• 제목/요약/키워드: inhibitory compound

검색결과 1,015건 처리시간 0.034초

두충(Eucommia ulmoides Oliv.)잎으로부터 Monoamine Oxidase B 억제활성물질의 분리 (Isolation of Monoamine Oxidase B Inhibitory Compound from the Leaves of Eucommia ulmoides Oliv.)

  • 안은미;한재택;이동욱;손형옥;권병목;백남인
    • Applied Biological Chemistry
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    • 제42권2호
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    • pp.166-169
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    • 1999
  • 두충잎으로부터 얻은 MeOH 추출물의 n-BuOH 분획으로부터 silica gel column chromatography를 반복하여 monoamine oxidase B (MAO-B) 억제 활성을 갖는 flavonoid 배당체를 분리하였다. 화합물의 화학구조를 스펙트럼 데이터의 해석과 산가수분해반응을 이용하여 $3-O-[{\beta}-D-glucopyranosyl\;(1{\rightarrow}2)\;{\beta}-D-xylopyranosyl]\;quercetin$으로 결정하였다. 이 화합물의 MAO-B 억제활성에 있어서의 $IC_{50}$ 값은 $8.05\;{\mu}mol/l$로 측정되었다.

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cAMP 신호전달과정을 통한 신규 천연유래물질 펩타이드 유도체의 미백 효능 연구 (Whitening Efficacy Study of Natural Compounds-Peptide Derivatives via cAMP Signaling Pathway)

  • 이혜숙;신경훈;류근석;지경엽;조인식;김한영
    • 대한화장품학회지
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    • 제37권3호
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    • pp.275-282
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    • 2011
  • MC1R의 길항제 역할을 하는 펩타이드와 tyrosinase를 저해하는 효능을 가지는 천연유래 물질을 유도체화하여 신규 미백소재를 개발하였다. 또한 이러한 새로운 기작에 의한 미백 효능을 평가할 수 있는 방법을 cAMP 신호전달 과정을 활용하여 제시하였다. 총 24종의 유도체를 합성하였고, cAMP assay의 결과를 통해 11종의 유도체를 선별하였으며, 선별된 유도체에 대하여 멜라닌 형성 억제 효능을 평가하여 본 평가 방법의 유효성을 확인하였다. 이 과정에서 RW를 서열에 포함하는 펩타이드 유도체가 특별히 멜라닌 형성 억제 효능이 높은 것을 알 수 있었다. 또한, cAMP assay는 MC1R의 antagonist라는 특정 타겟 물질을 디자인한 소재의 스크리닝 방법에는 활용할 수 있음을 알 수 있었다. 하지만, 미백소재로서의 가능성을 확인하기 위해서는 멜라닌 생성저해 시험과 병행하여야 할 것으로 판단된다.

황산카드뮴독성의 산화적 손상에 대한 부들 추출물의 항산화 효과 (Antioxidative Effect of Typha orientalis L. Extract on the Oxidative Stress Induced by Cytotoxicity of Cadmium Sulfate)

  • 윤기철;손영우
    • 한국환경보건학회지
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    • 제45권1호
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    • pp.62-70
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    • 2019
  • Objectives: This study was carried out to analyze the cytotoxicity of cadmium sulfate ($CdSO_4$) and the antioxidative effect of Typha orientalis L. (TO) extract on the oxidative stress induced by cytotoxicity of $CdSO_4$ in the cultured NIH3T3 fibroblasts. Methods: For this study, the cell viability and the antioxidative effects such as the inhibitory activity of lipid peroxidation (LP) and superoxide dismutase (SOD)-like activity and xanthine oxidase (XO)-inhibitory activity were assessed. Results: The cadmium sulfate significantly decreased cell viability in dose-dependently, and $XTT_{50}$ value was measured at $47.4{\mu}M$ of $CdSO_4$. The cytotoxicity of $CdSO_4$ was determined as highly toxic by Borenfreund and Puerner's toxic criteria. The butylated hydroxytoluene (BHT) as antioxidant significantly increased cell viability injured by $CdSO_4$-induced cytotoxicity in these cultures. In the protective effect of TO extract on $CdSO_4$-induced cytotoxicity, TO extract remarkably increased the inhibitory ability of LP and XO as well as SOD-like ability. Conclusions: From the above results, it is suggested that the oxidative stress is involved in the cytotoxicity of $CdSO_4$, and TO extract effectively protected $CdSO_4$-induced cytotoxicity by antioxidative effects. The natural component like TO extract may be a putative therapeutic agent for treatment of the toxicity induced by heavy metallic compound like $CdSO_4$ correlated with the oxidative stress.

세균으로부터 항진균성 물질의 생산 및 특성 (Production and Chracteristics oil Antifungal agents from Bacteria)

  • 김현수;육영민;여수환
    • KSBB Journal
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    • 제18권6호
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    • pp.490-494
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    • 2003
  • 토양으로부터 분리한 균주 중 항진균 활성이 우수한 균주를 선발하여 B-1이라 명명하였다. B-1의 항균성 물질 생산에 대한 배양조건을 검토하기 위해 최적배지, 탄소원, 질소원, pH, 온도별로의 영향을 조사하였다. PDB 배지에서 항균력이 우수하였으며 탄소원$.$질소원에는 별다른 영향이 없었다. pH와 온도에서는 각각 pH 5.0, 28$^{\circ}C$에서 항균력이 우수하였다. 항균 활성은 진균에서 강하게 나타났으며 일부 세균에서도 항균력을 나타내었다. 항진균성 물질은 산, 알칼리 처리 후 잔존 활성은 70∼80%로 나타났으며 열처리시 완전히 실활되어 열에 대해 상당히 불안정하다는 것을 확인하였다. 항균성 물질위 용매 전용성을 위해 TLC를 통하여 분석하였으며 plate assy를 실시하여 항균성물질을 확인하였다. 항진균성 물질의 대량생산을 위해 기본배지인 PDB를 직접 실험실 내에서 제조하였으며 시판의 PDB와 비교하였을때 항균성 물질 생산면에서나 가격면에서 더 나은 결과를 보였다.

Compound K, a Metabolite of Ginsenoside Rb1, Inhibits Passive Cutaneous Anaphylaxis Reaction in Mice

  • Bae, Eun-Ah;Trinh, Hien Trung;Yoon, Hae-Kyung;Kim, Dong-Hyun
    • Journal of Ginseng Research
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    • 제33권2호
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    • pp.93-98
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    • 2009
  • To understand the anti-allergic mechanism of compound K, which is a metabolite of ginsenoside Rb1, a main constituent of the root of Panax ginseng C.A. Meyer (family Araliaceae), its inhibitory effect against IgE-antigen complex IAC)-induced passive cutaneous anaphylaxis (PCA) reaction in mice and mRNA and protein expressions of allergic cytokines in lAC-stimulated RBL-2H3 cells were investigated. Orally administered ginsenoside Rb1 more potently inhibited PCA reaction when administered at 5 h prior to the lAC treatment than when administered at I h before. However, compound K orally administered 1 h before lAC treatment showed a more potent anti-PCA reaction effect than when treated at 5 h before. Orally administered ginsenoside Rb1 more potently inhibited PCA reaction induced by lAC in mice than intraperitoneally treated one, apart from orally administered its metabolite, compound K, which was more potent than the orally administered one. The compound K, a metabolite of ginsenoside Rb1, inhibited mRNA and protein expressions of IL-4 and TNF-${\alpha}$ and the activation of their transcription factor NF-$\kappa$B and MAPK in lAC-stimulated RBL-2H3 cells. These findings suggest that orally administered ginsenoside Rb1 may be dependent on its metabolism by intestinal microflora in the intestine and the compound K may improve allergic diseases by the inhibition of IL-4 and TNF-${\alpha}$ expresseion.

Inhibitory Effect of Doenjang(fermented Korean soy paste) Extracts and Linoleic Acid on the Growth of Human Cancer Cell Lines

  • Park, Kun-Young;Lee, Jeong-Min;Moon, Suk-Hee;Jung, Keun-Ok
    • Preventive Nutrition and Food Science
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    • 제5권2호
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    • pp.114-118
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    • 2000
  • The inhibitory effects of doenjang extracts and linoleic acid(LA) which was identified as one of the active compounds in doenjang on the growth of human cancer cells were studied, comparing to the actions on normal cells. Methanol extract and hexane fraction from doenjang exhibited the strong growth inhibitory effect on HT-29 human colon carcinoma cells. Inhibitory effects of chloroform, ethyl acetate, butanol and aqueous fractions on the cancer cells were observed, moderately or weakly. When cell counts of SNU-C$_1$human colon carcinoma cells were determined daily for 6 days, the inhibitory effect of hexane fraction on this cell line was higher than that of the methanol extract from doenjang. LA completely suppressed the growth of SNU-C$_1$cells after 4 days, while conjugated linoleic acid(CLA) resulted in 98% inhibition after 6 days. With the addition of LA and other free fatty acids such as stearic acid, oleic acid, linolenic acid and ${\gamma}$-linolenic acid (${\gamma}$-LnA) to the culture system, the growth of HT-29 cells and SNU-C$_1$cells was greatly suppressed after 6 days. Inhibitory effects of LA ${\gamma}$-LnA on the growth of these cells were stronger than other fatty acids. On the growth of AZ-521 human gastric carcinoma cells, LA and CLA completely cuppressed the growth of the cells after 4 days and 3 days, respectively. At the level of 0.001%~0.01% of LA, there was no cytotoxic effect on normal rat kidney cells and normal intestine human cells. These results showed that LA, a major active compound of doenjang, had strong inhibitory effects on the growth of human cancer cells without damaging normal cells.

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목질진흙버섯(Phellinus linteus) 균사체 추출물 제제 PLM-WE1의 식물 바이러스에 대한 감염억제 효과 및 활성성분의 동정 (Inhibitory Effects of PLM-WE1 Formulated from Extract of Phellinus linteus Mycelium against Plant Viruses Infection and Identification of Active Compound)

  • 권순배;배선화;최장경;이상용;김병섭;권용수
    • 식물병연구
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    • 제16권3호
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    • pp.259-265
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    • 2010
  • 목질진흙버섯(Phellinus linteus)을 액체 배양한 균사체의 열수 추출물을 이용하여 PMMoV 및 CMV에 대한 감염억제효과를 검정한 결과, PMMoV 및 CMV에 높은 감염억제효과가 발견되었다. 이 결과를 토대로, P. linteus 균사체의 열수추출물을 주성분으로 제제화한 PLM-WE1의 효능 평가를 위하여, PMMoV 및 CMV의 국부감염 기주식물에서 PLM-WE1의 바이러스 접종전 처리효과, 엽이면 처리시의 감염억제효과 및 PLM-WE1의 지속효과 실험을 수행하였다. 그 결과, PLM-WE1(처리농도 10 mg/ml)의 바이러스 접종전 처리시의 감염억제율은 PMMoV 99.2%와 CMV 80.3%이었으며, 본 제제(농도 5 mg/ml)의 엽이면 처리시의 감염억제율은 PMMoV 45.0%와 CMV 41.9%, 약효지속성은 처리 3일 후까지 PMMoV 75%와 CMV 62% 수준으로 감염억제 효과를 보였다. 바이러스 전신감염기 주식물을 이용한 감염억제효과는 PMMoV 75~85%와 CMV 75%이었다. PLM-WE1제제의 바이러스 감염억제 기작을 해석하기 위하여, 정제한 PMMoV에 제제를 혼합하여 전자현미경으로 관찰한 결과, 바이러스 입자의 형태적 변화는 관찰되지 않아, PLM-WE1의 바이러스 감염억제기작은 바이러스입자의 응집(aggregation) 작용과는 다른 기작에 의한 것임이 추정되었다. 목질진흙버섯 균사체로부터 식물바이러스 감염억제 성분의 분리 및 동정을 위하여 유기용매분획, 산 가수분해 및 에탄올 분별침전을 실시하여 고활성 분획을 수득하였다. 이 분획물을 $^1H$-NMR 및 $^{13}C$-NMR을 이용하여 분석한 결과, $\alpha$- 또는 $\beta$-glucan이 결합된 다당류(polysaccharide)로 확인되었다.

장양(藏釀) 기술이 사용된 전통 고숙성 된장에서 유래한 o-Dihydroxyisoflavone 유도체의 생리활성 (o-Dihydroxyisoflavone Derivatives from Highly Aged Korean Fermented Soybean Paste by Jang Yang Process and Its Biological Activity)

  • 김동현;박준성;박녹현;문은정;유선혜;김덕희;김한곤
    • 대한화장품학회지
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    • 제35권3호
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    • pp.203-208
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    • 2009
  • 된장은 한국의 독특한 발효 식품이며 장양이라 불리는 전통적인 제조 방법에 의해 제조된다. 이에 본 연구에서는 고숙성 된장에서 새롭게 생성된 성분과 그것의 생리활성을 측정하였다. 5년 숙성된 된장으로부터 새로운 o-dihydroxyisoflavone인 7,3',4'-trihydroxyisoflavone과 기존에 알려진 두 가지의 o-dihydroxyisoflavone을 각각 분리하여 다른 isoflavone과의 항산화 효과 및 미백효과를 비교 측정하였다. Diphenyl-1-picrylhydrazyl (DPPH) 활성 저해 효과는 7,8,4'-trihydroxyisoflavone (compound 1), 7,3',4'-trihydroxyisoflavone (compound 2) 그리고 6,7,4'-trihydroxyisoflavone (compopund 3)은 각각 $21.5{\pm}0.2$, $28.7{\pm}0.4$ 그리고 $32.6{\pm}0.6$ ($IC_{50}$)을 나타낸 반면 daidzein은 이들에 비해 약한 DPPH 활성 저해 효과를 나타냈다. Superoxide 소거 효과는 L-ascorbic acid에 비해 compound 1 ($IC_{50}=18.10{\pm}0.2{\mu}M$)과 2 ($IC_{50}=10.54{\pm}0.4{\mu}M$)가 보다 효과적인 반면 compound 3과 daidzein은 이들에 비해 낮은 활성을 나타냈다. 또한 melan-a cells에서 o-dihydroxyisoflavone 유도체들의 티로시나제 활성과 멜라닌 생성을 비교 측정하였다. 특히 Compound 1 ($IC_{50}=11.21{\pm}0.2{\mu}M$), 2 ($IC_{50}=5.23{\pm}0.6{\mu}M$)의 경우 compound 3과 daidzein에 비해 티로시나제 활성을 억제하는데 효과가 있었으며 또한 멜라닌 생성을 50 % 억제할 때의 결과에서 이들 화합물은 각각 $12.23{\pm}0.7{\mu}M$ (1), $7.83{\pm}0.7{\mu}M$ (2)과 같이 멜라닌 생성 억제 효능을 나타내었다. 따라서 고숙성 된장에서 유래한 7,3',4'-trihydroxyisoflavone은 항산화 및 미백효과를 가지는 화장품 소재로써 사용 가능하리라 판단된다.

Inhibitory Effects of 12 Ginsenosides on the Activities of Seven Cytochromes P450 in Human Liver Microsomes

  • Jo, Jung Jae;Shrestha, Riya;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • 제7권4호
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    • pp.106-110
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    • 2016
  • Ginseng, a traditional herbal drug, has been used in Eastern Asia for more than 2000 years. Various ginsenosides, which are the major bioactive components of ginseng products, have been shown to exert numerous beneficial effects on the human body when co-administered with drugs. However, this may give rise to ginsenoside-drug interactions, which is an important research consideration. In this study, acassette assay was performed the inhibitory effects of 12 ginsenosides on seven cytochrome P450 (CYP) isoforms in human liver microsomes (HLMs) using LC-MS/MS to predict the herb-drug interaction. After incubation of the 12 ginsenosides with seven cocktail CYP probes, the generated specific metabolites were quantified by LC-MS/MS to determine their activities. Ginsenoside Rb1 and F2 showed strong selective inhibitory effect on CYP2C9-catalyzed diclofenac 4'-hydroxylation and CYP2B6-catalyzed bupropion hydroxylation, respectively. Ginsenosides Rd showed weak inhibitory effect on the activities of CYP2B6, 2C9, 2C19, 2D6, 3A4, and compound K, while ginsenoside Rg3 showed weak inhibitory effects on CYP2B6. Other ginsenosides, Rc, Rf, Rg1, Rh1, Rf, and Re did not show significant inhibitory effects on the activities of the seven CYPs in HLM. Owing to the poor absorption of ginsenosides after oral administration in vivo, ginsenosides may not have significant side effects caused by interaction with other drugs.

Anti-oxidization Effect of Extracts from Oriental Medicine and Cereal Medium Where Tricholoma matsutake Mycelia were Cultured

  • Kim, Hae-Ja;Lee, Ki-Nam
    • 동의생리병리학회지
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    • 제22권3호
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    • pp.672-677
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    • 2008
  • In order to explore the anti-oxidization effect of oriental medicine and cereal medium(OCM) where Tricholoma matsutake mycelia were cultured, measurement of hot water extract and UMPM(extraction method using ultra sonic waves, micro waves, micro bubble) extract, the total polyphenol content of crude polysaccharide from each extract, SOD-like activity, electron donating ability(EDA), xanthine oxidase inhibitory activity, and tyrosinase inhibitory activity was conducted. The total polyphenol content of each extract was found to be 16.36% for hot water extract(HE) group and 15.73% for UMPM extract(UE) group and the amount of crude polysaccharide precipitated into ethanol of extracts was found to be 8.79% for UMPM ethanol extract(UEE) group and 6.48% for hot water ethanol extract(HEE) group. As a result of measurement of SOD-like activity by concentration of each extract, it was found to be 96.17% for UE group, 91.23% for HE group, 91.33% for UEE group, and 87.11% for HEE group at 20 mg/mL. In the case of EDA, it was found to be 47.55% for UE group, 44.93% for HE group, 25.38% for UEE group, and 18.36% for HEE group. And in the cases of the rates of xanthine oxidase inhibitory activity and tyrosinase inhibitory activity, as the concentration of each extract increased, the inhibition rate increased accordingly. As a result of comparison between hot water extract method and UMPM extract method using extracts obtained from oriental medicine compound medium where Tricholoma matsutake mycelia were cultured, all of the extracts were judged to have a high anti-oxidization effect. In particular, UMPM extracts were found to have higher polyphenol content, SOD-like activity, EDA, xanthine oxidase inhibitory activity and tyrosinase inhibitory activity compared to hot water extract method. In this regard, extracts obtained from OCM where Tricholoma matsutake mycelia were cultured are considered to have high availability as functional material when and if they are prepared using UMPM extract method.