Design, synthesis, and biological evaluation of dinuclear bismuth(III) complexes with Isoniazid-derived Schiff bases.

Four dinuclear bismuth(III) Schiff-base complexes bearing Schiff-base ligands have been synthesized and structurally characterized by single-crystal X-ray diffraction, elemental analysis, and spectral techniques (FT-IR, NMR and MS). The analytical data reveal the bismuth(III) complexes possess 1:1 metal-ligand ratios. In vitro biological studies have revealed that bismuth(III) complexes displayed much higher antibacterial and antitumor activities than their parent ligands, which involves two gram-negative (S. aureus, B. subtili) and two gram-positive (E. coli, P. aeruginosa) bacteria, and human gastric cancer SNU-16 cells. The power-time curves of S. pombe exposed to tested compounds were detected by bio-microcalorimetry. Some thermokinetic parameters (k, Pmax,tG and Qtotal) were derived based on the metabolic power-time curves, and their quantitative relationships with the concentrations (c) were further discussed.

Synthesis, crystal structure and spectroscopic studies of bismuth(III) complex with 2-substituted benzimidazole ligands.

Reaction of BiCl3 with 2-(2-hydroxy-3-methoxyphenyl)benzimidazole (HL) in tetrahydrofuran (THF) under reflux gave mononuclear complex of formula [Bi(HL)2Cl3·H2O]. The binding interaction of the complex with bovine serum albumin (BSA) was investigated using the fluorescence quenching method. The experimental results showed that the complex could bind to BSA in the proportion of about 1:1. The binding reaction was spontaneous and hydrophobic force played major role in the reaction. The binding of the complex to BSA could change the microenvironment and conformation of BSA.

TLR4/NF-κB signaling contributes to chronic unpredictable mild stress-induced atherosclerosis in ApoE-/- mice.

OBJECTIVE: Chronic stress is an important risk factor for atherosclerotic diseases. Our previous studies have shown that chronic unpredictable mild stress (CUMS) accelerates atherosclerosis and up-regulates TLR4/NF-κB expression in apoE-/- mice. However, TLR4/NF-κB signaling whether directly contributes to the development of atherosclerosis in CUMS mice is unclear. We hypothesized that the interference of TLR4/NF-κB can ameliorate CUMS-induced inflammation and atherosclerosis in apoE-/- mice. METHODS: ApoE-/- mice were exposed to 12 weeks CUMS. Ad-siRNA TLR4 was given by tail vein injection (10 µl/mouse, every 5 days), and PDTC (an inhibitor of NF-κB) was given by intraperitoneal injection (60 mg/kg, once a day). Plasma corticosterone concentrations were determined by solid-phase 125I radioimmunoassay. Atherosclerosis lesions in aortic sinuses were evaluated and quantified by IMAGEPRO PLUS. Western blotting was used to detect the expression of TLR4, NF-κB, and IL-1ß in aortas of the mice. Plasma lipid profiles, IL-1ß, TNF-α, and MCP-1 were measured by ELISA. RESULTS: Our results indicated that CUMS apoE-/- mice treatment with siRNA TLR4 significantly decreased atherosclerosis and down-regulated TLR4, NF-κB, and inflammatory cytokines. PDTC also remarkably reduced atherosclerosis and the levels of IL-1ß, TNF-α and MCP-1 in plasma. However, Treatment with siRNA TLR4 or PDTC had no effect on plasma corticosterone levels, and lipid profiles. CONCLUSIONS: TLR4/NF-κB pathway may participate in CUMS-induced atherosclerosis through activation of proinflammatory cytokines in apoE-/- mice. Our data may provide a new potential therapeutic target for prevention of CUMS -induced atherosclerosis.

Population sizes and group characteristics of Siberian Crane (Leuco-geranus leucogeranus) and Hooded Crane (Grus monacha) in Poyang Lake Wetland.

Both the Siberian Crane (Leucogeranus leucogeranus) and Hooded Crane (Grus monacha) have limited population sizes and are considered endangered by domestic Chinese and international agencies. To document the current size of their respective populations and characterize their groups, between October 2012 and April 2013 we undertook fieldwork at four nature reserve areas within the Poyang Lake wetlands. We divided Poyanghu National Nature Reserve (PYH) into the Wucheng (PWC) and Hengfeng areas (PHF), because each are each located in different counties. Our fieldwork showed that the Siberian Crane occurred mainly in PYH (364 in the PHF, 158 in the PWC) and the Nanjishan Wetland National Nature Reserve (NJS, with 200 individuals). The Hooded Crane was mainly distributed in PYH (302 in the PHF and 154 in the PWC). Family groups accounted for more than 50% of the total number of groups among both species, with Hooded Cranes forming more family groups than Siberian Cranes. Typically, these groups were formed of two adults with one offspring (Siberian Crane), and two adults with two offspring (Hooded Crane), with the mean family group size of the Siberian Crane and Hooded Crane being respectively 2.65 ± 0.53 (n=43) and 3.09 ± 0.86 (n=47) individuals per group. The mean collective group size of the Siberian Crane and Hooded Crane included 28.09 ± 24.94 (n=23) and 28.94 ± 27.97 (n=16) individuals per group, respectively, with the proportion of juveniles among Hooded Cranes being more than double that seen among the Siberian Cranes.

Synthesis of nordihydroguaiaretic acid derivatives and their bioactivities on S. pombe and K562 cell lines.

Nordihydroguaiaretic acid (NDGA) and its synthetic analogues are potentially useful in treating diseases related to cancers, diabetes, viral and bacterial infections, and inflammation. In this paper, we report the optimal synthetic methods and the bioactivity study of terameprocol 2, NDGA derivative 3, and its cyclized analogue 4. The IC50 of these three compounds 2, 3 and 4 on the growth metabolism of Schizosacchromyces pombe and K562 cell lines were determined by microcalorimetry. The preliminary results showed that the compounds 2, 3 and 4 possessed good inhibition activities on S. pombe and K562 cell lines, and exhibited bidirectional biological effect and Hormesis effect. In particular, terameprocol 2 was found to possess the most potent inhibitory effect on K562 cell lines.

[Control of residual humic acid and residual aluminium in water with enhanced coagulation].

Control of residual humic acid and residual aluminium in water with enhanced coagulation was investigated. The influence of various factors on the coagulation was studied, in order to reach the maximum humic acid removal and the minimum aluminium residue simultaneously. Results showed that residual humic acid was controlled below 0.04 cm(-1) and residual aluminium kept at about 0.1 mg/L in water with pH value between 6 and 6.5, the AlCl3 dosage of 0.5 x 10(-3) mol/L, under the temperature of 20 degrees C. Addition 0.01 mol/L of CaCl2 could improve the enhanced coagulation effect. Because the suspended granule concentration changes with seasons, the influence of the kaoline dosage on the humic acid removal process was studied.