EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2017
·
IF 4.519
Bing Wang,Rui-Mo Zhao,Ji Zhang,Yan-Hong Liu,Zheng Huang,Qing-Ying Yu,Xiao-Qi Yu
Although numerous cationic lipids have been developed as non-viral gene vectors , the structure-activity relationship (SAR) of these materials remains unclear and needs further investigation. In this work, a series of lysine-derived cationic lipids containing linkages with different rigidity were designed and synthesized. SAR studies showed that lipids with rigid aromatic linkage could promote the formation of tight liposomes and enhance DNA condensation, which is essential for the gene delivery process. These lipids could give much higher transfection efficiency than those containing more flexible aliphatic linkage in various cell lines. Moreover, the rigid aromatic linkage also affords the material higher serum tolerance ability. Flow cytometry assay revealed that the target lipids have good cellular uptake, while confocal microscopy observation showed weaker endosome escape than Lipofectamine 2000. To solve such problem and further increase the transfection efficiency, some lysosomotropic reagents were used to improve the endosome escape of lipoplex. As expected, higher transfection efficiency than Lipofectamine 2000 could be obtained via this strategy. Cytotoxicity assay showed that these lipids have lower toxicity in various cell lines than Lipofectamine 2000, suggesting their potential for further application. This work demonstrates that a rigid aromatic linkage might distinctly improve the gene transfection abilities of cationic lipids and affords information to construct safe and efficient gene vector towards practical application.
研究领域:
分子生物学
·
基因治疗
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
·
2018
·Vol. 34
·期 4
·536-540
·
IF 1.248
Xue Longqi,Feng Yusha,Song Yan,Wang Rui,Liu Dahai,Du Jianshi,Yang Qingbiao,Li Yaoxian
A novel water-soluble hybrid fluorescein-coumarin dye(FLNC) fluorescence ratiometric probe to recognize OCl − was designed and synthesized. The most prominent feature of the probe is that the molecular structure contains two different fluorophores, and the fluorescein moiety was connected to coumarin moiety by diacylhydrazine linker. When OCl − was added, the two fluorophores in the FLNC probe could have a rapid respond simultaneously, with high selectivity and sensitivity towards OCl – among other reactive oxygen species/reactive nitrogen species(ROS/RNS) and anions, and the detection limit was measured to be 0.30 μmol/L. In addition, the color changes of the solution could be observed by the naked eye and have a short response time(completed within 1 min), which suggestes that the probe FLNC has the potential to be used for real-time detection.
研究领域:
分析化学
·
生物化学
·
荧光光谱
✓ 已验证
DOI
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2023
·Vol. 332
·期 10
·4179-4190
·
IF 1.6
Wang Yaoxuan,Duan Siyihan,Song Wanrong,Duan Tao,Zhu Lin
The efficient removal of uranium from aqueous solutions is critical for ecological safety. Herein, a novel phytic acid and melamine covalent polymer adsorbent (named PEM) was designed and synthesized through a simple one-pot method, and its adsorption performance and mechanism of U(VI) were systematically investigated. The maximum adsorption capacity on U(VI) achieved 505.05 mg g −1 at pH 4.0, calculated with the Langmuir model, which was much higher than most other adsorbents under the same environment. Importantly, the reaction reached equilibrium quickly in the initial 20 min at 298 K. The sorption process conformed to a pseudo-second-order kinetics model and Langmuir model, indicating that the chemisorption of the monolayer was dominant. Overall, the synthesized PEM could be utilized as an easy, efficient, less time-consuming material for the removal of uranium from acidic nuclear wastewater. Graphical abstract
研究领域:
环境科学
·
化学工程
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
ChemMedChem
·
2023
·Vol. 18
·期 23
·e202300468
·
IF 3.4
Jingjie Fang,Ziyi Shang,Kumaravel Kaliaperumal,Zhiran Ju,Fen-Er Chen
Graphical This study presents a design strategy, synthesis, and evaluation of balanced COX inhibitors derived from natural anti-inflammatory ascidian metabolites and celecoxib, highlighting their potential therapeutic value in the context of inflammation. The serious adverse effects caused by non-selective and selective cyclooxygenase-2 (COX-2) inhibitors remain significant concerns for current anti-inflammatory drugs. In this study, we present the design and synthesis of a novel series of celecoxib analogs incorporating a hydrazone linker, which were subjected to in silico analysis to compare their binding poses with those of clinically used nonsteroidal anti-inflammatory drugs (NSAIDs) against COX-1 and COX-2. The synthesized analogs were evaluated for their inhibitory activity against both COX enzymes, and compound 6 m , exhibiting potent balanced inhibition, was selected for subsequent in vitro anti-inflammatory assays. Treatment with 6 m effectively suppressed the NF-κB signaling pathway in lipopolysaccharide (LPS)-stimulated murine RAW264.7 macrophages, resulting in reduced expression of pro-inflammatory factors such as inducible nitric oxide synthase (iNOS), COX-2, tumor necrosis factor- α (TNF-α), interleukin-6 (IL-6), IL-1β, as well as decreased production of prostaglandin E 2 (PGE 2 ), nitric oxide (NO), and reactive oxygen species (ROS). However, 6 m has no effect on the MAPK signaling pathway. Therefore, due to its potent in vitro anti-inflammatory activity coupled with lack of cytotoxicity, 6 m represents a promising candidate for further development as a new lead compound targeting inflammation.
研究领域:
药理学
·
药物化学
·
炎症研究
·
药物设计
✓ 已验证
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2023
·
IF 9.5
Yanhui Guo,Lukun Li,Shuheng Huang,Han Sun,Yutong Shao,Zhiliang Li,Fengling Song
Water is ubiquitous in natural systems where it builds an essential environment supporting biological supramolecular polymers to function, transport, and exchange. However, this extreme polar environment becomes a hindrance for the superhydrophobic functional π-conjugated molecules, causing significant negative impacts on regulating their aggregation pathways, structures, and properties of the subsequently assembled nanomaterials. It especially makes the self-assembly of ultrathin two-dimensional (2D) functional nanomaterials by π-conjugated molecules a grand challenge in water, although ultrathin 2D functional nanomaterials have exhibited unique and superior properties. Herein, we demonstrate the organic solvent-free self-assembly of one-molecule-thick 2D nanosheets based on exploring how side chain modifications rule the aggregation behaviors of π-conjugated macrocycles in water. Through an in-depth understanding of the roles of linking groups for side chains on affecting the aggregation behaviors of porphyrins in water, the regulation of molecular arrangement in the aggregated state (H- or J-type aggregation) was attained. Moreover, by arranging ionic porphyrins into 2D single layers through J-aggregation, the ultrathin nanosheets (thickness ≈ 2 nm) with excellent solubility and stability were self-assembled in pure water, which demonstrated both outstanding 1O2 generation and photothermal capability. The ultrathin nanosheets were further investigated as metal- and carrier-free nanodrugs for synergetic phototherapies of cancers both in vitro and in vivo, which are highly desirable by combining the advantages and avoiding the disadvantages of the single use of PDT or PTT.
研究领域:
材料科学
·
纳米技术
·
生物医学工程
·
癌症研究
·
光化学
✓ 已验证
DOI
PubMed
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2020
·Vol. 34
·期 4
·e5451
·
IF 3.14
Shuang Huang,Xi Hong,Yong Sun,He-Zhen Cui,Quan Zhou,Yue-Jian Lin,Xiu-Feng Hou
Six tridentate NNN ligand precursors derived from 2-(pyridin-2-yl)benzo[d]thiazole(PBT) with different linkers, PBT NN X N (X = NH, NMe, O, S) ( 1a – 1f ), have been successfully prepared. The electronic properties of PBT NN X N ligands are well tunable by differing linkers between PBT skeleton and the pyridine ring, and/or by introducing electron-donating/withdrawing groups on the pyridine ring (R = OMe or F). The ligand precursors and representative complexes Ru ( PBT NN NH N )Cl 2 (PPh 3 ) ( 2a ), Ru ( PBT NN NMe N )Cl 2 (PPh 3 ) ( 2b ), and Ru ( PBT NN S N )Cl 2 (PPh 3 ) ( 2f ) have been characterized by NMR spectroscopy, high-resolution mass spectroscopy, and Fourier transform infrared (FT-IR). The molecular structures of 1f , 2a , and 2f have been determined by X-ray diffraction study. The results indicate that PBT NN NH N ligand in the complex presented coplanar with two five-membered chelating rings. It should be noted that 2a featuring a NH group exhibits superior performance compared to those with other linkers (such as NMe, O, or S). A variety of heterocyclic and aromatic nitriles with aromatic and aliphatic alcohols have been explored in α -alkylation for good to excellent yields. Based on kinetic experiments and mechanistic studies, a proposed mechanism was put forward. Ru-H species and benzaldehyde, which was oxidized from benzyl alcohol, were detected in the catalytic cycle.
研究领域:
无机化学
·
有机化学
·
催化
·
材料科学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）