• Title/Summary/Keyword: active agents

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Synthesis and Antiinflammatory-analgesic Activity of Monovalent and Bivalent Aminoantipyrines (Monovalent와 bivalent aminoantipyrine 유도체의 합성과 항염 진통활성)

  • 김승재;권오혁;전상철;박상민;임채욱;임철부
    • YAKHAK HOEJI
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    • v.46 no.3
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    • pp.149-154
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    • 2002
  • Six novel 4-aminoantipyrine derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity were compared with antiprine. Succinyl chloride and Ac $_2$O were reacted with glycine, respectively, to give glycine compounds (3-4, 9-10), which were treated with hydroxysuccinimide and dicyclohexyl carbodiimide to yield active esters (5-6, 11-12), and then reacted with 4-aminoantipyrine to prepare 4-aminoantipyrine derivatives (7-8, 13-14). 4-Aminoantipyrine reacted with succinyl chloride and Ac $_2$O, respectively, to give succinyl bis aminoantipyrine (15) and acetyl aminoantipyrine (16). Compounds (7), (8) and (13) gave comparable antiinflammatory activity to antipyrine.

Synthesis of New Triazolyl-N,N-Dialkyldithiocarbamates as Antifungal Agents

  • Ozkirimli Sumru;Apak T. Idil;Kiraz Muammer;Yegenoglu Yildiz
    • Archives of Pharmacal Research
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    • v.28 no.11
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    • pp.1213-1218
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    • 2005
  • N,N-Dialkylditihiocarbamate derivatives have been well known as broad-range fungicides. In this study, the triazole derivatives of ten new N,N-disubstituted dithiocarbamates (3a-j) were synthesized and their structures were identified by spectral and elemental analysis. Results of the antifungal activity studies showed that some of the compounds tested were active against M. canis, M. gypseum, and T rubrum at the concentration of 12.5 $\mu$g/mL when c1otrimazol was used as a standard.

Isolation and Properties of Cytotoxic Antibiotics Produced by Myxococcus stipitatus JW150 (Myxococcus stipitatus JW150이 생산하는 세포독성 물질의 분리 및 특성)

  • 안종웅;이정옥
    • YAKHAK HOEJI
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    • v.46 no.2
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    • pp.108-112
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    • 2002
  • Drug resistance is one of the most significant impediments to successful chemotherapy of cancer. Multidrug-resistance (MDR) is characterized by decreased cellular sensitivity to anticancer agents due to the overexpression of P-glycoprotein. By employing a resistant subline of HCT15 to adriamycin (CL02), we undertook the screening for agents which were effective to multidrug-resistant cancer cells. As a result, a myxobacterial strain JW150 was selected for study since an activity against CL02 cells was discovered in the strain. Cytotoxicity-guided fractionation of the culture broth led to the isolation of cystothiazole A and melithiazole F. The producing organism was identified as Myxococcus stipitatus by taxonomic comparison with type strains of Myxococcus sp. as well as its morphological and physiological characteristics. Cystothiazole A and melithiazole F demonstrated potent cytotoxicity against certain human cancer cells with $IC_{50}$ values ranging from 0.03~ $0.72{\mu}{\textrm{g}}$/ml. Both compounds were interestingly as active against drug-resistant sublines CL02 and CP70 as against the corresponding parental cells.

Ar-turmerone and $\beta-atlantone$ induce internucleosomal DNA fragmentation associated with programmed cell death in human myeloid leukemia HL-60 cells

  • Paek, Sang-Hyun;Kim, Geon-Joo;Han, Seung-Jeong;Yum, Sung-Kwan
    • Archives of Pharmacal Research
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    • v.19 no.2
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    • pp.91-94
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    • 1996
  • In the course of a search for antitumor agents, we found that the extract of Curcuma longa was effective in inducing apoptosis or programmed cell death (PCD) in human myeloid leukemia cells (HL-60). Active compounds for PCD were isolated from the hexanic extraction of the rhizome of Curcuma longa. With the several chromatographies, and spectral data, they were identified as ar-turmerone and $\beta-atlantone$. The present results demonstrate that the exposure of human myeloid leukemia HL-60 cells to clinically achievable concentrations of arturmerone (TU) or .$\beta-atlantone$(AT) produced internucleosomal DNA fragmentation of approximately 200 base-pair multiples, and the morphological changes characteristic of cells undergoing apoptosis or PCD. This findings suggest that these agents may exert their antitumoral activity, in part, through induction of apoptosis(PCD).

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Anti-Tumor Necrosis Factor Therapy in Intestinal Behçet's Disease

  • Park, Jihye;Cheon, Jae Hee
    • Gut and Liver
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    • v.12 no.6
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    • pp.623-632
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    • 2018
  • Intestinal Behçet's disease is a rare, immune-mediated chronic intestinal inflammatory disease; therefore, clinical trials to optimize the management and treatment of patients are scarce. Moreover, intestinal Behçet's disease is difficult to treat and often requires surgery because of the failure of conventional medical treatment. Administration of anti-tumor necrosis factor-${\alpha}$, a potential therapeutic strategy, is currently under active clinical investigation, and evidence of its effectiveness for both intestinal Behçet's disease and inflammatory bowel diseases has been accumulating. Here, we review updated data on current experiences and outcomes after the administration of anti-tumor necrosis factor-${\alpha}$ for the treatment of intestinal Behçet's disease. In addition to infliximab and adalimumab, which are the most commonly used agents, we describe agents such as golimumab, etanercept, and certolizumab pegol, which have recently been shown to be effective in refractory intestinal Behçet's disease. This review also discusses safety issues associated with anti-tumor necrosis factor-${\alpha}$, including vulnerability to infections and malignancy.

Anti-asthmatic agents of Gastrodia elata Rhizoma MeOH extracts

  • Jang, Yong-Un;Suh, Mu-Hyun;Lee, Ji-Yun;Sim, Sang-Soo;Whang, Wan-Kyun;Kim, Chang-Jong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.299.2-299.2
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    • 2002
  • For the activity-guided separation on anti-asthmatic action from 4 fractions as n-hexane (yield. 0.09%), EtOAc (0.48%), BuOH (3.0%) and H2O (5.17%) fractions from MeOH extract (11.64%) of powdered Gastrodia elata Rhizoma (GER), some biological active agents were isolated by column chromatography (column, silica gel: elution solvent. CHCl3 : MeOH) according to the method of Junko Hayashi et. al. and Heihachiro Taguchi et. al. (omitted)

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Anti-inflammatory agents of Gastrodia elata Rhizoma fractions

  • Lee, Ji-Yun;Jang, Yong-Un;Suh, Mu-Hyun;Sim, Sang-Soo;Kim, Chang-Jong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.300.1-300.1
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    • 2002
  • From 4 fractions as n-hexane (yield. 0.09%), EtOAc (0.48%). BuOH (3, 0%) and H2O (5.17%) fraction from MeOH extract (11, 64%) of powdered Gastrodia elata Rhizoma (GER) for the activity-guided separation on anti-inflammatory action. some biological active agents were isolated by column chromatography (column. silica gel: elution solvent. CHCl3 : MeOH) according to the method of Junko Hayashi et. al. and Heihachiro Taguchi et. al. Compound I, II, III, IV, V as phenolic derivatives were isolated in the EtOAc and BuOH fractions. (omitted)

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Tourism Market Segmentation Based on Shopping Information Sources (쇼핑정보원 활용에 따른 해외여행자 시장세분화 및 세분시장 특성 연구)

  • Jeon, Yangjin
    • Journal of the Korea Fashion and Costume Design Association
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    • v.19 no.2
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    • pp.117-128
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    • 2017
  • This study confirmed the types of shopping information sources during travel abroad, and developed a profile of tourists in terms of demographics, travel, and shopping behavior. Shopping information sources and characteristics of shopping products were identified first. Thereafter, travelers were segmented by their information-seeking behavior. An online survey method was used to get data from Korean vacationers in their 20s-50s, while factor analysis, cluster analysis, ${\chi}^2$ test and ANOVA were applied to analyze data. The results were as follows. First, the shopping information sources of overseas tourists were composed of four factors including sources from travel agents/media, information from travel books and local sources, and word-of-mouth sources. Also, four factors in product types and four product attributes were identified. Second, tourists were clustered into two groups, active and passive shopping information seekers, based on shopping source behavior. Third, two groups differed in terms of demographics, showing an older age and higher income for active shopping source seekers. Active shopping information users tended to join package trips with family members, and they were more satisfied with the trip. With regard to shopping, active shopping source seekers spent more money for shopping and preferred all kinds of shopping goods with an emphasis on travel shopping. In conclusion, shopping information sources seemed to be a meaningful tool for segmenting tourists. Rich, older, family tourists would be an major target market for local retailers.

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Electrochemical characteristics of active carbon prepared by chemical activation for anode of lithium ion battery (이차전지 음극용 화학적 활성화법으로 제조된 활성탄의 전기화학적 특성)

  • Lee, Ho-Yong;Kim, Tae-Yeong;Lee, Jong-Dae
    • Journal of the Korean Applied Science and Technology
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    • v.32 no.3
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    • pp.480-487
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    • 2015
  • In this study, several kinds of active carbons with high specific surface area and micro pore structure were prepared from the coconut shell charcoal using chemical activation method. The physical property of prepared active carbon was investigated by experimental variables such as activating chemical agents to char coal ratio, flow rate of inert gas and temperature. It was shown that chemical activation with KOH and NaOH was successfully able to make active carbons with high surface area of $1900{\sim}2500m^2/g$ and mean pore size of 1.85~2.32 nm. The coin cell using water-based binder in the electrolyte of LiPF6 dissolved in mixed organic solvents (EC:DMC:EMC=1:1:1 vol%) showed better capacity than that of oil-based binder. Also, it was found that the coin cell of water-based binder shows an improved cycling performance and coulombic efficiency.

Synergistic Antibacterial Activity of an Active Compound Derived from Sedum takesimense against Methicillin-Resistant Staphylococcus aureus and Its Clinical Isolates

  • Jeong, Eun-Tak;Park, Seul-Ki;Jo, Du-Min;Khan, Fazlurrahman;Choi, Tae Ho;Yoon, Tae-Mi;Kim, Young-Mog
    • Journal of Microbiology and Biotechnology
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    • v.31 no.9
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    • pp.1288-1294
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    • 2021
  • There are a growing number of reports of hospital-acquired infections caused by pathogenic bacteria, especially methicillin-resistant Staphylococcus aureus (MRSA). Many plant products are now being used as a natural means of exploring antimicrobial agents against different types of human pathogenic bacteria. In this research, we sought to isolate and identify an active molecule from Sedum takesimense that has possible antibacterial activity against various clinical isolates of MRSA. NMR analysis revealed that the structure of the HPLC-purified compound was 1,2,4,6-tetra-O-galloyl-glucose. The minimum inhibitory concentration (MIC) of different extract fractions against numerous pathogenic bacteria was determined, and the actively purified compound has potent antibacterial activity against multidrug-resistant pathogenic bacteria, i.e., MRSA and its clinical isolates. In addition, the combination of the active compound and β-lactam antibiotics (e.g., oxacillin) demonstrated synergistic action against MRSA, with a fractional inhibitory concentration (FIC) index of 0.281. The current research revealed an alternative approach to combating pathogenesis caused by multi-drug resistant bacteria using plant materials. Furthermore, using a combination approach in which the active plant-derived compound is combined with antibiotics has proved to be a successful way of destroying pathogens synergistically.