Design, synthesis, and SAR study of novel flavone 1,2,4-oxadiazole derivatives with anti-inflammatory activities for the treatment of Parkinson's disease.

Inflammation is one of a major feature of Parkinson's disease (PD) which poses a threat to people's health in the world. It has been reported that antioxidation and anti-inflammation have significant effects on the treatment of PD. 1,2,4-oxadiazole and flavone derivatives have remarkable antioxidant and anti-inflammatory activities. In order to find highly effective drugs for PD treatment, based on the remarkable anti-inflammatory and antioxidant activities of the 1,2,4-oxadiazole pharmacophore and the flavonoid pharmacophore, we designed and synthesized a novel series of 3-methyl-8-(3-methyl-1,2,4-oxadiazol-5-yl)-2-phenyl-4H-chromen-4-one derivatives by pharmacophore combination, and evaluated their anti-inflammatory and antioxidation activities for PD treatment. Preliminary structure-activity relationship (SAR) analysis was conducted by their inhibitory activities against reactive oxygen species (ROS) and NO release in LPS-induced BV2 Microglia cells, and the optimal compound Flo8 exhibited the most potent anti-inflammatory and antioxidant activities. Both in vivo and in vitro results showed that Flo8 inhibited neuronal apoptosis by inhibiting inflammatory and apoptotic signaling pathways. In vivo studies also showed that the compound Flo8 ameliorated motor and behavioral deficits and increased serum dopamine levels in MPTP-induced PD model mice. Taken together, this study demonstrated the compound Flo8 could be a promising agent for the treatment of PD.

Porous BCN nanotubular fibers: growth and spatially resolved cathodoluminescence.

Porous boron carbonitride nanotubular fibers with BCN stoichiometry and homogeneous B, C, and N species distribution were fabricated via the CVD method. Spatially resolved cathodoluminescence measurements on individual nanostructures revealed intense ultraviolet emission centered at 319 nm, suggesting the characteristics of a semiconductor with a band gap of 3.89 eV. It is believed that the present nanostructures may have a variety of applications in ultraviolet optical devices, hydrogen storage systems, and field emission apparatus.

Growth of semiconducting GaN hollow spheres and nanotubes with very thin shells via a controllable liquid gallium-gas interface chemical reaction.

An in situ liquid gallium-gas interface chemical reaction route has been developed to synthesize semiconducting hollow GaN nanospheres with very small shell size by carefully controlling the synthesis temperature and the ammonia reaction gas partial pressure. In this process the gallium droplet does not act as a catalyst but rather as a reactant and a template for the formation of hollow GaN structures. The diameter of the synthesized hollow GaN spheres is typically 20-25 nm and the shell thickness is 3.5-4.5 nm. The GaN nanotubes obtained at higher synthesis temperatures have a length of several hundreds of nanometers and a wall thickness of 3.5-5.0 nm. Both the hollow GaN spheres and nanotubes are polycrystalline and are composed of very fine GaN nanocrystalline particles with a diameter of 3.0-3.5 nm. The room-temperature photoluminescence (PL) spectra for the synthesized hollow GaN spheres and nanotubes, which have a narrow size distribution, display a sharp, blue-shifted band-edge emission peak at 3.52 eV (352 nm) due to quantum size effects.

Plasma-sprayed hydroxyapatite+titania composite bond coat for hydroxyapatite coating on titanium substrate.

A two-layer hydroxyapatite (HA)/HA+TiO(2) bond coat composite coating (HTH coating) on titanium was fabricated by plasma spraying. The HA+TiO(2) bond coat (HTBC) consists of 50 vol% HA and 50 vol% TiO(2) (HT). The microstructural characterization of the HTH coatings before and after heat treatment was conducted by using scanning electron microscopy (SEM), electron probe microanalyser (EPMA), X-ray diffractometer (XRD) and transmission electron microscopy (TEM), in comparison with that of HT coating and pure HA coating. The results revealed that HA and TiO(2) phases layered in an alternating pattern within the HTBC, and the HTBC bonded well to HA top coating (HAT coating) and Ti substrate. The as-sprayed HT coating consists mainly of crystalline HA, rutile TiO(2) and amorphous Ca-P phase. The post-spray heat treatment at 650 degrees C for 120 min effectively restores the structural integrity of HA by transforming non-HA phases into HA. It was found that there exists interdiffusion of the elements within the HTBC, but no chemical product between HA and TiO(2), such as CaTiO(3) was formed. The cross-sectional morphologies confirmed that there is a shift towards a relatively tighter bonding from the HAT coating/HTBC interface in the as-sprayed HTH coating to the HTBC/Ti substrate interface in the heat-treated HTH coating. On quenching the coatings into water, the surface cracking indicates more apparently the positive effect of the HTBC on the decrease of residual stress in HAT coating. The in situ surface cracking also suggests that the stress on the surface of the HTH coating is stable under subjection to a repetitious heat treatment. The toughening and strengthening of HTBC is thought to be mainly due to TiO(2) as obstacles embarrassing cracking, the reduction of the near-tip stresses resulting from stress-induced microcracking and the decrease of CTE mismatch. In the HTH composite coating, the HAT coating is toughened by the decreased CTE mismatch with Ti through the addition of HTBC, which bonds well to the Ti substrate via its TiO(2) hobnobbing with the Ti oxides formed on Ti substrate.