• 제목/요약/키워드: Guanidine

검색결과 131건 처리시간 0.023초

6-구아니디노퀴나졸린 유도체의 합성 및 EGFR 저해 활성 (Synthesis and EGFR Inhibitory Activity of 6-Guanidinoquinazoline Derivatives)

  • 유경호;이여란
    • 한국응용과학기술학회지
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    • 제25권2호
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    • pp.240-251
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    • 2008
  • The central role of tyrosine phosphorylation in cell proliferative signaling mechanisms provides another target for chemotherapy. The aim of this research is to develop new quinazoline derivatives that possess the inhibitory activity for depidermal growth factor receptor (EGFR) tyrosine kinase (TK) as protein kinase inhibitors. In this work, a series of new 4-anilino-6-guanidino-7-methoxyquinazoline derivatives (12a-l) were synthesized by the introduction of guanidine moiety at C-6 of quinazoline nucleus and evaluated for their EGFR TK inhibitory activities.

Function of hepatocyte growth factor in gastric cancer proliferation and invasion

  • Koh, Sung Ae;Lee, Kyung Hee
    • Journal of Yeungnam Medical Science
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    • 제37권2호
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    • pp.73-78
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    • 2020
  • Cancer incidence has been increasing steadily and is the leading cause of mortality worldwide. Gastric cancer is still most common malignancy in Korea. Cancer initiation and progression are multistep processes involving various growth factors and their ligands. Among these growth factors, we have studied hepatocyte growth factor (HGF), which is associated with cell proliferation and invasion, leading to cancer and metastasis, especially in gastric cancer. We explored the intercellular communication between HGF and other surface membrane receptors in gastric cancer cell lines. Using complimentary deoxyribonucleic acid microarray technology, we found new genes associated with HGF in the stomach cancer cell lines, NUGC-3 and MKN-28, and identified their function within the HGF pathway. The HGF/N-methyl-N'-nitroso-guanidine human osteosarcoma transforming gene (c-MET) axis interacts with several molecules including E-cadherin, urokinase plasminogen activator, KiSS-1, Jun B, and lipocalin-2. This pathway may affect cell invasion and metastasis or cell apoptosis and is therefore associated with tumorigenesis and metastasis in gastric cancer.

PHMG (polyhexamethylene guanidine) 흡입독성참고치 산출을 통한 가습기살균제 노출등급 분류 및 특성 (Classification and Characterization of Exposure Rating in Humidifier Disinfectants through Calculation of PHMG Reference Concentration)

  • 김은채;류현수;박진현;최영태;허정;이슬아;조은경;최윤형;조만수;양원호
    • 한국환경보건학회지
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    • 제46권3호
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    • pp.335-343
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    • 2020
  • Objectives: The Korean Ministry of Environment has identified cases of people suspected of suffering lung disease potentially caused by polyhexamethylene guanidine (PHMG) used in humidifier disinfectants (HDs). Exposure assessment for the HDs was conducted using a questionnaire during face-to-face interview. The main purposes of this study were to develop a methodology to effectively classify levels of exposure to HDs based on a questionnaire. Methods: We first identified the overall participants' exposure characteristics by HD exposure levels; Second, we selected misclassified subjects and investigated characteristics of overestimated and underestimated subjects, focusing on exposure cases to PHMG-containing HDs. An inhalation reference concentration (RfC) for PHMG was produced on the basis of inhalation toxicity values. We made a cross-tabulation of the exposure classes (Exposure classes 1-to-4) by clinical classes based on the RfC. When the value of the exposure class minus the clinical class was 0 or 1, we assumed these were true values. When the value was ≥2 and ≤ -2, we assigned these cases to the overestimation group and underestimation group, respectively. Results: The overestimated group may have already recovered and responded excessively due to psychological anxiety or in order to receive compensation. On the other hand, relatively high mortality rates and surrogate responses for those under 10 years of age may have resulted in inaccurate exposure assessment for underestimated groups. For the characteristics of exposure, it was shown that for the underestimated group, the exposure was relatively weaker than the overestimated group, even though a high overall clinical rating was determined. Conclusions: This study may suggest ways to reduce bias and overcome the limitations of current HD exposure assessment.

Humidifier disinfectant lung injury, how do we approach the issues?

  • Choi, Jihyun Emma;Hong, Sang-Bum;Do, Kyung-Hyun;Kim, Hwa Jung;Chung, Seockhoon;Lee, Eun;Choi, Jihyun;Hong, Soo-Jong
    • Environmental Analysis Health and Toxicology
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    • 제31권
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    • pp.19.1-19.7
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    • 2016
  • A large portion of the Korean population has been exposed to toxic humidifier disinfectants (HDs), and considering that the majority of the victims are infants, the magnitude of the damage is expected to be considerably larger than what has currently been revealed. The current victims are voicing problems caused by various diseases, including but not limited to lung, upper respiratory tract, cardiovascular, kidney, musculoskeletal, eye, and skin diseases, etc. However, there has been difficulty in gaining validation for these health problems and identifying causal relationships due to lack of evidence proving that toxic HD is the specific causes of extrapulmonary diseases such as allergic rhinitis. Furthermore, the victims and bereaved families of the HD case have not received any support for psychological distress such as post-traumatic stress disorder, depression, feelings of injustice, and anger caused by the trauma. In addition, because the underlying mechanisms of the toxic materials within the HDs such as polyhexamethylene guanidine phosphate, poly(oxyalkylene guanidine) hydrochloride, chloromethylisothiazolinone /methylisothiazolinone have yet to be determined, the demand for information regarding the HD issue is growing. The victims of the HD cases require support that goes beyond financial aid for medical costs and living expenses. There is a desperate need for government-led integrated support centers that provide individualized support through health screenings; in other words, we need an integrated facility that provides the appropriate social support to allow the victims to recover their physical and mental health, so as to well prepare them to return to a normal life. The implementation of such a plan requires not only the close cooperation between those departments already directly involved such as the Ministry of Environment and the Ministry of Health and Welfare, but also active support on a national scale from pan-governmental consultative bodies.

피리디니움 디나이트라아마이드염의 합성과 특성연구 (Synthesis and Characterization of Pyridinium Dinitramide Salt)

  • 김우람;권윤자;조영민
    • 공업화학
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    • 제27권4호
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    • pp.397-401
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    • 2016
  • 새로운 고체산화제 화합물인 pyridinium dinitramide (Py-DN)는 환경 및 인체에 독성이 적은 비염소계의 에너지물질로서 고체 추진제 뿐만 아니라 단일계 추진제로 활용이 가능한 high performance green propellant (HPGP) 물질이다. 합성반응은 술팜산칼륨(potassium sulfamate, $NH_2SO_3K$)을 출발물질로 시작하였으며, 합성된 Py-DN의 화학적인 구조특성을 적외선분광법과 가시광선-자외선분광법으로 관찰하였다. 또한, 유사한 물성의 친환경 고체산화제인 ammonium dinitramide[ADN, $NH_4N(NO_2)_2$]와 guanidine dinitramide[GDN, $NH_2C(NH_2)NH_2N(NO_2)_2$]의 열특성을 TG/DSC로 분석하여 상대 비교하였다. 본 연구에서 합성한 Py-DN염의 흡열온도는 $77.4^{\circ}C$, 분해온도는 $144.7^{\circ}C$, 발열에너지는 1739 J/g으로 기존의 DN계열 물질보다 열적 반응이 빠르므로 분해온도가 상대적으로 낮아 단일계 추진제의 촉매 분해 시 촉매의 예열온도를 낮출 수 있어 로켓추력기의 연료로 활용할 경우, 낮은 분해온도 적용성에 장점이 있다.

헛개나무 잎 추출물의 항돌연변이원성 및 암세포 성장억제효과 (Antimutagenic and Cytotoxic Effects of Hovenia dulcis Thumb Leaves Extracts)

  • 박선희;장은영
    • 한국식품영양과학회지
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    • 제36권11호
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    • pp.1371-1376
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    • 2007
  • 예로부터 약용으로 이용되어온 헛개나무 잎을 이용하여 항돌연변이원성 및 암세포 성장 저해효과를 조사하였다. 헛개나무 잎의 돌연변이 억제 효과를 Ames test로 검색한 결과, 헛개나무 잎의 메탄올 추출물과 분획물 그 자체의 돌연변이원성은 없었으며, 헛개나무 잎의 메탄올 추출물은 직접 변이원인 N-methyl-N#-nitro-N-nitroso-guanidine(MNNG)와 간접변이원인 benzo(a)pyrene(B(a)P)의 돌연변이 유발성을 크게 저해하였다. 또한 메탄올 추출물에서 분리한 분획물들도 유의성 있는 돌연변이 억제효과를 나타내었으며 특히 헥산, 클로르포름, 부탄올 분획물의 경우는 물 분획물보다 MNNG와 B(a)P에 대해서 더 큰 항돌연변이 효과를 나타내었다. 그리고 헛개나무 잎의 메탄올 추출물과 그 분획물들의 사람의 암세포주인 HT29와 HepG2에 대한 성장 저해 효과를 MTT assay로 검토한 결과 헛개나무 잎의 메탄올 추출물과 헥산, 클로로포름 분획물들이 높은 암세포 성장 저해 효과를 나타내었으며 농도 의존적인 경향을 보였다. 그러나 사람의 정상 간세포인 Chang cell에서는 세포독성이 나타나지 않았다. 이상의 실험 결과로 헛개나무 잎은 발암물질로부터 생체를 보호하는 물질을 함유하고 있을 것으로 사료된다.

가습기 살균제 피해자 호흡기로 흡입된 가습기 살균제 양 추정 - 호흡기 외부(external) 및 내부 노출(internal exposure) 추정 방법과 사례 - (Estimation of Humidifier Disinfectant Amounts Inhaled into the Respiratory System)

  • 박동욱;류승훈;임흥규;김선경;노현석;차원석;박두용
    • 한국환경보건학회지
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    • 제42권3호
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    • pp.141-146
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    • 2016
  • In South Korea, many cases of humidifier disinfectant-associated lung injury (HDLI) have been reported among people who used humidifier products containing humidifier disinfectant (HD). The objectives of this study are to estimate both airborne HD concentration in the room where HD was used and the amount of humidifier disinfectant absorbed into the respiratory system. Information and data on the HDs were collected using a structured questionnaire and home environmental investigations include the volume of HD (ml) and hours used per day, concentration of disinfectants contained in the HD brand (${\mu}g/ml$), volume of the room ($m^3$), assumed ventilation rate ($m^3/hr$) and breathing rate assumed ($m^3/hr$). We used children aged under five years old as a sample and estimated both airborne HD concentrations and amount of HD absorbed into the respiratory system. The estimated airborne concentration of HD in the room ranged from 68 to $369{\mu}g/m^3$ for PHMG (polyhexamethylene guanidine phosphate) and from 16 to $239{\mu}g/m^3$ for PGH (oligo (2-(2-ethoxy) ethoxyethyl guanidine). The amount of HD absorbed in the respiratory system per day was estimated to range from 227 to $1,225{\mu}g$ for PHMG and from 53 to $794{\mu}g$ for PGH. In conclusion, a great amount of HD was likely absorbed into respiratory system, likely beyond the level of the capacity of the immune system to remove the HD absorbed.

Camostat 및 분해산물 4-(4-guanidinobenzoyloxy)phenylacetic acid의 전자분무 이온화 텐덤 질량 fragmentation 패턴 (Electrospray ionization tandem mass fragmentation pattern of camostat and its degradation product, 4-(4-guanidinobenzoyloxy)phenylacetic acid)

  • 권순호;신혜진;박지명;이경률;김영진;이상후
    • 분석과학
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    • 제24권2호
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    • pp.78-84
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    • 2011
  • 본 연구에서는 양성 및/또는 음성 이온 방식으로 저에너지 충돌-유발 분해(CID)를 이용한 serine protease 저해제인 camostat 와 그것의 분해산물인 4-(4-guanidinobenzoyloxy)phenylacetic acid (GBPA)의 분해 패턴을 전자분무 소스가 있는 사중극자 텐덤 질량분석기(ESI-MS/MS)를 이용하여 최초로 조사하였다. Camostat의 양이온 CID 질량 스펙트럼 분석결과, 분자구조내 에스테르 결합을 이루는 카르보닐 기와 산소 원자사이의 단일 결합(C-O) 분해가 우선적으로 일어나고, guanidine 기의 초기 손실보다는 N,Ndimethylcarbamoylmethyl기의 초기 손실이 더 잘 일어난다는 것이 특징적으로 확인되었다. GBPA의 양이온 CID 스펙트럼의 경우는, 4-guanidinobenzoyloxy 기에 있는 카르보닐 기와 산소원자 사이의 초기 분해가 일어나서 m/z 145에서 가장 강도가 높은 피크를 만들었다. 반면에, GBPA의 음이온 스펙트럼은 m/z 312의 모분자 이온에서 $CO_2$와 NH=C=NH의 순차적인 중성 손실로 인하여 m/z 226의 가장 강도가 높은 피크가 특징적으로 생성되었다.

한국산 녹두와 중국산 녹두에 있어서 Lectin의 생화학적 특성 비교 (Comparison of Biochemical Characterization of Korean and Chinese Mung Bean Lectin)

  • 노광수
    • 생명과학회지
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    • 제24권6호
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    • pp.603-611
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    • 2014
  • 한국산과 중국산 녹두 종자에서 0.15 M NaCl/0.1 M sodium phosphate buffer (pH7.0)에 의한 추출, $(NH_4)_2SO_4$ 침전, 최종적으로 Sephadex G-100을 이용한 affinity chromatography에 의해 lectin을 분리한 다음, 이들의 생화학적 특성을 조사, 비교하였다. 사람의 적혈구는 trypsin의 처리 유무와 상관없이 응집반응이 일어나지 않으며, 토끼의 적혈구에서는 trypsin을 처리한 경우에만 응집반응이 일어났다. 두 녹두 종자 lectin의 분자량은 SDS-PAGE를 통해 54 kDa와 28 kDa로 확인되었다. 한국산 녹두 종자 lectin의 최적 반응 온도는 $60^{\circ}C$이며, 중국산 녹두 종자 lectin의 경우는 $50^{\circ}C$로 나타났다. 종자 lectin이 열에 가장 안정한 온도는 한국산의 경우는 $50^{\circ}C$이며, 중국산의 경우 $40-50^{\circ}C$로 밝혀졌다. 한국산 녹두 종자 lectin은 pH 3.2에서 가장 높은 활성을 보였으며, 중국산 녹두 종자 lectin은 pH 6.2에서 가장 높은 활성을 보였다. 변성제를 처리했을 때, thiourea와 guanidine-HCl과는 혈액 응집이 일어나지 않아 변성작용이 일어남을 알 수 있었고, urea와는 혈액 응집이 일어나지 않아 변성작용이 일어나지 않음을 알 수 있었다. D-glucose외 6가지의 탄수화물에 대한 특이성이 나타나지 않았다. 또한 두 녹두 종자의 lectin은 $Ca^{2+}$, $Co^{2+}$, $Cu^{2+}$, $Cu^{2+}$, $Mg^{2+}$$Mn^{2+}$ 등의 금속이온에 대한 특이성이 없었다.

연도별 가습기 살균제 피해자 분포 고찰 - 폐 손상 중심 - (Distribution of Health Problems Associated with Humidifier Disinfectant by Year)

  • 박동욱;류승훈;노현석
    • 한국환경보건학회지
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    • 제42권6호
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    • pp.365-374
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    • 2016
  • Objectives: Studies are needed to examine the characteristics of health effects reported by people who used humidifier disinfectant (HD), including the distribution of victims. Methods: We analyzed the distribution of health effects including lung injury that were asserted by a total of 699 individuals who registered with the first through third national programs to determine health effects associated with the use of HD. Results: We found that HD-associated lung injury (HDLI) occurred every year from 2002 through 2011, and in 2011 for 37.2% (n=96) of the total of 258 clinically evaluated HDLI victims. More than half of the victims responded that they were victimized between 2010 and 2011. This was consistent among all classifications by sex, age, HD brand and HD chemical ingredient. Conclusion: This study assumed that the major reason for the outbreak of the health effect between 2010 and 2011 could be the variations in concentrations and physical properties related to polyhexamethylene guanidine (PHMG). Further studies are necessary to examine if some factors related to the chemical disinfectants contained in HD brands may have caused the massive outbreak of health effects including HDLI.