• Title/Summary/Keyword: Active compounds

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오배자의 항산화 활성성분 및 자유라디칼 소거효과 (Constituents of Antioxidative Activity and Free Radical Scavenging Effect from Galla Rhois (Rhus javanica Linne))

  • 이승배;임태진;이광회;차배천
    • 생약학회지
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    • 제31권2호
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    • pp.185-189
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    • 2000
  • This study was carried out to investigate the structure of antioxidative constituents and the free radical scavenging effect of the main ingredients from Galla Rhois(Rhus javanica Linne). Antioxidative activities of n-hexane, EtOAc and BuOH extracts of Galla Rhois were similar or even higher than that of natural (tocopherol) or synthetic antioxidant (BHA). It is suggested that major fractions for the antioxidative activity of Galla Rhois were the n-hexane, EtOAc and BuOH extract compartments. In the subsequently experiment, one active compound from n-hexane extract, three active compounds from EtOAc extract and one active compound from BuOH extract were isolated. Their chemical structures were identified as syringic acid, protocatechuic acid, gallic acid methylester, gallic acid and $1,2,3,4,6- penta-O-galloyl-{\beta}-D-glucose$ on the basis of the speculation of spectral data and chemical reaction. Among the compounds, protocatechuic acid, gallic acid methylester and $1,2,3,4,6- penta-O-galloyl-{\beta}-D-glucose$ showed most potent radical scavenging effect using DPPH method.

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Agelas속의 미동정 해면으로부터 항말라리아 활성을 갖는 Dibromosceptrin의 분리 (Isolation of Dibromosceptrin with Antimalarial Activity from the Unidentified Sponge, Agelas sp.)

  • 박영범;이종수;임치원
    • 생약학회지
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    • 제35권3호통권138호
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    • pp.189-193
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    • 2004
  • In order to find some lead compounds for the treatment of opportunistic infections of malaria and pathogenic microbes, an undescribed Indonesian sponge Agelas sp. collected at Manado, Indonesian Waters, was suggested containing active compounds. Crude ethanolic extract of the sponge exhibited significant in vitro antimalarial and antimicrobial activity against Plasmodium falciparum (D6 colne) with $IC_{5O}$ values of $8\;{\mu}/ml$ and against pathogenic microbes such as Candida albicans $(150\;{\mu}/ml)$, Cryptococcus neoformans $(<20\;{\mu}/ml)$, Staphylococcus aureus $25\;{\mu}/ml$, methicillin-resistant Staphylococcus aureus $(<20\;{\mu}/ml)$, and Pseudomonas aeruginosa $(<20\;{\mu}/ml)$. Active compound (5.0 mg) was isolated from the ethanolic extracts of the sponge and purified by using silica gel and ODS column, successively. Active compound was elucidated as dibromosceptrin $(C_{22}H_{24}Br_2N_{10}O_2)$ by detailed analysis of FTESI-MS and comparison of $^1H,\;^{13}C$, DEPT and HMQC NMR spectral data with those reported.

Comparison of Some 3-(Substituted-Benzylidene)-1, 3-Dihydro-Indolin Derivatives as Ligands of Tyrosine Kinase Based on Binding Mode Studies and Biological Assay

  • Olgen, Sureyya
    • Archives of Pharmacal Research
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    • 제29권11호
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    • pp.1006-1017
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    • 2006
  • A series of 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2'-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of $p60^{c-Src}$tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitor PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2'-dithiobis 3-(substituted-benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

Isoquinolines: Are they possible candidate for $Ca^{2+}$ blockers\ulcorner

  • 장기철;윤용진;조수동;정원석
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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    • pp.217-217
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    • 1994
  • Calcium entry blockers, capable of inhibiting transmembrane influx of extracellular calcium through specific calcium channels, are useful drugs in the treatment of angina pectoris, hypertension, cardiac arrythmia, and various cardiovascular disorders. Compounds having isoquinoline structures have recently been reported to possess calcium antagonistic action. Therefore, in the present study, we have attempted to synthesize some isoquinoline and related compound.; in order to search for potentially effective chemicals acting on cardiovascular system, and evaluated their pharmacological properties focusing on calcium antagonistic actions. Almost all of the compounds so far synthesized, had inhibitory action against phenylephrine or high potassium-induced contraction in vascular smooth muscle with different degrees of potencies depending on their structures, However, some of tetrahydroisoquinoline analogs showed directly inhibit calcium current in isolated rabbit cardiac myocytes examined by patch clamp techniques. The pharmacological properties of these compounds need more intensive investigation as to whether these chemicals may have developed as a new cardiovascular active drugs. Therefore, we are now under investigation of the mechanism of action of these compounds.

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버섯원물과 버섯 추출물 그리고 버섯 유래 화합물을 포함한 식품과 기능성식품 (Foods and functional foods containing mushroom, mushroom extracts, and mushroom-derived compounds)

  • 조한교;신현재
    • 한국버섯학회지
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    • 제15권4호
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    • pp.155-163
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    • 2017
  • Mushrooms and their extracts including purified ingredients, are currently used as foods, functional foods (and/or nutraceuticals), and medicines. These products have numerous bioactive compounds such as polysaccharides (mainly ${\beta}$-glucans), glycoproteins, nucleotide analogs, terpenoids, and polyphenols, which have exhibited antioxidant, antimicrobial, anticancer, antiviral, anti-obesity, and immunomodulatory activities. In this review, we discuss the current information on the biactivities of 10 popular mushrooms in Korea. We also summarize the information on mushrooms and the active compounds derived from them, as well as mushroom-based products such as foods, functional foods, and medicines. We believe this review could provide useful information for scientists and consumers who seek to develop new products and promote healthy food habits and lifestyle.

Synthesis and Antinociceptive Activity of (5-Chloro-2(3H)-Benzoxazolon-3-yl) Propanamide Derivatives

  • Onkol, Tijen;Sahin, M.Fethi;Yidirim, Engin;Erol, Kevser;Ito, Shigero
    • Archives of Pharmacal Research
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    • 제27권11호
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    • pp.1086-1092
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    • 2004
  • In this study, (5-chloro-2(3H)-benzoxazolon-3-yl)propanamide derivatives were synthesized. The chemical structures of the compounds were elucidated by their IR and $^1H-NMR$ spectral data and microanalysis. The compounds were tested for anti nociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods. The varying levels of anti nociceptive activity of the compounds were compared with those of dipyrone and aspirin. Among these compounds, compound 5e, 5g, and 5h have been found to be significantly more active than the others and the standards in all the tests.