• Title/Summary/Keyword: Non-competitive inhibition

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Lipase Inhibitory Mode of Dieckol Isolated from Eisenia bicyclis Ethanol Extract (Eisenia bicyclis 에탄올 추출물로부터 분리한 Dieckol의 Lipase 저해 Mode)

  • Jung, Seul-A;Kim, Koth-Bong-Woo-Ri;Kim, Dong-Hyun;Cho, Ji-Young;Kim, Tae-Wan;Ahn, Dong-Hyun
    • Microbiology and Biotechnology Letters
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    • v.41 no.1
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    • pp.112-118
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    • 2013
  • This study was performed to investigate the possible use of Eisenia bicyclis (EB) ethanol extract to inhibit activity against lipase. In tests, the lipase inhibitory activity of EB ethanol extract was noted as being 43, 27, and 24% at concentrations of 5, 2.5, and 1 mg/ml, respectively. Isolation was carried out by liquid and liquid extraction, silica-gel column chromatography, and HPLC. The results showed that the lipase inhibitory activity of the ethyl acetate (EA) fraction from EB ethanol extract exhibited the strongest lipase inhibitory activity with an $IC_{50}$ value of 1.31 mg/ml. The EA fraction was separated using silica-gel column chromatography and we obtained 22 sub-fractions. Amongst them, the EA1 fraction showed the highest lipase inhibitory activity with an $IC_{50}$ value of 0.54 mg/ml. Eight peaks were obtained from the EA1 fraction by HPLC. Fraction 5 also showed a strong lipase inhibitory activity with an $IC_{50}$ value of 0.37 mg/ml. The fraction 5 was identified as dieckol and the inhibition pattern analyzed from Lineweaver-Burk plots revealed a non-competitive inhibitor. These results suggest that EB has potential as a natural anti-obesity agent.

Free Radical Scavenging Activities and Inhibitory Effect on Xanthine Oxidase by Acetone Extract from Buckwheat (수원 5호 메밀 채소 추출물의 유리라디칼 소거 및 Xanthine Oxidase 활성 저해)

  • Kim, Young-Soon;Cho, Jung-Soon;Suh, Hyung-Joo
    • Applied Biological Chemistry
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    • v.40 no.3
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    • pp.254-258
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    • 1997
  • To examine the characteristics of the antioxidative property of Buckwheat components, acetone extracts from a buckwheat, Suwon 5, was fractionated using five solvents. Hexane, ethylacetate, ether, butanol and water fractions were obtained. Butanol fraction showed the greatest electron donating ability and inhibitory effect on lipid peroxidation. It also showed the most excellent activity in the superoxide radical scavenging activity by xanthine/xanthine oxidase-cytochrome c reduction system. Spectrophotogram of butanol fraction was similar to that of rutin. Superoxide radical scavenging activity was related to the contents of rutin. Inhibitory effect of each fraction on xanthine oxidase was also measured. Butanol fraction had the strongest inhibitory effect on xanthine oxidase and $IC_{50}\;was\;3.1\;{\mu}g$. The inhibition type of butanol fraction on xanthine oxidase turned out to be a mixture of the uncompetitive and non-competitive modes.

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Effects of Ginsenoside Metabolites on GABAA Receptor-Mediated Ion Currents

  • Lee, Byung-Hwan;Choi, Sun-Hye;Shin, Tae-Joon;Hwang, Sung-Hee;Kang, Ji-Yeon;Kim, Hyeon-Joong;Kim, Byung-Ju;Nah, Seung-Yeol
    • Journal of Ginseng Research
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    • v.36 no.1
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    • pp.55-60
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    • 2012
  • In a previous report, we demonstrated that ginsenoside Rc, one of major ginsenosides from Panax ginseng, enhances ${\gamma}$-aminobutyric acid (GABA) $receptor_A$ ($GABA_A$)-mediated ion channel currents. However, little is known about the effects of ginsenoside metabolites on $GABA_A$ receptor channel activity. The present study investigated the effects of ginsenoside metabolites on human recombinant $GABA_A$ receptor (${\alpha}_1{\beta}_1{\gamma}_{2s}$) channel activity expressed in Xenopus oocytes using a two-electrode voltage clamp technique. M4, a metabolite of protopanaxatriol ginsenosides, more potently inhibited the GABA-induced inward peak current ($I_{GABA}$) than protopanaxadiol (PPD), a metabolite of PPD ginsenosides. The effect of M4 and PPD on $I_{GABA}$ was both concentration-dependent and reversible. The half-inhibitory concentration ($IC_{50}$) values of M4 and PPD were 17.1${\pm}$2.2 and 23.1${\pm}$8.6 ${\mu}M$, respectively. The inhibition of $I_{GABA}$ by M4 and PPD was voltage-independent and non-competitive. This study implies that the regulation of $GABA_A$ receptor channel activity by ginsenoside metabolites differs from that of ginsenosides.

Photoprotection and Anti-inflammatory Effects of Chinese Medical Plants (약용식물추출물의 광보호 효과와 항염증 효과 연구)

  • Jin-Hwa, Kim;Sung-Min, Park;Gwan-Sub, Sim;Bum-Chun , Lee;Hyeong-Bae, Pyo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.2
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    • pp.227-233
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    • 2004
  • Chronic exposure to solar radiation, particularly ultraviolet (UV) light, causes a variety of adverse reactions on human skin, such as sunburn, photoaging and photocarcinogenesis. Free radicals and reactive oxygen species (ROS) caused by UV exposure or other environmental facts play critical roles in cellular damage. And, repeated-UV irradiation activated the expression of the matrix metalloproteinase (MMP) and induced skin irritation. Therefore, the development of effective and safe photoprotectants that can reduce and improve the skin damage has been required. The purpose of this study was to investigate the photo-protective effect of several chinese medical plants (Juniperus chinensis) on the UV -induced skin cell damages. We tested free radical and superoxide scavenging effect in vitro. Fluorometric assays of the proteolytic activities of MMP-1 (collagenase) were performed using fluorescent collagen substrates. UVA induced MMP-1 synthesis and activity were analyzed by enzyme-linked immunosorbent assay (ELISA) and gelatin-based zymography in skin fibroblasts. We also examined anti-inflammatory effects by the determination test of proinflammatory cytokine, interleukin 6 in HaCaT keratinocytes. Expression of prostaglandin E$_2$ (PGE$_2$) after UVB irradiation was measured by competitive enzyme immunoassay(EIA) using PGE$_2$ monoclonal antibody. In the human skin we tested anti-irritation effect on the SLS-induced damage skin after appling the extract containing emulsion. We found that Juniperus chinensis extract had potent radical scavenging effect by 98% at 100$\mu\textrm{g}$/mL. The extract of Juniperus chinensis showed strong inhibitory effect on MMP-1 activities by 97% at 100 $\mu\textrm{g}$/mL and suppressed the UVA induced expression of MMP-1 by 79% at 25$\mu\textrm{g}$/mL. This extract also showed strong inhibition on MMP-2 activity in UVA irradiated fibroblast by zymography. In the test of proinflammatory cytokines of human keratinocytes Juniperus chinensis extract decreased expression of interleukin 6 about 30%. The amount of PGE$_2$ by HaCaT keratinocytes was significantly increased at the doses of above 10 mJ/$\textrm{cm}^2$ of UVB (p < 0.05). At the concentrations of 3.2-25$\mu\textrm{g}$/mL of this extract, the production of PGE$_2$ by HaCaT keratinocytes (24 h after 10mJ/$\textrm{cm}^2$ UVB irradiation) was significantly inhibited in culture supernatants (p < 0.05). In SLS-induced skin irritation model in vivo, we found to reduce skin erythema and improve barrier recovery after appling Juniperus chinensis extract containing emulsion when compared to irritated non-treated and placebo-treated skin. Our results suggest that Juniperus chinensis extract can be effectively used for the prevention of UV and SLS-induced adverse skin reactions and applied as anti-aging and anti-irritation cosmetics.