Assessment of the in vitro toxicity of calixarenes and a metal-seamed calixarene: a chemical pathway for clinical application

Calixarenes are known to form host–guest complexes and supramolecular nanoassemblies with well-defined architectures. However, the use of these materials in conjunction with drug moieties is still under explored. One reason is the insufficient biocompatibility studies. Our present study represents a systematic in vitro investigation of the cytotoxicity associated with C-methylresorcin[4]arene, C-methylpyrogallol[4]arene, p-phosphonated calix[8]arene and a metal-seamed calixarene–copper(II) complex, using human HEK293 and rat C6G cell lines and two different cell viability assays (MTT and CellTiter-Glo) to avoid species-biased results. All compounds showed low to moderate toxicity. The trend in the CC₅₀ values indicated that the suppression of the coordination ability and the presence of phosphonate groups decrease the overall cytotoxicity of the compounds. The results of this study not only establish calixarenes and their immediate families as potential drug carriers and drug modifiers, but also reveal a pathway for fine-tuning their toxicological behaviour by appropriate chemical modification.     

Two Stable Heterometal‐MOFs as Highly Efficient and Recyclable Catalysts in the CO2 Coupling Reaction with Aziridines

Two stable heterometal‐organic frameworks, {Na[LnCo(DATP)₂(Ac)(H₂O)](NO₃)?DMA?11 H₂O}_n (Ln=Er( 1 ) and Yb( 2 )), have been prepared with H₂DATP (4′‐(3,5‐dicarboxyphenyl)‐2,2′:6′,2′′′‐terpyridine) as organic building block. These two isostructural compounds featuring two‐dimensional layer architectures possess outstanding thermal stabilities and excellent chemical stabilities in common organic solvents and different acid/base solutions with pH range changing from 1 to 13. Moreover, compounds 1 and 2 serving as heterogeneous catalysts can efficiently catalyse the CO₂ fixation reaction with various aziridines to result in corresponding oxazolidinones at 70 °C. Importantly, a good recyclable performance of 1 for at least 10 cycles is observed based on the experimental results, which are further confirmed by PXRD, TGA and ICP analyses.     

Solvent Effect on the Photocatalytic Activity of g-C3N4/BiOBr and its Effect on Degradation of Acetochlor

Russian Journal of Physical Chemistry A - g-C3N4/BiOBr composites were obtained via solvothermal method. XRD, SEM, FTIR, UV–Vis DRS, BET, and BJH methods were used to characterize the...     

Rare-earth metal derivatives supported by aminophenoxy ligand: Synthesis,characterization and catalytic performance in lactide polymerization

A library of rare-earth metal derivatives supported by an aminophenoxy ligand was prepared and their catalytic performance in lactide polymerization was investigated. It was found that the synthetic strategy had a profound effect on the formation of aminophenoxy rare-earth metal complexes. Amine elimination between Ln[N(SiMe₃)₂]₃(μ-Cl)Li(THF)₃ (Ln = Yb, Y) and 1 equiv. of the aminophenol [HONH] ([HONH] = ο-OCH₃-C₆H₄NHCH₂(3,5-^tBu₂-C₆H₂-2-OH)) in toluene gave the unexpected heterobimetallic bis(aminophenoxy) rare-earth metal complexes [ON]₂LnLi(THF)₂ (Ln = Yb ( 1 ), Y ( 2 )). When the reactions were carried out in THF and TMEDA, amine elimination produced the aminophenoxy rare-earth metal amide complexes {[ON]LnN(SiMe₃)₂}₂ (Ln = Yb ( 5 ), Y ( 6 )) in ca 85% isolated yields. Complexes 5 and 6 could also be obtained from salt metathesis reaction of {[ON]LnCl(THF)}₂ (Ln = Yb ( 3 ), Y ( 4 )) with NaN(SiMe₃)₂ in a 1:2 molar ratio. In addition, treatment of complexes 3 and 4 with NaOAr (Ar = &bond;C₆H₄-4-^tBu) and (SiMe₃)₂NC(NPrⁱ)₂Na in 1:4 and 1:2 molar ratios provided the corresponding aminophenoxy rare-earth metal derivatives {[ON](μ-OAr)Ln(μ-OAr)Na(THF)₂}₂ (Ln = Yb ( 7 ), Y ( 8 )) and {[ON]Ln[(ⁱPrN)₂CN(SiMe₃)₂]}₂ (Ln = Yb ( 9 ), Y ( 10 )), respectively. These complexes were fully characterized, and their molecular structures were determined using single-crystal X-ray diffraction. Polymerization experiments showed that complexes 1 , 2 , 5 , 6 , 9 and 10 were highly active for the ring-opening polymerization of l -lactide in toluene, and complex 1 promoted l -lactide polymerization in a controlled fashion. The polymerization of rac-lactide initiated by the neutral aminophenoxy rare-earth metal complexes 5 , 6 , 9 and 10 in THF afforded heterotactic polymers.     

Mechanical effects of acupuncture

Acupuncture, a physiotherapy, has been widely accepted all around the world. This study focuses on the influence of membrane structures and explains the acupuncture sensations from the aspect of mechanical properties. By mathematical modeling and numerical simulation, the scientific meaning of the acupuncture depth is investigated and phenomena and theory of acupuncture are discussed. The simulation results show that (a) the fascial structure is the main contributor to the force on the needle, the axial force will gradually increase before piercing the fascial, and suddenly decrease after piercing the fascial; (b) there is an inverse relationship between the needle radius and the maximum radial stress, which indicates that the needle should not be too sharp to cause local stress concentration and piece the fascia layer; and (c) the simulation results of comprehensively considering the static friction and sliding friction is identical with the experiment results. This study proposes a preliminary study of mechanical effects of acupuncture manipulation, clarifies key factors affecting the stress on the needle, and explains the objective requirement of acupuncture depth to effective treatment.     

A health performance evaluation method of multirotors under wind turbulence

Nonlinear Dynamics - As an unmanned system, the multirotor has gained widespread attention in practical aviation engineering, because of its ease of use, reliability and maintainability. From the...     

AlGaN/GaN高电子迁移率器件外部边缘电容的物理模型

AlGaN/GaN HEMT外部边缘电容Cofd是由栅极垂直侧壁与二维电子气水平壁之间的电场构成的等效电容.本文基于保角映射法对Cofd进行物理建模,考虑沟道长度调制效应,研究外部偏置、阈值电压漂移和温度变化对Cofd的影响:随着漏源偏压从零开始增加,Cofd先保持不变再开始衰减,其衰减速率随栅源偏压的增加而减缓;AlGaN势垒层中施主杂质浓度的减小和Al组分的减小都可引起阈值电压的正向漂移,正向阈值漂移会加强沟道长度调制效应对Cofd的影响,导致Cofd呈线性衰减.在大漏极偏压工作情况下,Cofd对器件工作温度的变化更加敏感.     

Solubilization of Hexyl Aminolevulinate by Surfactants for Tumor Fluorescence Detection

Hexyl aminolevulinate (HAL) is a lipophilic derivative of 5-aminolevulinic acid (5-ALA) and can induce more protoporphyrin IX (PpIX) formation and stronger fluorescence intensity (FI) than 5-ALA, which will greatly facilitate photodynamic diagnosis and therapy. The main drawback of HAL is its low solubility in neutral aqueous media. In this study, surfactants were used to increase HAL solubility in the cell culture medium and serum, followed by in vitro fluorescence formation measurement in human pancreatic cancer cells (SW1990) and in vivo fluorescence detection in tumor-bearing mice. The results showed that Tween 80 (TW80) and Kolliphor® HS 15 (HS15) increased the solubility of HAL in the selected media. Although TW80 and HS15 exhibited in vitro cytotoxicity at high concentrations (5 mg mL⁻¹), they facilitated fluorescent signal formation at the early stage of cell incubation. When surfactants were used, the FI should be determined without the routine washing process because surfactant-containing culture medium caused the loss of synthesized PpIX during the washing process. When HAL dissolved in TW80 solution was injected intraperitoneally into pancreatic cancer-bearing mice at a dose of 50 mg kg⁻¹, the tumors exhibited red fluorescence, which indicated that systemic administration of surfactant-solubilized HAL might be applicable for tumor fluorescence detection in vivo.