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Four lanthanide complexes with 8‐hydroxyquinoline‐2‐aldehyde‐2‐hydrazinopyridine (H‐L1), 8‐hydroxyquinoline‐2‐aldehyde‐2‐hydrazimidazole (H‐L2): [Sm(L1)2][Sm(L1)(NO3)3]·CHCl3·2CH3OH (1), [Gd(L1)2][Gd(L1)(NO3)3]·CHCl3·2CH3OH (2), [Sm(L2)(NO3)2]2·CH3OH (3), and [Eu(L2)(NO3)2]2·CH3OH (4) were synthesized and characterized. In vitro cytotoxicity evaluation showed that the ligands and four lanthanide complexes exhibited cytotoxicity to the five tested tumor cell lines. Among them, complex 1 showed the best antiproliferative activity against NCI‐H460 tumor cells. Mechanistic studies demonstrated that complex 1 arrested the cell cycle of NCI‐H460 cells in G1 phase and induced mitochondria‐mediated apoptosis, which resulted in the loss of mitochondrial membrane potential, enhanced intracellular Ca2+ levels and reactive oxygen species generation. In addition, complex 1 affected the expression levels of intracellular apoptosis‐related proteins and activated the caspase‐3/9 in NCI‐H460 cells. Therefore, complex 1 is a potential anticancer agent. [ABSTRACT FROM AUTHOR]

An efficient and operationally simple method for the synthesis of β-keto sulfones through the BF3·OEt2-promoted reaction of alkynes and sodium sulfinates is developed. With its facile and selective access to the targets, it features good functional group compatibility, mild conditions, easily available starting materials, and good yields. Notably, the reaction does not require metal catalysts or chemical reagents with pungent odors. [ABSTRACT FROM AUTHOR]

Highlights: • Deep Underground Space (DUS) can be used for special transport functions. • DUS resource context of Shanghai City and depth-scape planning priorities. • DUS planning and management policy benchmarking from Finland and Japan. • Development strategy for DUS at the city scale, district scale and project scale. • Policy guideline is proposed for short-term planning and long-term development. Abstract Urban Underground Infrastructures (UUI) are crucial for megacities that are suffering weak adaptabilities of environmental threats while facing fast economic growth from highly concentrated urban developments. Because of the urbanization and densification of cities globally, Metropolitan Authorities must prioritize the use of shallow and deep Urban Underground Space (UUS). Effective management of such space requires specifications of use for the varying levels within these. The specifications are defined as “Vertical zoning” (namely “Depth-scape”). This paper suggests a strategy for an economic development plan for Shanghai in China. Its specific focus is that of Deep Underground Space (DUS). The authors also suggest that this strategy may be transferable to other cities experiencing similar urbanization and densification, globally. In urban centers, surface buildings and facilities have been connected through shallow tunnel transport systems for pedestrian, utility, vehicle, metro, train, at a micro scale. For a larger urban territory, Special transport systems ensuring city’s security, resiliency and sustainability are usually built in the deep underground, such as: disaster evacuators, flood drainers (“sponge city creators”), terminal freight deliveries, waste movers, energy transmitters, cavern connecters and deep shaft elevators. A strategy proposed in this paper will incorporate these macro scale deep infrastructures into the economic development plan of Shanghai city. Methods applied in this paper include: Resources potential evaluation framework, Strategic benchmarking model, Conceptual infrastructure planning and Investment project appraisal scheme. Integration between municipal infrastructures and underground infrastructures is beneficial for the long-term operation of megacities, where utility systems and municipal facilities keep sizing up to meet future demand. Infrastructure integration becomes a must rather than an option. Developing Special Transport Systems in the Deep Underground Space (DUS) will allow a megacity to scale up its infrastructure stock, save surface land resources, protect societal assets, mitigate calamity losses, sustain operability and improve livability. [ABSTRACT FROM AUTHOR]

Highlights: [•] Integrated planning process for sustainable undergroundisation. [•] Macro scale development potential appraisal (Deep City Applicability Scores). [•] City scale policy formulation for underground urbanism (case study: Geneva city). [•] Large urban scale potential zoning and development forecast (case study: Suzhou city). [•] Micro scale economic premium index assessment and building project marketability. [Copyright &y& Elsevier]

[Display omitted] • A donor-accepter-donor (D-A-D) type probe 3a is concisely synthesized. • Probe 3a can show intense blue fluorescence and large Stokes shift. • F- initiates the cleavage of Si-C bond of 3a , resulting in emission quenching. • Probe 3a displays fast response and highly sensitivity towards fluoride ion. • Probe 3a can be processed as portable tools for F- visualization detection. Excessive fluoride ion (F-) in the environment can affect health and even endanger life when ingested by the human body. However, most fluoride probes have the disadvantages of low sensitivity and long detection time. Herein, fluorescent probe 3a is successfully synthesized by linking two acetylenyltrimethylsilyl groups at both ends of the fluorinated benzothiadiazole core. After the addition of F- to 3a , the emission at 436 nm is significantly quenched and slightly blue-shifted. It is confirmed by electrospray ionization high-resolution mass spectrometry (ESI-HRMS) and density functional theory calculations (DFT) that these changes are due to the F- triggered Si-C bond cleavage and the subsequent inactivation of intramolecular charge transfer (ICT). The detection limit and response time of probe 3a for F- are 10-8 mol/L and 25 s, respectively. Importantly, fluorescent material 3a can be processed into portable test tools for the visual detection of fluoride ion. [ABSTRACT FROM AUTHOR]

Polylactic acid (PLA) is one of promising biocompatible and biodegradable polyester. Poly(2-hydroxyethyl methacrylate) (PHEMA) is a polymer with good hydrophilicity. The hydrophilic PHEMA may improve PLA's amphiphilic properties. Hence, directly starting from hydroxyethyl methacrylate (HEMA), lactic acid (LA), maleic anhydride (MAH) and 2,2'-azobis(2-methyl-propionitrile) (AIBN), a series of new amphiphilic copolymers PLA20MHn were obtained through direct melt polycondensation (DMP) and subsequent free radical polymerization (FRP) in one pot. The results show that PLA20MHn can self-assemble in aqueous solution to form stable spherical micelles and dissolve hydrophobic pyrene molecules. What's more, The CMC value can be adjusted by the polymerization ratio. Therefore, this method is expected to further realize the encapsulation and controlled release of hydrophobic drug molecules for systemic circulation in vivo. [ABSTRACT FROM AUTHOR]

Organic thioethers play an important role in the discovery of drugs and natural products. However, the green synthesis of organic sulfide compounds remains a challenging task. The convenient and efficient synthesis of 5-alkoxy-3-halo-4-methylthio-2(5H)-furanones from DMSO is performed via the mediation of 1,3-dibromo-5,5-dimethylhydantoin (DBDMH), affording a facile route for the sulfur-functionalization of 3,4-dihalo-2(5H)-furanones under transition metal-free conditions. This new approach has demonstrated the functionalization of non-aromatic Csp2-X-type halides with unique structures containing C-X, C-O, C=O and C=C bonds. Compared with traditional synthesis methods using transition metal catalysts with ligands, this reaction has many advantages, such as the lower temperature, the shorter reaction time, the wide substrate range and good functional group tolerance. Notably, DMSO plays multiple roles, and is simultaneously used as an odorless methylthiolating reagent and safe solvent. [ABSTRACT FROM AUTHOR]

Four mononuclear terpyridine complexes [Cu(H-La)Cl2]·CH3OH (1), [Cu(H-La)Cl]ClO4 (2), [Cu(H-Lb)Cl2]·CH3OH (3), and [Cu(H-Lb)(CH3OH)(DMSO)](ClO4)2 (4) were prepared and fully characterized. Complexes 1–4 exhibited higher cytotoxic activity against several tested cancer cell lines especially BEL-7402 cells compared to cisplatin, and they showed low toxicity towards normal human liver cells. ICP-MS detection indicated that the copper complexes were accumulated in mitochondria. Mechanistic studies demonstrated that the copper complexes induced G0/G1 arrest and altered the expression of the related proteins of the cell cycle. All copper complexes reduced the mitochondrial membrane potential while increasing the intracellular ROS levels and the release of Ca2+. They also up-regulated Bax and down-regulated Bcl-2 expression levels, caused cytochrome c release and the activation of the caspase cascade, and induced mitochondrion-mediated apoptosis. Animal studies demonstrated that complex 1 suppressed tumor growth in a mouse xenograft model bearing BEL-7402 tumor cells. [ABSTRACT FROM AUTHOR]

Six pyrazolopyrimidine Rh (III)/Pd(II) complexes were prepared and exhibited excellent cytotoxic activity, complex 5 and 6 induced cell cycle arrest, apoptosis and ER stress, suppressed cells proliferation in vivo. [Display omitted] • Six pyrazolopyrimidine Rh(III)/pd(II) complexes were synthesized and characterized. • Structure activity relationship (SAR) of the complexes was studied. • Complexes 1 – 6 exhibited excellent antitumor activity against various tumor cells. • Complexes 5 and 6 induced cell cycle arrest, apoptosis and ER stress. • Complex 5 and 6 inhibited the growth of T-24 in vivo. Six pyrazolopyrimidine rhodium(III) or palladium(II) complexes, [Rh(L1)(H 2 O)Cl 3 ] (1), [Rh(L2)(CH 3 OH)Cl 3 ] (2), [Rh(L3)(H 2 O)Cl 3 ] (3), [Rh 2 (L4)Cl 6 ]·CH 3 OH (4), [Rh(L5)(CH 3 CN)Cl 3 ]·0.5CH 3 CN (5), and [Pd(L5)Cl 2 ] (6), were synthesized and characterized. These complexes showed high cytotoxicity against six tested cancer cell lines. Most of the complexes showed higher cytotoxicity to T-24 cells in vitro than cisplatin. Mechanism studies indicated that complexes 5 and 6 induced G2/M phase cell cycle arrest through DNA damage, and induced apoptosis via endoplasmic reticulum stress response. In addition, complex 5 also induced cell apoptosis via mitochondrial dysfunction. Complexes 5 and 6 showed low in vivo toxicity and high tumor growth inhibitory activity in mouse tumor models. The inhibitory effect of rhodium complex 5 on tumor growth in vivo was more pronounced than that of palladium complex 6. [ABSTRACT FROM AUTHOR]

Context:Sonchus oleraceusL. (Asteraceae) (SO) is a dietary and traditional medicinal plant in China. However, its underlying mechanism of action as an anti-inflammatory agent is not known. Objective:This study evaluates the anti-inflammatory activity of aqueous extract of SO. Materials and methods:The extract of SO was used to treat RAW 264.7 cells (in the working concentrations of 500, 250, 125, 62.5, 31.3 and 15.6 μg/mL) for 24 h. Pro-inflammatory cytokines and mediators produced in LPS-stimulated RAW 264.7 cells were assessed. Meanwhile, the expression level of TLR-4, COX-2, pSTATs and NF-κB was tested. Moreover, the anti-inflammatory activity of the extractin vivowas assessed using xylene-induced mouse ear oedema model and the anti-inflammatory compounds in the extracts were analyzed by HPLC-MS. Results:SO extract significantly inhibited the production of pro-inflammatory cytokines and mediators at gene and protein levels with the concentration of 31.3 μg/mL, and suppressed the expression of TLR-4, COX-2, NF-κB and pSTAT in RAW 264.7 cells. The anti-inflammatory activity of SOin vivohas significant anti-inflammatory effects with the concentration of 250 and 125 mg/kg, and less side effect on the weights of the mice at the concentration of 250 mg/kg. Moreover, HPLC-MS analysis revealed that the anti-inflammatory compounds in the extract were identified as villosol, ferulaic acid, β-sitosterol, ursolic acid and rutin. Discussion and conclusion:This study indicated that SO extract has anti-inflammatory effectsin vitroandin vivo, which will be further developed as novel pharmacological strategies in order to defeat inflammatory diseases. [ABSTRACT FROM PUBLISHER]

Ethnopharmacological relevance Sonchus oleraceus (L.) L (SO) and Juniperus sabina L (JS) are traditional medicinal plants in China. And the aqueous extracts of them have been used to treat tumor, inflammatory diseases, infection and so on in Chinese folk culture. However, the underlying mechanisms of their anti-tumor activities have not been illustrated yet. Objective This study aims to evaluate the inhibitory effects of aqueous extracts from SO and JS on tumor cells. Materials and methods The prepared aqueous extracts of SO and JS were used to treat HepG-2 and K562 tumor cells, while the human peripheral blood mononuclear cells (PBMCs) were set as normal control. The viabilities, cell cycle and apoptosis of tumor cells after extracts treatment were assessed, in addition the expression of apoptosis-related genes (FasL, caspase 3, 6, 7, 8, 9, and 10) were analyzed. Meanwhile, the adherence and migration of HepG-2 were tested, and the expression levels of MMPs and ICAM-1 were analyzed. On top of that, the pSTAT in the two cells were also analyzed and suggested the related signaling pathway that the extracts acted on with in these tumor cells. Results Results showed that aqueous extracts of SO and JS have inhibitory effects on HepG-2 and K562 cells by decreasing cell viability and inducing apoptosis via up-regulation of the expression of the apoptosis-related genes FasL, caspase 3 and caspase 9. The extracts had different IC 50 on tumor cells and PBMCs, which could block the tumor cell cycle at the G 0 /G 1 stage and significantly inhibit the adherence of HepG-2 cells. The extracts inhibited migration of these cells by inhibiting the expression of ICAM-1, MMP-2 and MMP-9. Further study indicated that the inhibition of pSTAT1 and 3 might be responsible for the inhibitory effects of the extracts on tumor cells. Discussion and conclusion The results of this study indicated that SO and JS extracts had the anti-tumor effects, which may be developed as novel anti-tumor drugs and used in cancer therapy. [ABSTRACT FROM AUTHOR]