A new pyrazolo4,3-i/pyriinidine derivative-. Synthesis and anti-inflammatory activity / 中国药理学通报

Aim To design and synthesizea new pyrazolo[4,3-d] pyrimidine derivative for the purpose of developing novel anti-inflammatory agents, and to revealthe possible anti-inflammatory mechanisms of thenew compound using preliminary studies. Methods The changes of the cell morphology were investigated via the microscope. The influence of title compound on the NO production of the L P S - stimulated RAW264. 7 cells was measured by Griess assay. The gene relative transcription levels of TNF-a, IL - 6 and IL-lß were evaluated by qRT-PCR. COX-2 expression was measured by qRT-PCR and western blot. NF-KB/NLRP3 inflammasome signaling pathway were investigated by Western blot. The changes of lung tissue were observed by HE staining in vivo experiments of mice. Results Preliminary mechanism researches revealed that the ti - tle compound could inhibit nitric oxide (NO) generation as well as the expression of COX-2, TNF-a, IL - 6, and IL - lβ by NF-KB/NLRP3 inflammasome signaling pathway in RAW264. 7 cells. Furthermore, it could simultaneously improve the morphology of the cells and relieve acute lung injury in mice. Conclusions The new pyrazolo [4, 3-α] pyrimidine derivative has anti-inflammatory activity through NF-KB/NLRP3 inflammasome signaling pathway.

Catalytic hydrothermal liquefaction of rice straw for production of monomers phenol over metal supported mesoporous catalyst.

The catalytic (SBA-15, Ni/SBA-15, Al/SBA-15 and Ni-Al/SBA-15) hydrothermal liquefaction (HTL) of rice straw biomass was examined at different temperature with different amount of catalyst in the presence of different solvents. In comparison with water solvent liquefaction, the bio-oil yield significantly increased under alcoholic solvent (ethanol and methanol). The highest bio-oil yield was observed for water (44.3 wt%) with Ni-Al/SBA-15, while for ethanol (56.2 wt%), and for methanol (48.1 wt%) with, Ni/SBA-15 catalyst. The loading of Ni and Al on SBA-15, the acid strength of the catalyst enhanced. Bio-oils yield were analyzed with the help of GC-MS, FT-IR, NMR, GPC and CHNS. From the GC-MS analysis, the main monomeric phenolic compounds were produced, phenol, 4-ethyl-phenol, 2-methoxy-phenol, 2-methoxy-4-ethyl-phenol and Vanillin. It was observed by CHNS and GPC analysis of the bio-oil, compared to the non-catalytic liquefaction reaction, the catalytic liquefaction reaction promotes the hydrogenation/hydrodeoxygenation and produced lower molecular weight bio-oils.

A highly selective chemosensor for Al3+ based on 2-oxo-quinoline-3-carbaldehyde Schiff-base.

A new Schiff-base ligand (1) with good fluorescence response to Al(3+), derived from 2-oxo-quinoline-3-carbaldehyde and nicotinic hydrazide, had been synthesized and investigated in this paper. Spectroscopic investigation revealed that the compound 1 exhibited a high selectivity and sensitivity toward Al(III) ions over other commonly coexisting metal ions in ethanol, and the detection limit of Al(3+) ions is at the parts per billion level. The mass spectra and Job's plot confirmed the 1:1 stoichiometry between 1 and Al(3+). Potential utilization of 1 as intracellular sensors of Al(3+) ions in human cancer (HeLa) cells was also examined by confocal fluorescence microscopy.

A highly selective turn-on fluorescent chemosensor for zinc ion in aqueous media.

In the paper, a novel rhodamine6G based fluorescent chemosensor bearing 3-carbaldehyde chromone was designed and synthesized. According to the fluorescence behavior toward several metal ions, it showed highly selectivity and sensitivity to Zn(II) over other commonly coexistent metal ions (Cu(II), Cd(II), Hg(II), Mg(II), K(I), Pb(II), Fe(III) and Cr(III)) in aqueous environment (pH = 7.4). Meanwhile the binding constant between Zn(II) and chemosensor achieved 6.21 × 10(11) M(-1) in aqueous media. Moreover, according to the Job plot, 1:1 stoichiometry between Zn(II) and sensor was deduced in aqueous media (pH = 7.4). The good selectivity and sensitivity in aqueous media effectively enhanced the application value of the fluorescent chemosensor for Zn(II).

An effective Cu(II) quenching fluorescence sensor in aqueous solution and 1D chain coordination polymer framework.

In the article, a novel fluorescent probe for the copper cation based on fluorescence quenching mechanism was designed. It exhibited high selectivity for Cu(II) over other common metal ions in aqueous media. Furthermore the coordination between Cu(II) and the organic molecule sensor fabricated an interesting 1D chain coordination polymer framework.

Synthesis, characterization, DNA binding properties and antioxidant activity of Ln(III) complexes with Schiff base ligand derived from 3-carbaldehyde chromone and aminophenazone.

A novel Schiff base ligand, chromone-3-carbaldehyde-aminophenazone (L) and its Ln(III) (Ln = La, Yb) complexes were synthesized and characterized by physicochemical methods. The interaction between the ligand, Ln(III) complexes and calf thymus DNA in physiological buffer (pH=7.10) was investigated by using UV-vis spectroscopy, fluorescence spectra, ethidium bromide experiments and viscosity measurements, indicating that the studied compounds can all bind to DNA via an intercalation binding mode and the complexes have stronger binding affinity than the free ligand alone. Furthermore, antioxidant activity of the ligand and its complexes was determined by superoxide and hydroxyl radical scavenging methods in vitro, suggesting that Ln(III) complexes inhibit stronger antioxidant activity than the ligand alone and some standard antioxidants, such as mannitol and vitamin C.

Crystal structures, DNA-binding and cytotoxic activities studies of Cu(II) complexes with 2-oxo-quinoline-3-carbaldehyde Schiff-bases.

Three novel 2-oxo-quinoline-3-carbaldehyde Schiff-bases and their Cu(II) complexes were synthesized. The molecular structures of Cu(II) complexes were determined by X-ray crystal diffraction. The DNA-binding modes of the complexes were also investigated by UV-vis absorption spectrum, fluorescence spectrum, viscosity measurement and EB-DNA displacement experiment. The experimental evidences indicated that the ligands and Cu(II) complexes could interact with CT-DNA (calf-thymus DNA) through intercalation, respectively. Comparative cytotoxic activities of ligands and Cu(II) complexes were also determined by MTT [3-(4,5-dimethyl-2-thiazoyl)-2,5-diphenyl-2H-tetrazolium bromide] and SRB (sulforhodamine B) methods. The results showed that the three Cu(II) complexes exhibited more effective cytotoxic activity against HL60 cells and HeLa cells than corresponding ligands. Also, CuL(3) showed higher cytotoxic activity than CuL(1) and CuL(2).

Synthesis, crystal structure, DNA interaction and antioxidant activities of two novel water-soluble Cu2+ complexes derivated from 2-oxo-quinoline-3-carbaldehyde Schiff-bases.

Two novel 2-oxo-quinoline-3-carbaldehyde (4'-hydroxybenzoyl) hydrazone, thiosemicarbazone ligands and its corresponding Cu(2+) complexes were synthesized, and the two complexes' structures were determined by X-ray single crystal diffraction. The interaction of the two Cu(2+) complexes with calf thymus DNA (CT-DNA) was investigated by electronic absorption spectroscopy, fluorescence spectroscopy and viscosity measurement. The experimental evidences indicated that the two water-soluble Cu(2+) complexes could strongly bind to CT-DNA via an intercalation mechanism. The intrinsic binding constants of complexes 1 and 2 with CT-DNA were 7.31 x 10(6) and 2.33 x 10(6)M(-1), respectively. Furthermore, the antioxidant activities (hydroxyl radical and superoxide) of the two water-soluble metal complexes were determined by hydroxyl radical and superoxide scavenging method in vitro.