• 제목/요약/키워드: Lead compound

검색결과 346건 처리시간 0.021초

Potent Inhibition of Monoamine Oxidase B by a Piloquinone from Marine-Derived Streptomyces sp. CNQ-027

  • Lee, Hyun Woo;Choi, Hansol;Nam, Sang-Jip;Fenical, William;Kim, Hoon
    • Journal of Microbiology and Biotechnology
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    • 제27권4호
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    • pp.785-790
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    • 2017
  • Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

Compound IKD-8344, a Selective Growth Inhibitor Against the Mycelial Form of Candida albicans, Isolated from Streptomyces sp. A6792

  • HWANG EUI IL;YUN BONG SIK;YEO WOON HYUNG;LEE SANG HAN;MOON JAE SUN;KIM YOUNG KOOK;LIM SE JIN;KIM SUNG UK
    • Journal of Microbiology and Biotechnology
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    • 제15권4호
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    • pp.909-912
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    • 2005
  • In the course of screening for selective growth inhibitors against the mycelial form of Candida albicans, we isolated a Streptomyces sp. A6792 from soils. The inhibitor was isolated from the above bacterium and identified through several spectral analyses with UV and mass spectrophotometries, and various NMR. The compound was determined to be a macrocyclic dilactone antibiotic, IKD-8344 (molecular weight: 844, molecular formula: $C_{48}H_{76}O_{12}$). The compound selectively inhibited the growth of mycelial form of C. albicans with an MIC of 6.25 ${\mu}g/ml$. It also exhibited strong inhibitory effect preferentially on the mycelial form of various Candida spp. including C. krusei, C. tropicalis, and C. lusitaniae, with MICs ranging from 1.56 to 25 ${\mu}g$/ml. Furthermore, the compound showed no significant toxicity against SPF ICR mice up to 60 mg/kg. These results suggest that IKD-8344 is a useful lead compound for the development of novel antifungal agents, based on the preferential growth inhibition against Candida spp.

Calcium sulfate-Hydroxyapatite 혼합재의 물성 및 치근천공 치유효과에 관한 연구 (THE PHYSICAL PROPERTIES AND HEALING EFFECT OF CALCIUM SULFATE-HYDROXYAPATITE COMPOUND ON ROOT PERFORATION)

  • 이승종;김경남
    • Restorative Dentistry and Endodontics
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    • 제22권2호
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    • pp.739-750
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    • 1997
  • Treatment of root perforation elicits special considerations due to its blood-contaminated circumstances. It is known that conventional dental restorative materials are all leaking. Calcium sulfate is the material which react with water to become chemically set. This study, therefore, was performed to develop a new compound containing calcium sulfate and to evaluate its physical and biological characteristics. Three materials were used, IRM, calcium sulfate, calcium sulfate-hydroxyapatite compound. The composition of the calcium sulfate-hydroxyapatite compound was basically 50 % of calcium sulfate and 50 % of hydroxyapatite mixed with guajacol. The materials were mixed in conventional way and underwent four physical test procedures, setting time, solubility test, compressive strength, and marginal leakage test. All materials were evaluated under the scanning electron microscope to examine the marginal sealing ability. Animal experiment was also performed to test the materials' tissue response. Twenty-four dog's premolars were tested with either furcation perforations or apical retro-fillings. From the results, we found that calcium sulfate possess the good marginal sealing ability. However, calcium sulfate creates many voids which is caused by crystal thrusting action when it reacts with water. It seemed that the voids caused disintegration of the material which eventually lead to tissue reaction. By compounding calcium sulfate and hydroxyapatite, we were able to obtain the better physical properties but it showed larger marginal gap between the material and the root surface. Within the six weeks observation period, both IRM and calcium sulfate-hydroxyapatite compound showed good tissue responses in animal experiment. It is concluded that calcium sulfate would be the material of choice in root perforation repair, but the physical property needs to be further improved.

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Electrical properties of (Na0.5Bi0.5)(Zr0.75Ti0.25)O3 ceramic

  • Lily, Lily;Yadav, K.L.;Prasad, K.
    • Advances in materials Research
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    • 제2권1호
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    • pp.1-13
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    • 2013
  • Lead-free compound $(Na_{0.5}Bi_{0.5})(Zr_{0.75}Ti_{0.25})O_3$ was prepared using conventional ceramic technique at $1070^{\circ}C$/4h in air atmosphere. X-ray diffraction analysis showed the formation of single-phase orthorhombic structure. Permittivity data showed low temperature coefficient of capacitance ($T_{CC}{\approx}5%$) up to $100^{\circ}C$. Complex impedance studies indicated the presence of grain boundary effect, non-Debye type dielectric relaxation and evidences of a negative temperature coefficient of resistance. The ac conductivity data were used to evaluate the density of states at Fermi level and apparent activation energy of the compound.

Sn-Cu-Ni계를 이용한 Pb-free wave Soldering의 공정 적용 및 신뢰성에 관한 연구 (A study on the implementation of wave soldering process and the solder joint reliability of it using Sn-Cu-Ni lead-free solder)

  • 유충식;정종만;김진수;김미진
    • 한국마이크로전자및패키징학회:학술대회논문집
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    • 한국마이크로전자및패키징학회 2001년도 추계 기술심포지움
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    • pp.89-98
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    • 2001
  • Pb-free wave soldering process of AC Adapter was implemented by six sigma method using Sn-Cu-Ni type solder. The solder joint appearance, microstructural change, a lift-off phenomenon and reliability were evaluated through thermal shock teal. $(Cu,Ni)_6Sn_5$-type intermetallic compound of which thickness is about 5 micron was found at solder joint between Sn-Cu-Ni solder and copper land. After applying the thermal shock test of as-soldered product up to 750 cycles, no crack was found at the solder joint and the newly developed product was superior to conventions; one in terms of productivity and reliability.

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Antimicrobial Property of $(+)-Lyoniresinol-3{\alpha}-O-\beta-D-Glucopyranoside$ Isolated From the Root Bark of Lycium chinense Miller Against Human Pathogenic Microorganisms

  • Lee Dong Gun;Jung Hyun Jun;Woo Eun-Rhan
    • Archives of Pharmacal Research
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    • 제28권9호
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    • pp.1031-1036
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    • 2005
  • [ $(+)-Lyoniresinol-3{\alpha}-O-\beta-D-glucopyranoside$ ] (1) was isolated from an ethyl acetate extract of the root bark from Lycium chinense Miller, and its structure was determined using 1D and 2D NMR spectroscopy including DEPT, HMQC, and HMBC. $(+)-Lyoniresinol-3{\alpha}-O-\beta-D-glucopyranoside$ exhibited potent antimicrobial activity against antibiotic-resistant bacterial strains, methicillin-resistant Staphylococcus aureus (MRSA) isolated from patients, and human pathogenic fungi without having any hemolytic effect on human erythrocytes. In particular, compound 1 induced the accumulation of intracellular trehalose on C. albicans as stress response to the drug, and disrupted the dimorphic transition that forms pseudo-hyphae caused by the pathogenesis. This indicates that $(+)-Lyoniresinol-3{\alpha}-O-\beta-D-glucopyranoside$ has excellent potential as a lead compound for the development of antibiotic agents.

트랜스퍼 금형에 있어서 IC 폐키지의 성형 유동 해석에 관한 연구 (A Study on the Molding Analysis of IC Package in Transfer mold)

  • 구본권
    • 한국공작기계학회:학술대회논문집
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    • 한국공작기계학회 1995년도 추계학술대회 논문집
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    • pp.64-67
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    • 1995
  • Transfer Molding is currently the most widely used process for encapsulation integrated circuits(;IC). Although the process has been introduced over 20 years ago, generating billions of parts each year, it is far from being optimized. With each new mold, epoxy mold, epoxy mold compound, and lead-frame, lengthy period and expensive qualification runs have to be performed to minimized defects ranging from wire sweep, incomplete fill, and internal voids etc. This studies describes how simulation can be applied to transfer molding to yield acceptable design and processing parameter. The non-isothermal filling of non-newtonian reactive epoxy molding compound(;EMC) in a multi-cavity mold is analyzed. Sensitivity analysis is conducted to investigate the influence of process deviations on the final molded profile. This study trend is carried out by following some heuristic process guidelines.

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Screening for bioactive compounds from natural products by ELISA assay

  • Iwanami, Naoko
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.34-37
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    • 1998
  • Combinatorial chemistry is one of the most interested topics in the area of drug discovery. One of the most important points is how to find a lead compound that gives the seed structure for designing of a combinatorial library. Natural products is suitable for searching a new bioactive compound with new structure. We have carried out systematic screening works to find natural products possessing the effects on inter-and intra-cellular signaling. Two hundreds extracts of medical plants and two thousands microbial culture broth samples have been tested for the induction and inhibition of IL-2 or IL-6 production (Fig. 1). ELISA is an efficient method for screenings from such a large number of samples. Now, we apply this method to search prion- binding agents.

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Marmatite 鑛의 直接酸浸出에 關한 硏究 (第3報) Marmatite 鑛의 酸浸出과 黃化物의 電極電位에 關한 硏究 (Direct Acid Leaching of Zinc from Marmatite Ores 3 Acid Leaching of Marmatite Ores and the Electrode Potential Behavior of Sulfides)

  • 김재원
    • 대한화학회지
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    • 제11권1호
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    • pp.38-43
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    • 1967
  • In order to explain the positive catalytic action of copper compound for the rate of leaching of zinc sulfide minerals, the electrode and redox potentials of both synthetic and natural sulfides were measured at various conditions of temperatures and pressures. The potentials of Chalcopyrite and copper sulfide were considerably higher than that of zinc sulfide, whereas lead sulfide and Galena had slightly lower potentials than that of zinc sulfide. At elevated temperatures and pressures, the same tendency was obtained. By means of comparing the calculated and measured values of potentials for sulfides, it was suggested that the electrode potentials in acid solution were generated by oxidation of sulfur ion. As a result, it was concluded that the catalytic action of copper compound in the leaching of synthetic zinc sulfide should be arised from the galvanic action between sulfides keeping intimate contact one another in which copper sulfide worked as cathodic and zinc sulfide as anodic part analogous to the metal corrosion under galvanic action.

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A First Synthesis of Isofagar-idine:Topoisomerase I Inhibitor

  • Cho, Won-Jea;Miyoji Hanaoka
    • Archives of Pharmacal Research
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    • 제19권3호
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    • pp.240-242
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    • 1996
  • We have reported the convenient biomimetic methodology for the synthesis of all kinds of substituent pattern benzo[c]phenanthridine alkaloids (Hanaoka et al., 1990; Hanaoka et al., 1991). Regioselective demethylation of C-8 position on oxyfagaridine (5), an intermediate for the synthesis of Fagaridine (4), would afford the precursor for the synthesis of Isofagaridine because the strong hydrogen bonding between amide and hydroxyl group of C-7 position probably resists to be reacted with week base and electrophiles. Thus, a selective alkylation of dihydroxy compound supposed to be possible and be lead to the target compound, Isofagaridine.

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