• Title/Summary/Keyword: inhibitory compounds

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Isolation of Dineolignans, Saucernetin-7 and -8, with Nitric Oxide Inhibitory Activity and NMR assignment from Saururus chinensis

  • Lee, Kyung-Tae;Jung, Hyun-Ju;Park, Hee-Juhn
    • Korean Journal of Plant Resources
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    • v.19 no.6
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    • pp.655-659
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    • 2006
  • Two dineolignans (1,2) with nitric oxide inhibitory activities were isolated from Saururus chinensis (Saururaceae) using silica gel column chromatography. Although the structures, saucernetin-7 (1) and -8 (2), have been already reported, NMR assignment of the two compounds was completed aided by 2D-NMR spectroscopy including $^1H-^1H$ COSY, $^1H-^{13}C$ COSY, HMBC and NOESY NMR spectra. Compounds 1 and 2 exhibited significant nitride oxide inhibitory activity in LPS-induced RAW 264.7 cells with $IC_{50}$ values of $11.3{\mu}M\;and\;7.1{\mu}M$, respectively.

Anticancer Effect of Doenjang in in vitro Sulforhodamine B (SRB) Assay (된장의 in vitro Sulforhodamine B (SRB) Assay에 의한 암세포 증식 억제 효과)

  • 이숙희;임선영;박건영
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.28 no.1
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    • pp.240-245
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    • 1999
  • Growth inhibitory effect of doenjang(Korean soypaste) methanol extracts in SRB assay using AGS human gastric adenocarcinoma cell, Hep 3B human hepatocellular carcinoma cell and HT 29 human colon cancer cell was studied. The treatment of doenjang methanol extracts(2mg/assay) to the AGS, Hep 3B and HT 29 cancer cells inhibited the growth of the cancer cells by 55%, 60%, and 71%, respectively. Doenjang methanol extracts exhibited the highest inhibitory effect among other soybean fermented foods and original materials in the SRB assay. In addition, to separate active compounds of doenjang methanol extracts, we fractionated the doenjang with hexane, methanol, dichloromethane, ethylacetate and butanol. Growth inhibitory effect on the AGS, Hep 3B, HT 29 and MG 63 cancer cells was the highest in the fractions of dichloromethane and ethylacetate among other solvent fractions of the doenjang. These results showed that some compounds contained in the fractions of dichloromethane and ethylacetate might play a role on the anticanceric effect of doenjang.

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Cholinesterase Inhibitory Activity of Two Farnesylacetone Derivatives from the Brown Alga Sargassum sagamianum

  • Ryu, Geon-Seek;Park, Soo-Hee;Kim, Eun-Sook;Choi, Byoung-Wook;Ryu, Shi-Yong;Lee, Bong-Ho
    • Archives of Pharmacal Research
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    • v.26 no.10
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    • pp.796-799
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    • 2003
  • Two known farnesylacetone derivatives (1 and 2) were isolated from the Korean brown alga Sargassum sagamianum off Jeju Island, Korea. Compounds 1 and 2 were identified as (5E,10Z)-6, 10, 14-trimethylpentadeca-5, 10-dien-2, 12-dione and (5E,9E,13E)-6, 10,4-trimethylpentadeca-5,9,13-trien-2,12-dione, respectively, by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with $IC_{50}$ values of 65.0∼48.0 and 34.0∼23.0 $\muM$, respectively.

Butyrylcholineesterase(BChE) Inhibitors from a Brown Alga Sargassum sp.

  • Park, Soo-Hee;Ryu, Geon-Seek;Choi, Byoung-Wook;Lee, Bong-Ho
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.375.3-375.3
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    • 2002
  • In continuing search for BChE-inhibitory compounds from Korean marine algae. we found a highly potent inhibitory activity in the methanolic extract of Sargassum species. After partition of the MeOH extract between $CHCl_3$ and 30% MeOH. the former layer was subjected to a series of ODS flash chromatography. silica column chromatography. and preparative TLC to afford three compounds (1-3). Detailed structural elucidation of them is in progress. Compound 1 showed potent BChE-inhibitory activity with $IC_{50}$ values of 11 ng/mL. (omitted)

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Cholinesterase-inhibitory Farnesylacetone Derivatives from the Brown Alga Sargassum sagamianum

  • Park, Soo-Hee;Hwang, Jeong-Won;Lee, Bong-Ho;Choi, Byoung-Wook;Ryu, Geon-Seek
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.206.2-206.2
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    • 2003
  • In continuing search for bioactive compounds from Korean marine algae, we found cholinesterase-inhibitory activity in the methanolic extract of brown alga Sargassum sagamianum. After partitioning between CHCl$_3$ and 30% MeOH, the former layer was purified by a series of ODS flash, silica column, gel-filtration on Sephadex LH-20, and HPLC to give two farnesylacetone derivatives. Their structures were identified by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with IC$\sub$50/ values of 65.0∼48.0 ${\mu}$M and 34.0∼23.0 ${\mu}$M, respectively. (omitted)

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Aldose Reductase Inhibition Effect of PhenolicvCompounds Isolated from Paulownia coreana Bark

  • Kim, Jin-Kyu;Lee, Yeon-Sil;Lim, Soon-Sung;Bae, Young-Soo
    • Journal of the Korean Wood Science and Technology
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    • v.38 no.2
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    • pp.159-164
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    • 2010
  • Nine compounds, caffeic acid, naringenin, apigenin, luteolin, kaempferol, verbascoside, isoverbascoside, isocampneoside II, and cistanoside F, were isolated from the EtOAc and n-BuOH fractions of P. coreana bark. The structures of these compounds (1-9) were elucidated by spectroscopic methods and literature data. All the isolates were subjected to in vitro bioassay to evaluate their inhibitory activity against rat lens aldose reductase. Among these, compounds 6 and 8 indicated the significant inhibitory activity on rat lens aldose reductase with $IC_{50}$ values of 2.67 and 5.59 ${\mu}M$, respectively. Especially, The inhibition activity of acteoside was 3.9 times better than that of quercetin as a positive control (10.6 ${\mu}M$). These results suggested that phenylethanoid glycosides are likely to be the potential compounds for the prevention and/or treatment of diabetic complications.

Anti-Inflammatory and PPAR Transactivational Effects of Oleanane-Type Triterpenoid Saponins from the Roots of Pulsatilla koreana

  • Li, Wei;Yan, Xi Tao;Sun, Ya Nan;Ngan, Thi Thanh;Shim, Sang Hee;Kim, Young Ho
    • Biomolecules & Therapeutics
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    • v.22 no.4
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    • pp.334-340
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    • 2014
  • In this study, 23 oleanane-type triterpenoid saponins were isolated from a methanol extract of the roots of Pulsatilla koreana. The NF-${\kappa}B$ inhibitory activity of the isolated compounds was measured in $TNF{\alpha}$-treated HepG2 cells using a luciferase reporter system. Compounds 19-23 inhibited $TNF{\alpha}$-stimulated NF-${\kappa}B$ activation in a dose-dependent manner, with $IC_{50}$ values ranging from $0.75-8.30{\mu}M$. Compounds 19 and 20 also inhibited the $TNF{\alpha}$-induced expression of iNOS and ICAM-1 mRNA. Moreover, effect of the isolated compounds on PPARs transcriptional activity was assessed. Compounds 7-11 and 19-23 activated PPARs the transcriptional activity significantly in a dose-dependent manner, with $EC_{50}$ values ranging from $0.9-10.8{\mu}M$. These results suggest the presence of potent anti-inflammatory components in P. koreana, and will facilitate the development of novel anti-inflammatory agents.

Isolation and structure elucidation of antifungal compounds from the antarctic lichens, Stereocaulon alpinum and Sphaerophorus globosus

  • Kim, Young-Shin;Lim, Chi-Hwan
    • Korean Journal of Agricultural Science
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    • v.47 no.1
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    • pp.183-191
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    • 2020
  • Lichens are composite organisms consisting of a symbiotic association of a fungus with a photosynthetic partner (the photobiont or phycobiont), usually either a green alga or cyanobacterium. According to more recent studies, the biological activities of lichens and lichen substances include an antibiotic activity, antitumor and antimutagenic activity against human immunodeficiency virus (HIV), allergenic activity, plant growth inhibitory activity, and enzyme inhibitory activity. This study screened lichen extracts with a potent in vitro antifungal activity against plant diseases caused by phytopathogenic fungi. The compounds were isolated from Stereocaulon alpinum and Sphaerophorus globosus, and their chemical structures were identified as methyl hematommate, methyl β-orsellinate, 5-hydroxyferulic acid, sphaerophorin, and 2-heptyl-4,6-dimethoxybenzoic acid by electron ionization mass spectrometry (EI-MS) and nuclear magnetic resonance (NMR) spectral analyses. In vitro disease control against Alternaria mali, Cochliobolus miyabeanus, Colletotrium gloeosporioides, and Verticillum dahliae was evaluated. And among the five compounds, only methyl hematommate was effective against A. mali, C. miyabeanus, and C. gloeosporioides. The compounds were isolated from these lichens, which have a similar biosynthetic pathway, respectively. This is the first report of these compounds being isolated from these lichens.

Chemical Constituents from the Aerial Parts of Artemisia absinthium and Its Inhibitory Effects of Nitric Oxide Production in RAW264.7 and BV2 Microglia (쓴쑥 지상부의 화학성분과 RAW264.7 및 BV2 미세아교세포에서 Nitric Oxide 생성 억제효과)

  • Ko, Hae Ju;Lee, Hwan;Lee, Dong-Sung;Woo, Eun-Rhan
    • Korean Journal of Pharmacognosy
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    • v.49 no.1
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    • pp.1-6
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    • 2018
  • Six compounds, eupatilin (1), dammaradienyl acetate (2), glutinol acetate (3), $3{\beta}-acetoxyoleanan-12-one$ (4), taraxasterol (5) and quercetin-3,4'-dimethyl ether (6) were isolated from the aerial parts of Artemisia absinthium. The chemical structures of compounds 1-6 were determined by the basis of physico-chemical properties and spectroscopic methods such as 1D and 2D NMR. Among them, compounds 2-5 were isolated from this plant for the first time. The inhibitory effects of these isolated compounds against nitric oxide (NO) production in LPS-induced RAW264.7 cells or BV2 microglia were also examined. Among the tested compounds, compound 1, eupatilin, inhibited the production of NO in LPS-induced RAW264.7 cells and BV2 microglia, respectively.

Biological Activity of Flavonoids Isolated from Aster tataricus L. (자원에서 분리한 플라보노이드의 생리활성)

  • Choi, Doo-Youn;Choi, Eun-Jin;Jin, Qing-long;Shin, Ji-Eun;Woo, Eun-Rhan
    • Korean Journal of Pharmacognosy
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    • v.40 no.2
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    • pp.123-127
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    • 2009
  • In an ongoing investigation into anti-oxidative compounds from natural products, the EtOAc soluble fraction of Aster tataricus L. (Compositae) showed significant anti-oxidative activity on the NBT superoxide scavenging assay. By means of an activity-guided purification, three flavonoids, kaempferol (1), quercetin (2), astragalin (3) and one monoterpene glycoside, shionoside A (4) were isolated. Their structures were determined spectral analyses. Compounds 2 and 3 showed potent antioxidative activity, while, compounds 1 and 4 were inactive $IC_{50}$>120${\mu}g/mL$. In addition, these compounds were examined for the effect of interleukin-6 (IL-6) production in TNF-${\alpha}$ stimulated MG-63 cell. Compounds 1-3 showed negligible inhibitory activity against IL-6 production in $TNF-{\alpha}$ stimulated $MG-6{\beta}$ cell, and compound 4 was inactive.