• Title/Summary/Keyword: active compound

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Anxiolytic Activities of Sanguisorbae Radix (지유(Sanguisorbae Radix)의 항 불안 활성)

  • Lee, So-Young;Chung, Sung-Hyun
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.733-741
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    • 1994
  • To detect anxiolytic activity from Sanguisorbae Radix we used various animal models of fear or anxiety that are sensitive to known anxiolytic drugs. While diazepam showed significant anxiolytic activities in all five animal models empolyed in this study, $5-HT_3$ antagonist ondansetron and ethylacetate fraction of Sanguisorbae Radix did show anti-anxiety effects in social interaction and two compartment exploration tests. Ethylacetate fraction of Sanguisorbae Radix and 5-HT related drugs like ondansetron and buspirone, however, seem to have merit over diazepam in terms of not causing drowsiness. Among ten subfractions obtained from ethylacetate fraction of Sanguisorbae Radix by silica gel chromatography, subfraction I showed higher anxiolytic activities than subfraction DEF in two animal models, social interaction and two compartment exploration tests. There is growing evidence for the role of 5-HT in the control of anxiety. We hope that new compound(s) will be found from the active fractions of Sanguisorbae Radix as a potential anxiolytic agent in the future.

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A Potential Target of Tanshinone IIA for Acute Promyelocytic Leukemia Revealed by Inverse Docking and Drug Repurposing

  • Chen, Shao-Jun
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.10
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    • pp.4301-4305
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    • 2014
  • Tanshinone IIA is a pharmacologically active ingredient extracted from Danshen, a Chinese traditional medicine. Its molecular mechanisms are still unclear. The present study utilized computational approaches to uncover the potential targets of this compound. In this research, PharmMapper server was used as the inverse docking tool andnd the results were verified by Autodock vina in PyRx 0.8, and by DRAR-CPI, a server for drug repositioning via the chemical-protein interactome. Results showed that the retinoic acid receptor alpha ($RAR{\alpha}$), a target protein in acute promyelocytic leukemia (APL), was in the top rank, with a pharmacophore model matching well the molecular features of Tanshinone IIA. Moreover, molecular docking and drug repurposing results showed that the complex was also matched in terms of structure and chemical-protein interactions. These results indicated that $RAR{\alpha}$ may be a potential target of Tanshinone IIA for APL. The study can provide useful information for further biological and biochemical research on natural compounds.

Molecular Orbital Consideration of the Conformation and Biological Activities of Medical Drug, N,N-Diethyl-m-toluamide (양자역학 이론에 의한 의약품 N,N-디메틸-m-톨루아미드의 분자구조와 약리효과에 관한 연구)

  • Kim, Ui Rak;Seo, Bae Seok;Lee Myung Jae
    • Journal of the Korean Chemical Society
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    • v.19 no.4
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    • pp.213-217
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    • 1975
  • N,N-Diethyl-m-toluamide is the active ingredient in insect repellant against malaria mosquito. It is remarkable that if the methyl group is in either of the other isomeric positions(ortho or para) the compound is ineffective as an insect repellant. Semiempirical quantum mechanical treatment are applied to these molecules to explain the difference, using the extended Huckel theory, the theoretical predictions for the preferred conformation are compared with experimental results.

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Synthesis of Triazoloquinoxalines as Antitubercular Agents

  • Sekhar, Kondapalli Venkata Gowri Chandra;Rao, Vajja Sambasiva;Kumar, Dalip
    • Bulletin of the Korean Chemical Society
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    • v.32 no.8
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    • pp.2657-2660
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    • 2011
  • 1,2,4-Triazoles and quinoxalines were found to display various pharmacological activities. Hence a series of 1-aryl-4-methyl-1,2,4-triazolo[4,3-a]quinoxalines were synthesized. Due to various advantages of organic reactions under solvent-free conditions these compounds were developed using iodobenzene diacetate under solvent-free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, $^{13}C$ NMR and HRMS. All the synthesized compounds were investigated for their antitubercular activity and 5g was found to the most active compound.

Synthesis of certain 2-aminoadmantane derivatives as potential antimicrobial agents

  • Eisa, Hassan M.;Tantawy, Atif S.;El-Kerdawy, Mohamed-M.
    • Archives of Pharmacal Research
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    • v.13 no.1
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    • pp.74-77
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    • 1990
  • N-(2-Amamantyl)-N-(5-arylhydrazono-6-methyl-4-oxopyrimidin-2-yl) guanidines (IIIa, b), 2-(2-admantyl-amino)-4-amino-s-triazine (IVa) and its 6-chloromethyl derivative (IVb) were prepared by cylization of 1-(2-admantyl) biguanide HCl (I) with ethyl 2-arylhydrazono-3-oxobutyrates (II), ethyl formate and ethyl chloroacetate, respectively. Where 1-(2-admantyl)-3-(4, 5-dioxo-2-imidazolidinylidene)guanidine (V) was used as intermediate for the synthesis of amides (VIIa, b), hydrazide (VIII) and azomethine derivatives (IX, b) of alkyl 2-(2-admantyl-amino)-4-amino-2-triazine-6-carboxylates (VI a, b). The antimicrobial testing of the prepared compounds proved that compound 1Xb was the most active. It showed a marked bacteriostatic effect against Staphylococcus aureus and Bacillus subtilis.

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Development of Resource Planning System for Compound Semiconductor Chip Manufacturing (화합물 반도체 칩 생산을 위한 자원관리 시스템 개발)

  • 나동길;박지훈;김동원
    • Proceedings of the Korean Operations and Management Science Society Conference
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    • 2000.04a
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    • pp.201-204
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    • 2000
  • 본 연구의 목적은 화합물 반도체를 생산하는 중소기업의 정보시스템을 설계하고 개발하여 적용하는데 있다. 제품의 수주에서 일정계획수립, 제품 재고관리 및 원·부자재 관리, 생산 가동율 등 생산활동전반에 걸친 업무 흐름을 분석하여 이에 사용되는 기초정보를 얻어내고, 이들 기반으로 관리자를 위한 관리정보와 의사결정자를 위한 경영정보를 Web상에 가시화 하는 시스템을 개발한다. 인터넷을 활용함으로써 기업 정보를 원격지에서 조회, 검색 할 수 있고 빠른 의사결정을 지원할 수 있도록 한다. 또한 기업 내부의 인트라넷 시스템과 연동하여 부서간 업무연락 및 정보시스템에서 발생하는 의사결정 요구사항을 쌍 방향으로 전달함으로써 그 활용도를 더욱 높인다. 본 시스템은 영업, 물류, 생산, 구매, 자재 인사, 회계 개발 등 기업 전체에 대한 자원관리를 위해 설계되었다. 개발된 시스템은 주문/수주정보관리, 제품재고관리, 원·부자재관리, 공정관리, 입출고 관리 등으로 구성되어 있다. 중소기업환경에 적합한 MS-SQL Server를 DB server로 사용하였고 Windows-NT기반의 ASP ( Active Server Page)를 사용하여 전 모듈을 개발함으로써 인터넷이 지원되는 모든 곳에서 접근 가능하도록 하였다.

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Anti-stress effect of Hervchoke juice in ICR mice and SD rats

  • Lee, Blendyl T.;Jeong, Seung-Hwa;Cheong, Chae-Hoon;Yang, Sung-Jin;Cheong, Jae-Hoon
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.68-68
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    • 2003
  • Herbchoke solution produced by Choa pharmaceutical company contained pyroligneous liquid and extracts from artichoke leaves. Pyroligneous liquid is produced by process carbonizing Oak in 350∼400$^{\circ}C$. It contain water 96%, acetic acid 3% and organic compound 1%. There are 200 kinds of constituents including minerals, vitamin B-complex and organic acids in it. The organic acids of them were presumed as active materials. It is traditionally used for treatment of stress related disorder, hepatic disease, immune disorder, G-I disorder and inflammatory disease. Extracts from artichoke leaves are traditionally used for treatment of stress related disorder, that is, hepatic disease, dyspeptic disorder, hyperlipidemic disorder and diuretic disorder. The aim of this study was to investigate anti-stress effects of Hervchoke juice produced from Choa pharmaceutical company.

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Determination of Silybin B in the Different Parts of Silybum marianum using HPLC-UV

  • Rodriguez, Joyce P.;Quilantang, Norman G.;Lee, Ju Sung;Lee, Jeong Min;Kim, Hyun Young;Shim, Jae Suk;Lee, Sanghyun
    • Natural Product Sciences
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    • v.24 no.2
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    • pp.82-87
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    • 2018
  • Silymarin is the standardized extract from Silybum marianum which consists mainly of flavonoids and polyphenols. It is highly regarded for its hepatoprotective ability. Silybin B is a flavonolignan and one of the active components of silymarin. The content of silybin B in various parts of S. marianum was analyzed by HPLC-UV. Results show that the extract of seeds contain the highest amount of silybin B (7.434 mg/g DW). The petioles of S. marianum showed a low content of silybin B. This study revealed that seeds of S. marianum contain high amount of silybin B and could be a good source of the compound.

Antibacterial Activity of Panduratin A Isolated from Kaempferia pandurata against Porphyromonas gingivalis

  • Park, Kyung-Min;Choo, Jeong-Han;Sohn, Jong-Hee;Lee, Sun-Hee;Hwang, Jae-Kwan
    • Food Science and Biotechnology
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    • v.14 no.2
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    • pp.286-289
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    • 2005
  • Active antibacterial compound against periodontitis-causing bacterium Porphyromonas gingivalis was isolated from Kaempferia pandurata and identified as panduratin A. Minimum inhibitory concentration (MIC) value of panduratin A was $4\;{\mu}g/mL$, much lower than those of other natural antibacterial agents. Panduratin A also showed antibacterial activity against Prevotella intermedia ($2\;{\mu}g/mL$), P. loescheii ($4\;{\mu}g/mL$), and cariogenic Streptococcus mutans ($4\;{\mu}g/mL$). Damage on cell wall and perturbation of cytoplasmic membrane of panduratin A-treated P. gingivalis were visualized through transmission electron microscopy. These results suggest panduratin A, exhibiting strong and preferential antiperiodontal and anticariogenic activities, may be utilized in functional foods for prevention of oral diseases.

Isolation of Hepatic Drug Metabolism Inhibitors from the Rhizomes of Curcuma zedoaria

  • Shin, Kuk-Hyun;Kim, Ok-Nam;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • v.12 no.3
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    • pp.196-200
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    • 1989
  • The methanolic extract of the Rhizome of Curcuma zedoaria exhibited a significant prolongation of hexobarbital (HB)-induced hypnosis. Through liquid chromatography of an ether soluble fraction. monitoring by bioassay, three sequiterpenes, germacrone (A), curzerenone (B) and germacrone epoxide (C) were isolated as active consituents. A single treatment (100-200 mg/kg, i.p.) of each compound showed not only a significant prolongation of HB-induced sleeping time but also a significant inhibition of aminopyrine N-demethylase activity in mice, and further exhibited a typical type I binding spectra with oxidized rat hepatic cytochrome P-450 induced by phenobarbital. All of the compounds provoked a sleep episode at a subhypnotic dose of HB, implying that they possess CNS depressant properties.

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