Study on the stoichiometry and affinity of the arsenicals bound to HSA is an important step toward a better understanding of arsenic toxic effects. After incubation of AsIII or AsV with HSA at the physiological conditions (pH 7.43 and 37 °C), the free arsenicals and arsenic-HSA complexes were separated and detected by the combined techniques of microdialysis and liquid chromatography with hydride generation atomic fluorescence spectroscopy (MD–LC–HGAFS). The decrease of AsIII peak response rather than AsV indicated that HSA reacted with AsIII but not AsV. The binding plots indicated that the binding between HSA and AsIII was in Scatchard pattern when the concentration ratios of AsIII to HSA were ≤1:1. The strong binding sites (n1) were 1.6 and the stability constant (K1) was 1.54 × 106 M−1. When the concentration ratios of AsIII to HSA were >1:1, the binding was in Plasvento pattern with the stability constant K2 ≅ 0 and no specific binding of AsIII with HSA. On the contrary, AsV did not show binding with HSA. The results showed that AsIII reacted with HSA more readily than AsV, which provides a chemical basis for arsenic toxicity.
In this paper, we study a generalized Burgers equation ut+(u2)x=tuxx, which is a non-uniformly parabolic equation for t>0. We show the existence and uniqueness of classical solutions to the initial-value problem of the generalized Burgers equation with rough initial data belonging to . 相似文献
Type II diabetes mellitus is a chronic metabolic disorder that can lead to serious cardiovascular, renal, neurologic, and retinal complications. While several drugs are currently prescribed to treat type II diabetes, their efficacy is limited by mechanism-related side effects (weight gain, hypoglycemia, gastrointestinal distress), inadequate efficacy for use as monotherapy, and the development of tolerance to the agents. Consequently, combination therapies are frequently employed to effectively regulate blood glucose levels. We have focused on the mitochondrial sodium-calcium exchanger (mNCE) as a novel target for diabetes drug discovery. We have proposed that inhibition of the mNCE can be used to regulate calcium flux across the mitochondrial membrane, thereby enhancing mitochondrial oxidative metabolism, which in turn enhances glucose-stimulated insulin secretion (GSIS) in the pancreatic beta-cell. In this paper, we report the facile synthesis of benzothiazepines and derivatives by S-alkylation using 2-aminobenzhydrols. The syntheses of other bicyclic analogues based on benzothiazepine, benzothiazecine, benzodiazecine, and benzodiazepine templates are also described. These compounds have been evaluated for their inhibition of mNCE activity, and the results from the structure-activity relationship (SAR) studies are discussed. 相似文献
Sb3+-doped Sr3(PO4)2 crystals has been synthesized using phosphoric acid, strontium hydroxide and antimony powder as the raw materials through a hydrothermal reaction method. The crystallinity and the microstructure were investigated using X-ray diffraction and scanning electron microscopy. The photoluminescent property was investigated using luminescent spectrometer. Phase pure Sr3(PO4)2 crystal was obtained and it has a shape of hexagonal rod. It showed the emission and excitation peaks at 396, 250, and 215 nm, respectively, indicating that the emission is attributed to 3P1-1S0 transition and the excitation is attributed to 1S0-3P1 and 1S0-1P1 transition. It was also observed that the intensity of photoluminescence is thermally stable up to 673 K. 相似文献
Series of diorganotin(IV) complexes of 4-X-benzohydroxamic acid [X = NH2 (HL1), NO2 (HL2) or F (HL3)] formulated as [R2SnL2] and [R2Sn(L)]2O (R = Me, Et, nBu or Ph) have been prepared and characterized by FT-IR, 1H, 13C and 119Sn NMR spectroscopies, elemental analyses, FAB+-MS and melting point determination. They are stable in air, soluble in alcohols and in hydroalcoholic solution and, in some cases, in water. Their in vitro antitumor activity against a series of human tumor cell lines was tested and, in a few of them, is identical to, or even higher than, that of cisplatin. For the mononuclear dialkyltin compounds, the activity generally increases with the length of the carbon chain of the alkyl ligand, being higher for the complexes with benzohydroxamato ligands bearing an electron-acceptor substituent (X = NO2 or F). No structure-activity relationship based on the Hammett’s σp constant, or related ones, has been recognized. 相似文献