• 제목/요약/키워드: ring structure

검색결과 1,337건 처리시간 0.031초

Isolation of a Natural Antioxidant, Dehydrozingerone from Zingiber officinale and Synthesis of lts Analogues for Recognition of Effective Antioxidant and Antityrosinase Agents

  • Kuo, Ping-Chung;Damu, Amooru G.;Cherng, Ching-Yuh;Jeng, Jye-Fu;Teng, Che-Ming;Lee, E-Jian;Wu, Tian-Shung
    • Archives of Pharmacal Research
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    • 제28권5호
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    • pp.518-528
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    • 2005
  • In the present study, the antioxidative and inhibitory activity of Zingiber officinale Rosc. Rhizomes-derived materials (on mushroom tyrosinase) were evaluated. The bioactive co mponents of Z. officinale rhizomes were characterized by spectroscopic analysis as zingerone and dehydrozingerone, which exhibited potent antioxidant and tyrosinase inhibition activities. A series of substituted dehydrozingerones [(E)-4-phenyl-3-buten-2-ones] were prepared in admirable yields by the reaction of appropriate benzaldehydes with acetone and the products were evaluated in terms of variation in the dehydrozingerone structure. The synthetic analogues were examined for their antioxidant and antityrosinase activities to probe the most potent analogue. Compound 26 inhibited Fe$^{2+}$-induced lipid peroxidation in rat brain homogenate with an IC$_{50}$ = 6.3${\pm}$0.4 ${\mu}$M. In the 1,1-diphenyl- 2-picrylhydrazyl (DPPH) radical quencher assay, compounds 2, 7, 17, 26, 28, and 29 showed radical scavenging activity equal to or higher than those of the standard antioxidants, like ${\alpha}$-tocopherol and ascorbic acid. Compound 27 displayed superior inhibition of tyrosinase activity relative to other examined analogues. Compounds 2, 17, and 26 exhibited non-competitive inhibition against oxidation of 3,4- dihydroxyphenylalanine (L-DOPA). From the present study, it was observed that both number and position of hydroxyl groups on aromatic ring and a double bond between C-3 and C-4 played a critical role in exerting the antioxidant and antityrosinase activity.

In situ Gel Forming Stereocomplex Composed of Four-Arm PEG-PDLA and PEG-PLLA Block Copolymers

  • Jun, Yeo-Jin;Park, Kyung-Min;Joung, Yoon-Ki;Park, Ki-Dong;Lee, Seung-Jin
    • Macromolecular Research
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    • 제16권8호
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    • pp.704-710
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    • 2008
  • Injectable hydrogels are quite promising materials due to their potential to minimize invasive implantation and this provides versatile fitness irrespective of the damaged regions and facilitates the incorporation of bioactive agents or cells. In situ gel formation through stereocomplex formation is a promising candidate for injectable hydrogels. In this paper, a new series of enantiomeric, four-arm, PEG-PLA block copolymers and their stereocomplexed hydrogels were prepared by bulk ring-opening polymerization of D-lactide and L-lactide, respectively, with stannous octoate as a catalyst. The prepared polymers were characterized by $^1H$ nuclear magnetic resonance (NMR) spectroscopy, Fourier-transform infrared (FT IR) spectroscopy, gel permeation chromatography (GPC) and thermal gravitational analysis (TGA), confirming the tailored structure and chain lengths. The swelling and degradation behavior of the hydrogels formed from a selected copolymer series were observed in different concentrations. The degradation rate decreased with increasing polymer content in the solution. The rheological behavior indicated that the prepared hydrogel underwent in situ gelation and had favorable mechanical strength. In addition, its feasibility as an injectable scaffold was evaluated using a media dependence test for cell culture. A Tris solution was more favorable for in situ gel formation than PBS and DMEM solutions were. These results demonstrated the in situ formation of hydrogel through the construction of a stereocomplex with enantiomeric, 4-arm, PEG-PLA copolymers. Overall, enantiomeric, 4-arm, PEG-PLA copolymers are a new species of stereocomplexed hydrogels that are suitable for further research into injectable hydrogels.

Study on the clinical application of Iridological Constitution to the Gynecological disease diagnose (홍채(虹彩) 체질(體質)의 부인과(婦人科) 임상(臨床) 응용(應用)에 관(關)한 연구(硏究) -불임, 자궁근종, 난소낭종 환자를 중심으로)

  • Lee, Bo-Ra;Lee, Jung-Eun;Jung, Jin-Hong;Yoo, Dong-Youl;Park, Kyung-Mi
    • The Journal of Korean Obstetrics and Gynecology
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    • 제15권4호
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    • pp.136-148
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    • 2002
  • This study was performed to investigate the relation between Iridological constitution and Gynecological disease. Iris is one of the most complicated part of our bodies. It reflects perfectly organ's status, toxic accumulation, person's characteristics and healing effects. Many signs of Iridology were closely researched to examine the relation between Iridology and disease. After studying these matters, we could find that lacuna and auto-nerve wreath are intimately related. Especially the portions of auto-nerve wreath loss are accorded with the organ's present illness. Most of patients have scurf ring and vessel congestion sign. Large Intestine's structure also shows us the meaningful result that ballooned is the most common, spasticity and stricture are next. Connective tissue weakness constitution is 39.22%, complex 35.29% and blood-originated 25.49%. According to the three-step constitution by the Genetic facter, average type is 52.94%, weak type 35.29% and strong type 11.76%. Above these results, we can reach a conclusion that Iridological constitution are intimately related with Gynecological disease. And further study are requested to get a objectivity in a Gynecological diagnose. Iridology is a bright prospective study and interesting diagnostic method. If we deeply investigate this science, before long we can have a great outcome and more objective diagnostic skill.

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Multiple Congenital Vascular Anomalies In a Lakeland Terrier: Computed Tomographic Angiographic Evaluation

  • JANG, Moonjung;CHEON, Sangkyung;KIM, Wanhee;CHOI, Mincheol;YOON, Junghee
    • Journal of Veterinary Clinics
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    • 제35권3호
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    • pp.114-118
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    • 2018
  • A 3-month-old intact male Lakeland terrier was presented with recurring regurgitation after removing cervical esophageal foreign body by endoscopy. Blood and urine analysis, radiography, ultrasonography, fluoroscopic esophagography, computed tomographic angiography (CTA) were performed. In radiography and fluoroscopic esophagography, vascular ring anomaly was considered as the primary cause of megaesophagus, and CTA with gas-inflation of the esophagus was performed. Compressed esophagus, persistent right aortic arch (PRAA), aberrant left subclavian artery (LSA), and a venous structure which was confirmed in surgery to be incomplete type persistent left cranial vena cava (PLCVC) connected with the left side azygos vein were observed. Left deviation of the trachea was also revealed in CT, which implies the compression by left ligamentum arteriosum. Therefore, type 3 PRAA with left ligamentum arteriosum and aberrant LSA, was considered as a prior differential diagnosis. Surgical repair was performed and the clinical signs improved. This report describes CTA characteristics of combination of PRAA with aberrant LSA, incomplete PLCVC and Lt. azygos vein in a dog. Although not every vascular anomaly does induce clinical sign, some types can complicate the surgical procedure, and cause clinical signs. Therefore, thorough evaluation of vascular anomalies in the thorax is important, and CTA is a useful method in identifying multiple vascular anomalies in dogs.

Molecular Holographic QSAR Analysis on the Bonding Affinity Constants between Nicotin Acetylcholine Receptors and New 3-Benzylidenemyosmine Analogues and Molecular Design (새로운 3-Benzylidenemyosmine 유도체와 Nicotin Acetylcholine 수용체 사이의 결합 친화력 상수에 관한 HQSAR 분석과 분자설계)

  • Jang, Seok-Chan;Sung, Nack-Do
    • Applied Biological Chemistry
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    • 제50권2호
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    • pp.127-131
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    • 2007
  • The molecular design and holographic (H) quantitative structure-activity relationships (HQSARs) on the binding affinity constants between new 3-benzylidenemyosmine analogues and nicotin acetylcholine receptors (nAChRs) of American cockroach (Periplaneta. americana L.) were studied quantitatively. The optimized HQSAR model (IV-2) for the binding affinity constants was derived from fragment distinction of hydrogene atoms in fragment size, 5${\sim}$8 bin. The statistical results of the HQSAR model (IVI-2) exhibited the best predictability and fitness for the binding affinity constants based on the cross-validated value (q$^2$=0.507) and non cross-validated value (r$^2_{nev.}$=0.944). From the graphical analyses of atomic contribution maps, it was revealed that the binding affinity constants depends upon the anabaseine ring in molecule and the most active compounds were designed by optimized HQSAR model (VI-2).

Expression of Rat Hepatic Glutathione-S-Transferases by Benzoazoles (Benzoazole계 화합물이 glutathione-S-transferases의 유도발현에 미치는 영향)

  • 서경원;김연정;김태완;김효정;조민경;김상건
    • Environmental Analysis Health and Toxicology
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    • 제13권3_4호
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    • pp.55-61
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    • 1998
  • Glutathione-S-transferases (GSTs) detoxify electrophilic xenobiotics and reactive metabolites. Recently benzene-fused heterocycles have been shown to increase the total amount of hepatic GSTs in rats. Primarily this study aimed to determine the induction of GSTs by benzoazoles (BAs) including benzoxazole (BX), 2-methylbenzoxazole (M-BX), 2,5-dimethyl benzoxazole (D-BX), benzothiazole (BT), aminobenzothiazole (A-BT) and 2-mercaptobenzothiazole (M-BT) in rats. Hepatic cytosol and poly(A)$^+$ mRNA were prepared from rats after oral administration of BX, BT, M-BX, D-BX, A-BT and M-BT for 5 consecutive days at doses of 1 mmol/kg. Western immunoblot and northern blot analysis were conducted with rabbit anti-GST Ya, Yb$_1$, Yb$_2$, Yc antibodies and cDNA probes containing = 500 bps in the specific coding regions of Ya, Yb$_1$, Yb$_2$, Yc$_1$, and Yc$_2$, respectively. All BAs increased the amount of enzymes and mRNA levels of GSTs. BT was the most effective inducer of GSTs among the compounds examined in this study. Although A-BT and M-BT, the derivatives of BT, induced GSTs, these chemicals had lesser effect on induction of GSTs than BT. The derivatives of BX also induced less GSTs than the parent compound and the addition of methyl group to the benzene ring of BX reduced the induction of GSTs. BAs had better inductive effects on the class $\alpha$(Ya, Yc) than class $\mu$ GSTs (Yb$_1$, Yb$_2$). BAs enhanced mRNA levels of GSTs in parallel with the protein levels. These results indicate that 1) most of BAs induced various isozymes of GSTs, 2) the induction of GSTs appears to be correlated with the chemical structure of the derivatives, and 3) the expression of GST by BAs is presumably under the transcriptional regulation.

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Synthesis of Novel Benzofuran and Related Benzimidazole Derivatives for Evaluation of In Vitro Anti-HIV-1, Anticancer and Antimicrobial Activities

  • Rida, Samia M.;El-Hawash, Soad A.M.;Fahmy, Hesham T.Y.;Hazzaa, Aly A.;El-Meligy, Mostafa M.M.
    • Archives of Pharmacal Research
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    • 제29권10호
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    • pp.826-833
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    • 2006
  • Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

A New Method to Estimate the Magnetic Field Modulation Effect of Brushless Doubly-Fed Machine with Cage Rotor

  • Liu, Hanghang;Han, Li;Gao, Qiang
    • Journal of international Conference on Electrical Machines and Systems
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    • 제1권3호
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    • pp.330-335
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    • 2012
  • Brushless doubly-fed machine (BDFM) doesn't use brush and slip ring, and has advantages such as high system reliability, small capacity of its frequency converter, low system cost, adjustable power factor and speed, etc. At the same time, it has good applicable potentials on the variable frequency motors and the variable speed constant frequency generators. However, due to the complicacy and particularity of BDFM in the structure and operating mechanism, the effect of magnetic field modulation directly influences the operating efficiency of BDFM. To study the effect of different cage rotor structures on the magnetic field modulation of BDFM, the rotor magnetomotive force (MMF) of BDFM with cage rotor is studied by the analytical method. The components and features of rotor harmonic MMFs are discussed. At the same time, the method to weaken the higher harmonics is analyzed by the theoretic formulae. Furthermore, the magnetic field modulation mechanism is expounded on in detail and the relationship between the magnetic field modulation effect and the operating efficiency of BDFM is established. And then, a new method for estimating the magnetic field modulation effect is proposed. At last, the magnetic field modulation effects of four BDFM prototypes with different cage rotor structures are compared by the MMF analysis and the efficiency data of electromagnetic design. The results verify the effectiveness of the new method for estimating the magnetic field modulation effect of BDFM with cage rotor.

The Method of Thermal Crack Control about the LNG Tank Wall in Winter (LNG 저장탱크 벽체의 동절기 온도균열제어 방안)

  • Son, Young-Jun;Ha, Jae-Dam;Um, Tai-Sun;Lee, Jong-Ryul;Baek, Seung-Jun;Park, Chan-Kyu
    • Proceedings of the Korea Concrete Institute Conference
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    • 한국콘크리트학회 2008년도 춘계 학술발표회 제20권1호
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    • pp.637-640
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    • 2008
  • Since the first underground LNG tank was constructed in Incheon, continuously many LNG tanks were constructed in Tongyoung and Pyongtaek. The storage capacity of LNG tank increased by 200,000kl and the structure size and the concrete mixing design has changed. The crack of concrete induced by the heat of hydration is a serious problem, particularly in massive concrete structures. In order to control the thermal crack of massive concrete, the low heat portland cement(type Ⅳ) is applied to bottom annular part, bottom central part, lower walls and ring beam. In this study, in order to thermal crack control about the LNG tank wall(lot 8 of #16 Pyongtaek LNG tank) in winter, analysed the concrete temperature, the extention of term, the curing condition and the concrete mixing design. When the concrete mixing design is changed from OPC+FA25% to LHC+FA25%, the thermal crack index is 1.33 and satisfied with construction specifications(over 1.2).

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Rotational Antenna based Clutter Imaging Algorithm in Helicopter Landing Mode (헬리콥터에 장착된 회전 안테나를 이용한 착륙지형의 이미지 생성 기법)

  • Bae, Chang-Sik;Jeon, Hyeon-Mu;Kim, Jae-Hak;Yang, Hoon-Gee
    • Journal of the Korea Institute of Information and Communication Engineering
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    • 제20권10호
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    • pp.1860-1866
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    • 2016
  • Helicopter-related collision accidents with structures mostly occur at landing, especially in a limited visibility environment, which necessitates some secondary equipment like a radar that can generate stationary clutter image. In this paper, we propose an algorithm that makes an image of stationary ground clutter in two dimensional range and azimuth angle domain. We present a mathematical model for the received signals from each clutter patch in the iso range ring and analyze their clutter and Doppler characteristics, assuming that a helicopter-borne radar has a rotational antenna. We propose a filter structure, which suppresses side lobe signal components while extracting a main lobe signal component, and suggest a solution for a problem stemmed from the filtering process. Finally, by conducting a simulation we show the performance of the suggested imaging algorithm on a two dimensional virtual scenario of the topographic clutter.