Four 1,5-diphenyl-3-aromatic heterocyclyl-2-pyrazoline-based sulfonium salt photoacid generators (PAGs) with different aromatic heterocycles substituted on C3 atom and dimethyl sulfonium group on C5 atom were synthesized. These PAGs were highly photosensitive in the 365–425 nm light-emitting diode region, and the intramolecular charge transfer from the pyrazoline ring to sulfonium salts induced efficient photolysis and high ΦH+. The heterocycles as well as their substituted positions significantly influenced the energy of the S2 orbital, which was determined by the electrochemical and absorption properties of the PAGs. The raising of the S2 orbital energy enlarged the energy gap of S0–S2 and S1–S2, resulting in blue shift of the absorption spectra and increase in the quantum yield of photoacid generation (ΦH+), respectively. When the energy of excited electrons was higher than that of the S2 orbital, the transition from S0 to S2 (π–π*) occurred before the C-S cleavage on S1 and the PAGs showed high ΦH+ values (0.52–0.72). The transition from S0 to S1 (π–σ*) occurred when the energy of electrons is lower than that of the S2 orbital, and the PAGs showed low ΦH+ value. The photopolymerization kinetics demonstrated that these PAGs were highly efficient cationic photoinitiators. 相似文献
Kahweol, a compound from Coffea arabica, possesses antioxidant, anti-inflammatory, and antitumour properties. However, an anti-adipogenic effect has not yet been reported. In this study, we have shown that kahweol has an anti-adipogenic effect on 3T3-L1 adipocytes. Kahweol significantly inhibited the differentiation of intracellular lipid accumulation in 3T3-L1 adipocytes, without being cytotoxic. It also downregulated the expression of adipogenesis-related gene, including an adipocytokine, adiponectin. This anti-adipogenic effect stems from an ability to inhibit key adipogenic regulators, including PPARγ and C/EBPα. These results demonstrate that kahweol significantly inhibits the differentiation of 3T3-L1 cells, and suggest that it has potential as a novel anti-obesity treatment. 相似文献
C-11 (2-((7-Ethyl-3-methyl-8-(4-(2-(methyl(pyridin-2-yl)-amino)-ethoxy)phenyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl)methyl)benzonitrile-one hydrochloride), which is based on the structure of rosiglitazone, was first synthesized in our laboratory and shown to be a promising anti-obesity drug candidate in our previous pharmacological study. Considering the importance of metabolic fate in vivo in the further development of drug candidates during early drug discovery, it is essential to characterize the metabolism of C-11 in vivo. In this work, a method based on ultra-high performance liquid chromatography combined with quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) was successfully developed to investigate the in vivo metabolic profile of C-11 in rats. Rat urine, feces, and plasma samples were collected from male Sprague–Dawley rats after intravenous administration of C-11 in a single dose of 30 mg kg−1 body weight. Besides the parent drug, a total of 25 metabolites (including 18 phase I and 7 phase II metabolites) were detected and tentatively identified by comparing their mass spectrometry profiles with those of C-11. This enabled the metabolic pathways of C-11 to be proposed for the first time. Our results revealed that N-depyridinylation, N-demethylation, hydroxylation, glucuronidation, and sulfate conjugation are the predominant metabolic pathways of C-11 in rats. The present study provides systematic information on the metabolism of C-11 in vivo, which should lead to a better understanding of its safety and mechanism of action.
The directional drifting of particles/molecules with broken symmetry has received increasing attention. Through molecular dynamics simulations, we investigate the effects of various solvents on the time-dependent directional drifting of a particle with broken symmetry. Our simulations show that the distance of directional drift of the asymmetrical particle is reduced while the ratio of the drift to the mean displacement of the particle is enhanced with increasing mass, size, and interaction strength of the solvent atoms in a short time range. Among the parameters considered, solvent atom size is a particularly influential factor for enhancing the directional drift of asymmetrical particles, while the effects of the interaction strength and the mass of the solvent atoms are relatively weaker. These findings are of great importance to the understanding and control of the Brownian motion of particles in various physical, chemical, and biological processes within finite time spans. 相似文献
Acta Mathematicae Applicatae Sinica, English Series - In this paper, a diffusive predator-prey system of Holling type functional III is considered. For one hand, we considered the possibility of... 相似文献
In this study, we postulated that the optical retardation magnitude could be used to evaluate the stability of the LC phase through the Mueller matrix polarimeter method in LC emulsion. In addition, we found that the increase of cetearyl alcohol concentration induced the more periodic dense lattice structure in crystalline phase of LC lamellae and the sorbitan olivate was relatively more responsible for higher ordering in LC phase compared to C12–20 alkyl glucoside in terms of molecular parallel packing on the basis of the optical retardation magnitude. Furthermore, it was confirmed that the LC emulsion had higher skin barrier function owing to lower TEWL and higher reflectance than ordinary emulsion on human skin and maintained a uniform phase without phase separation for 8 weeks. 相似文献
A new chalcone-based probe containing coumarin and naphthol at both ends has been synthesized via aldol condensation. The uniqueness of the newly derived probe can be ascribed to the presence of naphthol and coumarin units acting as binding site and signaling element, respectively. The fluorogenic behaviors toward various anions were investigated. The probe was characterized by various spectroscopic techniques and the in-depth study led to show excellent selectivity and sensitivity for fluoride ions. The hydrogen bonding thus formed with fluoride anion provides remarkable fluorometric responses. The interactions of the probe with fluoride ions were determined by fluorescence, FT-IR and NMR spectroscopic techniques. The exploratory studies by fluorescent spectral changes augur well for the naked-eye sensing applications. 相似文献