Advanced Materials Research Vols. 781-784

Abstract: Using conical flask culture for simulation of small-scale fermentation, we studied the changes in β-defensin-2 (HBD-2) protein expression when HBD-2-harbording engineered bacteria were exposed to different culture conditions, culture media, incubation temperatures, pH values, and inducer concentrations. We also performed computer simulation-based structural analysis of the target protein. Our results showed that HBD-2 fusion protein was most abundantly expressed in the engineered bacteria cultured in M₉B₂ medium at 32°C at a pH range of 7.3 to 7.5 upon induction by 1.2 mmol/L IPTG. Computer simulation-based structure analysis showed that enhanced hydrophilicity of the recombinant protein did not reduce the epitopes of HBD-2 fusion protein and that HBD-2 fusion protein kept the same structure as that of the native protein.

Abstract: Seven novel aryloxy-acetyl ferrocene derivatives were parallel synthesized under microwave irradiation conditions from chloroacetyl ferrocenes and substituted phenols with the aim of obtaining potential antioxidant agents. The target compounds were identified by IR, ¹H NMR, MS and elemental analysis, and their antioxidant assays indicated that all the aryloxy-acetyl ferrocenes had certain effect on eliminating 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. Their antioxidation activity significantly improved when rising the temperature until the temperature was 35°C. The structure-activity relationship analysis showed the electron-donating substituted aryloxyl group could strengthen the radical scavenging abilities, while the electron-withdrawing effects would block antioxidant abilities.

Abstract: The synthesis and interleukin-6 (IL-6) inhibitory activities for a series of 3-alkyloxylindolizine derivatives were described. The target products were characterized by NMR, IR, ESI-MS and elemental analysis, and two compounds revealed better IL-6 inhibitory effects on LPS-induced IL-6 expression in mouse macrophages with the corresponding inhibition ratio of 66% and 74% at 100 μM. The bioactive compounds might be a good generation for further optimization as potential anti-inflammatory agents.

Abstract: With the aim of obtaining potential IL-6 inhibitor for the treatment of rheumatoid arthritis, four 3-aryloxylindolizine derivatives were synthesized from the 2-bromopyridine and aryl propargyl ether through the Sonogashira coupling/5-endo-trig cycloisomerization domino strategy. These compounds were characterized by NMR, IR, EI-MS and elemental analysis. Their biological activities were evaluated by the bacterial lipopolysaccharide (LPS) stimulation of mouse cells on the RAW264.7 inflammation model. All the compounds revealed good anti-inflammatory activities with the inhibitions of 71~82% against IL-6 at 100 μM. The bioactive 3-aryloxylindolizines might be used as potential anti-inflammatory drugs.

Abstract: Five novel bisabolonalone hydrazone carboxamides were synthesized as potential anti-ulcer agents. Their structures were characterized by NMR, IR and ESI-MS. All of the compounds possessed the better H⁺/K⁺-ATPase inhibitory activity than the commercial omeprazole with the IC₅₀ of 18~68 μM in vitro. These compounds could be potentially use for the treatment of ulcer related diseases.

Abstract: A strain of bacillus alkalophilus12-7 which could produce glucanotransferase (CGTase) forming γ-cyclodextrin was screened. Cyclodextrin production technology conditions were studied, and we mainly discussed the influence of enzymatic reaction conditions on γ-cyclodextrin production by glucanotransferase. The results show that enzymatic reaction conditions are pH 8.0, temperature 60°C, enzyme amount 500 U/g starch, glycyrrhizic acid concentration 2%, DE 6 ~ 11, γ- CD yield is good, edible canna starch and tapioca starch are suitable substrate for CGTase in production of γ- CD, pullulanase in increased the γ- CD yield is limited.

Abstract: A new phenanthroimidazole platinum (II) complex has been synthesized and characterized by IR, NMR, ESI-MS, element analysis. The affinities of the complex toward ct-DNA was determined by circular dichroism absorption (CD), UV-Vis absorption. Results indicate that the complex interact with ct-DNA by classical intercalating mode. The cytotoxicities of the complex was screened against four cancer cell lines and normal cells of HL-7702 in comparison to cisplatin and it showed a higher activity than cisplatin, with IC₅₀ values in the range 8.7417.11 μmol/L. Furthermore, the complex displayed lower cytotoxic activities to HL-7702 (normal cell) compared with the cancer cell lines.

Abstract: A new platinum (II) complex has been synthesized and characterized by IR, NMR, ESI-MS and element analysis. The affinities of the complex toward telomeric G-quadruplex DNA [Htel-21] has been investigated by CD, UVVis. The results revealed that the complex can induce and stabilizes the antiparallel telomeric G-quadruplex DNA, and bind very strongly to G-quadruplex DNA. The inhibition ratio of the complex was screened against four cancer cell lines in comparison to cisplatin and it showed a higher activity than cisplatin.

Abstract: Microcrystalline Cellulose and Sarcandrae extract powder were used to study the relationships of pharmaceutical properties of powders before and after mixing operation. The theoretical values of the physical quantities of the binary mixture were calculated based on the random mixing theory. The measured values of angle of repose, hygroscopicity of binary mixture were larger than that of theoretical calculations. The effective Kawakita a and b for the MCC had changed by mixing operation. The parameters of blend powder reduced compared with MCC except D-1. The results suggested that the mixing behavior was not a complete random or simple superposition operation for the rough and sticky particles. The mixing process would create novel particles and the physical quantities of novel particles would changes regularly.

Abstract: Four bisabolangelone oxime ether derivatives were synthesized and separated as potential anti-ulcer agents. Their structures were characterized by NMR, IR and ESI-MS. Preliminarily H⁺/K⁺-ATPase activity evaluation indicated that all the target oxime ethers exhibited the better H⁺/K⁺-ATPase inhibitory activities than the commercial omeprazole with the IC₅₀ of 17~46 μM. These compounds might be used as potential anti-ulcer agents in the treatment of acid-related diseases.