(12)TE in O/W emulsions, POE(12)TE in dispersions, POE(18)TE in solubilizations and POE(50)TE in gelations were shown to be excellent which was considered due to the structural characteristic and formation of liquid crystals of POE(n)TEs. By the development and applications of these excel lent multi-functional surfactants, innovative functional cosmetics were successfully formulated.

시료내 라이신 : 에너지 비율이 이유 자돈의 성장 및 영양소 소화율에 미치는 영향 DE RATIO ON THE GROWTH PERFORMANCE AND NUTRIENT DIGESTIBILITY IN WEANED PIGS

한인규,김진동,현충남,이지훈,강완병,현영 한국영양사료학회 1999 韓國營養飼料學會誌 Vol.23 No.5

본 연구는 현대의 빠르게 성장하는 이유자돈에서 사료내 Lys : DE 비율이 이유자돈의 성장 및 영양소 소화율에 미치는 영향을 알아보기 위하여 실시되었다. 평균체중 5.70±0.14의 이유자돈 (Yorkshire×Landrace×Duroc) 100두를 공시하였고, 제 1기 (0∼14일) 동안, 두 수준의 에너지 (3,400과 3,600 ㎉ DE/㎏)와 두 수준의 Lys : DE 비율 (4.4와 4.9 g/Mcal), 제 2기 (15∼28일) 동안, 두 수준의 에너지 (3,300과 3,500 ㎉ DE/㎏)와 두 수준의 Lys : DE 비율 (4.4와 4.9 g/Mcal)이 되도록, 2×2 요인법으로 설계하였으며 4처리 5반복 반복당 5두의 이유자돈이 공시되었다. 시험 전기간 (0∼28일)동안, 일당중체량 (ADG)은 저 에너지-고 Lys : DE구가 저 에너지-저 Lys : DE구 보다 높았으며, 사료요구율 (FCR)은 고 에너지-고 Lys : DE구가 저 에너지-고 Lys : DE구를 제외한 나머지 처리구들 보다 낮은 경향을 보여 주었으나 유의한 수준은 아니였다. 사료내 Lys : DE 비율이 높아짐에 따라 ADG가 높아지는 경향을 보여 주었으나 유의하지는 않았다 (P>0.05). 그러나 FCR은 Lys : DE 비율이 높아짐에 따라 유의하게 개선되었으며 (P<0.05). 에너지 수준에 따른 차이는 관찰되지 않았다. 제 1기 동안 영양소 소화율은 사료내 에너지수준에 따라 영향받지 않았다. 건물소화율과 총에너지 소화율은 Lys : DE 비율이 증가함에 따라 유의하게 개선되었다 (P<005). 제 2기 동안 조지방을 제외한 영양소 소화율은 사료내 에너지 수준간에 따라 영향받지 않았다. 사료내 Lys : DE 비율에 따른 영양소 소화율에 있어 유의한 차이는 관찰되지 않았다. 제 1기 동안 필수 및 비필수 아미노산 소화율에 있어서는, 처리에 따른 유의한 차이가 관찰되지 않았다. 그러나 제 2기 동안 총필수 아미노산과 총 아미노산 소화율이 사료내 Lys : DE 비율이 증가함에 따라 유의하게 개선되었다 (P<0.05). 본 실험결과는 이유자돈이 4.4 g Iysine/Mcal DE 수준보다 4.9 g Iysine/Mcal DE 수준의 사료를 효과적으로 이용할 수 있음을 제시해 주었다. This study was carried out to evaluate the effect of lysine:energy ratio (Lys : DE) on growth performance and nutrient digestibility of weaned pigs. A total of 100 pigs (Yorkshire × Landrace × Duroc) averaging 5.7±0.14 ㎏ of initial body weight were employed. Two levels of dietary energy (3,400 and 3,600 ㎉ DE/㎏) with two levels of Lys : DE ratio (4.4 and 4.9 g/Mcal) for phase I period (0 to 14 d) and two levels of energy (3,300 and 3,500 ㎉ DE/㎏) with two levels of Lys : DE ratio (4.4 and 4.9 g/Mca1) for phase II period (15 to 28 d) were involved in a two × two factorial arrangement, respectively. Each treatment had five replicates with five pigs per replicate. During phase I period (0 to 14 d), no difference between groups in ADFI, and feed conversion rate (FCR) was significant. However, FCR was significantly improved with increased Lys : DE ratio (P<0.05). During phase II period (15 to 28 d), ADG, ADFI and FCR were not significantly (P<0.05) different among groups. There was no interaction between dietary energy concentration and Lys : DE ratio in growth performances of weaned pigs. FCR, however, was improved with increased energy level and Lys : DE ratio (P<0.05). During the overall period (0 to 28 d), there was no interaction between dietary energy concentration and Lys : DE ratio in growth performances of weaned pigs. However, there was a tendency for higher ADG with higher Lys : DE ratio. FCR was significantly improved with increased Lys : DE ratio (P<0.05), but was not affected by dietary energy concentration. During phase I period (0 to 14 d), no differences in nutrients digestibilities were observed between dietary energy levels. Between dietary Lys : DE ratios, dry matter (DM) and gross energy (GE) digestibilities were significantly (P<0.05) improved with higher Lys : DE ratio. During phase II period (15 to 28 d), no differences in nutrients digestibilities except energy levels. Between dietary Lys : DE ratios, no significant differences in nutrients digestibilities was observed. In regard to amino acids digestibilities, during phase I period (0 to 14 d), average values of essential amino acids (EAA), non-essential amino acids (NEAA) and total amino acids digestibilities were not significantly influenced by dietary energy levels and Lys : DE ratios. During phase II period ( 15 to 28 d), pigs fed high Lys : DE ratio diets showed significantly (P<0.05) higher total EAA and total amino acids digestibilities. The digestibilities of threonine, methionine, phenylalnine and serine were significantly improved as the dietary Lys : DE ratio increased. In conclusion, the results of the current experiment indicate that fast-growing weaned pigs might be able to use more effectively diets contatining 4.9 g lysine/Mcal DE compared to diets containing 4.4 g lysine/Mcal DE.

계단형 텅스텐 결정면의 질소 흡착에 관한 연구 : Ⅱ. W(210) 및 W(310)면

최대선(D. S. Choi),한종훈(J. H. Han),백선목(S. M. Paik),박노길(N. G. Park),김욕욱(Y. W. Kim),황정남(C. N. Whang) 한국진공학회(ASCT) 1996 Applied Science and Convergence Technology Vol.5 No.4

장전자 방출법으로 텡스텐 (210)면 및 (310)면(100)면의 질소 흡착에 의한 일함수의 변화에 heat of desorption을 측정하였으며 Thermal Desortion Spectra(TDS) 결과로부터 adsorption site를 예측하였다. 텅스텐 (210)면 및 (310)면에 에 질소가 흡착될 때 흡착율에 따라 일함수는 증가하다가 각 면에 대하여 흡착율 5 Langmuir일때 최대 변화량 0.29 eV및 0.20 eV에서 포화되었다. TDS 결과는 이 면들은 낮은 dose의 영역에서 각각 3개의 흡착 site가 있음을 보였으며 이 흡착 site들 중 α₁state의 spectrum의 강도는 (210)면에서 보다 (310)면에서 상대적으로 강해짐을 보였다. 또한 (210)와 (310)면의 α₁ 과 β₂ state의 흡착 site에 흡착된 질소의 dipole moment의 방향은 이 흡착 site들에 대응되는 (100)면의 α₁ 과 β₂state의 흡착 site에 흡착된 질소의 dipole moment의 방향과 반대 방향으로 측정되었으며 이 현상으로부터 질소의 상대적인 흡착 위치를 예측하였다. The heat of desorption and the work function change induced by nitrogen adsorption on the stepped tungstein surface planes, W(210) and W(310), are measured using the Field Electron Emission Microscope(FEM). The adsoption sites are predicted from the Thermal Desortion Spectra(TDS). The work function change of both W(210) and W(310) planes increase as increasing the nitrogen dose and saturates at the nitrogen dose about 5 Langmuir to 0.29 eV and 0.20 ev respectively. We find three adsorption site on each plane for the low dose range. The TDS result shows that the intensity of α₁, state on W(310) is much stronger than that of α₁ state on W(210), and the direction of nitrogen dipole moment adsorbed on the sites correspond to α₁, and β₂ states on W(210) and W(310) planes are in the opposite direction to that of the equivalent states on W(100) plane. From this observation we can predict the relative atomic position in the zdirection (perpendicular direction to the surface) of nitrogen molecules/atoms adsorbed on these sites.

Imazapyr 유도체의 제초활성에 미치는 3 - ( N - methyl - N ( X ) - 치환 - Phenylaminooxoacetyl ) Group 의 영향

성낙도(N . D . Sung),유택승(T . S . Ryu),장해성(H . S . Chang),김대황(D . W . Kim) 한국응용생명화학회 1994 Applied Biological Chemistry (Appl Biol Chem) Vol.37 No.6

New seventeen imazapyr derivatives, 2-(4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl)-3-(N-methyl-N-X(sub.)-phenylaminooxoacetyl)pyridine, 6 were synthesized and their pre-emergence herbicidal activity(pI_(50) in vivo against Corn (Zea mays L.) and Pigweed (Amaranthus viridis L.) were studied by the pot test under paddly conditions. (quantitative structure activity relationships (QSARs) were analyzed using the physicochemical parameters of substituent(X) on the phenyl ring of 3-(N-methyl-N-X(sub.)-phenylaminooxoacetyl) group and regression analysis. The herbicidal activities were related to the steric effect of X-substituent. The effect was rationalized by paraholic function of MR and L₁, where the optimal values were MR=5.56 (Zea mays L.) and L₁=3.34 Å (Amaranthus viridis L.). Among them, 2,5-difluoro substituted compound, 6i showed good herbicidal activity against Pigweed with excellent tolerance to Corn.

Disposition and metabolism of (2S,3S,4R)-N''-cyano-N-(6-amino-3,4-dihydro-3-hydroxy-2-methyl-2-dimethoxy methyl-2H-benzopyran-4-yl)-N'-benzylguanidine, a novel neuroprotective agent for ischemia-reperfusion damage, in rats

Kim, N. S.,Yoo, H. H.,Lee, M. W.,Kim, H. S.,Kim, D. H. Taylor & Francis 2007 Xenobiotica Vol.37 No.5

<P> The metabolism and disposition of KR31378 (a benzopyran derivative and a novel neuroprotective agent) were investigated following single oral or intravenous administration of [14C]-KR31378 to rats. [14C]-KR31378 was rapidly absorbed after oral dosing with an oral bioavailability of greater than 71%. The maximum plasma concentration and area under the curve of total radioactivity in rat plasma increased proportionally to the administered dose. KR31378 was distributed over all organs and tissues except for brain, eyeball and testis, and declined by first order kinetics up to 24 h after dosing. Excretion of the radioactivity was 29.5% of the dose in the urine and 58.5% in the feces within 2 days after oral administration. Biliary excretion of the radioactivity in bile duct-cannulated rats was about 66.0% for the first 24 h. KR31378 was extensively metabolized by ring hydroxylation, O-demethylation, oxidation and reduction with subsequent N-acetylation and O-glucuronide conjugation. N-acetylated conjugates (M2, M10, M11, M12, M14, and M15) were identified as the predominant metabolites in rats.</P>

Imazethapyr 유도체의 제초활성에 미치는 3 - ( N - methyl - N - ( X ) - 치환 - phenylaminooxoacetyl ) group 의 영향

성낙도(N . D . Sung),김현재(H . J . Kim),장해성(H . S . Chang),김대황(D . W . Kim) 한국응용생명화학회 1993 Applied Biological Chemistry (Appl Biol Chem) Vol.36 No.5

New twenty five Imazethapyr derivatives, [2-(4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl)-3-(N-methyl-N-X(sub.)-phenylaminooxoacetyl)-5-methylpyridine] were synthesized. and The quantitative structure activity relationships (QSARs) between their post-emergence herbicidal activity(pI_(50)) values in vivo against Barnyard grass (Echinochloa crus-galli) and physicochemical parameters of substituents(X) of 3-(N-methyl-N-X(sub.)-phenylaminooxoacetyl) group have been studied. From the basis on the findings, in case of post-emergence, the activities were dependent on the steric constant(E_s$lt;0) and electron donating (σ$lt;0) effect by subsitituents(X) of 3-(N-methyl-N-X(sub.)phenylaminooxoacetyl) group. Therefore, The most effective compound, 15 (4-t-butyl group) and 20 (3,5-dimethyl group) were examined in this study. And the conditions on the compounds predicted to show higher herbicidal activity were also discussed.

Implication of intracellular ROS formation, caspase-3 activation and Egr-1 induction in platycodon D-induced apoptosis of U937 human leukemia cells

Shin, D.Y.,Kim, G.Y.,Li, W.,Choi, B.T.,Kim, N.D.,Kang, H.S.,Choi, Y.H. Masson Pub. USA, Inc 2009 BIOMEDICINE AND PHARMACOTHERAPY Vol.63 No.2

Platycodon D is a major constituent of triterpene saponins found in the root of Platycodon grandiflorum, Platycodi Radix, which is widely used in traditional Oriental medicine for the treatment of many chronic inflammatory diseases. The results of previous studies have shown that this compound has in vitro growth-inhibitory activity in human cancer cells, however, the mechanism by which this action occurs is poorly understood. In this study, we examined the effects of platycodon D on the production of reactive oxygen species (ROS) and evaluated the association of these effects with apoptotic tumor cell death using a human leukemic U937 cell line. The results of this study demonstrate that platycodon D mediates ROS production, and that this mediation is followed by a decrease in mitochondrial membrane potential (MMP, ΔΨ<SUB>m</SUB>), activation of caspase-3, and cleavage of poly (ADP-ribose) polymerase (PARP). Both the cytotoxic effects and apoptotic characteristics induced by platycodon D treatment were significantly inhibited by z-DEVD-fmk, a caspase-3 inhibitor, which demonstrates the important role that caspase-3 plays in the observed cytotoxic effect. Additionally, the transcription factor early growth response-1 (Egr-1) gene was transcriptionally activated and the levels of non-steroidal anti-inflammatory drug (NSAID)-activated gene-1 (NAG-1) protein were elevated in platycodon D-treated U937 cells. However, the quenching of ROS generation in response to treatment with a ROS scavenger, N-acetyl-l-cysteine, reversed the platycodon D-induced apoptosis effects via inhibition of Egr-1 activation, ROS production, MMP collapse, and the subsequent activation of caspase-3. Although further studies are needed to demonstrate that increased expression of Egr-1 by platycodon D leads directly to NAG-1 induction and subsequent apoptosis, our observations clearly indicate that ROS induced through Egr-1 activation are involved in the early molecular events involved in the platycodon D-induced apoptotic pathway.

Effect of annealing of graphene layer on electrical transport and degradation of Au/graphene/n-type silicon Schottky diodes

Kim, D.J.,Kim, G.S.,Park, N.W.,Lee, W.Y.,Sim, Y.,Kim, K.S.,Seong, M.J.,Koh, J.H.,Hong, C.H.,Lee, S.K. Elsevier Sequoia 2014 JOURNAL OF ALLOYS AND COMPOUNDS Vol.612 No.-

We have investigated the effect of annealing of graphene sheets on the electrical properties of Au/graphene/n-type silicon Schottky diode. Large scale graphene sheets were grown by chemical vapor deposition and then annealed at 300, 400, and 500<SUP>o</SUP>C; one sheet was left un-annealed as the control. The diodes were fabricated by transferring the graphene sheets directly onto n-type Si substrates and the current-voltage (I-V) and capacitance-voltage (C-V) characteristics were evaluated. The average values of the Schottky barrier height (SBH) and ideality factor (η) for the as-fabricated Au/graphene/n-type silicon Schottky diode from I-V measurements were determined to be ~0.8+/-0.01eV and ~1.79+/-0.05, respectively, whereas the SBH from C-V measurements was ~0.89+/-0.01eV. The electrical transport characteristics measured at room temperature indicated that annealing of graphene sheet prior to the transfer of the graphene onto the n-Si substrates significantly reduces the electric degradation of the Schottky diodes, even though no distinct differences in other electric properties, including ideality factors and SBHs, before or after annealing of the graphene sheets were observed. Thus, by simply annealing the graphene sheets at 500<SUP>o</SUP>C, we found that the Au/graphene/n-type silicon Schottky diode showed an approximately 3.3-fold lower series resistance as compared with the un-annealed Schottky diode under air exposure of up to 7days. These annealed diodes showed significantly reduced electrical degradation by removing the potentially trapped H<SUB>2</SUB>O and/or O<SUB>2</SUB> at the interface between the graphene layer and the n-Si substrate.

Production of recombinant human acid α-glucosidase with high-mannose glycans in gnt1 rice for the treatment of Pompe disease

Jung, J.W.,Huy, N.X.,Kim, H.B.,Kim, N.S.,Van Giap, D.,Yang, M.S. Elsevier Science Publishers 2017 Journal of biotechnology Vol.249 No.-

<P>Lysosomal storage diseases are a group of inherited metabolic disorders. Patients are treated with enzyme replacement therapy (ERT), in which the replacement enzymes are required to carry terminal mannose or mannose 6-phosphate residues to allow efficient uptake into target cells and tissues. N-acetylglucosaminyl-transferase-I (GnTI) mediates N-glycosylation in the cis cisternae of the Golgi apparatus by adding N-acetylglucosamine to the exposed terminal mannose residue of core N-glycan structures for further processing. Mutant rice lacking GnTI produces only high mannosylated glycoproteins. In this study, we introduced a gene encoding recombinant human acid alpha-glucosidase (rhGAA), which is used in ERT for Pompe disease, into gnt1 rice callus by particle bombardment. Integration of the target gene into the genome of the gnt1 rice line and its mRNA expression were confirmed by PCR and Northern blot, respectively. Western blot analysis was performed to confirm secretion of the target proteins into the culture media. Using an indirect enzyme linked immunosorbent assay, we determined the maximum expression of rhGAA to be approximately 45 mg/L, 13 days after induction. To assay the enzymatic activity and determine the N-glycan profile of rhGAA, we purified the protein using a 6 x histidine tag. The in vitro alpha-glucosidase activity of rhGAA from gnt1 rice callus (gnt1-GAA) was 3.092 U/mg, similar to the activity of the Chinese hamster ovary cell-derived GAA (3.154 U/mg). N-glycan analysis revealed the presence of high-mannose N-glycans on gnt1-GAA. In addition, the production of high-mannose GAA using gnt1 rice calli as an expression host was characterized, which may aid the future development of therapeutic enzymes for the treatment of Pompe disease.</P>