• 제목/요약/키워드: inhibitory compounds

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박태기나무의 잎으로부터 피부멜라닌 색소생성 억제성분의 분리 (The Isolation of the Inhibitory Constitutents on Melanin Polymer Formation from the Leaves of Cercis chinensis)

  • 김소영;김진준;장태수;정시련;이승호
    • 생약학회지
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    • 제30권4호
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    • pp.397-403
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    • 1999
  • Tyrosinase plays an important role in the process of melanin polymer biosynthesis. Therefore, the enzyme inhibitors have been of great concern as cosmetics to have skin-whitening effects on the local hyperpigmentation. During the search for new inhibitory compounds on melanin polymer biosynthesis from natural sources, MeOH extracts of 589 higher plants were tested for the inhibitory effect on tyrosinase activity by the muschroom tyrosinase assay in vitro. Among plants tested, the leaves of Cercis chinensis exhibited potent inhibitory effect on mushroom tyrosinase activity. Subsequently seven active compounds were isolated from the ethyl acetate soluble part of acetone extract of the leaves of C. chinensis by the activity guided fractionation monitoring the inhibitory effect on tyrosinase activity. Their chemical structures were identified as $kaempferol-3-0-{\alpha}-L-rhamnoside$, quercitrin, $myricetin-3-0-{\alpha}-L-rhamnoside$, myricetin-3-0-(2'-O-galloyl)- ${\alpha}$ -L-rhamopyranoside (desmanthin), (-)-epicatechin-3-0-gallate, (-)-epigallocatechin-3-0-gallate, and methyl gallate on the basis of the speculation of spectral data and chemical reaction. Among the flavonol rhamnosides, myricetin-3-0-(2'-O-galloyl)- -L-rhamnoside(desmanthin) showed most potent inhibitory effect on tyrosinase activity and the structure of B-ring in flavonol moiety was related to the activity. (-)-Epigallocatechin-3-O-gallate having pyrogallol group in flavan-3-ol moiety exhibited more potent inhibitory effect than (-)-epicatechin-3-0-gallate having catechol group in flavan-3-ol moiety on mushroom tyrosinase activity.

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Higenamine 유도체들의 혈소판응집 억제작용 (Platelet Anti-aggregating Activities of Higenamine Analogs)

  • 윤혜숙;백승환;이종란
    • 약학회지
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    • 제30권5호
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    • pp.245-252
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    • 1986
  • Various structural analogs of higenamine, 1-(4'-hydroxylbenzyl)-6,7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline, were synthesized and their inhibitory activities against platelet aggregation induced by either arachidonic acid, ADP or collagen. Among the twenty-five compounds tested, inhibitory activity is favored by the 3, 4-dihydroisoquinoline system with the methyl bridge between the two aromatic rings replaced by either ethyl or ethenyl group. N-Methyl quaternization decreased the inhibitory activities. * 이논문의 내용중 편집상의 오류가 있습니다. 그에대한 정오표는 v.31, n.1의 45p.에 있습니다.

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Production of Bacteriocins by Strains of Lactobacillus acidophilus from Different Animal Origins

  • Kim, Sae-Hun
    • 한국유가공학회:학술대회논문집
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    • 한국유가공기술과학회 1996년도 추계 제43회 유가공 심포지움
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    • pp.30-34
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    • 1996
  • Twenty seven strains of Lactobacillus acidophilus among 92 isolated from fecal contents of humans, pigs, calves, chickens, rodents and turkeys demonstrated inhibitory attributed to bacteriocin(s). The bacteriocin(s) were heat stable and nondialyzable proteinous compounds and exhibited narrow inhibitory spectra of activity. Neither hydrogen peroxide nor low pH were responsible for inhibitory action. All of the producer strains were resistant to their own bacteriocin or bacteriocin(s) produced by other strains. The bacteriocins from several strains from different host species were purified for further characterization. The bacteriocin(s) all exhibited similar characteristics.

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생약의 파골 세포 분화 저해활성 검색 (Inhibitory Activity of Medicinal Plants against Differentiation of Osteoclasts)

  • 이준원
    • 생약학회지
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    • 제40권2호
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    • pp.83-88
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    • 2009
  • Bone is continuously remodeled by osteoblasts and osteoclasts. Osteoclasts play an important role in bone metabolism by resorbing the bone matrix. Thus, the compounds inhibiting osteoclasts can improve bone diseases such as osteoporosis. The methanol extracts of 159 herbal medicines were screened for the inhibitory activity against differentiation of osteoclasts. Among the tested extracts, Achuranthis Radix and Corydalis Tuber showed relatively strong inhibitory activity against differentiation of osteoclasts, whereas they have no significant effect on proliferation of osteoclasts.

Cacao Bean Husk 추출물의 Glucosyltransferase 저해효과 (Inhibitory Effect of Cacao Bean Husk Extract on Glucosyltransferase from Streptococus mutans B13)

  • 권익부;이용우안봉전이신영
    • KSBB Journal
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    • 제8권1호
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    • pp.75-82
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    • 1993
  • The inhibitory effect of cacao bean husk (CBH) extract on glucosyltransferase(GTasc) from Streptococcus mutans B13 was investigated. Water solube extract from CBH showeda sarong inhibitory effect (88-89%) on GTase from Streptococcus mutans Bl3. GTase inhibitors from sequential extraction by hot water or water-methanol had the strongest inhibition. Sources, fermentation, and types of solvents and fumigation processes did not influence the effect. These active compounds proved to be polyphones through acid hydrolytic analysis of the precipitates by ammonium sulfate or ethanol and proteinase K. It was also confirmed by additional column chromatography of Sephadex G-50, Sephadex LH-20 and DEAE-Sephdex A-50.

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Tyrosinase Inhibitory Prenylated Flavonoids from Sophora flavescens

  • Kim, Soo-Jin;Son, Kun-Ho;Chang, Hyun-Wook;Kang, Sam-Sik;Kim, Hyun-Pyo
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.151.2-151.2
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    • 2003
  • For the purpose of the development of a skin-whitening agent, Sophora flavescens was evaluated for tyrosinase inhibitory activity and its active principles were identified followed activity-guided isolation. The ethanol extract and dichloromethane fraction from S. flavescens showed significant inhibition of mushroom tyrosinase. From the dichloromethane fraction, three known prenylated flavonoids, sophoraflavanone G, kuraridin, and kurarinone, were isolated. Compared with kojic acid ($IC_50$=20.5 $\mu$M), these compounds possessed more potent tyrosinase inhibitory activity. (omitted)

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경상도 전통마른오징어 식해의 향기성분 및 기능성 (Functional and Volatile Flavor Compounds in Traditional Kyungsando Squid sikhe)

  • 최청;이희덕;최희진;손준호;김성;손규목;차원섭
    • 한국식품과학회지
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    • 제33권3호
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    • pp.345-352
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    • 2001
  • 경상도 전통마른오징어 식해를 제조하여 $5^{\circ}C$에서 보관하면서 GC와 GC-MS를 이용하여 향기성분의 원인 물질을 분석, 동정하였다. 식해에서 동정된 물질 중에서 ${\alpha}-zingibirene$이 19.73 mg/kg으로 전체상대 농도에서 가장 높았으며 (Z)-Di-2-propenyl disulfide, ${\alpha}-curcumene$, methyl alkyl disulfide, $(E-E)-{\alpha}-farnesene$, pentanol, z-citral, $3-ethyl-1,2-dithi-5-ene-{\beta}-elemene$, acetic acid 및 ${\beta}-phelland$ rene의 함량 순으로 동정되어 이러한 성분들이 식해의 주요성분으로 나타났다. 식해의 향기성분은 hydrocarbone류가 49종, 알데히드류가 15종, 알콜류가 33 종, 케톤류 및 에스테류 11 종을 포함하여 총 162 종을 동정하였다. 식해의 메탄올 추출물을 용매 분획하여 얻은 각 분획물의 전자공여능을 측정한 결과 $200\;{\mu}m$ DPPH radical을 50% 환원시키는데 필요한 $SC_{50}$ 값이 헥산과 물층에서는 효과가 나타나지 않았으며, ethylacetate 층은 $310.64\;{\mu}g/mL$, butanol 층은 $1096.49\;{\mu}g/mL$으로 나타났다. 혈압상승 억제효과를 살펴본 결과 헥산과 물 분획물에서는 전혀 효과가 없었으며 ethylacetate층에서는 $IC_{50}$이 1.623 mg/mL, butanol 층에서는 1.303 mg/mL의 저해효과를 나타내었으며, xanthine oxidase에 대한 $IC_{50}$은 ethyl acetate 층은 3.591 mg/mL, butanol 층은 2.083 mg/mL로 나타났다.

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Synthesis and Antifungal Activity of 6,7-Bis-[S-(Aryl)thio]-5,8-Quinolinediones

  • Ryu, Chung-Kyu;Sun, Yang-Jung;Shim, Ju-Yeon;You, Hea-Jung;Choi, Ko-Un;Lee, Hee-Soon
    • Archives of Pharmacal Research
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    • 제25권6호
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    • pp.795-800
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    • 2002
  • 6,7-Bis-[S-(aryl)thio]-5,8-quinolinediones 4 and 5 were synthesized by the substitution of 6,7-dichloro-5,8-quinolinediones with appropriate arylthiols. Their antifungal activity were tested in vitro for their growth inhibitory activities against pathogenic fungi in comparison with flucytosine. The antifungal activities were significantly improved by S-(aryl)thio moieties of the compounds 4 and 5. The all tested compounds 4 and 5 showed generally good activities against C. albicans and A. niger ranging from 0.8 to 25 $\mu\textrm{g}$/ml. Among them, compounds 4d-4h and 5a-5c exhibited also good activities against C. krusei and C. tropicalis. The activities of compounds 4j and 4I were comparable to those of flucytosine against all tested fungi.

DNA Topoisomerases I and II Inhibitory Activity and Cytotoxicity of Compounds from the Stems of Parthenocissus tricuspidata

  • Woo, Mi Hee;Zhao, Bing Tian;Tran, Manh Hung;Jeong, Su Yang;Ma, Eun Sook;Min, Byung Sun
    • Bulletin of the Korean Chemical Society
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    • 제34권9호
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    • pp.2675-2679
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    • 2013
  • Activity-directed isolation of the methylene chloride fraction from the stems of Parthenocissus tricuspidata have led to the identification of two new compounds (1-2): 1-(2',3',5'-trihydroxyphenyl)-2-(4"-hydroxyphenyl)-ethane-1,2-(E)-epoxide (1, tricuspidatin A) and erythro-1-(3',5'-dihydroxyphenyl)-2-(4"-hydroxyphenyl)-ethane-1,2-diol (2, tricuspidatin B), together with four known compounds (3-6): ${\beta}$-sitosterol (3), nonacosan-1-ol (4), 3-(4-hydroxy-3-methoxyphenyl)-2-propenoic acid hexacosyl ester (5) and betulinic acid (6). Their chemical structures were elucidated based on spectroscopic (IR, UV, MS, 1D and 2D NMR) and physicochemical analyses. Compounds 1 and 2 showed strong DNA topoisomerase II inhibitory activity at both concentrations of 20 and $100{\mu}M$. In addition, 3 exhibited strong cytotoxic activity against the HT-29 and HepG2 cancer cell lines, and 6 showed strong cytotoxicity against the HT-29 and MCF-7 ones.

Polyacetylenes from the Tissue Cultured Adventitious Roots of Panax ginseng C.A. Meyer

  • Xu, Guang-Hua;Choo, Soo-Jin;Ryoo, In-Ja;Kim, Young-Hee;Paek, Kee-Yoeup;Yoo, Ick-Dong
    • Natural Product Sciences
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    • 제14권3호
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    • pp.177-181
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    • 2008
  • Five polyacetylenes, ginsenoyne K (1), (Z)-1-methoxyheptadeca-9-en-4,6-diyne-3-one (2), panaxydol (3), panaxydiol (4), and (E)-heptadeca-8-en-4,6-diyne-3,10-diol (5) were isolated from the adventitious roots of Panax ginseng and their chemical structurFive polyacetylenes, ginsenoyne K (1), (Z)-1-methoxyheptadeca-9-en-4,6-diyne-3-one (2), panaxydol (3), panaxydiol (4), and (E)-heptadeca-8-en-4,6-diyne-3,10-diol (5) were isolated from the adventitious roots of Panax ginseng and their chemical structures were elucidated by interpretation of spectroscopic data. Among the isolated compounds, compounds 2 and 5 were reported for the first time as a natural product. Ginsenoyne K (1) showed dose-dependent inhibitory effect on dopa oxidase activity of tyrosinase.es were elucidated by interpretation of spectroscopic data. Among the isolated compounds, compounds 2 and 5 were reported for the first time as a natural product. Ginsenoyne K (1) showed dose-dependent inhibitory effect on dopa oxidase activity of tyrosinase.