• Title/Summary/Keyword: active compound

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Percutaneous Absorption Characteristics of Antidepressant Paroxetine (항우울제인 Paroxetine의 피부 투과 특성 연구)

  • Jung, Duck-Chae;Hwang, Sung-Kwy;Oh, Se-Young
    • Journal of the Korean Applied Science and Technology
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    • v.28 no.2
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    • pp.170-177
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    • 2011
  • Transdermal drug delivery(TDS) offers many important advantages. For instance, it is easy and painless, it protects the active compound from gastric enzymes, and it avoids the hepatic first-pass effect. Also, it is simple to terminate the therapy if any adverse or undesired effect occurs. But skin is a natural barrier, and only a few drugs can penetrate the skin easily and in sufficient quantities to be effective. Therefore, in recent years, numerous studies have been conducted in the area of penetration enhancement. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharide, such as xanthan gum and algin were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers and drug contents. Among these polysaccharide, the permeation rate of Paroxetine such as lipophilic drug was the fastest in xanthan gum matrix in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

A Study on Curing Reaction of 1-Chlobutadiene-Butadiene Copolymer by Moisture (1-Chlorobutadiene-Butadiene Copolymer의 수가교반응(水架橋反應)에 관한 연구(硏究)(I))

  • Yoo, Chong-Sun;Paik, Nam-Chul
    • Elastomers and Composites
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    • v.22 no.3
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    • pp.195-203
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    • 1987
  • In this study, as one of the developing ways of the functional elastomer, improvement of the functionality of CB-BR was attempted through moisture curing reaction. The curing reaction of CB-BR was determined with an use of 3-aminopropyltriethoxysilane(APS) as a crosslinking agent, also a solution reaction with an active chlorine of CB-BR was elucidated by using a reaction kinetics theory and a study of physical property was made through moisture curing on the compound of 3-aminopropyltriethoxysilane and CB-BR The results of this study obtained are as follows : 1) CB-BR reacted easily with APS in the liquid state and the reaction rate coefficient and activation energy were as follows : 2) Optimum pressure condition of moisture cured elastomer(CB-BR+APS) was 20 minutes at $150^{\circ}C$, and the crosslinked elastomer was close to the theoretical value (q=1) for Flory's equation($\frac{\alpha}{\alpha-1}=q{\nu}RT$)

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Semiempirical Calculations of Hyperpolarizabilities for Quinoline Derivatives (Quinoline계 분자의 초분극률에 관한 반경험적 계산)

  • Ryu Ungsik;Choi Donghoon;Kim Nakjoong;Lee Yoon Sup
    • Journal of the Korean Chemical Society
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    • v.37 no.1
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    • pp.62-67
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    • 1993
  • The microscopic origin of nonlinear optical properties of quinoline derivatives have been investigated theoretically using MOPAC-AM1 method. In order to prepare promising nonlinear optical active polymers of polyquinoline derivatives, the optimized positions of strong electron donor and electron acceptor are determined in the heterocyclic ring for the energetically favorable structures. For each compound, the effect of the substituted positions on the microscopic nonlinear coefficients were investigated. Polyquinoline was already evaluated to have outstanding physical and mechanical properties so that its monomeric analogues were designed and synthesized for developing new second and third order nonlinear optical main chain polymers. Using the MOPAC-AM1 method, properties calculated include the intrinsic ground-state dipole moments, the polarizabilities, first and second hyperpolarizabilities under the condition of finite-field $(\omega$ = 0).

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APPLICATION OF THERMOFORMED APPLIANCES IN PEDIATRIC DENTISTRY (소아치과 임상에서의 Thermoformed Appliance의 적용)

  • Kim, Shin;Jeong, Tae-Sung;Yang, Chul-Ho
    • Journal of the korean academy of Pediatric Dentistry
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    • v.25 no.3
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    • pp.539-544
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    • 1998
  • Thermoformed appliance, which has been recently introduced for dental usage, is an appliance made of thermoformed sheets and formed with positive or negative pressure under heat. Thermoplastic material is a kind of plastics and can be repeatedly softened by heat. It is classified into hard elastic foil, hard/soft compound foil and soft elastic foil, including BIOPLAST, BIOCRYL, IMPRELON, etc. It has been developed in 1969 and is available in various thickness, shape and color. There are two types of Vacuum former for thermoplastic materials; the pressure type and suction type. The former is much better than the latter for fabrication of various appliances due to its higher pressure. The authors have applied these appliances to some cases - chin cap, active retainer, individual Fluoride tray, mouth protector, bracket transfer mask, bruxism splint(night guard), Essix appliance - by pressure type Vacuum former($Biostar^{(R)}$). The thermoplastic appliances have numerous advantages such as simple procedure, short working time, clean and transparent product, less objectionable taste. But its outstanding advantage would be its excellent biocompatibility bacause it has no monomer and hence no tissue irritation. Although there is some limitations in its usage, it can be used widely for various purposes especaily for pediatric dentistry.

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Heat Treatment Effect of Seed on Synthesis of Chemical Manganese Dioxide (CMD) and Electrochemical Properties of LiMn2O4 obtained from the CMD (Chemical Manganese Dioxide (CMD) 합성에서의 Seed의 열처리 효과 및 그 CMD로부터 제조되는 LiMn2O4의 전지특성)

  • Kim, Sung-Wook;Cho, Hae-Ran;Roh, Gwang Chul;Park, Sun-Min
    • Korean Chemical Engineering Research
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    • v.51 no.4
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    • pp.460-464
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    • 2013
  • A series of Mn compound were prepared by seed-assisted method. The seed used in this reaction was manufactured by calcination of $MnCO_3$ at various temperatures and effects of the calcination temperature on seed-assisted reaction were investigated. With increase of the calcination temperature, CMD (${\gamma}-MnO_2$) was recovered after seed-assisted reactions. LMO used as cathode active material in the Li-ion batteries were synthesized from Mn source obtained in the seed-assisted reaction and the electrochemical properties (rate capability, cycle life performance and specific capacity) of the LMO were investigated. The LMO synthesized from the CMD which is obtained by the reaction with seed prepared by calcination of $MnCO_3$ more than $350^{\circ}C$ shown good electrochemical properties.

Effects of Oxygen Enrichment on the Structure of Premixed Methane/Fluorinated Compound Flames (메탄-불소계 화합물의 예혼합화염 구조에서 산소 부화의 효과)

  • Lee, Ki-Yong
    • Transactions of the Korean Society of Mechanical Engineers B
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    • v.35 no.8
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    • pp.839-845
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    • 2011
  • We performed numerical simulations of freely propagating premixed flames at atmospheric pressure to investigate the influence of trifluoromethane on $CH_4/O_2/N_2$ flames under oxygen enrichment. Trifluoromethane significantly contributed toward a reduction in flame speed, the magnitude of which was larger in terms of the physical effect than the chemical effect. More trifluoromethane could be added and consumed on oxygen-enriched $CH_4/O_2/N_2$ flames. $CHF_3$ was decomposed primarily via $CF_3{\rightarrow}CF_2{\rightarrow}CF{\rightarrow}CF:O{\rightarrow}CO$ and $CHF_3+M{\rightarrow}CF_2+HF+M$ played an important role in oxygen-enhanced flames. When an inhibitor was added to oxygen-enriched flames, the position of the maximum concentration of active radicals was shifted to a relatively low temperature range, and the net rate of OH became higher than that of H.

Inhibitory mechanism of Korean Red Ginseng on GM-CSF expression in UVB-irradiated keratinocytes

  • Chung, Ira;Lee, Jieun;Park, Young Sun;Lim, Yeji;Chang, Do Hyeon;Park, Jongil;Hwang, Jae Sung
    • Journal of Ginseng Research
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    • v.39 no.4
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    • pp.322-330
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    • 2015
  • Background: UV-irradiated keratinocytes secrete various proinflammatory cytokines. UV-induced skin damage is mediated by growth factors and proinflammatory cytokines such as granulocyte macrophage colony stimulating factor (GM-CSF). In a previous study, we found that the saponin of Korean Red Ginseng (SKRG) decreased the expression of GM-CSF in UVB-irradiated SP-1 keratinocytes. In this study, we attempted to find the inhibitory mechanism of SKRG on UVB-induced GM-CSF expression in SP-1 keratinocytes. Methods: We investigated the inhibitory mechanism of SKRG and ginsenosides from Panax ginseng on UVB-induced GM-CSF expression in SP-1 keratinocytes. Results: Treatment with SKRG decreased the expression of GM-CSF mRNA and protein induced by irradiation of UVB in SP-1 keratinocytes. The phosphorylation of ERK was induced by UVB at 10 min, and decreased with SKRG treatment in SP-1 keratinocytes. In addition, treatment with SKRG inhibited the UVB-induced phosphorylation of epidermal growth factor receptor (EGFR), which is known to be an upstream signal of ERK. From these results, we found that the inhibition of GM-CSF expression by SKRG was derived from the decreased phosphorylation of EGFR. To identify the specific compound composing SKRG, we tested fifteen kinds of ginsenosides. Among these compounds, ginsenoside-Rh3 decreased the expression of GM-CSF protein and mRNA in SP-1 keratinocytes. Conclusion: Taken together, we found that treatment with SKRG decreased the phosphorylation of EGFR and ERK in UVB-irradiated SP-1 keratinocytes and subsequently inhibited the expression of GM-CSF. Furthermore, we identified ginsenoside-Rh3 as the active saponin in Korean Red Ginseng.

Phenolic Compounds Obtained from Stems of Couepia ulei with the Potential to Induce Quinone Reductase

  • Jang, Dae-Sik;Park, Eun-Jung;Kang, Young-Hwa;Vigo, Jose-Schunke;James-G.Graham;Fernando-Cabieses;Harry-H.S.Fong;John-M.Pezzuto;A.Douglas-Kinghorn
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.169-172
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    • 2004
  • Activity-guided fractionation of the EtOAc-soluble extract of the stems of Couepia ulei, using a bioassay based on the induction of quinone reductase (QR) in cultured Hepa 1c1c7 mouse hepatoma cells led to the isolation of two active compounds, a new natural product, erythro-2,3-bis(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-o1 (1), and a known compound, evofolin-B (2), along with five inactive compounds all of known structure, viz., betulinic acid, oleanolic acid, pomolic acid, ($\pm$)-syringaresinol, and ursolic acid. These isolates were identified by analysis of physical and spectral data. Compounds 1 and 2 exhibited QR inducing activity, with observed CD (concentration required to double induction) values of 16.7 and 16.4 $\mu\textrm{M}$, respectively.

Synthesis of a Sulfonic Acid Analogues of Peptides (Tauryl-L-Histidine) (Tauryl-L-Histidine 의 合成)

  • Park, Won-Kil
    • Journal of the Korean Chemical Society
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    • v.5 no.1
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    • pp.38-41
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    • 1961
  • By varying groups on biologically active molecules, it is possible to produce analogues which sometimes inhibit the action of the parent compound. Such is true of taurine(${\beta}$-amino-ethane sulfonic acid)as an analogue of ${\beta}$-alanine and of pantoyl taurine for pantothenic acid. It seemed possible that the sulfonic acid analogues of amino acids built into peptides might possibly produce inhibition of the parent peptide. Tauryl-L-histidine was selected to prepare as an analogue of carnosine(${\beta}$-alanyl-L-histidine). There were several reasons for this choice. Camosine causes a slight contraction of isolated uterine muscle and inhibition of this action can be easily tested. Also, taurine, being a ${\beta}$-amino sulfonic acid, is much more stable than the ${\beta}$-amino sulfonic acids. Phthalyl tauryl-L-histidine methyl ester was prepared by condensing phthalyl tauryl chloride with histidine methyl ester in chloroform. The yields were quite low possibly due to reaction between the acid chloride and the imidazole of histidine. Approximately 50 per cent yield of crude amorphous product was obtained, but upon purification by crystallization they yielded only 25 percent of a pure product. The methyl ester was removed by acid hydrolysis to prevent partial cleavage of the phthalyl group. Crystalline tauryl histidine was then obtained from this acid by removal of the phthalyl group by hydrazinolysis. Tests for inhibition were carried out by comparing the action of camosine on isolated uterine muscle before and after tauryl histidine had been added to the bath surrounding the muscle strip. Only in very high relative concentrations of tauryl histidine was there any demonstrable inhibition.

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The Antifungal Test: An Efficient Screening Tool for the Discovery of Microbial Metabolites with Respiratory Inhibitory Activity

  • Han, Jae Woo;Kim, Bomin;Oh, Mira;Choi, Jaehyuk;Choi, Gyung Ja;Kim, Hun
    • Mycobiology
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    • v.48 no.4
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    • pp.326-329
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    • 2020
  • Valuable natural compounds produced by a variety of microorganisms can be used as lead molecules for development of new agrochemicals. Furthermore, high-throughput in vitro screening systems with specific modes of action can increase the probability of discovery of new fungicides. In the current study, a rapid assay tested with various microbes was developed to determine the degree of respiratory inhibition of Saccharomyces cerevisiae in two different liquid media, YG (containing a fermentable carbon source) and NFYG (containing a non-fermentable carbon source). Based on this system, we screened 100 fungal isolates that were classified into basidiomycetes, to find microbial secondary metabolites that act as respiratory inhibitors. Consequently, of the 100 fungal species tested, the culture broth of an IUM04881 isolate inhibited growth of S. cerevisiae in NFYG medium, but not in YG medium. The result is comparable to that from treatment with kresoxim-methyl used as a control, suggesting that the culture broth of IUM04881 isolate might contain active compounds showing the inhibition activity for respiratory chain. Based on the assay developed in this study and spectroscopic analysis, we isolated and identified an antifungal compound (-)-oudemansin A from culture broth of IUM04881 that is identified as Oudemansiella venosolamellata. This is the first report that (-)-oudemansin A is identified from O. venosolamellata in Korea. Taken together, the development of this assay will accelerate efforts to find and identify natural respiratory inhibitors from various microbes.