• Title/Summary/Keyword: P2P Agent

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Synthesis of SATE Prodrug of 6'-Fluoro-6'-methyl-5'-noradenosine Nucleoside Phosphonic Acid as a New Class of Anti-HIV Agent

  • Li, Hua;Yoo, Jin-Cheol;Baik, Young-Chan;Lee, Won-Jae;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • v.31 no.9
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    • pp.2514-2518
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    • 2010
  • A very simple synthetic route of a novel SATE prodrug type of 6'-fluoro-6'-methyl-5'-noradeonosine carbocyclic nucleoside phosphonic acid is described. The key fluorinated alcohol intermediate 7 was prepared from the epoxide intermediate 6a via selective ring-opening of epoxide. Coupling of 7 with $N^6$-bis-Boc-adenine under a Mitsunobu reaction followed by phosphonation and deprotection afforded the carbocyclic phosphonic acid. The chemical stability of the bis(SATE) derivative 13 was measured at neutral (pH 7.2) and slightly acidic (Milli-Q water, pH 5.5) pH. The antiviral activity test of the SATE prodrug 13 and its parent nucleoside phosphonic acid 11 were evaluated against HIV-1.

Preparation of Coating Agent for Fresh-Cut Fruit on Cake and Its Storage Characteristics (케이크용 신선편의 과일 코팅제의 제조 및 저장 특성)

  • Park, Jung-Eun;Yeon, Soo-Ji;Kim, Dong-Ho;Park, Yeo-Jin;Jang, Keum-Il
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.42 no.12
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    • pp.2019-2027
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    • 2013
  • In this study, we tried to develop a coating agent for the fresh-cut fruits used in cakes. First, the coating agent mixing ratios of sugar, pectin, sodium alginate, carrageenan, xanthan gum, vitamin C, and purified water were selected to be 55, 2, 2, 0.04, 0.1, 0.05, and 40.81% (w/w), respectively. In a freeze-thaw stability of the coating agent, the viscosity remained constant for 3 cycles of freezing and thawing repetition process, but showed a slightly decreasing trend in the 4th repetition process (P<0.05). On the other hand, the sugar content, pH, and chromaticity remained constant even in the 4th repetition process. Pineapple coated with the coating agent had smaller weight loss, hardness changes, and total bacteria distribution compared to the uncoated pineapple (P<0.05). In the chromaticity, both of the two pineapples experienced browning with increasing storage duration, as L value decreases and b value increases. However, when the color difference was compared, the progress of browning for the uncoated pineapple was faster than the coated pineapple. Also, the progress of browning at $4^{\circ}C$ was found to be slower than the progress of browning at $25^{\circ}C$. Therefore, the storage stability of the fresh-cut fruits could be improved by coating the fresh-cut fruits for cakes with the coating agent and storing at a low temperature, which would contribute to extending the shelf-life of cakes.

Study of Dyeing Properties by Swelling Agent on meta-aramid Fiber with Cationic Dyes (Swelling agent에 따른 메타계 아라미드 섬유의 Cationic dye 염색특성)

  • Kim, Eun-Mi;Park, Chung-Won;Choi, Jae-Hong
    • Textile Coloration and Finishing
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    • v.24 no.1
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    • pp.1-7
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    • 2012
  • Dyeing and fastness characteristics of 100% meta-aramid fiber were investigated with cationic dyes and swelling agents under various dyeing conditions such as dyeing temperature and pH of dye bath. Dye exhaustion started at around $80^{\circ}C$ and settled down at $130^{\circ}C$. Among swelling agents used, N-methyl formanilide showed comparatively higher K/S values comparing to 1-phenoxypropan-2-ol. Under weak acidic conditions in the range pH 5 to 7, the exhaustion of cationic dyes could be enhanced leading to higher adsorption and stability of colorimetric property. Wash and rubbing fastness were generally good but low light fastness found can be attributable to the poor photo-stability of the cationic dyes.

Development of constant current device for using in the water treatment controller with Ni-Tl-P alloy deposits (Ni-Tl-P합금피막을 이용한 수처리장치용 정전류소자의 개발)

  • Ryu, Il-Kwang
    • Journal of environmental and Sanitary engineering
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    • v.18 no.3 s.49
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    • pp.35-42
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    • 2003
  • The electric resistance and constant current were investigated on the nickel-thallium-phosphorus alloy deposits by electroless-plating. The Ni-Tl-P alloy deposits were achieved with a bath using sodium hypophosphit as the reducing agent and sodium citrate as the comlexing agent. The basic plating solution is composed of 0.1M NiSO$_4$, 0.005${\sim}$0.0IM Tl$_2$S0$_4$, 0.1${\sim}$O.2M sodium hypophosphite and 0.02${\sim}$O.IM sodium citrate and the plating condition were pH 5${\sim}$6, temperrature 80$_4$90${\circ}$C. The results obtained are summarized as follows: 1) The crystal structure of deposit was amorphous structure as deposited state, became microcrystallized centering on Ni(111) plane by heat treatment at 200${\circ}$C, and grew as polycrystalline Ni, Ni$_3$P, Ni$_5$p$_2$,Tl, etc. by heat treatment higher than 350${\circ}$C. The grain size of plated deposits was grown up to 28.3~42.0nm by heat treatment for 1hour at 500${\circ}$C. 2) The electrical resistivity showed a comparatively high value of 192.5$_4$208.3 ${\mu}$${\Omega}$Cm and its thermal stability was great with resistivity value less than 0.22% in the thermal surroundings of 200${\circ}$C. 3) Ni-Tl-P alloy deposit showed such good constant current-making-effect in the variation of electric voltage, heat treatment temperature, and the composition of the deposit that it can be put to practical use as the matter of constant current device.

Studies on the Development of a Thrombolytic Agent from Korean Snake Venom II. Characterization and Thrombolytic Activity of a Pretense from the Venom of a Protease from the Venom of A. bromhoffi brevicaudus (한국 독사독으로부터의 혈전 용해제 개발에 관한 연구 II. 살모사(A. bromhoffi brevicaudus) 사독 Protease의 특성과 혈전 용해능에 관한 연구)

  • Kim, Byoung-Jae;Lee, Mun-Han;Rim, Jong-Seop;Lee, Hang;Lee, Hye-Suk;Kim, Jong-Ho;Chai, Chang-Su
    • Biomolecules & Therapeutics
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    • v.3 no.2
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    • pp.165-170
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    • 1995
  • The biochemical properties of the fibrinolytic protease of 50,800 Da isolated from the venom of Kgdistrodon blomhoffi brevicaudus were characterized. The enzyme hydrolyzed the carboxyl side of arginine in the synthetic chromogenic peptides, N-Benzoyl-Phe-Val-Arg-pNA and N-p-Tosyl-Gly-Pro-Arg-pNA, and the enzyme activity was inhibited by phenylmethylsulfonylfluoride indicating that the enzyme belongs to the serine protease family. The pretense showed maximum activity at pH 7.5 and inhibited by ZnCl$_2$, CuSO$_4$, but not by soybean trypsin inhibitor, pepstatin A, 2-mercaptoethanol and EDTA. The fm value determined with N-p-Tosyl-Gly-Pro-Arg-pNA was 0.2 mM. The thrombolytic activity of the purified enzyme was evaluated by platelet aggregation test in rabbits. While the platelet count ratio in blood of the rabbits injected with thrombin alone declined from 1.0 to 0.6 within 7 min and maintained around 0.6 for 24 hours thereafter, the ratio rapidly recovered from around 0.6 to 0.8 in 1 hr, to 1.0 in 24 hrs when the rabbits were sequentially treated with thrombin and the purified enzyme. The result showed that the serine protease from A. blomhoffi brevicoudus of 50,800 Da had a thrombolytic activity in vivo and the enzyme might be developed as a therapuetic agent for the treatment of thrombic disease.

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Study on the Cationic Dyeing Properties of Polyamide-imide Fiber using 2-Hydroxyacetophenone as a Swelling Agent (아세토페논 팽윤제를 이용한 폴리아미드-이미드 섬유의 캐치온 염색특성 연구)

  • Son, Hyun Sik;Kim, Kyung Min;Kim, Ji Hye;Sim, Ji Hyun;Park, Sung Min;Oh, Sang Yeob
    • Textile Coloration and Finishing
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    • v.27 no.4
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    • pp.301-308
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    • 2015
  • This study optimizes dyeing conditions for polyamide-imide fabric using cationic dyes. Dyeing and fastness characteristics of polyamide-imide fabric were investigated with three cationic dyes and 2-hydroxyacetophenone as a swelling agent under various dyeing conditions such as dye and swelling agent concentrations, dyeing temperature and time, pH of dye bath. The dyeing properties were evaluated in terms of dye exhaustion, K/S value and color fastness. The optimized dyeing temperature and time were $130^{\circ}C$ for 90 min for the dyes. Under weak acidic conditions in the range pH 5 to 7, the exhaustion of cationic dyes could be enhanced leading to higher adsorption. Wash and rubbing fastness properties were generally good, while light fastness was slightly low, which can be attributed to the poor photo-stability of the cationic dyes.

Fermentation of a Potential Biocontrol Agent, Bacillus amyloliquefaciens SKU-78 Strain (풋마름병균의 길항세균 Bacillus amyloliquefaciens SKU-78의 대량 배양 조건 확립)

  • Kim, Shin-Duk;Cho, Hong-Bum
    • Korean Journal of Microbiology
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    • v.50 no.1
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    • pp.84-86
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    • 2014
  • Mass production of biocontrol agent is an essential step for its commercial use. Media composition and culture conditions for production of Bacillus amyloliquefaciens SKU-78, a potential biocontrol agent against bacterial wilts, were optimized by a flask culture. Low cost media combining nitrogen and carbon sources were tested. Maximum cell growth (> $2{\times}10^9$ CFU/ml) was obtained in a medium of 5% soy flour combined with 3% corn starch after 24 h cultivation. The optimum initial pH, temperature and shaking speed was 5.5, $30^{\circ}C$ and 150-250 rpm, respectively. Fermentation of SKU-78 was scaled up in 30 L fermenter and the profiles of cell density, pH, dissolved oxygen and spore formation were recorded. After 8 h lag phase, exponential growth occurred and reached at maximum viable cell number ($1.2{\times}10^{11}$ CFU/ml) after 20 h. The SKU-78 strain grown in a low cost medium exhibited the high suppression of bacterial wilts. The results indicate that SKU-78 strain can be produced in a low cost medium and provide a basis for scaling up to industrial level.

Effects of Blowing and Nucleating Agents on the Foaming Properties of Nylon 6

  • Jung-soo Kim;Sung Yeol Kim
    • Elastomers and Composites
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    • v.58 no.2
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    • pp.65-69
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    • 2023
  • To reduce the weight of the engineering plastic Nylon 6 resin, two high-temperature foaming agents, p-toluenesulfonyl semicarbazide (PTSS) and 5-phenyltetrazole (5-PT) (0-10 phr), were added and foamed without other additives. We investigated the effects of the foaming agent type and content on the foam density (g/cm3) and percent weight reduction rate of the Nylon 6 foam, and 5-PT exhibited better foaming performance than PTSS. In the case of 5-PT, the weight reduction rate was above 36% when the blowing agent content was 1.5 phr or higher, indicating that 5-PT is an effective blowing agent for reducing the Nylon 6 foam weight. Additionally, we studied the effect of the nucleating agent Talc content (0-0.4 phr) on Nylon 6 foaming, and the nucleating agent Talc considerably reduced foaming.

Inhibitory Effect of Panax notoginseng and Berberine on LPS-induced iNOS, COX-2 and Prostaglandin E2

  • Lee, Boo-Young;Moon, Jin-Young;Kim, Cherl-Ho;Park, Won-Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.20 no.5
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    • pp.1327-1333
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    • 2006
  • Many traditional herbal remedies exhibit several beneficial effects including anti-inflammation. Panax notoginseng Buck F.H. Chen. is used as a therapeutic agent to stop haemorrhages and a tonic to promote health in Korean and Chinese medicine. The pharrnacokinetic profiles of the main P. notoginseng are still not accurately investigated. The exact mechanism of the anti-inflammatory action of P. notoginseng, however, has not been determined. In the present study, we examined the effect of P. notoginseng on lipopolysaccharide (LPS)-induced nitric oxide (NO) production, and inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) gene expression in RAW264.7 macrophages. The results indicated that P. notoginseng concentration-dependently inhibited LPS-induced NO production. Furthermore, P. notoginseng inhibited the expression of LPS-induced iNOS and COX-2 proteins without an appreciable cytotoxic effect on RAW264.7 cells. Berberine also inhibited LPS-induced iNOS protein as potently as P. notoginseng. This was consistent with the findings that P. notoginseng and also berberine inhibited prostaglandin E2 synthesis induced by LPS.

Asiatic Acid Promotes p21WAF1/CIP1 Protein Stability through Attenuation of NDR1/2 Dependent Phosphorylation of p21WAF1/CIP1 in HepG2 Human Hepatoma Cells

  • Chen, Jin-Yuan;Xu, Qing-Wen;Xu, Hong;Huang, Zong-Hai
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.2
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    • pp.963-967
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    • 2014
  • Previous studies have suggested anti-tumor effects of asiatic acid in some human cancer cell lines. This agent is reported to increase the levels of $p21^{WAF1/CIP1}$ in human breast cancer cell lines. However, the molecular mechanisms have not been established. Here we report that asiatic acid up-regulates $p21^{WAF1/CIP1}$ protein expression but not the level of $p21^{WAF1/CIP1}$ mRNA in HepG2 human hepatoma cells. Furthermore, we found that the asiatic acid induced increase of $p21^{WAF1/CIP1}$ protein was associated with decreased phosphorylation (ser-146) of $p21^{WAF1/CIP1}$. Knockdown of NDR1/2 kinase, which directly phosphorylates $p21^{WAF1/CIP1}$ protein at ser-146 and enhances its proteasomal degradation, increased the levels of $p21^{WAF1/CIP1}$ protein and eliminated the regulation of $p21^{WAF1/CIP1}$ stability by asiatic acid. At the same time, the expression of NDR1/2 kinase decreased during treatment with asiatic acid in HepG2 cells. Moreover, asiatic acid inhibited the proliferation of HepG2 cells, this being attenuated by knockdown of $p21^{WAF1/CIP1}$. In conclusion, we propose that asiatic acid inhibits the expression NDR1/2 kinase and promotes the stability of $p21^{WAF1/CIP1}$ protein through attenuating NDR1/2 dependent phosphorylation of $p21^{WAF1/CIP1}$ in HepG2 cells.