• 제목/요약/키워드: enzyme inhibitory activity

검색결과 1,012건 처리시간 0.027초

Sulfatase 1 mediates the inhibitory effect of angiotensin II type 2 receptor inhibitor on angiotensin II-induced hypertensive mediator expression and proliferation in vascular smooth muscle cells from spontaneously hypertensive rats

  • Kim, Hye Young;Cha, Hye Ju;Kim, Hee Sun
    • Journal of Yeungnam Medical Science
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    • 제34권1호
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    • pp.43-54
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    • 2017
  • Background: Extracellular sulfatases (Sulfs), sulfatase 1 (Sulf1) and sulfatase 2 (Sulf2), play a pivotal role in cell signaling by remodeling the 6-O-sulfation of heparan sulfate proteoglycans on the cell surface. The present study examined the effects of Sulfs on angiotensin II (Ang II)-induced hypertensive mediator expression and vascular smooth muscle cells (VSMCs) proliferation in spontaneously hypertensive rats (SHR). Methods: Ang II receptors, 12-lipoxygenase (12-LO), and endothelin-1 (ET-1) messenger RNA (mRNA) expressions in SHR VSMCs were analyzed by real-time polymerase chain reaction and Western blotting. VSMCs proliferation was determined by [$^3H$]-thymidine incorporation. Results: Basal Sulfs mRNAs expression and enzyme activity were elevated in SHR VSMCs. However, Sulfs had no effect on the basal or Ang II-induced 12-LO and ET-1 mRNA expression in SHR VSMCs. The inhibition of Ang II-induced 12-LO and ET-1 expression by blockade of the Ang II type 2 receptor ($AT_2\;R$) pathway was not observed in Sulf1 siRNA-transfected SHR VSMCs. However, Sulf2 did not affect the action of $AT_2\;R$ inhibitor on Ang II-induced 12-LO and ET-1 expression in SHR VSMCs. The down-regulation of Sulf1 induced a reduction of $AT_2\;R$ mRNA expression in SHR VSMCs. In addition, the inhibition of Ang II-induced VSMCs proliferation by blockade of the $AT_2\;R$ pathway was mediated by Sulf1 in SHR VSMCs. Conclusion: These findings suggest that extracellular sulfatase Sulf1 plays a modulatory role in the $AT_2\;R$ pathway that leads to an Ang II-induced hypertensive effects in SHR VSMCs.

어성초(魚腥草) 추출물의 항여드름 효과에 관한 연구 (The Effects of Houttuyniae Herba extract on the Activity of Anti-bacteria, Anti-inflammation and Anti-oxidation)

  • 전오도;서형식
    • 대한약침학회지
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    • 제11권1호
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    • pp.119-125
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    • 2008
  • Objective : This experimental study was performed to investigate the effects of Houttuyniae Herba extract on anti-inflammation and anti-oxidation. Methods : The cytotoxicity of Houttuyniae Herba water extract and ethanol extract about viability of Raw 264.7 cell were tested using a colormetric tetrazolium assay(MTT assay). We investigated the inhibitory effects of Houttuyniae Herba water extract and ethanol extract on Propionibactrium acnes using paper disk diffusion method. To investigate the anti-inflammation effects of Houttuyniae Herba water extract and ethanol extract on LPS-induced macrophage Raw 264.7 cell, we used ELISA kit. We evaluated anti-oxidation effects of Houttuyniae Herba water extract and ethanol extract on HaCaT cell by Enzyme recycling method. Results : 1. In Houttuyniae Herba water extract and ethanol extract, cell toxicity depended on the density and wasn't difference between two extracts. 2. Houttuyniae Herba water extract and ethanol extract has not the significant inhibition effect of Propionibactrium acnes. 3. Concentration of 50, $100{\mu}g/m{\ell}$ Houttuyniae Herba water extract inhibited the production of NO in the Raw 264.7 cell stimulated with LPS. 4. All extracts except for $20{\mu}g/m{\ell}$ Houttuyniae Herba water extract showed anti-oxidation effect by decreasing the DPPH radicals. Conclusion : These results indicate that Houttuyniae Herba extract has anti-inflammation and anti-oxidation effects. If further study is performed, the use of Houttuyniae Herba extract will be valuable and benificial in the therapy of Propionibactrium acnes.

알코올 발효성 야생 효모, Aureobasidium pullulans P-1의 균학적 특성과 막걸리 발효 특성 (Microbiological Characteristics of Alcoholfermenting Wild Yeast, Aureobasidium pullulans P-1 and Its Makgeolli Fermentation Characteristics)

  • 홍용철;한상민;이종수
    • 한국균학회지
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    • 제46권3호
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    • pp.307-314
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    • 2018
  • 본 연구는 알코올 발효능이 우수한 야생 효모를 막걸리 발효에 응용할 목적으로 충남 예산군 예당저수지 야생화에서 분리한 비병원성 야생 효모들 중 에탄올 생산 우수 효모로 선발한 Aureobasidium pullulans P-1의 균학적 특성과 막걸리 발효 조건을 조사하였다. A. pullulans P-1는 출아에 의해 영양증식을 하였고 자낭포자를 생성하는 유포자 효모로서 내당성과 에탄올 내성이 강한 호염성 야생 효모이었다. A. pullulans P-1의 yeast extract-peptone-dextrose 배양액을 주모로 증자미와 입국과 물이 혼합된 술밑에 5% 첨가한 후 $25^{\circ}C$에서 1~10일간 발효시키면서 발효 중의 이화학적 성질의 변화를 조사한 결과, 에탄올 함량은 $25^{\circ}C$로 10일간 발효시켰을 때 가장 많은 8.45%를 생성하였고 관능 특성이 우수하였으며 항고혈압 활성 안지오텐신 전환효소 저해활성이 71.1%로 높았다.

Anti-diabetic Effects of CCCA, CMESS, and Cordycepin from Cordyceps militaris and the Immune Responses in Streptozotocin-induced Diabetic Mice

  • Yun, Yun-Ha;Han, Shin-Ha;Lee, Seung-Jeong;Ko, Sung-Kwon;Lee, Chong-Kil;Ha, Nam-Joo;Kim, Kyung-Jae
    • Natural Product Sciences
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    • 제9권4호
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    • pp.291-298
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    • 2003
  • Anti-diabetic effect of various fractions of Cordyceps militaris (CM), CCCA (crude cordycepin containing adenosine), CMESS (ethanol soluble supernatant), and cordycepin were evaluated in streptozotocin (STZ) induced diabetic mice, CMESS showed potent inhibitory activity of 34.7% in starch-loaded mice (2 g/kg) while acarbose as a positive standard exhibited 37.8% of inhibition rate. After 3 days administration (50 mg/kg), cordycepin (0.2 mg/kg), and acarbose (10 mg/kg) dramatically reduced blood glucose level (inhibition ratio: 46.9%, 48.4% and 37.5% respectively). CCCA that has high contents of cordycepin (0.656 mg/4 mg) did not influence on reducing blood glucose level. The proliferation of splenocytes and peritoneal macrophages derived from STZ-induced diabetic mice administered samples were evaluated out by addition of mitogens to see the stability of the usage of these herbal medicines. Proliferation of T-lymphocyte was significantly decreased; while NO production was increased more than two fold to STZ control in the cordycepin-administered group. Changes of serum enzyme levels of glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) were also evaluated. Cordycepin administered group was appeared to acarbose. We conclude that CMESS and cordycepin may be useful tools in the control of blood glucose level in diabetes and promising new drug as an anti-hyperglycemic agent without defects of immune responses and other side effects.

3-페닐-1-이소퀴놀린아민이 신경세포에서 베타 아밀로이드 전구단백질의 대사에 미치는 영향 (Effects of 3-Phenyl-1-isoquinolinamine on the Metabolism of ${\beta}$-Amyloid Precursor Protein in Neuroblastoma Cells)

  • 임재윤;조원제
    • 약학회지
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    • 제54권6호
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    • pp.529-534
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    • 2010
  • Alzheimer's disease (AD) is characterized pathologically by the presence of intracellular neurofibrillary tangles and deposition of ${\beta}$-amyloid ($A{\beta}$) peptides, which are generated by processing of amyloid precursor protein (APP). It is urgent to develop effective therapies for the treatment of AD, since our society rapidly accelerate aging. $A{\beta}$ peptides have been believed to be neurotoxic and now are also considered to have effects on the mechanism of memory formation. Recently, we investigated that a quinoline compound from natural product reduced the secretion of $A{\beta}$ from the neuroblastoma N2a cells (NL/N cell line) overexpressing APPswe. In this study, 3-phenyl-1-isoquinolinamine, a synthetic isoquinoline compound was analyzed to determine its effects on the metabolism of APP. It inhibited the secretion of $A{\beta}$ peptides from the N2a NL/N cell line. Beta-site APP cleaving enzyme (BACE) fluorescence resonance energy transfer (FRET) assay revealed that it inhibited BACE activity in a dose dependent manner. Immunoblotting study showed that it inhibited APP stabilization and expression and it slightly increased the stablization and the expression of ${\gamma}$-secreatase component from the N2a NL/N cell line. We suggest that 3-phenyl-1-isoquinolinamine inhibits APP metabolism and $A{\beta}$ generation by the means of BACE inhibitory mechanism. This is the first report that 3-phenyl-1-isoquinolinamine inhibits the secretion of $A{\beta}$ peptides from neuroblastoma cells.

골담초 효모 발효 추출물의 피부 미백 효능에 관한 연구 (Skin Whitening Effects of Caragana sinica Rehder Extract Fermented by Saccharomyces cerevisiae KCTC 7913)

  • 석지현;이선영;채은정;최신욱
    • 대한화장품학회지
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    • 제36권3호
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    • pp.207-213
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    • 2010
  • 본 연구는 미생물에 의한 골담초(Caragana sinica Rehder) 발효 추출물의 항산화 효과 및 피부 미백 효능에 관한 연구로 골담초에 S. cerevisiae KCTC 7913를 첨가하여 발효를 통해 얻어진 발효 추출물을 B16F10 멜라닌 세포에 처리한 결과, 농도의존적으로 멜라닌 생성 억제 효능이 증가한 것으로 확인하였으며, 추출물 내 유효 성분인 resveratrol의 함량이 발효 전의 추출물에 비해 증가함을 확인하였다. 멜라닌 생성 과정의 주요 단백질인 tyrosinase의 활성 억제 또한 골담초 추출물에 비해 골담초 발효 추출물의 효능이 우수함을 확인하였으며, 골담초 발효 추출물의 피부 자극 또한 일어나지 않는 것으로 확인되어 피부에 안전한 화장품 원료로서의 사용이 가능할 것으로 사료된다.

국내 사육 닭에서 분리된 Ornithobacterium rhinotracheale (OR)균의 약제 감수성 및 항체보유율에 대한 연구 (A Study on Antibacterial Activity and Seroprevalence of Ornithobacterium rhinotracheale Isolated from the Domestic Chickens)

  • 전우진;권용국;윤여성;김재홍
    • 미생물학회지
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    • 제39권3호
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    • pp.161-165
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    • 2003
  • Ornithobacterium rhinotracheale(OR)은 최근에 알려진 그람음성 간균으로서 가금류에서 호흡기감염을 일으킨다. OR균의 항생제 감수성과 OR에 대한 국내발생현황을 조사하기 위하여 11개 OR분리주의 8중 항생제에 대한 최소발육억제농도(MIC)와 국내 달의 OR 항체보유율을 조사하였다. 모든 분리주는 ampicillin, tetracycline 및 doxycycline에 대하여 높은 감수성을 나타내었다. MIC는 각각 0.38~2 ${\mu}g$ /ml, 0.094~3 ${\mu}g$/ml, 0.094~3 ${\mu}g$/ml으로 ciprofloxacin, norfloxacin, enrofloxacin및 ofloxacin의 MIC는 대부분 3 ${\mu}g$/ml~48 ${\mu}g$/ml로 나타났고 gentamicin에 대하여는 모든 분리주가 저항성을 나타내었다. 시판되는 OR ELISA검사 kit를 사용하여, 국내에서 사육하는 육계 및 육용종계와 산란계 188계군에 대한 항체보유율을 검사한 결과, 육계 5계군(4%),육용종계 17계군(50%),산란계 16계군(55.2%)이 OR항체 양성계군으로 나타났다. 이 결과로 보아 OR은 국내 양계장내 광범위하게 만연되어 있을 것으로 보인다.

양파로부터 분리한 생리활성분획이 생리활성 및 지질대사에 미치는 영향 (Effect of Biologically Active Fractions from Onion on Physiological Activity and Lipid Metabolism)

  • 우희섭;안봉전;배종호;김성;최희진;한호석;최청
    • 한국식품영양과학회지
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    • 제32권1호
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    • pp.119-123
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    • 2003
  • 양파를 80% ethanol로 추출하여 Sephadek LH-20 column chromatography로 fraction I, II 및 III의 생리활성물질을 분리하여 angiotensin converting enzyme(ACE), xanthine oxidase, tyrosinase의 저해작용 효과와 지질대사를 검토하였다 Fraction I과 II의 ACE 저해작용은 50 ppm 농도에서 80% 이상의 효소 저해효과를 나타내었고 fraction III에서는 500 ppm 농도에서 90% 효소저해작용을 보였다. 100 ppm 농도에서 fraction III의 xantine oxidase 효소저해 효과는 82.5%로 나타났으며 tyrosinase의 저해효과는 42.6%이었다. 효소저해작용이 가장 강한 fraction III를 2개월 동안 고지방식이에 첨가하여 혈장 및 간장에서 지질대사에 미치는 영향을 분석한 결과 혈장에서는 총지질, 중성지질이 대조군에 비하여 유의성 있게 감소하였다. 간의 콜레스테롤량도 약 50% 정도 감소하는 결과를 얻었다.

인체의 자궁암과 간암조직에서의 단백질 분해활성의 변화 (Correlation Between Malignant Phenotypes and Changes in Overall Proteolytic Capacity of Human Cervix and Liver Cancer)

  • 기윤;박상철;하두봉;정진하
    • 한국동물학회지
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    • 제32권1호
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    • pp.48-54
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    • 1989
  • 인체의 자궁암과 간암조직들이 나타내는 몇 종류의 단백질 분해효소들과 Anti-trypsin의 활성도를 정상조직의 것들과 비교하여서, 암의 종양성 형질과 단백질 분해활성의 변화사이에 어떤 상관관계가 있는지를 조사하였다. Casein과 Insulin의 분해 활성도는, 자궁암에서 2-3배 정도 증가하는 반면, 간암에서는 1/2에서 1/5정도로 감소하였다. 이와는 대조적으로, Anti-trypsin의 활성도는 자궁암에서 약 1/10정도로 감소하였고 간암에서는 2배 가량 증가하였다. 한편, Plamin-like enzyme과 Plasminogen activator의 활성도는 자궁암과 간암조직 모두에서 정상 조직에서보다 10-20% 정도 높게 나타났다. 이러한 결과는, 정상조직 내의 단백질 분해활성도가 단백질 분해효소들과 이들의 활성을 저해하는 단백질들의 균형에 의하여 조절됨을 시사하며, 암조직들에서는 각 암조직들의 종양특이성에 따라 단백질 분해효소와 저해단백질들 사이의 균형이 깨어짐에 따라 단백질 분해활성도가 다르게 나타남을 보여준다.

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Sesaminol Glucosides의 기억력 회복능 및 ${\beta}$, ${\gamma}$-Secretase (Protective Effect of Sesaminol Glucosides on Memory Impairment and ${\beta}$, ${\gamma}$-Secretase Activity In Vivo)

  • 이선영;손동주;하태열;홍진태
    • 약학회지
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    • 제49권2호
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    • pp.168-173
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    • 2005
  • Alzheimers disease (AD) is the most prevalent form of neurodegenerations associated with aging in the human population. This disease is characterized by the extracellular deposition of beta-amyloid (A ${\beta}$) peptide in cerebral plaques. The A ${\beta}$ peptide is derived from the ${\beta}$-amyloid precursor protein ( ${\beta}$APP). Photolytic processing of ${\beta}$APP by ${\beta}$-secretase(beta-site APP-cleaving enzyme, BASE) and ${\gamma}$-secretase generates the A ${\beta}$ peptide. Several lines of evidence support that A ${\beta}$-induced neuronal cell death is major mechanisms of development of AD. Accordingly, the ${\beta}$-and ${\gamma}$-secretase have been implicated to be excellent targets for the treatment of AD. We previously found that sesaminol glucosides have improving effect on memory functions through anti-oxidative mechanism. In this study, to elucidate possible other mechanism (inhibition of ${\beta}$-and ${\gamma}$-secretase) of sesaminol glucosides, we examined the improving effect of sesaminol glucosides in the scopolamine (1 mg/kg/mouse)-induced memory dysfunction using water maze test in the mice. Sesaminol glucosides (3.75, 7.5 mg/kg/6ml/day p.o., for 3 weeks) reversed the latency time, distance and velocity by scopolamine in dose dependent manner. Next, ${\beta}$-and ${\gamma}$-secretase activities were determined in different regions of brain. Sesaminol glucosides dose-dependently attenuated scopolamine-induced ${\beta}$-secretase activities in cortex and hippocampous and ${\gamma}$-secretase in cortex. This study therefore suggests that sesaminol glucosides may be a useful agent for prevention of the development or progression of AD, and its inhibitory effect on secretase may play a role in the improving action of sesaminol glucosides on memory function.