• Title/Summary/Keyword: ATM inhibition

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Molecular Structure of PCP Pincer Complexes: Poisoning Catalyst on the Dehydrogenation of Alkanes (알칸의 탈수소화반응에서의 촉매독 화합물의 분자구조)

  • Lee Ji Hyun;Chun Sang Jin;Kwon Ki Hyeok;Lee Do Weon
    • Korean Journal of Crystallography
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    • v.16 no.1
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    • pp.43-53
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    • 2005
  • The dihydrido P-C-P pincer complex, $IrH_2{C_6H_3-2,6-(CH_2PBu_2^t)_2}$ (1), was successfully prepared from the reaction of the hydrochloride complex, $IrClH (C_6H_3-2,6-(CH_2PBu_2^t)_2}$, and super acid $(LiBEt_3H)$ under 1 atm of hydrogen in pentane solution at room temperature and followed by Heating at $130^{\circ}C$ in vacuo. Jensen recently found that the dihydrido P-C-P pincer complex 1 is a highly active homogeneous catalyst for the transfer dehydrogenation of alkanes with unusual longterm stability at temperatures as high as $200^{\circ}C$. The treatment of dihydrido complex 1 with nitrogen, water, carbon dioxide, and carbon monoxide in presence of tert-butylethylene (the) at room temperature in an appropriate solution gave the dinitrogen complex, $[Ir{C-6H_3-2,6-(CH_2PBu_2^t)_2}]_2({\mu}-N_2)$ (2), the hydrido hydroxyl complex, $IrH(OH){C_6H_3-2,6-(CH_2PBu_2^t)_2}$ (3), the carbon dioxide complex, $Ir({\eta}^2-CO_2) {C_6H_3-2,6-(CH_2PBu_2^t)_2}$ (including the bicarbonate complex, $IrH({\kappa}^2-O_2COH){C_6H_3-2,6-(CH_2PBu_2^t)_2}\;(4))$, and the carbonyl complex, $Ir(CO) {C_6H_3-2,6-(CH_2PBu_2^t)_2}\;(5)$ (including the carboxyl complex, $IrH(C(O)OH) {C_6H_3-2,6-(CH_2PBu_2^t)_2}\;(6))$, in good yield, respectively. These P-C-P iridium complexes were isolated and characterized by $^1H,\;^{13}C,\;^{31}P\; NMR$, and IR spectroscopy. In addition, the complexes (1-6) were characterized by a single crystal X-ray crystallography. These complexes account for these small molecules' inhibition of dehydrogenation of alkanes catalyzed by the dihydrido complex 1.

Cariporide Enhances the DNA Damage and Apoptosis in Acid-tolerable Malignant Mesothelioma H-2452 Cells

  • Lee, Yoon-Jin;Bae, Jin-Ho;Kim, Soo-A;Kim, Sung-Ho;Woo, Kee-Min;Nam, Hae-Seon;Cho, Moon-Kyun;Lee, Sang-Han
    • Molecules and Cells
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    • v.40 no.8
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    • pp.567-576
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    • 2017
  • The $Na^+/H^+$ exchanger is responsible for maintaining the acidic tumor microenvironment through its promotion of the reabsorption of extracellular $Na^+$ and the extrusion of intracellular $H^+$. The resultant increase in the extracellular acidity contributes to the chemoresistance of malignant tumors. In this study, the chemosensitizing effects of cariporide, a potent $Na^+/H^+-exchange$ inhibitor, were evaluated in human malignant mesothelioma H-2452 cells preadapted with lactic acid. A higher basal level of phosphorylated (p)-AKT protein was found in the acid-tolerable H-2452AcT cells compared with their parental acid-sensitive H-2452 cells. When introduced in H-2452AcT cells with a concentration that shows only a slight toxicity in H-2452 cells, cariporide exhibited growth-suppressive and apoptosis-promoting activities, as demonstrated by an increase in the cells with pyknotic and fragmented nuclei, annexin V-PE(+) staining, a $sub-G_0/G_1$ peak, and a $G_2/M$ phase-transition delay in the cell cycle. Preceding these changes, a cariporide-induced p-AKT down-regulation, a p53 up-regulation, an ROS accumulation, and the depolarization of the mitochondrial-membrane potential were observed. A pretreatment with the phosphatidylinositol-3-kinase (PI3K) inhibitor LY294002 markedly augmented the DNA damage caused by the cariporide, as indicated by a much greater extent of comet tails and a tail moment with increased levels of the p-histone H2A.X, $p-ATM^{Ser1981}$, $p-ATR^{Ser428}$, $p-CHK1^{Ser345}$, and $p-CHK2^{Thr68}$, as well as a series of pro-apoptotic events. The data suggest that an inhibition of the PI3K/AKT signaling is necessary to enhance the cytotoxicity toward the acidtolerable H-2452AcT cells, and it underlines the significance of proton-pump targeting as a potential therapeutic strategy to overcome the acidic-microenvironment-associated chemotherapeutic resistance.

Effect of Nutrient Supply Cut-off Periods Before Harvest on Storability of Chicon (수확 전 단수처리가 치콘 저장성에 미치는 영향)

  • Jung, Hyun-Jin;Choi, In-Lee;Son, Jin-Sung;Seo, Hyun-Taek;Won, Jae-Hee;Kang, Ho-Min
    • Journal of Bio-Environment Control
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    • v.20 no.4
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    • pp.406-411
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    • 2011
  • This study was conducted to find out the effect of cut-off period (0 hour, 3 hours, 6 hours, 12 hours, and 24 hours) to supply nutrient solution for chicon forcing at that was predrying treatment on the storability of chicon. The cut-off treatment increased dry matter rate, respiration rate, and ethylene production rate. The dry matter rate of chicon increased, as the cut-off period increased, but the respiration rate and ethylene production rate of chicon was highest in 12 hours and 6 hours cut-off treatment, respectively, and then their rates decreased, as the cut-off period prolonged. The weight loss at cut-off 6 hours treatment was lower than other treatments during $10^{\circ}C$ storage temperature. The cut-off 6 hours treatment showed higher carbon dioxide and oxygen concentration in 10,000 cc/$m^2$/day/atm oxygen permeability film package during storage period than control and showed a little predrying effect but was not statistically significant. At $4^{th}$ day, the ethylene concentration reached higher than other storage day and after that decreased but was not statistically significant. The quality of chicon for 3 hours, 6 hours, 24 hours cut-off treatments on storability showed higher than other treatments, accordingly. The 6 hours cut-off treatment showed the inhibited effect of the degree of browning of chicon cutting plane. The effect of 6 hours cut-off treatment on storability of chicon showed proper predrying effect, reduced moisture loss and browning inhibition apparently during $10^{\circ}C$ storage.

Effect of Chlorine Dioxide, Cold Plasma Gas Sterilization and MAP Treatment on the Quality and Microbiological Changes of Paprika During Storage (이산화염소 및 저온 플라즈마 가스 살균 및 MAP 처리가 파프리카의 저장 중 품질과 미생물학적 변화에 미치는 영향)

  • In-Lee, Choi;Joo Hwan, Lee;Yong Beom, Kwon;Yoo Han, Roh;Ho-Min, Kang
    • KOREAN JOURNAL OF PACKAGING SCIENCE & TECHNOLOGY
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    • v.28 no.3
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    • pp.223-229
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    • 2022
  • This study was conducted to investigate the effect of packaging methods and sterilization treatment on storability and microbial control in paprika fruits. When treated with chlorine dioxide gas for 3, 6, and 12 hours and cold plasma gas for 1, 3, and 6 hours, and then packed in a carton box and stored in a 8 ± 1℃ chamber for 7 days, chlorine dioxide treated 12 hours and plasma treated 6 hours was prevented the development of E·coli and YM(yeast and mold). Accordingly, the control was treated with chlorine dioxide for 12 hours and plasma for 6 hours, packed using a carton box and 40,000 cc·m-2·day-1·atm-1 OTR film (MAP), and stored in a 8 ± 1℃ chamber for 20 days. Fresh weight loss rate during storage was less than 1% in the MAP treatments, and the visual quality of the MAP treatments was above the marketability limit until the end of storage. There was no difference in the contents of oxygen, carbon dioxide, and ethylene in the film. In the case of firmness, the chlorine dioxide treatments was low, and the Hunter a* value, which showed chromaticity, was highest in the Plasma 6h MAP treatment. Off-odor was investigated in the MAP treatments, but it was very low. The rate of mold growth on the fruit stalk of paprika was the fastest and highest in the chlorine dioxide treated box packaging treatments, and the lowest in the chlorine dioxide treated MAP treatments at the end of storage. The aerobic count in the pulp on the storage end date was the lowest in the plasma treated box packaging treatments, the lowest number of E·coli in the chlorine dioxide treated MAP treatments, and the lowest yeast & mold in the chlorine dioxide treated box packaging treatments. As a result, for the inhibition of microorganisms during paprika storage, it is considered appropriate to treat plasma for 6 hours before storage regardless of the packaging method.