• Title/Summary/Keyword: novel compound

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Synthesis, Structure and Biological Properties of a Novel Copper (II) Supramolecular Compound Based on 1,2,4-Triazoles Derivatives

  • Qiu, Guang-Mei;Wang, Cui-Juan;Zhang, Ya-Jun;Huang, Shuai;Liu, Xiao-Lei;Zhang, Bing-Jun;Zhou, Xian-Li
    • Bulletin of the Korean Chemical Society
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    • v.33 no.8
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    • pp.2603-2608
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    • 2012
  • A novel mononuclear supramolecule of copper(II) has been synthesized with Ippyt ligand (Ippyt=3-(4'-imidazole phenyl)-5-(pyrid-2''-yl)-1,2,4-triazole) (1). Compound 1, namely [$Cu(Ippyt)_2(H_2O)_2$], has been characterized by single-crystal X-ray diffraction, IR spectrum, elemental analysis and thermogravimetric analysis. Structure determination reveals that the elongated-octahedral geometry is formed in the vicinity of the copper (II) atom being coordinated by four nitrogen atoms from two Ippyt ligands occupying the equatorial position and two oxygen atoms from two coordinated water molecules in the axial position, which together form the $N_4O_2$ donor set. Hydrogen bonding interactions between nitrogen and oxygen atoms result in the set up of a supramolecular network architecture. Biological properties including antibacterial activity and superoxide dismutase (SOD) mimetic activity of compound 1 have been investigated by agar diffusion method and the modified Marklund method, respectively. The results indicate that compound 1 exhibits a stronger antibacterial efficiency than the parent ligand and it also has a certain radical-scavenging activity.

A Novel Organotellurium Compound (RT-01) as a New Antileishmanial Agent

  • Cantalupo Lima, Camila Barbara;Arrais-Silva, Wagner Welber;Rodrigues Cunha, Rodrigo Luiz Oliveira;Giorgio, Selma
    • Parasites, Hosts and Diseases
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    • v.47 no.3
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    • pp.213-218
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    • 2009
  • Leishmaniasis is a neglected disease and endemic in developing countries. A lack of adequate and definitive chemotherapeutic agents to fight against this infection has led to the investigation of numerous compounds. The aim of this study was to investigate the effect of RT-01, an organotellurane compound presenting biological activities, in 2 experimental systems against Leishmania amazonensis. The in vitro system consisted of promastigotes and amastigotes forms of the parasite, and the in vivo system consisted of L.amazonensis infected BALB/c mice, an extremely susceptible mouse strain. The compound proved to be toxic against promastigotes and amastigotes. The study also showed that treatment with RT-01 produces an effect similar to that treatment with the reference antimonial drug, Glucantime, in L.amazonensis infected mice. The best results were obtained following RT-01 intralesional administration (720 ${\mu}g$/kg/day); mice showed significant delay in the development of cutaneous lesions and decreased numbers of parasites obtained from the lesions. Significant differences in tissue pathology consisted mainly of no expressive accumulation of inflammatory cells and wellpreserved structures in the skin tissue of RT-01-treated mice compared with expressive infiltration of infected cells replacing the skin tissue in lesions of untreated mice. These findings highlight the fact that the apparent potency of organotellurane compounds, together with their relatively simple structure, may represent a new avenue for the development of novel drugs to combat parasitic diseases.

Two Flavonoid-Based Compounds from Murraya paniculata as Novel Human Carbonic Anhydrase Isozyme II Inhibitors Detected by a Resazurin Yeast-Based Assay

  • Sangkaew, Anyaporn;Samritsakulchai, Nawara;Sanachai, Kamonpan;Rungrotmongkol, Thanyada;Chavasiri, Warinthorn;Yompakdee, Chulee
    • Journal of Microbiology and Biotechnology
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    • v.30 no.4
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    • pp.552-560
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    • 2020
  • Human carbonic anhydrase (CA) isozyme II has been used as protein target for disorder treatment including glaucoma. Current clinically used sulfonamide-based CA inhibitors can induce side effects, and so alternatives are required. This study aimed to investigate a natural CA inhibitor from Murraya paniculata. The previously developed yeast-based assay was used to screen 14 compounds isolated from M. paniculata and identified by NMR analysis for anti-human CA isozyme II (hCAII) activity. Cytotoxicity of the compounds was also tested using the same yeast-based assay but in a different cultivation condition. Two flavonoid candidate compounds, 5, 6, 7, 8, 3', 4', 5'-heptamethoxyflavone (4) and 3, 5, 7, 8, 3', 4', 5'-heptamethoxyflavone (9), showed potent inhibitory activity against hCAII with a minimal effective concentration of 10.8 and 21.5 μM, respectively, while they both exhibited no cytotoxic effect, even at the highest concentration tested (170 μM). The results from an in vitro esterase assay of the two candidates confirmed their hCAII inhibitory activity with IC50 values of 24.0 and 34.3 μM, respectively. To investigate the potential inhibition mechanism of compound 4, in silico molecular docking was performed using the FlexX and SwissDock software. This revealed that compound 4 coordinated with the Zn2+ ion in the hCAII active site through its methoxy oxygen at a distance of 1.60 Å (FlexX) or 2.29 Å (SwissDock). The interaction energy of compound 4 with hCAII was -13.36 kcal/mol. Thus, compound 4 is a potent novel flavonoid-based hCAII inhibitor and may be useful for further anti-CAII design and development.

Chemical Structure and Isolation of Novel Glucosyltransferase Inhibitor from Artocarpus heterophyllus folium (Jack Fruit 잎으로부터 새로운 Glucosyltransferase 저해물질 분리 및 화학구조)

  • An, Bong-Jeun
    • Korean Journal of Food Science and Technology
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    • v.29 no.6
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    • pp.1304-1308
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    • 1997
  • In the course of studies for anti-plaque agents, novel procyanidin structure isolated from Artocarpus heterophyllus folium was established by thiolysis and spectroscopic analysis. The chemical structure was identified for $(-)-epiafzelecin-(4{\beta}{\rightarrow}8)-afzelecin-(4{\alpha}-8)-catechin$ containing the trimeric flavan-3-ols and molecular weight was 833[M-H] by FAB-MS negative ion method. The inhibitory effect on the glucosyltransferase activity was investigated, novel compound showed complete inhibition at 1.0 mM and inhibited on the glucosyltransferase noncompetitively.

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Phenolic and Furan Type Compounds Isolated from Gastrodia elata and their Anti-Platelet Effects

  • Pyo Mi Kyung;Jin Jing Ling;Koo Yean Kyoung;Yun-Choi Hye Sook
    • Archives of Pharmacal Research
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    • v.27 no.4
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    • pp.381-385
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    • 2004
  • Nine phenolic ($1\~9$) and two furan type (10, 11) compounds, were isolated from the methanolic extract of the tuber of Gastrodia elata Blume (Orchidaceae) in the course of continuing search for platelet anit-aggregating plant components. Compound 1 was identified as 4,4'-dihy-droxybenzyl sulfone, a novel compound for the best of our knowledge. Compound 10, 5-hydroxymethyl-2-furancarboxaldehyde, was isolated for the first time from this plant. Compound 1 ($IC_{50};\;83{\mu}M$) was about four times more inhibitory to U46619 induced aggregation than ASA ($IC_{50};\340{\mu}M$). Compound 9, 4,4'-dihydroxy-dibenzylether, ($IC_{50};\;5{\mu}M$, $3{\mu}M\;and\;33{\mu}M$, respectively) was $10\~}80$ fold more potent than ASA ($IC_{50};\;420\;{\mu}M,\;53\;{\mu}M\;and\;340\;{\mu}M$ respectively) to collagen, epinephrine and U46619 induced aggregation, although it is less active than ASA to AA induced aggregation.

Compound-Type Hybrid Energy Storage System and Its Mode Control Strategy for Electric Vehicles

  • Wang, Bin;Xu, Jun;Cao, Binggang;Li, Qiyu;Yang, Qingxia
    • Journal of Power Electronics
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    • v.15 no.3
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    • pp.849-859
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    • 2015
  • This paper proposes a novel compound-type hybrid energy storage system (HESS) that inherits the unique advantages of both battery/supercapacitor (SC) and the SC/battery HESSs for electric vehicles (EVs). Eight operation modes are designed to match this system. A mode control strategy is developed for this HESS on the basis of these modes, and five classes of operation modes are established to simplify this strategy. The mode control strategy focuses on high operating efficiency and high power output. Furthermore, the compound-type HESS is designed such that the SC is the main priority in braking energy absorption. Thus, this HESS can operate efficiently and extend battery life. Simulation results also show that the compound-type HESS can not only supply adequate power to the motor inverter but can also determine suitable operation modes in corresponding conditions. Experimental results demonstrate that this HESS can extend battery life as well. The overall efficiency of the compound-type HESS is higher than those of the battery/SC and the SC/battery HESSs.

Identification of Loliolide with Anti-Aging Properties from Scenedesmus deserticola JD052

  • Dae-Hyun Cho;Jin-Ho Yun;Jina Heo;In-Kyoung Lee;Yong-Jae Lee;Seunghee Bae;Bong-Sik Yun;Hee-Sik Kim
    • Journal of Microbiology and Biotechnology
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    • v.33 no.9
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    • pp.1250-1256
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    • 2023
  • Herein, different extracts of Scenedesmus deserticola JD052, a green microalga, were evaluated in vitro as a potential anti-aging bioagent. Although post-treatment of microalgal culture with either UV irradiation or high light illumination did not lead to a substantial difference in the effectiveness of microalgal extracts as a potential anti-UV agent, the results indicated the presence of a highly potent compound in ethyl acetate extract with more than 20% increase in the cellular viability of normal human dermal fibroblasts (nHDFs) compared with the negative control amended with DMSO. The subsequent fractionation of the ethyl acetate extract led to two bioactive fractions with high anti-UV property; one of the fractions was further separated down to a single compound. While electrospray ionization mass spectrometry (ESI-MS) and nuclear magnetic resonance (NMR) spectroscopy analysis identified this single compound as loliolide, its identification has been rarely reported in microalgae previously, prompting thorough systematic investigations into this novel compound for the nascent microalgal industry.

Antifungal Activity of Magnolol and Honokiol

  • Bang, Kyu-Ho;Kim, Yoon-Kwan;Min, Byung-Sun;Na, Min-Kyun;Rhee, Young-Ha;Lee, Jong-Pill;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.23 no.1
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    • pp.46-49
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    • 2000
  • Two neolignan compound, magnolol $(5,5^{l}-diallyl-2,2^{l}-dihydroxybiphenyl, 1)$ and honokiol $(5,5^{l}-diallyl-2,4^{l}-dihydroxybiphenyl, 2)$ were isolated from the stem bark of Magnolia obovata and evaluated for antifungal activity against various human pathogenic fungi. Compound 1 and 2 showed significant inhibitory activities against Trichophyton mentagrophytes, Microsporium gypseum, Epidermophyton floccosum, Aspergillus niger, Cryptococcus neoformans, and Candida albicans with minimum inhibitory concentrations (MIC) in a range of $25-100{\mu}g/ml$. Therefore, compound 1 and 2 could be used as lead compounds for the development of novel antifungal agents.

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A Study on the transformer characteristics using a compound Core (컴파운드 코어를 이용한 변압기 특성에 관한 연구)

  • Hwang, Sun-Min;Ahn, Tae-Young
    • Proceedings of the KIEE Conference
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    • 2001.07b
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    • pp.959-961
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    • 2001
  • In this paper, a novel plastic type compound core for a transformer and inductor of DC-DC converter proposed. The experimental results and application potentials of a Flyback DC-DC converter based the plastic type compound core are presented. The experimental converter, that has a maximum power of 24W, switching frequency of 200kHz and input voltage of 110-220V, has been successfully implemented. A maximum power conversion efficiency of the experimental converter was measured at 76%, and the output was regulated at 12V within 0.2% tolerance.

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A Novel Boost PFC Converter Employing ZVS Based Compound Active Clamping Technique with EMI Filter

  • Mohan, P. Ram;Kumar, M. Vijaya;Reddy, O.V. Raghava
    • JSTS:Journal of Semiconductor Technology and Science
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    • v.8 no.1
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    • pp.85-91
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    • 2008
  • A Boost Power Factor Correction (PFC) Converter employing Zero Voltage Switching (ZVS) based Compound Active Clamping (CAC) technique is presented in this paper. An Electro Magnetic Interference (EMI) Filer is connected at the line side of the proposed converter to suppress Electro Magnetic Interference. The proposed converter can effectively reduce the losses caused by diode reverse recovery. Both the main switch and the auxiliary switch can achieve soft switching i.e. ZVS under certain condition. The parasitic oscillation caused by the parasitic capacitance of the boost diode is eliminated. The voltage on the main switch, the auxiliary switch and the boost diode are clamped. The principle of operation, design and simulation results are presented here. A prototype of the proposed converter is built and tested for low input voltage i.e. 15V AC supply and the experimental results are obtained. The power factor at the line side of the converter and the converter efficiency are improved using the proposed technique.