• Title/Summary/Keyword: }inhibitor$

검색결과 6,775건 처리시간 0.028초

Anticancer Effect of COX-2 Inhibitor DuP-697 Alone and in Combination with Tyrosine Kinase Inhibitor (E7080) on Colon Cancer Cell Lines

  • Altun, Ahmet;Turgut, Nergiz Hacer;Kaya, Tijen Temiz
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권7호
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    • pp.3113-3121
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    • 2014
  • Colorectal cancer remains one of the most common types of cancer and a leading cause of cancer death worldwide. In this study, we aimed to investigate effects of DuP-697, an irreversible selective inhibitor of COX-2 on colorectal cancer cells alone and in combination with a promising new multi-targeted kinase inhibitor E7080. The HT29 colorectal cancer cell line was used. Real time cell analysis (xCELLigence system) was conducted to determine effects on colorectal cell proliferation, angiogenesis was assessed with a chorioallantoic membrane model and apoptosis was determined with annexin V staining. We found that DuP-697 alone exerted antiproliferative, antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. For the antiproliferative effect the half maximum inhibition concentration ($IC_{50}$) was $4.28{\times}10^{-8}mol/L$. Antiangiogenic scores were 1.2, 0.8 and 0.5 for 100, 10 and 1 nmol/L DuP-697 concentrations, respectively. We detected apoptosis in 52% of HT29 colorectal cancer cells after administration of 100 nmol/L DuP-697. Also in combination with the thyrosine kinase inhibitor E7080 strong antiproliferative, antiangiogenic and apoptotic effects on HT29 colorectal cancer cells were observed. This study indicates that DuP-697 may be a promising agent in the treatment of colorectal cancer. Additionally the increased effects observed in the combination with thyrosine kinase inhibitor give the possibility to use lower doses of DuP-697 and E7080 which can avoid and/or minimize side effects.

Angiotensin-Converting Enzyme Inhibitor(ACE Inhibitor)에 의해 유발된 안면부 맥관부종(angioedema) 치험례 (A Case of Angioedema Induced by Angiotensin-Converting Enzyme Inhibitor)

  • 하유군;정기용;백종우;김동우;박종형;전찬용;최유경
    • 대한한방내과학회지
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    • 제28권2호
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    • pp.399-407
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    • 2007
  • Angioedema is a localized transient swelling of sudden onset that can occur in the face, lips, tongue, hand, feet, respiratory system and gastrointestinal system. Angioedema is classified as allergy, hereditary, idiopathic or induced by medication as like aspirin, nonsteroidal anti-inflammatory agents, opiates, antibiotics, and angiotensin-converting enzyme. Angiotensin-converting enzyme inhibitors are widely prescribed for hypertension and heart failure. This drug is commonly associated with angioedema which may be potentially life threatening. We experienced a case of angioedema induced by ACE inhibitor (angiotensin-converting enzyme inhibitor) in a 74-year-old patient who took ACE inhibitor to control hypertension during hospitalization. We thought the angioedema in the face had relation to myenzhong (面腫, mienjong) in oriental medicine. Weiling-tang (Wiryung-tang) was effective for angioedema in the face. As a result the symptoms disappeared rapidly. After 6 days, the patient's symptoms had notably improved.

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The ABA Effect on the Accumulation of an Invertase Inhibitor Transcript that Is Driven by the CAMV35S Promoter in ARABIDOPSIS

  • Koh, Eun-Ji;Lee, Sung June;Hong, Suk-Whan;Lee, Hoi Seon;Lee, Hojoung
    • Molecules and Cells
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    • 제26권3호
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    • pp.236-242
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    • 2008
  • Invertase (${\beta}$-D-fructofuranosidase; EC 3.2.1.26) catalyzes the conversion of sucrose into glucose and fructose and is involved in an array of important processes, including phloem unloading, carbon partitioning, the response to pathogens, and the control of cell differentiation and development. Its importance may have caused the invertases to evolve into a multigene family whose members are regulated by a variety of different mechanisms, such as pH, sucrose levels, and inhibitor proteins. Although putative invertase inhibitors in the Arabidopsis genome are easy to locate, few studies have been conducted to elucidate their individual functions in vivo in plant growth and development because of their high redundancy. In this study we assessed the functional role of the putative invertase inhibitors in Arabidopsis by generating transgenic plants harboring a putative invertase inhibitor gene under the control of the CaMV35S promoter. A transgenic plant that expressed high levels of the putative invertase inhibitor transcript when grown under normal conditions was chosen for the current study. To our surprise, the stability of the invertase inhibitor transcripts was shown to be down-regulated by the phytohormone ABA (abscisic acid). It is well established that ABA enhances invertase activity in vivo but the underlying mechanisms are still poorly understood. Our results thus suggest that one way ABA regulates invertase activity is by down-regulating its inhibitor.

한국산 검정콩 ${\alpha}-Amylase$ 저해물질의 분리 및 정제 (Purification of ${\alpha}-Amylase$ Inhibitor from Black Bean in Korea)

  • 문주석;배영일;심기환
    • 한국식품과학회지
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    • 제27권5호
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    • pp.762-767
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    • 1995
  • 한국산 두류 중의 ${\alpha}-Amylase$ 저해물질의 이화학적 특성에 관한 기초자료를 얻기 위하여 검정콩으로부터 ${\alpha}-Amylase$ 저해물질을 분리, 정제하여 다음과 같은 결과를 얻었다. 검정콩 ${\alpha}-Amylase$ 저해물질도 SDS-PAGE상에서 단일밴드를 확인하였고, capillary electrophoresis에서 순도를 확인하였으며, 정제된 저해물질의 비활성도는 544.0 units/mg, 정제도는 약 18배였으며, SDS-PAGE 상에서 분자량은 25 KD이였다. 검정콩 ${\alpha}-Amylase$ 저해물질의 주요 아미노산은 glutamic acid, aspartic acid 및 lysine 순이었다. 정색반응 결과 검정콩 ${\alpha}-Amylase$ 저해물질은 당단백질로 추정되었으며, 탄수화물 함량은 3.2%로 나타났다.

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B16 Melanoma 세포에서 Protein Kinase 억제제들이 Cyclic AMP 경로를 통한 멜라닌 생성에 미치는 영향 (Effects of Protein Kinase Inhibitors on Melanin Production in B16 Melanoma Cells Stimulated via Cyclic AMP-dependent Pathway)

  • 차상복;조남영;윤미연;임혜원;김경원;박영미;이지윤;이진희;김창종
    • 약학회지
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    • 제47권1호
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    • pp.31-36
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    • 2003
  • To investigate the effect of protein kinase on melanin production via cAMP-dependent pathway, we measured the melanin amount and tyrosinase activity in B16 melanoma cells stimulated by alpha-melanocyte stimulating hormone (MSH), forskolin and 8-Br-cAMP. MSH, forskolin and 8-Br-cAMP significantly increased both melanin production and tyrosinase activity in B16 cells. Melanin production and tyrosinase activity by MSH are significantly inhibited by cyclic AMP-dependent protein kinase inhibitor (KT5720) and protein kinase C down-regulation treated with PMA. Bisindolmaleimide (1$\mu$M), protein kinase C inhibitor, significantly inhibited melanin production and tyrosinase activity stimulated by MSH, forskolin and 8-Br-cAMP with the following order of potency: MSH>forskolin>8-Br-cAMP. Tyrosine kinase inhibitor, genistein and DHC, significantly inhibited both, but the inhibitory effect was more potent in 8-Br-cAMP-stimulated B16 cells than MSH-stimulated cells. NFkB inhibitor (parthenolide) significantly inhibited melanin production and tyrosinase activity. Neither melanin production nor tyrosinase activity induced by MSH, forskolin and 8-Br-cAMP were affected by KN-62 (calmodulin-dependent protein kinase II inhibitor), PD098059 (mitogen-activated protein kinase inhibitor, MAPKK) and worthmannin (phosphatidylinositol 3-kinase inhibitor). These results suggest that both protein kinase C and tyrosine kinase are involved in melanin production by cyclic AMP-dependent pathway and NFkB pathway may play an important role in cyclic AMP-dependent melanin production in B16 melanoma cells.

저탄장 자연발화에 미치는 표면차단제 영향에 관한 수치 해석적 연구 (Numerical Study on the Effects of Surface-inhibitors on the Spontaneous Ignition of Coal Stockpile)

  • 김재관;박석운;신동익
    • 한국화재소방학회논문지
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    • 제33권2호
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    • pp.20-29
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    • 2019
  • 본 논문에서는 저탄장 석탄더미 표면부에 자연발화 차단제를 도포하였을 경우 자연발화 현상에 미치는 영향을 수치해석적인 방법을 통해 살펴보았다. 먼저 자연발화 차단제를 도포하지 않은 경우를 해석하여 선행연구 결과와 비교하여 본 연구의 수치해석방법을 검증한 후 다양한 자연발화 차단제 도포영역 및 위치에 따른 자연발화 방지효과를 분석하였다. 그 결과, 자연발화 차단제의 도포영역이 넓을수록 석탄더미 내부로의 산소유입이 차단되어 발화방지 효과가 컸으며, 자연발화 차단제를 석탄더미 바닥에서부터 도포하여야 발화방지 효과가 더욱 큰 것으로 나타났다. 자연발화 차단제의 제조비용 등의 경제적인 측면을 고려하여 효과적으로 도포하여야 한다.

Spatiotemporal expression and regulation of peptidase inhibitor 3 and secretory leukocyte protease inhibitor at the maternal-fetal interface in pigs

  • Soohyung Lee;Inkyu Yoo;Yugyeong Cheon;Hakhyun Ka
    • Animal Bioscience
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    • 제36권7호
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    • pp.1034-1043
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    • 2023
  • Objective: Two serine protease inhibitors, peptidase inhibitor 3 (PI3) and secretory leukocyte protease inhibitor (SLPI), play important roles in protease inhibition and antimicrobial activity, but their expression, regulation, and function at the maternal-fetal interface in pigs are not fully understood. Therefore, we determined the expression and regulation of PI3 and SLPI in the endometrium throughout the estrous cycle and at the maternal-fetal interface in pigs. Methods: Endometrial tissues during the estrous cycle and pregnancy, conceptus tissues during early pregnancy, and chorioallantoic tissues during mid to late pregnancy were obtained, and the expression of PI3 and SLPI was analyzed. The effects of the steroid hormones estradiol-17β (E2) and progesterone (P4) on the expression of PI3 and SLPI were determined in endometrial explant cultures. Results: PI3 and SLPI were expressed in the endometrium during the estrous cycle and pregnancy, with higher levels during mid to late pregnancy than during the estrous cycle and early pregnancy. Early-stage conceptuses and chorioallantoic tissues during mid to late pregnancy also expressed PI3 and SLPI. PI3 protein and SLPI mRNA were primarily localized to endometrial epithelia. In endometrial explant cultures, the expression of PI3 was induced by increasing doses of P4, and the expression of SLPI was induced by increasing doses of E2 and P4. Conclusion: These results suggest that the PI3 and SLPI expressed in the endometrium and conceptus tissues play an important role in antimicrobial activity for fetal protection against potential pathogens and in blocking protease actions to allow epitheliochorial placenta formation.

아질산칼슘 방청제를 사용한 시멘트 경화체 내의 염소이온 거동 특성 (Characteristics of Chloride Ion Behavior in an Cement Matrix Using Calcium Nitrite Inhibitor)

  • 신민철;안기용
    • 한국건설순환자원학회논문집
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    • 제12권2호
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    • pp.206-213
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    • 2024
  • 본 연구는 염소이온이 침투한 시멘트 모르타르에서의 아질산칼슘(Ca(NO2)2) 방청제의 방청 효과에 대한 실험적 연구이다. 이를 위하여 아질산칼슘 방청제를 함유한 시멘트 모르타르에 대하여 내부식성과 염화물 이동에 대한 실험을 실시하였다. 그 결과 아질산칼슘 방청제의 사용량을 증가하면 할수록 철근부식에 대한 염화물 임계 농도값이 증가한 반면, 염소이온의 이동속도는 빨라지는 것을 확인하였다. 그러나 아질산칼슘 방청제를 사용한 시멘트 모르타르의 경우 염소이온의 이동속도가 빨라서 부식 발생시간을 단언하는 것은 어려움이 있었다. 그러나 철근부식에 영향을 미치지 않을 아질산칼슘의 사용량은 본 연구의 범위에서는 시멘트 중량 대비 2.0~3.0% 수준의 결과를 나타내었다.

Thalidomide and a Dipeptidyl Peptidase 4 Inhibitor in a Rat Model of Experimental Autoimmune Myocarditis

  • Kyung-Jin Kim;Jun-Bean Park;Seung-Pyo Lee;Hyung-Kwan Kim;Yong-Jin Kim
    • Korean Circulation Journal
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    • 제53권12호
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    • pp.795-810
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    • 2023
  • Background and Objectives: Myocarditis is a potentially fatal disease, but curative treatments have not yet been established. Myocardial inflammation is an important pathogenesis of this disease, and immunosuppressants such as methylprednisolone and immunoglobulin have been used for treatment; however, the effectiveness needs to be improved. Thalidomide and dipeptidyl peptidase (DPP) 4 inhibitors were recently investigated regarding their immunomodulatory properties. This study aimed to test whether thalidomide or a DPP4 inhibitor (evogliptin) can improve the effectiveness of myocarditis treatment using a rat model of experimental autoimmune myocarditis (EAM). Methods: Rats with or without myocarditis were administered thalidomide at 100 mg/kg/day and DPP4 inhibitor at 10 mg/kg/day orally. Measurement of echocardiography, serum inflammatory cytokines, myocardial histopathological examination, and immunohistochemical staining for leukocytes, macrophages, CD4+ T cells, and cytoskeleton were performed after 3 weeks, and the fibrosis area was measured after 3 and 6 weeks. Results: Thalidomide and DPP4 inhibitor did not reduce the severity of myocarditis compared with the EAM without treatment rats by comparing the echocardiographic data, myocardial CD4+, macrophages, neutrophil infiltrations, and the heart weight/body weight ratio in 3 weeks. The levels of inflammatory cytokines were not lower in the thalidomide and DPP4 inhibitor-treated group than in the untreated group in 3 weeks. In 6 weeks, thalidomide and DPP4 inhibitors did not reduce the fibrosis area compared to untreated groups. Conclusions: Although thalidomide and the DPP4 inhibitor had an immunomodulatory effect and are used against inflammatory diseases, they did not ameliorate myocardial inflammation and fibrosis in this rat model of EAM.

콘크리트 내부로의 압입공법을 사용한 방청제의 침투깊이 및 농도에 관한 실험적 연구 (Experimental Study on the Penetration Depth and Concentration of Corrosion Inhibitor Using Press-in Method Into the Inside of Concrete)

  • 조형규;유조형;이한승
    • 한국구조물진단유지관리공학회 논문집
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    • 제13권5호통권57호
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    • pp.160-168
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    • 2009
  • 철근이 부식되면 오염된 콘크리트를 제거하고 철근방식을 하고 보수하는 방법과 방청제를 도포하는 방법으로는 철근위치에서 방청성능을 확보하기가 곤란한 실정이다. 이에 본 연구에서는 철근위치까지 방청제를 고압 침투시키기 위한 연구개발에 앞서 방청제 가압 침투 실험을 통하여 침투깊이를 측정하고 위치별 아질산이온의 양을 측정하여 물시멘트비, 압력, 가압시간에 따른 침투깊이 예측하고 우수한 방청성을 가지는 염화물이온과 아질산이온의 몰비 0.6 이상이 되는 물시멘트비와 압력, 가압시간을 산정하였다. 실험결과 물시멘트비가 방청제의 침투에 가장 큰 영향을 주며 또한 실험체의 깊이가 깊어질수록 침투시킨 방청제의 농도는 같지 않고 낮아지는 것을 알 수 있었다.