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Mono‐ and Dinuclear Phosphorescent Rhenium(I) Complexes: Impact of Subcellular Localization on Anticancer Mechanisms 下载免费PDF全文
Rui‐Rong Ye Dr. Cai‐Ping Tan Mu‐He Chen Liang Hao Prof. Liang‐Nian Ji Prof. Zong‐Wan Mao 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(23):7800-7809
Elucidation of relationship among chemical structure, cellular uptake, localization, and biological activity of anticancer metal complexes is important for the understanding of their mechanisms of action. Organometallic rhenium(I) tricarbonyl compounds have emerged as potential multifunctional anticancer drug candidates that can integrate therapeutic and imaging capabilities in a single molecule. Herein, two mononuclear phosphorescent rhenium(I) complexes ( Re1 and Re2 ), along with their corresponding dinuclear complexes ( Re3 and Re4 ), were designed and synthesized as potent anticancer agents. The subcellular accumulation of Re1–Re4 was conveniently analyzed by confocal microscopy in situ in live cells by utilizing their intrinsic phosphorescence. We found that increased lipophilicity of the bidentate ligands could enhance their cellular uptake, leading to improved anticancer efficacy. The dinuclear complexes were more potent than the mononuclear counterparts. The molecular anticancer mechanisms of action evoked by Re3 and Re4 were explored in detail. Re3 with a lower lipophilicity localizes to lysosomes and induces caspase‐independent apoptosis, whereas Re4 with higher lipophilicity specially accumulates in mitochondria and induces caspase‐independent paraptosis in cancer cells. Our study demonstrates that subcellular localization is crucial for the anticancer mechanisms of these phosphorescent rhenium(I) complexes. 相似文献
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AbstractIn this paper, we introduce white noise, telegraph noise and time delay to the two-dimensional foraging arena population system describing the prey and predator abundance. The aim is to find out how the interactions between white noise, telegraph noise and time delay affect the dynamics of the population system. Firstly, the existence of a global positive solution is verified. Then the long-time properties including the stochastically ultimate boundedness, extinction and some other asymptotic pathwise estimation of this population system are studied. Finally, the main results are illustrated by two examples. 相似文献
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AbstractThe present study explored the antidepressant-like activity of α-mangostin (α-MG) and the possible mechanism in this process in the tail suspension test (TST) in mice. The results revealed that α-MG (5?mg/kg, i.p.) exhibited markedly antidepressant-like activity, which could be reversed by pretreatment with haloperidol (a non-selective D2 receptor antagonist), bicuculline (a competitive GABA antagonist), p-chlorophenylalanine (an inhibitor of 5-HT synthesis). Meanwhile, α-MG also effectively increased the brain DA, 5-HT and GABA levels in mice exposed to TST, indicating that the antidepressant-like effect of α-MG might be mediated by the GABAergic, serotonergic and dopaminergic systems. 相似文献
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碳化硅功率MOSFET是宽禁带功率半导体器件的典型代表,具有优异的电气性能。基于低温环境下的应用需求,研究了1200 V碳化硅功率MOSFET在77.7 K至300 K温区的静/动态特性,定性分析了温度对碳化硅功率MOSFET性能的影响。实验结果显示,温度从300 K降低至77.7 K时,阈值电压上升177.24%,漏-源极击穿电压降低32.99%,栅极泄漏电流降低82.51%,导通电阻升高1142.28%,零栅压漏电流降低89.84%(300 K至125 K)。双脉冲测试显示,开通时间增大8.59%,关断时间降低16.86%,开关损耗增加48%。分析发现,碳化硅功率MOSFET较高的界面态密度和较差的沟道迁移率,是导致其在低温下性能劣化的主要原因。 相似文献
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Nonlinear Dynamics - An effective and simple method to solve nonlinear evolution partial differential equations is the self-similarity transformation, in which one utilizes solutions of the known... 相似文献
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Nonlinear Dynamics - In recent years, skeleton-based human action recognition has attracted substantial attentions. However, owing to the complexity and nonlinearity of human action data, it is... 相似文献