• 제목/요약/키워드: $S_N1$ mechanism

검색결과 719건 처리시간 0.028초

시호 Saponin의 혈소판 활성화 작용에 관한 연구 (Studies on Platelet Activation of Saikosaponin Isolated From Bupleuri Radix)

  • 박영현;송민주;김남수
    • 한국식품위생안전성학회지
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    • 제13권4호
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    • pp.355-359
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    • 1998
  • 식물중에서 배당체 일종인 saponins을 다량 함유한 시호(Bupleurum falcatum)로부터 생체 조절 기능을 갖는 유효성분을 분리하여 혈소판 활성화 작용을 통하여 뇌심혈관계 질환 연구에 이용하고자 시호 용매 분획물에서 분리 및 동정한 Saikosapini을 thronbin, collagen, arachidonic acid 등의 효능제(agonist)와 세포의 $Ca^{2+}$ 의존성을 비교연구하였다. 시호 용매추출물 중에 acetone 추출물이 혈소판 응집작용이 강하며, 그 유효성분을 분리 및 동정한 saikosaponin a와 d는 C16 위치에 각각 ${\alpha}와\;{\beta}$형의 OH기를 갖는 이성체로, saikosapnin d가 a보다 강한 응집작용을 갖는 구조활성관계를 나타내고 있다. 각 효능제에 따라서 혈소판 활성화에 대한 세포의 $Ca^{2+}$ 의존성은 thrombin > colagen $\geq$ PAF>PMA> arachidonic acid $\geq$ Ionophore A23187순으로 나타났다. 시호 추출물 및 saikosaponin의 혈소판 활성화 작용은 기존 효능제와 다른 세포의 $Ca^{2+}$의존성을 나타내는 것으로 사료된다.

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클로로필 a가 UVB 유도성 산화적 스트레스와 matrix metalloproteinases (MMPs) 활성화 및 콜라겐 합성에 미치는 영향 (Effects of Chlorophyll a on UVB-induced Cellular Responses and Type I pN Collagen Synthesis in vitro)

  • 전희영;김정기;서대방;이상준
    • 한국식품과학회지
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    • 제41권6호
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    • pp.700-705
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    • 2009
  • 본 연구에서는 식물에서 추출된 천연 클로로필 a를 이용하여 UVB에 의해 유도되는 산화적 손상 및 MMPs의 변화를 평가하고, 콜라겐의 합성에 미치는 영향을 알아보고자 하였다. 본 연구의 결과를 종합해 보면, 클로로필 a는 UVB에 의해 유도되는 ROS의 발생을 저해함으로써 그로부터 발생할 수 있는 일련의 물리화학적 혹은 생물학적 신호 전달을 방지하는 효능을 가지며, 지질 과산화 역시 억제하는 효과를 지닌다. 또한 피부의 콜라겐, 탄력 섬유 등 기질 단백질을 분해하는 효소인 MMPs의 발현 또는 활성을 억제하고 콜라겐의 합성을 촉진하는 효과를 보여 피부 광노화에 대한 예방제로서 클로로필의 임상 적용의 가능성을 확인 할 수 있었다. 현재까지 보고된 피부에 대한 클로로필의 효능은 DMBA 또는 TPA 등의 화학 물질로 유발된 피부암을 예방하거나 억제하는 효능에 대한 연구가 대부분이었으며, 본 연구와 같이 UVB에 의해 유발되는 세포 반응에 대한 클로로필 a의 효능연구는 체계적으로 이루어진 바가 없다. 따라서 본 연구는 클로로필의 피부암 예방 및 치료뿐 아니라 피부 노화의 예방 관점에서 클로로필의 효능을 검토하고 확인했다는 것에서 의미가 있다. 그러나 본 연구 결과만으로는 클로로필의 농도 의존적 효능에 대한 명확한 판단을 하기에 부족한 부분이 있어 클로로필 효능의 농도 의존성에 대한 검토가 필요할 것으로 보여진다. 클로로필의 농도에 따른 효능 및 세포 독성의 상관성을 파악하고 동물, 인체효능 용량에 대한 연구를 통해 가장 바람직한 효능을 나타내는 클로로필의 농도를 산정하기 위한 검토가 이루어져야 할 것이다. 또한 피부 노화 예방을 위한 유용한 소재로서 클로로필의 임상적 활용 가능성을 판단하기 위해서는 동물, 인체 시험을 통한 클로로필의 효능 검증이 체계적으로 진행되어야 할 것으로 보여진다.

1999년 경주 인근에서 3차례 발생한 지진들의 지진원 특성 분석 (Analysis on the source characteristics of three earthquakes nearby the Gyeongju area of the South Korea in 1999)

  • 최호선;심택모
    • 지질공학
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    • 제19권4호
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    • pp.509-515
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    • 2009
  • 1999년 경상북도 경주 인근에서 지역규모($M_L$) 3.0 이상의 지진이 3차례(4월 24일, 6월 2일, 9월 12일)에 걸쳐 발생하였다. 진앙의 위치를 재결정한 결과 이 지진들의 진앙 사이 거리는 반경 1 km 내에 포함된다. 파형역산을 수행하여 6월 2일 지진의 발진기구를 분석하였으며, 나머지 지진들은 P파와 S파의 초동극성 및 진폭비를 이용하여 발진기구를 분석하였다. 6월 2일 및 9월 12일 지진은 단층면해가 서로 비슷하고, 4월 24일 지진은 상기 지진들의 단층면해를 포함하나 그 분포 범위가 상대적으로 넓다. 이 지진들의 발진기구는 공통적으로 약간의 정단층 성분을 포함한 주향이동단층의 특성을 보이며, P축의 방향은 동북동-서남서 방향으로 한반도 주응력 방향에 대한 이전 연구결과와 부합한다. 진앙 사이의 거리, 지진파형의 유사성, 지진들을 공통으로 기록한 지진관측소 지진자료 극성의 동일성, 발진기구의 유사성 등을 고려했을 때, 이 지진들은 동일한 단층에서 발생했을 것으로 1999년 경상북도 경주 인근에서 지역규모($M_L$) 3.0 이상의 지진이 3차례(4월 24일, 6월 2일, 9월 12일)에 걸쳐 발생하였다. 진앙의 위치를 재결정한 결과 이 지진들의 진앙 사이 거리는 반경 1 km 내에 포함된다. 파형역산을 수행하여 6월 2일 지진의 발진기구를 분석하였으며, 나머지 지진들은 P파와 S파의 초동극성 및 진폭비를 이용하여 발진기구를 분석하였다. 6월 2일 및 9월 12일 지진은 단층면해가 서로 비슷하고, 4월 24일 지진은 상기 지진들의 단층면해를 포함하나 그 분포 범위가 상대적으로 넓다. 이 지진들의 발진기구는 공통적으로 약간의 정단층 성분을 포함한 주향이동단층의 특성을 보이며, P축의 방향은 동북동-서남서 방향으로 한반도 주응력 방향에 대한 이전 연구결과와 부합한다. 진앙 사이의 거리, 지진파형의 유사성, 지진들을 공통으로 기록한 지진관측소 지진자료 극성의 동일성, 발진기구의 유사성 등을 고려했을 때, 이 지진들은 동일한 단층에서 발생했을 것으로 추정된다. 파형역산을 수행한 결과 6월 2일 지진의 지진모멘트는 $3.9\;{\times}\;10^{14}N{\cdot}m$로 계산되었으며, 이 값은 모멘트규모 3.7에 해당한다. 스펙트럼 분석을 통해 계산된 모멘트규모는 3.8로, 파형역산에 의한 모멘트규모와 비슷하다. 평균 응력강하는 7.5 MPa로 추정되었다. 3개 지진들을 공통으로 기록한 단일 지진관측소의 스펙트럼을 서로 비교한 결과 4월 24일 및 9월 12일 지진의 모멘트규모는 각각 3.2, 3.4로 추정되었다.

염분에 대한 콩의 생리학적 반응지표 연구 (Parameters on Physiological Responses of Soybean (Glycine max Merr.) to Salinity)

  • 천상욱;박종환
    • 한국환경농학회지
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    • 제22권3호
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    • pp.185-191
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    • 2003
  • 본 연구는 "광안콩"의 20일 묘를 공시하여 $0{\sim}90\;mM$의 염분조건에서 콩의 생리학적 피해정도를 산정하고 내염성 품종선발과 육종계획에 요구되는 기초자료로 활용하고자 수행되었다. 엽록소의 함량은 정상적인 관수를 실시한 대조구에 비해 염분 처리에서 $15{\sim}60%$ 감소하였고 농도증가에 따라 감소정도가 크게 나타났다. 염분 처리에 따른 광합성과 호흡량은 각각 $28{\sim}48%$$16{\sim}34%$ 감소하였고 $O_2$ 생산 비율보다 $O_2$ 소모 비율이 높게 나타났다. 수분 potential은 정상 잎(-1.5 MPa)에 비해 염분처리에서는 농도별로 -2.13에서 -2.69 MPa로 직선적으로 감소하였다. 개화기 염처리에서 대조구 $13.3\;{\mu}g$의 약 $17{\sim}22%$로 감소한 $11.8{\sim}10.4\;{\mu}g$이었으며 증산저항은 $1.08{\sim}1.70\;S/m$로 증가하는 경향이었다. 콩 잎의 수분증산 저항에 미치는 염분의 영향은 잎 내부의 기층저항이 가장 심한 차이를 보였고 무처리에서 45.9 S/m인 반면 염분처리에서는 $53.5{\sim}56.6\;S/m$로 농도증가에 따라 증가하였으며 기공저항과 잎 경계면의 저항은 큰 차이를 보이지 않았다. 대부분의 무기물 함량은 뿌리보다 앞에서 축적량이 더 많게 나타났으나 $Na^+$만이 뿌리에 더 많이 축적되었고 N, P, $K^+$, $Ca^{2+}$$Mg^{2+}$는 무처리에 비해 오히려 그 축적량이 감소하였다. 염분처리에 따른 콩 잎의 유리 proline은 무처리($10.5\;{\mu}g$) 대비 $1.8{\sim}4.2$배 ($184{\sim}434\;{\mu}g$)로 염 농도가 증가함에 따라 축적량이 증가하는 경향이었다. Nitrate reductase의 활성은 염 농도가 증가함에 따라 증가하였으나 농도가 90 mM 염분 처리에서의 증가폭은 다소 둔화되는 경향이었다. 한편 peroxidase 활성 역시 염분농도가 증가함에 다라 증가하는 것으로 나타났다.

지하수 관개에 의한 수도의 멸준양상과 그 방지책에 관한 연구 (Studies on the Rice Yield Decreased by Ground Water Irrigation and Its Preventive Methods)

  • 한욱동
    • 한국농공학회지
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    • 제16권1호
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    • pp.3225-3262
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    • 1974
  • The purposes of this thesis are to clarify experimentally the variation of ground water temperature in tube wells during the irrigation period of paddy rice, and the effect of ground water irrigation on the growth, grain yield and yield components of the rice plant, and, furthermore, when and why the plant is most liable to be damaged by ground water, and also to find out the effective ground water irrigation methods. The results obtained in this experiment are as follows; 1. The temperature of ground water in tube wells varies according to the location, year, and the depth of the well. The average temperatures of ground water in a tubewells, 6.3m, 8.0m deep are $14.5^{\circ}C$ and $13.1^{\circ}C$, respercively, during the irrigation period of paddy rice (From the middle of June to the end of September). In the former the temperature rises continuously from $12.3^{\circ}C$ to 16.4$^{\circ}C$ and in the latter from $12.4^{\circ}C$ to $13.8^{\circ}C$ during the same period. These temperatures are approximately the same value as the estimated temperatures. The temperature difference between the ground water and the surface water is approximately $11^{\circ}C$. 2. The results obtained from the analysis of the water quality of the "Seoho" reservoir and that of water from the tube well show that the pH values of the ground water and the surface water are 6.35 and 6.00, respectively, and inorganic components such as N, PO4, Na, Cl, SiO2 and Ca are contained more in the ground water than in the surface water while K, SO4, Fe and Mg are contained less in the ground water. 3. The response of growth, yield and yield components of paddy rice to ground water irrigation are as follows; (l) Using ground water irrigation during the watered rice nursery period(seeding date: 30 April, 1970), the chracteristics of a young rice plant, such as plant height, number of leaves, and number of tillers are inferior to those of young rice plants irrigated with surface water during the same period. (2) In cases where ground water and surface water are supplied separately by the gravity flow method, it is found that ground water irrigation to the rice plant delays the stage at which there is a maximum increase in the number of tillers by 6 days. (3) At the tillering stage of rice plant just after transplanting, the effect of ground water irrigation on the increase in the number of tillers is better, compared with the method of supplying surface water throughout the whole irrigation period. Conversely, the number of tillers is decreased by ground water irrigation at the reproductive stage. Plant height is extremely restrained by ground water irrigation. (4) Heading date is clearly delayed by the ground water irrigation when it is practised during the growth stages or at the reproductive stage only. (5) The heading date of rice plants is slightly delayed by irrigation with the gravity flow method as compared with the standing water method. (6) The response of yield and of yield components of rice to ground water irrigation are as follows: \circled1 When ground water irrigation is practised during the growth stages and the reproductive stage, the culm length of the rice plant is reduced by 11 percent and 8 percent, respectively, when compared with the surface water irrigation used throughout all the growth stages. \circled2 Panicle length is found to be the longest on the test plot in which ground water irrigation is practised at the tillering stage. A similar tendency as that seen in the culm length is observed on other test plots. \circled3 The number of panicles is found to be the least on the plot in which ground water irrigation is practised by the gravity flow method throughout all the growth stages of the rice plant. No significant difference is found between the other plots. \circled4 The number of spikelets per panicle at the various stages of rice growth at which_ surface or ground water is supplied by gravity flow method are as follows; surface water at all growth stages‥‥‥‥‥ 98.5. Ground water at all growth stages‥‥‥‥‥‥62.2 Ground water at the tillering stage‥‥‥‥‥ 82.6. Ground water at the reproductive stage ‥‥‥‥‥ 74.1. \circled5 Ripening percentage is about 70 percent on the test plot in which ground water irrigation is practised during all the growth stages and at the tillering stage only. However, when ground water irrigation is practised, at the reproductive stage, the ripening percentage is reduced to 50 percent. This means that 20 percent reduction in the ripening percentage by using ground water irrigation at the reproductive stage. \circled6 The weight of 1,000 kernels is found to show a similar tendency as in the case of ripening percentage i. e. the ground water irrigation during all the growth stages and at the reproductive stage results in a decreased weight of the 1,000 kernels. \circled7 The yield of brown rice from the various treatments are as follows; Gravity flow; Surface water at all growth stages‥‥‥‥‥‥514kg/10a. Ground water at all growth stages‥‥‥‥‥‥428kg/10a. Ground water at the reproductive stage‥‥‥‥‥‥430kg/10a. Standing water; Surface water at all growh stages‥‥‥‥‥‥556kg/10a. Ground water at all growth stages‥‥‥‥‥‥441kg/10a. Ground water at the reproductive stage‥‥‥‥‥‥450kg/10a. The above figures show that ground water irrigation by the gravity flow and by the standing water method during all the growth stages resulted in an 18 percent and a 21 percent decrease in the yield of brown rice, respectively, when compared with surface water irrigation. Also ground water irrigation by gravity flow and by standing water resulted in respective decreases in yield of 16 percent and 19 percent, compared with the surface irrigation method. 4. Results obtained from the experiments on the improvement of ground water irrigation efficiency to paddy rice are as follows; (1) When the standing water irrigation with surface water is practised, the daily average water temperature in a paddy field is 25.2$^{\circ}C$, but, when the gravity flow method is practised with the same irrigation water, the daily average water temperature is 24.5$^{\circ}C$. This means that the former is 0.7$^{\circ}C$ higher than the latter. On the other hand, when ground water is used, the daily water temperatures in a paddy field are respectively 21.$0^{\circ}C$ and 19.3$^{\circ}C$ by practising standing water and the gravity flow method. It can be seen that the former is approximately 1.$0^{\circ}C$ higher than the latter. (2) When the non-water-logged cultivation is practised, the yield of brown rice is 516.3kg/10a, while the yield of brown rice from ground water irrigation plot throughout the whole irrigation period and surface water irrigation plot are 446.3kg/10a and 556.4kg/10a, respectivelely. This means that there is no significant difference in yields between surface water irrigation practice and non-water-logged cultivation, and also means that non-water-logged cultivation results in a 12.6 percent increase in yield compared with the yield from the ground water irrigation plot. (3) The black and white coloring on the inside surface of the water warming ponds has no substantial effect on the temperature of the water. The average daily water temperatures of the various water warming ponds, having different depths, are expressed as Y=aX+b, while the daily average water temperatures at various depths in a water warming pond are expressed as Y=a(b)x (where Y: the daily average water temperature, a,b: constants depending on the type of water warming pond, X; water depth). As the depth of water warning pond is increased, the diurnal difference of the highest and the lowest water temperature is decreased, and also, the time at which the highest water temperature occurs, is delayed. (4) The degree of warming by using a polyethylene tube, 100m in length and 10cm in diameter, is 4~9$^{\circ}C$. Heat exchange rate of a polyethylene tube is 1.5 times higher than that or a water warming channel. The following equation expresses the water warming mechanism of a polyethylene tube where distance from the tube inlet, time in day and several climatic factors are given: {{{{ theta omega (dwt)= { a}_{0 } (1-e- { x} over { PHI v })+ { 2} atop { SUM from { { n}=1} { { a}_{n } } over { SQRT { 1+ {( n omega PHI) }^{2 } } } } LEFT { sin(n omega t+ { b}_{n }+ { tan}^{-1 }n omega PHI )-e- { x} over { PHI v }sin(n omega LEFT ( t- { x} over {v } RIGHT ) + { b}_{n }+ { tan}^{-1 }n omega PHI ) RIGHT } +e- { x} over { PHI v } theta i}}}}{{{{ { theta }_{$\infty$ }(t)= { { alpha theta }_{a }+ { theta }_{ w'} +(S- { B}_{s } ) { U}_{w } } over { beta } , PHI = { { cpDU}_{ omega } } over {4 beta } }}}} where $\theta$$\omega$; discharged water temperature($^{\circ}C$) $\theta$a; air temperature ($^{\circ}C$) $\theta$$\omega$';ponded water temperature($^{\circ}C$) s ; net solar radiation(ly/min) t ; time(tadian) x; tube length(cm) D; diameter(cm) ao,an,bn;constants determined from $\theta$$\omega$(t) varitation. cp; heat capacity of water(cal/$^{\circ}C$ ㎥) U,Ua; overall heat transfer coefficient(cal/$^{\circ}C$ $\textrm{cm}^2$ min-1) $\omega$;1 velocity of water in a polyethylene tube(cm/min) Bs ; heat exchange rate between water and soil(ly/min)

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Chemical Modification of 5-Lipoxygenase from the Korean Red Potato

  • Kim, Kyoung-Ja
    • BMB Reports
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    • 제33권2호
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    • pp.172-178
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    • 2000
  • The lipoxygenase was purified 35 fold to homogeneity from the Korean red potato by an ammonium sulfate precipitation and DEAE-cellulose column chromatography. The simple purification method is useful for the preparation of pure lipoxygenase. The molecular weight of the enzyme was estimated to be 38,000 by SDS-polyacrylamide gel electrophoreses and Sepharose 6B column chromatography. The purified enzyme with 2 M $(NH_4)_2SO_4$ in a potassium phosphate buffer, pH 7.0, was very stable for 5 months at $-20^{\circ}C$. Because the purified lipoxygenase is very stable, it could be useful for the screening of a lipoxygenase inhibitor. The optimal pH and temperature for lipoxygenase purified from the red potato were found to be pH 9.0. and $30^{\circ}C$, respectively. The Km and Vmax values for linoleic acid of the lipoxygenase purified from the red potato were $48\;{\mu}M$ and $0.03\;{\mu}M$ per minute per milligram of protein, respectively. The enzyme was insensitive to the metal chelating agents tested (2 mM KCN, 1 and 10mM EDTA, and 1 mM $NaN_3$), but was inhibited by several divalent cations, such as $Cu^{++}$, $Co^{++}$ and $Ni^{++}$. The essential amino acids that were involved in the catalytic mechanism of the 5-lipoxygenase from the Korean red potato were determined by chemical modification studies. The catalytic activity of lipoxygenase from the red potato was seriously reduced after treatment with a diethylpyrocarbonate (DEPC) modifying histidine residue and Woodward's reagent (WRK) modifying aspartic/glutamic acid. The inactivation reaction of DEPC (WRK) processed in the form of pseudo-first-order kinetics. The double-logarithmic plot of the observed pseudo-first-order rate constant against the modifier concentration yielded a reaction order 2, indicating that two histidine residues (carboxylic acids) were essential for the lipoxygenase activity from the red potato. The linoleic acid protected the enzyme against inactivation by DEPC(WRK), revealing that histidine and carboxylic amino acids residues were present at the substrate binding site of the enzyme molecules.

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Modulation of Cytotoxicity by Nitric Oxide Donors during Treatment of Glioma with Anticancer Drugs

  • Park, Jeong-Jae;Kang, Jong-Sool;Lee, Hyun-Sung;Lee, Jong-Soo;Lee, Young-Ha;Youm, Jin-Young
    • Journal of Korean Neurosurgical Society
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    • 제38권5호
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    • pp.366-374
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    • 2005
  • Objective : Nitric oxide[NO] is implicated in a wide range of biological processes in tumors and is produced in glioma. To investigate the role of NO and its interaction with the tumoricidal effects of anticancer drugs, we study the antitumor activities of NO donors, with or without anticancer drugs, in human glioma cell lines. Methods : U87MG and U373MG cells were treated with the NO donors sodium nitroprusside[SNP] and S-nitroso-N-acetylpenicillamine[SNAP], alone or in combination with the anticancer drugs 1,3-bis[2-chloroethyl]-1-nitrosourea[BCNU] and cisplatin. Cell viability, cell proliferation, DNA fragmentation, nitrite level, and the expression of Bcl-2 and Bax were determined. Results : NO was markedly increased after treatment with SNP or SNAP; however, the addition of the anticancer drugs did not significantly affect NO production NO donors or anticancer drugs reduced glioma cell viability and, in combination, acted synergistically to further decrease cell viability in a dose- and time-dependent manner. Cell proliferation was inhibited and apoptosis were enhanced by combined treatment. Bax expression was increased by combined treatment, whereas Bcl-2 expression was reduced. The antitumor cytotoxicity of NO donors and anticancer drugs differed according to cell type. Conclusion : BCNU or cisplatin can inhibit cell viability and proliferation of glioma cells and can induce apoptosis. These effects are further enhanced by the addition of a NO donor which modulates the antitumor cytotoxicity of chemotherapy depending on cell type. Further biological, chemical, and toxicological studies of NO are required to clarify its mechanism of action in glioma.

백서의 반복적인 육체운동에 의한 사염화탄소 간독성의 증폭효과 (Potentiation of Carbon Tetrachloride Hepatotoxicity induced by Repeated Physical Exercise in adult Female rats)

  • 김수년;김영철
    • Toxicological Research
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    • 제8권2호
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    • pp.265-272
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    • 1992
  • Effects of repeated physical exercise on the carbon tetrachloride ($CCl_4$) hepatotoxicity were examined in adult female rats. Rats were introduced into a cylindrical rotating cage and forced to exercise for 1 hr each day, 6days/week, for 5 consecutive weeks at a speed starting from 10m/min, increased by 1m/min per day until the speed reached 27m/min. Significantly less body weight gain was observed in the exercise group suggesting that physical fitness had been induced in these animals. Eighteen hours following termination of the last exercise bout rats were treated with $CCl_4$(2 mmol/kg.ip). The $CCl_4$-induced heptotoxicity was significantly potentiated in the repeated exercise group compared to the resting sedentary animals as determined by changes in serum sorbitol dehydrogenase (SDH), glutamic oxaloacetic transaminase(GOT), glutamic pyruvic transaminase (GPT), and glucose-6-phosphatase(G-6-Pase) activities when measured 24hrs following the $CCl_4$ treatment. Hepatic drug metabolizing activity was determined in order to elucidate the underlying mechanism of potentiating action of the $CCl_4$ hepatotoxicity induced by repeated physical exercise. Repeated exercise increased the hepatic microsomal cytochrome P-450 contents and aminopyrine N-demethylase activity. The results suggest that the potentiation of $CCl_4$ hepatotoxicity by repeated exercise is associated with induction of the mixed function oxidase (MFO) enzyme system mediating the metabolism of $CCl_4$ to its active metabolite(s).

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Human Neutrophil Elastase Inhibitory Alkaloids from Chelidonium majus L.

  • Kim, Jeong Yoon;Lee, Ji Hye;Song, Yeong Hun;Jeong, Won Min;Tan, Xuefei;Uddin, Zia;Park, Ki Hun
    • Journal of Applied Biological Chemistry
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    • 제58권3호
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    • pp.281-285
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    • 2015
  • Human neutrophil elastase (HNE) represents a good therapeutic target for the treatment of inflammatory diseases as well as invasion of microorganism. The methanol extract of a aerial part of Chelidonium majus L. showed high activity against the neutrophil elastase with an $IC_{50}$ value of $100{\mu}g/mL$. Due to its potency, subsequent bioactivity-guided fractionation of methanol extract led to six alkaloids (1-6), which were identified as dihydrosanguinarine (1), (s)-stylopine (2), arnottianamide (3), (+)-chelidonine (4), spallidamine (5), and N-trans-feruloyltyramine (6). Among of them, three alkaloids (2, 5, and 6) inhibited HNE in a dose-dependent manner with $IC_{50}$ ranging between 11.6 and $51.0{\mu}M$. Lineweaver-Burk and Dixon plots, and their secondary replots showed that alkaloids (2, 5, and 6) were mixed inhibitors of HNE. The analysis of $K_I$ and $K_{IS}$ value proved that all inhibitors (2, 5, and 6) had reversible mixed type I mechanism.

Effects of Antioxidants on the Gamma-Radiation Damage of the Cultured Vascular Smooth Mucle Cells of Rat Aorta

  • Lee, Jong-Doo;Choi, Hyoung-Chul;Kang, Young-Jin;Kim, Myung-Se;Lee, Kwang-Youn
    • The Korean Journal of Physiology and Pharmacology
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    • 제11권5호
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    • pp.189-195
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    • 2007
  • To study the protective effects of antioxidants on the radiation damages of the cells, vascular smooth muscle cells(VSMC) from thoracic aorta of Sprague-Dawley rats were cultured and irradiated with gamma-ray. Cell viability was measured by direct cell counting and MTT assay, and flow cytometry was performed to measure fractional distributions of the cells. Gamma-ray irradiation inhibited cell proliferations accompanied with decreased G1 phase and increased S- and G2/M phases, and the maximum effects were observed at 1500 or 2000 cGy. Submaximal concentrations of antioxidants, such as allopurinol, vitamin C, N-acetylcycteine(NAC), lipoic acid, dihydrolipoic acid and rebamipide tended to increase the cell viability suppressed by low dose of radiation(500 cGy), and enalapril and vitamin E increased it significantly. Allopurinol, vitamin E, NAC, lipoic acid, captopril and enalapril significantly increased G1 phase. Allopurinol and vitamin E tended to increase c-Myc expression, detected by Western blot, that was reduced by the radiation, and enalapril increased it significantly. The cell viability and c-Myc expression were highly correlated(r=0.97) with each other. These results suggest that antioxidants, especially enalapril and vitamin E, recover the viability of VSMC from gamma-radiation injury, through a mechanism which includes increase of c-Myc protein expression.