• The Korean Journal of Pesticide Science
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• v.2 no.1
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• pp.18-23
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• 1998

In order to obtain leading compound for the development of new pesticide through the organic synthesis of natural products, the synthesis of ricinine, an active compound of Ricinus communis, was established and biological activities of synthetic compounds against insects were examined. The synthetic scheme of ricinine was composed of four steps by the spontaneous condensation of the cyanoacetyl chloride. A modified synthetic process was also estabilshed to enhance the synthetic yield by simple cyclization of ethoxymethylene malononitrile. In the bioassay results of synthetic ricinine and intermediates on four insects, the mortality of ricinine on brown planthopper (BPH, Nilaparvata lugens) and pea weevil(PW, Bruchus rufimanus) was 80% and 75% at the concentration of 1,000 ${\mu}g/ml$ respectively. Chloronorricinine and chlororicinic acid having chloride group in molecular structure gave 60% mortality on two-spotted mite (TSSM, Tetranychus urticae) at the concentration of 500 ${\mu}g/ml$. The mortality of compounds on house mosquito (HM, Culex pipens pallens) was meager at 10 ${\mu}g/ml$ level.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.159-164
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• 1998

The secondary hydroxy group at side chain of shikonin structure was selectively acylated with various haloacetic acids in presence of dicyclohexylcarbodiimide and 4-dimethylamin opyridine to produce haloacetylshikonin derivatives. The cytotoxicity of monohaloacetylshikonin derivatives against L1210 cells increased in the following order; monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml) > monobromoacetylshikonin ($ED_{50}$. 0.158${\mu}$g/ml) > monoiodoacetylshikonin ($ED_{50}$, 0.173${\mu}$g/ml). Introduction of larger halogen atoms decreased the cytotoxic activity, presumably due to steric hinderance. The cytotoxicity of chloroacetylshikonin derivatives was dependent on the number of chlorine atom, thus increasing in the following order; trichloroacetylshikonin (0.032${\mu}$g/ml) > dichloroacetylshikonin (0.059${\mu}$g/ml) > monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml). Thus, the electron withdrawing effect seems to be important for the cytotoxicity of chloroacetylshikonin derivatives. Consistent with the above, dichloroacetylshikonin (T/C. 182%) and trifluoroacetylshikonin (195%) showed higher T/C values than monochloroacetyl-(T/C, 122%), monobromoacetyl-(T/C, 154%) and monoiodoacetylshikonin (T/C, 117%) derivatives. Haloacetylshikonin derivatives showing lower cytoxic activities against L1210 cells exhibited lower T/C values. It seems that there is a relationship between the cytoxicity of haloacetylshikonin and their antitumor activity.

• Journal of Acupuncture Research
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• v.36 no.1
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• pp.33-37
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• 2019

Background: This study was designed to investigate the potential effects of Galgeungyulpitang for whitening and elasticity treatment by examining its effect on melanoma cells. Methods: The effects of Galgeungyulpitang on B16/F10 melanoma cell viability, production of melanin, tyrosinase and elastase, were investigated. Cell viability was measured by colorimetric assay that assesses cell metabolic activity (MTT assay). Melanin was measured by Hosei's method, tyrosinase was measured by Yogi's method and elastase was measured by James's method. Results: At concentrations higher than $500{\mu}g/mL$ Galgeungyulpitang, cell viability was significantly reduced ($p{\leq}0.05$). At concentrations of $500{\mu}g/mL$ and lower, morphological changes were not observed. The rate of melanin synthesis was significantly reduced to $73.49%{\pm}2.92%$ at a concentration of $500{\mu}g/mL$ Galgeungyulpitang compared with untreated cells (p < 0.05). Extracellular tyrosinase production was not significantly decreased in vitro, however, intracellular tyrosinase production was significantly reduced to $76.06%{\pm}2.17%$ when treated with Galgeungyulpitang at a concentration of $500{\mu}g/mL$ compared with the control (p < 0.05). Elastase Type 1 production was significantly reduced to $74.98%{\pm}3.24%$ and $69.62%{\pm}4.66%$ at concentrations of 250 and $500{\mu}g/mL$ Galgeungyulpitang, respectively (p < 0.05). Elastase Type 4 production was significantly reduced to $72.77%{\pm}3.52%$ at concentrations of 250 and $500{\mu}g/mL$ (p < 0.05). Conclusion: The results in this study showed that Galgeungyulpitang may inhibit melanin and tyrosinase synthesis, and inhibit elastase production, suggesting that Galgeungyulpitang may be potentially beneficial for skin whitening and loss of skin elasticity treatments.

• Proceedings of the Earthquake Engineering Society of Korea Conference
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• 2000.10a
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• pp.501-508
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• 2000

It is demanded to find the dynamic model of a real structure to design a controller. However, as the structure has inherently infinite number of degree-of-freedom, it is impossible to obtain an exact dynamic model of the structure. Instead a reduction model with finite degree-of-freedom is used for the design of a controller. So there exists uncertainty between a real model and a reduction model which causes poor performance of control. All these uncertainties can degrade the control performance and even cause the control instability. Thus, robust control strategy considering the above uncertainties can be an alternative one to guarantee the performance and stability of the control. This study deals with the experimental verification of robust controller design for the active mass driver. $\mu$-synthesis technique is employed as a robust control strategy. Some weights are chosen based on the difference between the initial plant with which the controller is designed and the perturbed plant to be controlled having the actuator uncertainty. The robustness of $\mu$-synthesis technique is compared with the result of LQG strategy, which does not consider the uncertainty.

• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2574-2580
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• 2012

The discovery that threosyl phosphonate nucleoside (PMDTA, $EC_{50}=2.53{\mu}M$) is a potent anti-HIV agent has led to the synthesis and biological evaluation of 5'-deoxy versions of threosyl phosphonate nucleosides. In the present study, (E)-3'-phosphonoalkenyl and 3'-phosphonoalkyl nucleoside analogues 13, 16, 20 and 23 were synthesized from acetol and tested for anti-HIV activity and cytotoxicity. The adenine analogue 16 was found to exhibit moderate in vitro anti-HIV-1 activity ($EC_{50}=22.2{\mu}M$).

• BMB Reports
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• v.30 no.3
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• pp.211-215
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• 1997

A photoactive analog of ATP, 3'(2')-O-(p-azidobenzoyl)-adenosine 5-triphosphate (AB-ATP) was synthesized by chemically coupling N-hydroxysuccinimidyl-4-azidobenzoate (NHS-AB) and ATP. The utility of AB-ATP as an effective active-site-directed photoprobe was demonstrated using catalytic subunit of protein kinase A as a model enzyme. Photoincorporation of AB-ATP was saturated with apparent dissociation constant of $30{\mu}m$ and protected completely by $100{\mu}m$ of ATP. When the enzyme was covalently modified by photolysis in the presence of saturating amounts of photoprobe, about 60% inhibition of enzyme activity was observed. These results demonstrate that AB-ATP has potential application as a probe to characterize ATP-binding proteins including protein kinases.

• Bulletin of the Korean Chemical Society
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• v.32 no.4
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• pp.1146-1152
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• 2011

The discovery of 2'-spirocyclopropyl-ribocytidine (J. Med. Chem. 2010, 53, 8150-8160) as a potent inhibitor of RNA synthesis by NS5B ($IC_{50}=7.3{\mu}M$), the RNA polymerase encoded by hepatitis C Virus (HCV), has led to the synthesis and biological evaluation of several carbocyclic versions of 2'-spiropropyl-nucleosides. The cyclopentenol intermediate 7 was successfully constructed via ring-closing metathesis (RCM) from divinyl 6. Spirocyclopropanation of enone 8 was effected by using (2-chloroethyl)-dimethylsulfonium iodide and potassium tert-butoxide to form the desired intermediate 9. The synthesized nucleoside analogues 21-24 were assayed for their ability to inhibit HCV RNA replication in a subgenomic replicon Huh7 cell line. Among them, the cytosine nucleoside analogue 22 exhibited significant anti-HCV activity ($EC_{50}= 8.2{\mu}M$).

• Applied Biological Chemistry
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• v.35 no.6
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• pp.470-474
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• 1992

For the further development of thelepin analog as antibiotic agents, we undertook the synthesis of spirobenzopyranone derivative ${\underline{5}}$ as thelepin analog by oxidative phenol coupling. The spirobenzopyranone analog ${\underline{5}}$ showed high activity against Bacillus subtilis (IFO 3108) in $5\;{\mu}g/disc$.

• The Korean Journal of Ceramics
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• v.1 no.3
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• pp.147-151
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• 1995

Porous composite of $Al_2O_3$ and AIN based mullite and SiC can be prepared by alumium reaction synthesis and atmosphere controllied sintering in order to improve the durability of a gas filter body. The porous $Al_2O_3$-AIN-mullite, which has a strength of 168 kg/$\textrm{cm}^2$ and porosity of 51.59%, could be obtained by stmospheric firing at $1600^{\circ}C$ and the porous $Al_2O_3$-AIN-SiC with a porosity of 33% and strength of 977 kg/$\textrm{cm}^2$, could also be prepared. The average pore size has been changed from 0.2$\mu\textrm{m}$ in a reduction atmosphere and to 2$\mu\textrm{m}$ in an air atmosphere, respectively.

• Particle and aerosol research
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• v.5 no.3
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• pp.111-122
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• 2009

This paper reviews about synthesis of nanoparticles by spark discharge and applications. A method of catalytic activation with Pd and Pt aerosol nanoparticles produced by spark discharge was introduced. After annealing, the catalytically activated substrate placed into a solution for electroless silver deposition. The silver was then formed only on the activated regions of the substrate. Silver line patterns having a width of $18{\mu}m$ and a height of $1{\mu}m$ were created with the ability to be effectively reproduced. Antimicrobial nanoparticles such as silver were used for removal of bioaerosols. Silver nanoparticles deposited air filters such as ACF filters were evaluated by antimicrobial test.