• 제목/요약/키워드: protease inhibition

검색결과 218건 처리시간 0.019초

Angiotensin I Converting Enzyme Inhibitory Activity of Krill (Euphausia superba) Hydrolysate

  • Kim Dong-Soo;Park Douck-Choun;Do Jeong-Ryong
    • Fisheries and Aquatic Sciences
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    • 제5권1호
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    • pp.21-27
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    • 2002
  • Angiotensin I converting enzyme inhibitory activities of shelled krill (Euphausia superba) hydrolysates by autolysis and by hydrolysis with commercial proteases were analyzed. Among the proteases, Alcalase was the most effective protease for the hydrolysis of krill considering the degree of hydrolysis $(87.5\%)$ and the ACE inhibitory activity $(60\%)$. Four hour hydrolysis suggested as the most suitable and economic. In order to establish the optimum hydrolysis condition of krill, degree of hydrolysis and ACE inhibitory activity as affected by Alcalase concentration and water amount added were statistically analyzed by response surface methodology (RSM). The optimum hydrolysis condition was $2.0\%$ Alcalase hydrolysis in 2 volumes (v/w) of water at $55\% for 4 hr. The hydrolysate prepared from the optimum hydrolysis condition was fractionated by molecular weight. The lower molecular weight fraction showed the higher ACE inhibitory activity. $IC_{50}$ of the fraction under 500 Da was 0.57mg protein/mL.

Yarrowia lipolytica TH65가 생산하는 Alkaline Proteinase의 정제 및 특성

  • 유춘발;김창화;진영호;진익렬
    • 한국미생물·생명공학회지
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    • 제24권3호
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    • pp.316-320
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    • 1996
  • An alkaline proteinase produced by Yarrowia lipolytica TH65 was purified by 40-65% ammonium sulfate fractionation, DEAE-cellulose chromatography, and gel filtration with Sephadex G-100 and Sephadex G-75. The purified enzyme was shown as a single band on SDS-PAGE, and its molecular weight 31,500. Optimum temperature and pH were 40$\circ$C and 8.5-9.0, respectively, and the enzyme was stable below 40$\circ$C and in the pH range of 6-8. The enzyme was strongly inhibited by divalent ions, completely by PMSF, and partially by EDTA, EGTA, and phenanthroline. But the inhibitory effect in the presence of EDTA, EGTA and phenanthroline could be reversed by addition of Ca$^{2+}$. Thus, these results indicated that the purified enzyme was an alkaline serine proteinase (E.C. 3.4.21.14).

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Rengyolone Inhibits Apoptosis via Etoposide-Induced Caspase Downregulation

  • Kim, Jin-Hee;Lee, Choong-Hwan
    • Journal of Microbiology and Biotechnology
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    • 제19권3호
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    • pp.286-290
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    • 2009
  • In the course of screening for substances inhibiting apoptosis of U937 human leukemia cells induced by etoposide ($10\;{\mu}g/ml$), Forsythiae fructus, which showed a high level of inhibition, was selected. The regulating compounds were purified from the ethyl acetate extract by silica gel column chromatography and HPLC. The active substance was purified and identified as rengyolone by spectroscopic methods. This compound showed inhibitory activity on caspase-3 induction, a major protease of the apoptosis cascade, with an $IC_{50}$ value of $38.96\;{\mu}M$ after 8 h of etoposide treatment in U937 cells. The expression level of caspase-3 and poly(ADP-ribose) polymerase (PARP) were dose-dependently inhibited by the compound, suggesting that rengyolone inhibits etoposide-induced apoptosis via downregulation of caspases.

Drug-herb interactions: Mechanisms involved and clinical implications of five commonly and traditionally used herbs

  • Ong, Chin Eng;Pan, Yan
    • 셀메드
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    • 제4권3호
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    • pp.17.1-17.8
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    • 2014
  • Herbal remedies are commonly used by patients worldwide. Because these herbal preparations share the same metabolic and transport proteins with prescribed medicines, the potential for a drug-herb interaction is substantial and is an issue of significant concern. This review paper summarizes drug-herb interactions involving inhibition or induction of cytochrome P450 enzymes, drug transporters as well as modulation of drug pharmacodynamics. An increasing number of in vitro and animal studies, case reports and clinical trials evaluating such interactions have been reported, and implications of these studies are discussed in this review. The most commonly implicated drugs in the interaction include anticoagulants, antiplatelets, immunosuppressants, anti-neoplastics, protease inhibitors, and some antidepressants. Pharmacokinetic and/or pharmacodynamic interactions of five commonly used herbal remedies (danshen, garlic, Ginkgo biloba, ginseng, and St John's wort) with these drugs are presented, with focus of discussion being the potentials for interaction, their mechanisms and clinical implications. There is a necessity for adequate pharmacovigilance to be carried out in minimizing unanticipated but often preventable drug-herb interactions.

Antilisterial Bacteriocin from Lactobacillus rhamnosus CJNU 0519 Presenting a Narrow Antimicrobial Spectrum

  • Jeong, Ye-Jin;Moon, Gi-Seong
    • 한국축산식품학회지
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    • 제35권1호
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    • pp.137-142
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    • 2015
  • A lactic acid bacterium presenting antimicrobial activity against a Lactobacillus acidophilus strain used for eradication of acid inhibition was isolated from a natural cheese. The 16S rRNA gene sequence of the isolate best matched with a strain of L. rhamnosus and was designated L. rhamnosus CJNU 0519. The antimicrobial activity of the partially purified bacteriocin of CJNU 0519 was abolished when treated with a protease, indicating the protein nature of the bacteriocin. The partially purified bacteriocin (rhamnocin 519) displayed a narrow antimicrobial activity against L. acidophilus, Listeria monocytogenes, and Staphylococcus aureus among several tested bacterial and yeast strains. Rhamnocin 519 in particular showed strong bactericidal action against L. monocytogenes.

유향 물 추출물의 HL-60 혈액암세포에서 세포사멸 유도효과 (The Water Extract of Boswellia carterii Induces Apoptosis in Human Leukemia HL-60 Cells)

  • 박래길;오광록;이광규;문연자;김정훈
    • 약학회지
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    • 제45권2호
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    • pp.161-168
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    • 2001
  • The possible mechanism of the antiproliferative and apoptotic effects of Boswellia carterri water extract were studied in HL-60 human leukemia cells. The cytotoxicity of HL-60 cells after the treatment of Boswellia carterii water extract showed dose- and time-dependent manner. The apoptotic effect of 300 $\mu$g/ml Boswellia carterii water extract was demonstrated by DNA laddering. The activity of caspase 3-1ike protease was markedly increased in HL-60 cells treated with Boswellia carterii water extract. Furthermore, the level of Bcl-2 was time-dependently reduced, whereas Bax protein level was enhanced by Boswellia carterii water extract treatment. In conclusion, our results suggest that apoptotic effect of Boswellia carterii water extract may partly mediated through activations of caspase-3 activity and Bax expression, and inhibition of Bcl-2 expression.

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Design, Syntheses and Biological Evaluations of Nonpeptidic Caspase 3 Inhibitors

  • Kim, Eun-Sook;Yoo, Sung-Eun;Yi, Kyu-Yang;Lee, Sun-Kyung;Noh, Jae-Sung;Jung, Yong-Sam;Kim, Eun-Hee;Jeong, Nak-Chul
    • Bulletin of the Korean Chemical Society
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    • 제23권7호
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    • pp.1003-1010
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    • 2002
  • Caspase 3, a member of cysteine protease family, is well known as a major apoptosis effector and is involved in cell death as a result of ischemic diseases such as stroke and myocardial infarction, therefore the inhibition of caspase 3 may protect those apoptotic cell damages. During the high-throughput screening of the compounds from the Korea Chemical Bank, berberine derivatives (A and B), an isoquinoline alkaloid, have been identified as potential inhibitors for caspase 3. Based on this finding we carried out molecular modeling study to identify the pharmacophoric elements of berberine structure which interact with a substrate-recognition binding site of caspase 3 and came up with several novel scaffolds. In this report, we will discuss the molecular modeling, syntheses and the enzyme inhibitory activities of these novel compounds.

Bacillus sp. HJ 57에 의한 버섯 병원균주의 생육억제 (Growth Inhibition of Mushroom Pathogen by Bacillus sp. HJ 57)

  • 서권일;갈상완;이성태;박경욱;이상원
    • 생명과학회지
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    • 제22권6호
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    • pp.799-806
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    • 2012
  • 발효된 버섯배지 및 부엽토 등으로부터 80여 종의 균주를 1차 분리하여 CMCase, amylase 및 protease활성이 높고 버섯질병균주에 대한 항균활성이 높으면서 표고버섯 및 팽이버섯의 생육에는 전혀 영향을 미치지 않는 HJ-57 항균미생물을 최종 분리균주로 선정하였다. 최종 선정한 HJ-57 항균미생물을 동정한 결과 Bacillus sp. HJ-57로 밝혀졌으며, 배양을 위한 배지의 초기 pH는 pH 7, 배양온도는 $35^{\circ}C$가 최적인 것으로 나타났다. Bacillus sp. HJ-57균주는 12 hr 배양하였을 때는 약간의 항균활성을 나타내었지만, 배양 36~48 hr 배양하였을 때는 비교적 높은 항균활성을 나타내었다. Bacillus sp. HJ-57 항균미생물은 팽이버섯 재배농가에서 사용하는 콘코프 함유배지상에서도 버섯질병균주인 세균 및 곰팡이에 대하여 매우 높은 항균활성을 나타내었다.

Antilisterial Effect of Bacteriocin SH01, Obtained from Enterococcus faecium SH01, in Ground Beef

  • Kim, Min-Ju;Jung, Miran;Kim, Wang June
    • 한국축산식품학회지
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    • 제35권2호
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    • pp.211-215
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    • 2015
  • From the previous study, Enterococcus faecium SH01 was isolated from mukeunji, an over-ripened kimchi, and it produced bacteriocin SH01. Bacteriocin SH01 showed an inhibitory effect against Listeria monocytogenes ATCC 19111, a bacterial strain causing human listeriosis. Crude bacteriocin SH01 was purified by ammonium sulfate precipitation and its inhibitory activity at two concentrations (500 and 1,000 AU/g) against Listeria monocytogenes ATCC 19111 was investigated in ground beef at increasing temperatures (5, 10, 15, and 20℃) for 8 d. The number of Listeria monocytogenes ATCC 19111 significantly decreased (p<0.05) as the concentration of bacteriocin increased from 500 to 1,000 AU/g. Intrinsic crude protease activities in ground beef were examined and increased as the temperature increased. Experiments varying both the concentrations of added bacteriocin SH01 and temperature demonstrated a maximum inhibition (2.33 log reduction of bacteria) in samples containing 1,000 AU/g of bacteriocin SH01 incubated at 20℃. When the crude bacteriocin SH01 solution (1,280 AU/mL) was incubated with crude protease solutions at different temperatures, its activity decreased by only half (640 AU/mL), as assessed in an agar well diffusion assay. The finding that the antilisterial activity of bacteriocin SH01 increased with temperature can be explained by the fact that higher temperatures increase bacterial membrane fluidity, thereby promoting the cellular penetration of bacteriocin SH01 into L. monocytogenes. Bacteriocin SH01 may be an excellent candidate as a biopreservative for controlling L. monocytogenes growth in ground beef.

부숙촉진 미생물 분리 및 분리균의 특성 (Isolation and Characteristics of Composting-promoting-bacteria)

  • 이영한;박상렬
    • 한국토양비료학회지
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    • 제34권6호
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    • pp.394-400
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    • 2001
  • 가축분 및 음식물 퇴비 132점에서 517균주를 분리하고 CMC와 xylan 및 PGA 배지에서 강한 활성을 가지는 10여개의 균주를 선별하여 배추종자 발아를 이용한 작물 inhibition test와 오이 육묘실험으로 growth test를 거쳐 생육이 가장 양호한 LYH201 균주를 야생균주로 선발하였다. Bergey's manual 방법으로 특성을 조사한 결과 LYH201균주는 Gram 양성균으로 내생포자 형성, oxidase, CMCCase, xylanase, catalase, V-P test, methyl red test, arabinose 등의 탄소원 이용성은 양성이었으며, indole을 생성하고, urease, lecithinase, dihydrolase test는 음성이었고, 전자현미경으로 관찰한 결과 길이가 $2.5{\sim}3.0{\mu}m$, 너비가 $0.5{\sim}0.7{\mu}m$의 간균인 Bacillus subtilis로 확인되었다. Bacillus subtilis LYH201 균주를 MMY를 이용하여 배양한 결과 온도 $50^{\circ}C$, pH 6.0에서 생육이 가장 좋았다.

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