Amide Moieties Modulate the Antimicrobial Activities of Conjugated Oligoelectrolytes against Gram-negative Bacteria

Cationic conjugated oligoelectrolytes (COEs) are a class of compounds that can be tailored to achieve relevant in vitro antimicrobial properties with relatively low cytotoxicity against mammalian cells. Three distyrylbenzene-based COEs were designed containing amide functional groups on the side chains. Their properties were compared to two representative COEs with only quaternary ammonium groups. The optimal compound, COE2−3C−C3-Apropyl , has an antimicrobial efficacy against Escherichia coli with an MIC=2 μg mL⁻¹, even in the presence of human serum albumin low cytotoxicity (IC₅₀=740 μg mL⁻¹) and minimal hemolytic activity. Moreover, we find that amide groups increase interactions between COEs and a bacterial lipid mimic based on calcein leakage assay and allow COEs to readily permeabilize the cytoplasmic membrane of E. coli. These findings suggest that hydrogen bond forming moieties can be further applied in the molecular design of antimicrobial COEs to further improve their selectivity towards bacteria.     

Coumarin Sulfonamides and Amides Derivatives: Design,Synthesis, and Antitumor Activity In Vitro

Coumarins possesses immeasurable antitumor potential with minimum side effects depending on the substitutions on the basic nucleus, which exhibits great prospects for antitumor drug development. In an attempt to develop novel antitumor candidates, a series of coumarin sulfonamides and amides derivatives were designed and synthetized. The majority of these derivatives showed good cytotoxic activity against MDA-MB-231 and KB cell lines, among which compound 9c was the most potent against MDA-MB-231 cells, with IC₅₀ value of 9.33 μM, comparable to 5-fluorouracil. Further investigation revealed that compound 9c had versatile properties against tumors, including inhibition of cell migration and invasion as well as inducing apoptosis. Reactive oxygen species (ROS) assay and western blotting analysis suggested that compound 9c promoted cancer cell apoptosis by increasing ROS levels and upregulating the expression of caspase-3 in MDA-MB-231 cells. These results indicated that compound 9c could be promising lead compound for further antitumor drug research.     

Natural killer cell-derived extracellular vesicle significantly enhanced adoptive T cell therapy against solid tumors via versatilely immunomodulatory coordination

Science China Chemistry - Insufficient tumor tropism, MHC class I molecules (MHC-I) defects of tumor cells, and immunosuppressive tumor micro-environment (TME) seriously imperil the efficacy of...     

Pyrazole-based trinuclear and mononuclear complexes: synthesis,characterization, DNA interactions and cytotoxicity studies

Transition Metal Chemistry - A new trinuclear Cu(II) complex [Cu3(μ3-OH)(μ-pz)3(Hpz)2(HCOO)(BTAO)Cl] (1) (Hpz = pyrazole, BTAO = 4,6-bis(dimethylamino)-1,3,5-triazin-2(1H)-one) and four...     

具有聚集诱导发光特性的含氟有机金属配合物的研究进展

近年来,具有聚集诱导发光(aggregation-induced emission,AIE)特性的化合物由于在聚集态或固态发光量子效率较高而受到很多关注.含氟的功能化合物,由于氟原子的存在,往往具有独特的结构和物理、化学及生物学性质.根据中心金属和配体的种类,汇总了具有A IE性质的且含有氟代配体的有机金属配合物的研究进展.这些含氟有机金属配合物主要是铱、铂、金配合物,在发光器件、化学传感、细胞成像、数据存储等方面具有潜在应用.还简要讨论了相关研究的发展前景.     

Carbon dots/Bi_2WO_6 composite with compensatory photo-electronic effect for overall water photo-splitting at normal pressure

Overall water photo-splitting is a prospective ideal pathway to produce ultra-clean H_2 energy by semiconductors.However,the band structure of many semiconductors cannot satisfy the requirement of H_2 and O_2 production at the same time.Herein,we illustrate that carbon dots(CDs)/Bi_2 WO_6 photocatalyst with compensatory photo-electronic effect has enhanced activity for overall water photo-splitting without any sacrificial agent.In this complex photocatalytic system,the photo-potential provided by CDs makes the CDs/Bi_2 WO6(C-BWO) composite could satisfy the band structure conditions for overall water photo-splitting.The C-BWO composite(3 wt% CDs content) exhibits optimized hydrogen evolution(oxygen evolution) of 0.28 μmol/h(0.12 μmol/h) with an approximate 2:1(H_2:O_2) stoichiometry at normal pressure.We further employed the in-situ transient photovoltage(TPV) technique to study the photoelectron extraction and the interface charge transfer kinetics of this composite catalyst.     

粗糙表面涂覆目标的太赫兹波散射特性研究

对具有涂覆层目标的太赫兹波段粗糙表面的散射特性进行了研究. 考虑到表面粗糙度的影响, 可先对反射系数进行修正, 再利用反射系数对等效电磁流进行修正, 得到粗糙涂覆表面的等效电磁流, 然后在物理光学方程的基础上得到粗糙表面涂覆目标的雷达散射截面; 最后进行图形电磁学可视化计算, 并采用Visual C++对模型进行OpenGL显示, 提取像素面元的有效信息对所得理论进行了仿真分析, 研究了不同入射角度、不同频率、不同介质、不同粗糙度和不同涂层厚度下的太赫兹波电磁散射特性, 得到了一些有参考价值的结论.     

Phase transitions in a holographic s $$$$ p model with back-reaction

In a previous paper (Nie et al. in JHEP 1311:087, arXiv:1309.2204 [hep-th], 2013), we presented a holographic s \(+\) p superconductor model with a scalar triplet charged under an SU(2) gauge field in the bulk. We also study the competition and coexistence of the s-wave and p-wave orders in the probe limit. In this work we continue to study the model by considering the full back-reaction. The model shows a rich phase structure and various condensate behaviors such as the “n-type” and “u-type” ones, which are also known as reentrant phase transitions in condensed matter physics. The phase transitions to the p-wave phase or s \(+\) p coexisting phase become first order in strong back-reaction cases. In these first order phase transitions, the free energy curve always forms a swallow tail shape, in which the unstable s \(+\) p solution can also play an important role. The phase diagrams of this model are given in terms of the dimension of the scalar order and the temperature in the cases of eight different values of the back-reaction parameter, which show that the region for the s \(+\) p coexisting phase is enlarged with a small or medium back-reaction parameter but is reduced in the strong back-reaction cases.     

Oligotriarylamines with a Pyrene Core: A Multicenter Strategy for Enhancing Radical Cation and Dication Stability and Tuning Spin Distribution

Monoamine 1 , diamines 2 – 4 , triamine 5 , and tetraamine 6 have been synthesized by substituting dianisylamino groups at the 1‐, 3‐, 6‐, and/or 8‐positions of pyrene. Diamines 2 – 4 differ in the positions of the amine substituents. No pyrene–pyrene interactions are evident in the single‐crystal packing of 3 , 4 , and 6 . With increasing numbers of amine substituents, the first oxidation potential decreases progressively from the mono‐ to the tetraamine. These compounds show intense charge‐transfer (CT) emission in CH₂Cl₂ at around 530 nm with quantum yields of 48–68 %. Upon stepwise oxidation by electrolysis or chemical oxidation, these compounds were transformed into radical cations 1 ^?+– 6 ^?+ and dications 2 ²⁺– 6 ²⁺, which feature strong visible and near‐infrared absorptions. Time‐dependent density functional theory studies suggested the presence of localized transitions from the pyrene radical cation and aminium radical cation, intervalence CT, and CT between the pyrene and amine moieties. Spectroscopic studies indicated that these radical cations and dications have good stability. Triamine 5 and tetraamine 6 formed efficient CT complexes with tetracyanoquinodimethane in solution. The results of EPR spectroscopy and density functional theory calculations suggested that the dications 2 ²⁺– 4 ²⁺ have a triplet ground state, whereas 5 ²⁺ and 6 ²⁺ have a singlet ground state. The dication of 1,3‐disubstituted diamine 4 exhibits a strong EPR signal.