Simple Synthesis of Multi-Halogen Pyrazino[1,2-a]indole-1,8(2H,5aH)-diones

Rui-Xia Yang,Yu-Cheng Zhao,Ling-Bin Kong,Sheng-jiao Yan,Jun Lin 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.10

A concise and efficient one-pot synthesis of multi-halogen pyrazino[1,2-a]indole-1,8(2H,5aH)-dione (MHPID) derivatives by the reaction of an enamino ester with multi-halogen benzoquinone derivatives is described. MHPIDs 3a–3d were obtained with good yields (78–83%) by refluxing enamino esters 1a and 1b and tetrahalogen-1,4-benzoquinones 2a and 2b for 24 h without the use of catalysts. Compounds 3e–3p were also obtained with excellent yields (69–92%) via the reaction of the phenyl-substituted enamino esters 1c–1h with tetrahalogen-1,4-benzoquinones 2a and 2b in CH3CN catalyzed by Cs2CO3. These two protocols are efficient and effective for the synthesis of MHPIDs.

Cell surface vimentin-targeted monoclonal antibody 86C increases sensitivity to temozolomide in glioma stem cells

Noh, Hyangsoon,Zhao, Qingnan,Yan, Jun,Kong, Ling-Yuan,Gabrusiewicz, Konrad,Hong, Sungguan,Xia, Xueqing,Heimberger, Amy B.,Li, Shulin Elsevier 2018 Cancer letters Vol.433 No.-

<P><B>Abstract</B></P> <P>Glioblastoma multiforme (GBM) is the most prevalent and aggressive brain tumor. The current standard therapy, which includes radiation and chemotherapy, is frequently ineffective partially because of drug resistance and poor penetration of the blood-brain barrier. Reducing resistance and increasing sensitivity to chemotherapy may improve outcomes. Glioma stem cells (GSCs) are a source of relapse and chemoresistance in GBM; sensitization of GSCs to temozoliomide (TMZ), the primary chemotherapeutic agent used to treat GBM, is therefore integral for therapeutic efficacy. We previously discovered a unique tumor-specific target, cell surface vimentin (CSV), on patient-derived GSCs. In this study, we found that the anti-CSV monoclonal antibody 86C efficiently increased GSC sensitivity to TMZ. The combination TMZ+86C induced significantly greater antitumor effects than TMZ alone in eight of 12 GSC lines. TMZ+86C–sensitive GSCs had higher CSV expression overall and faster CSV resurfacing among CSV<SUP>−</SUP> GSCs compared with TMZ+86C–resistant GSCs. Finally, TMZ+86C increased apoptosis of tumor cells and prolonged survival compared with either drug alone in GBM mouse models. The combination of TMZ+86C represents a promising strategy to reverse GSC chemoresistance.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Anti-CSV monoclonal antibody 86C sensitize GSCs to TMZ treatment. </LI> <LI> GSCs with higher CSV expression are more sensitive to TMZ+86C. </LI> <LI> GSCs with higher CSV resurfacing rate among CSV<SUP>−</SUP> cells are more sensitive to TMZ+86C. </LI> <LI> TMZ+86C increased apoptosis and prolonged survival in GBM models. </LI> <LI> Tumor-specific CSV antibody 86C can efficiently target human GSCs to increase their sensitivity to TMZ. </LI> </UL> </P>

Theoretical Study of the Reaction Mechanism for SiF₂ Radical with HNCO

Hou, Li-Jie,Wu, Bo-Wan,Kong, Chao,Han, Yan-Xia,Chen, Dong-Ping,Gao, Li-Guo Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.12

The reaction mechanism of $SiF_2$ radical with HNCO has been investigated by the B3LYP method of density functional theory(DFT), while the geometries and harmonic vibration frequencies of reactants, intermediates, transition states and products have been calculated at the B3LYP/$6-311++G^{**}$ level. To obtain more precise energy result, stationary point energies were calculated at the CCSD(T)/$6-311++G^{**}$//B3LYP/$6-311++G^{**}$ level. $SiF_2+HNCO{\rightarrow}IM3{\rightarrow}TS5{\rightarrow}IM4{\rightarrow}TS6{\rightarrow}OSiF_2CNH(P3)$ was the main channel with low potential energy, $OSiF_2CNH$ was the main product. The analyses for the combining interaction between $SiF_2$ radical and HNCO with the atom-in-molecules theory (AIM) have been performed.

Theoretical Study of the Reaction Mechanism for SiF2 Radical with HNCO

Li-Jie Hou,Bo-Wan Wu,Chao Kong,Yan-Xia Han,Dong-Ping Chen,Li-Guo Gao 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.12

The reaction mechanism of SiF2 radical with HNCO has been investigated by the B3LYP method of density functional theory(DFT), while the geometries and harmonic vibration frequencies of reactants, intermediates, transition states and products have been calculated at the B3LYP/6-311++G** level. To obtain more precise energy result, stationary point energies were calculated at the CCSD(T)/6-311++G**//B3LYP/6-311++G** level. SiF2+HNCO→IM3→TS5→IM4→TS6→OSiF2CNH(P3) was the main channel with low potential energy, OSiF2CNH was the main product. The analyses for the combining interaction between SiF2 radical and HNCO with the atom-in-molecules theory (AIM) have been performed.

Carbon-Ion-Implanted Nd, MgO-Codoped Near-Stoichiometric Lithium-Niobate Optical Waveguides

Ning-Ning Dong,Yang Tan,Yan-Xia Kong,Feng Chen,Hong-Ji Ma 한국물리학회 2009 THE JOURNAL OF THE KOREAN PHYSICAL SOCIETY Vol.55 No.6

Nd, MgO codoped near stoichiometric lithium niobate (Nd:MgO:SLN) is a promising laser gain crystal for infrared laser generations. We report on, to our knowledge for the first time, the planar waveguide formation in Nd:MgO:SLN crystal by MeV carbon ion implantation at dose of 1014 ions/cm2. The guiding properties are investigated by using the well-known m-line technique and end-face arrangement. The refractive index profiles of the waveguides show a typical “well + barrier” distribution, which could confine the light propagation in a non-leaky way. In addition, a numerical simulation of the light propagation shows that the waveguide modal distributions are in good agreement with the experimental data, which means potential applications for the formation of designable devices in Nd:MgO:SLN by using carbon ion implantation. Nd, MgO codoped near stoichiometric lithium niobate (Nd:MgO:SLN) is a promising laser gain crystal for infrared laser generations. We report on, to our knowledge for the first time, the planar waveguide formation in Nd:MgO:SLN crystal by MeV carbon ion implantation at dose of 1014 ions/cm2. The guiding properties are investigated by using the well-known m-line technique and end-face arrangement. The refractive index profiles of the waveguides show a typical “well + barrier” distribution, which could confine the light propagation in a non-leaky way. In addition, a numerical simulation of the light propagation shows that the waveguide modal distributions are in good agreement with the experimental data, which means potential applications for the formation of designable devices in Nd:MgO:SLN by using carbon ion implantation.

Intersubband Transitions in Nonpolar GaN-based Resonant Phonon Depopulation Multiple-Quantum Wells for Terahertz Emissions

Ya-Feng Song,Xiong-Xiong Kong,Wei-Bin Tang,Zhong-Qiang Suo,Huan Zhang,Chen-Yang Li,Qian Jia,Cai-Xia Xue,Yan-Wu Lu,Chao-Pu Yang 한국물리학회 2019 THE JOURNAL OF THE KOREAN PHYSICAL SOCIETY Vol.74 No.11

We investigate the polarization effect in intersubband transitions in polar and nonpolar GaN-based multiple-quantum well (MQW) structures for terahertz (THz) emissions by using systematic comparisons and design a nonpolar GaN/Al$_{0.2}$Ga$_{0.8}$N two-well-based MQW structure with an emitting photon of 7.27 THz (30.07 meV). Its lower energy separation (92.7 meV) matches the resonant phonon depopulation condition for better population inversion. It shows a lower threshold current density $J\rm_{th}$ at all temperatures (1.548 kA/cm$^2$ at 90 K) and a higher output power of up to 86.1 mW at 5.8 K and 33.6 mW at 100 K. Our results for the polar GaN MQW are very close to the experimental data in the literature. We find that the $J\rm_{th}$ of the nonpolar GaN MQW increases more slowly than that of the polar GaN MQW as temperature increases, indicating the nonpolar GaN MQW may be a worth-trying direction for improving the operation temperature. These results can provide meaningful references for the design and fabrication of nonpolar GaN-based THz MQW or quantum cascade structures.

In Vivo Protein Transduction: Delivery of PEP-1-SOD1 Fusion Protein into Myocardium Efficiently Protects against Ischemic Insult

You-en Zhang,Jia-ning Wang,Jun-ming Tang,Ling-yun Guo,Jian-ye Yang,Yong-zhang Huang,Yan Tan,Shou-zhi Fu,Xia Kong,Fei Zheng 한국분자세포생물학회 2009 Molecules and cells Vol.27 No.2

Myocardial ischemia-reperfusion injury is a medical problem occurring as damage to the myocardium following blood flow restoration after a critical period of coronary occlusion. Oxygen free radicals (OFR) are implicated in reperfusion injury after myocardial ischemia. The antioxidant enzyme, Cu, Zn-superoxide dismutase (Cu, Zn-SOD, also called SOD1) is one of the major means by which cells counteract the deleterious effects of OFR after ischemia. Recently, we reported that a PEP-1-SOD1 fusion protein was efficiently delivered into cultured cells and isolated rat hearts with ischemia-reperfusion injury. In the present study, we investigated the protective effects of the PEP-1-SOD1 fusion protein after ischemic insult. Immunofluorescecnce analysis revealed that the expressed and purified PEP-1-SOD1 fusion protein injected into rat tail veins was efficiently transduced into the myocardium with its native protein structure intact. When injected into Sprague-Dawley rat tail veins, the PEP-1-SOD1 fusion protein significantly attenuated myocardial ischemia-reperfusion damage; characterized by improving cardiac function of the left ventricle, decreasing infarct size, reducing the level of malondialdehyde (MDA), decreasing the release of creatine kinase (CK) and lactate dehydrogenase (LDH), and relieving cardiomyocyte apoptosis. These results suggest that the biologically active intact forms of PEP-1-SOD1 fusion protein will provide an efficient strategy for therapeutic delivery in various diseases related to SOD1 or to OFR.