Synthesis and Anti-Proliferative Activity of Novel Quinolin-8-ol Derivatives

Through the coupling of substituted benzaldehydes with 8-hydroxy 5-amino methyl quinoline scaffold, a series of new derivatives has been synthesized. In vitro growth inhibitory effects on cancer cell line model have been evaluated. Discussion on the chemical reactivity of these new polycyclic aromatic analogs to generate alkylating species led to the hypothesis that the presence of an imine moiety impedes the formation of quinone methide intermediate and consequently abolishes in part their antiproliferative activity.     

Nonlinear finite-element analysis and biomechanical evaluation of the lumbar spine

A finite-element analysis (FEA) model of an intact lumbar disc-body unit was generated. The vertebral body of the FEA model consisted of a solid tetrahedral core of trabecular bone surrounded by a cortical shell. The disc consisted of an incompressible nucleus surrounded by nonlinear annulus fibers embedded in a solid ground substance. The purpose was to create a FEA model suitable for clinical purposes as fracture assessment, instrumentation with pedicle screws, and bone remodeling. Testing of the FEA model was performed nonlinear for a number of loading conditions, and the results were compared with experimental data from the literature. The results showed good agreement. The formulation of the FEA model can be justified for the tested loading conditions.     

Primary treatment of left coronary artery diseases by percutaneous implantation of stents

Left main coronary artery (LM) stenting has only been reported in bail-out situations or absolute contraindications so surgery. The authors report the immediate and midterm results of primary Palmaz-Schatz stent implantation in two young patients without contraindication to surgery. The first patient, 58 year-old, was admitted for unstable angina in October 1994. Coronary angiography showed an isolated severe ostial lesion of the LM. After conferring with the surgical team which remained on stand-by, angioplasty and stent implantation were performed with excellent results, no complications and no restenosis on angiographic controls at 3 and 12 months. The patient remained asymptomatic 24 months later. The second patient, 38 year-old, was admitted in June 1995 for unstable angina, and coronary angiography showed a severe isolated stenosis in the middle of a long and wide LM. Primary coronary stenting was also performed with excellent results, no complication and no restenosis on angiographic controls at 4 and 8 months. This patient was still asymptomatic 16 months after stenting. These excellent immediate and medium-term results are encouraging and suggest that this form of treatment might be extended to patients with an isolated whether primary LM stent implantation could become a suitable alternative to surgery in the future.     

Effect of Water and Serum Absorption on Wear of Unirradiated and Crosslinked UHMWPE Orthopedic Bearing Materials

Abstract

In addition to confounding mass-based wear measurements in serum-lubricated hip simulator experiments, fluid absorption by the acetabular cups may simultaneously modify the wear resistance of the ultra-high molecular weight polyethylene (UHMWPE) from which they are composed. To decouple the fluid absorption and wear processes enabling clearer investigation of this effect, absorption was first imposed during an initial stage where UHMWPE was exposed to pressurized (10 MPa) fluid. This was followed by a second stage, where resultant wear behavior was assessed by a multidirectional pin-on-flat technique that, though still providing a serum-lubricating environment, does not promote the simultaneous fluid absorption occurring in hip simulator testing. Both unirradiated and highly crosslinked UHMWPE were investigated, each with both bovine calf serum and water soaking exposures of duration to 129 days. The pressurized soaking of a highly crosslinked UHMWPE decreased its wear resistance, causing an increase in wear rate by approximately 50% during subsequent serum-lubricated multidirectional pin-on-flat sliding tests as compared to non-soaked material. The magnitude of this effect did not appear to depend on whether the soaking fluid was water or serum, nor did it appear to depend on soak time provided it was at least of a 14-day duration, during which more rapid transient fluid absorption occurs. Such soaking did not produce as pronounced an effect on unirradiated UHMWPE, as its lack of wear resistance likely causes the absorption-affected surface region to be removed within the earliest stages of sliding contact.     

Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage

One of the great challenges of medicinal chemistry is to create novel, effective, chemotherapeutic agents that show specificity for cancer cells combined with low systemic toxicity. A novel idea is to target the enzymes of the NAD biosynthesis and recycling pathways given that cancer cells display a higher NAD turnover rate than healthy cells. To this end, the compound FK866 (APO866; (E)-N-[4-(1-benzoylpiperidin-4-yl) butyl]-3-(pyridin-3-yl) acrylamide), which blocks nicotinamide phosphoribosyltransferase (NMPRTase) has entered clinical trials as a potential chemotherapeutic agent. Here we report the synthesis of analogues of FK866 synthesized by click chemistry.     

Reconstruction of the rose of directions from a digital microhologram of fibres

Digital holography makes it possible to acquire quickly the interference patterns of objects spread in a volume. The digital processing of the fringes is still too slow to achieve on line analysis of the holograms. We describe a new approach to obtain information on the direction of illuminated objects. The key idea is to avoid reconstruction of the volume followed by classical three-dimensional image processing. The hologram is processed using a global analysis based on autocorrelation. A fundamental property of diffraction patterns leads to an estimate of the mean geometric covariogram of the objects projections. The rose of directions is connected with the mean geometric covariogram through an inverse problem. In the general case, only the two-dimensional rose of the object projections can be reconstructed. The further assumption of unique-size objects gives access with the knowledge of this size to the three-dimensional direction information. An iterative scheme is suggested to reconstruct the three-dimensional rose in this special case. Results are provided on holograms of paper fibres.     

栓菌漆酶的异源表达及重组酶碳端和氮端组氨酸标签修饰对酶学特性的影响

以来源Trametes sp.C30 的LAC3漆酶基因为研究对象,通过引物设计进行突变,在其C端和N端进行延长,分别引入6 个组氨酸标签,并异源表达于酿酒酵母Saccharomyces cerevisiae中,将获得的重组酶进行比较发现漆酶末端氨基酸序列的改变对酶学性质的影响较大。C端引入组氨酸标签的重组酶的表达量不受影响,但是在N末端引入组氨酸标签的重组酶表达量只有LAC3的一半。添加组氨酸标签的融合蛋白对ABTS和SGZ两种底物的亲和力得到增强。而在酸碱稳定性耐受方面,与LAC3相比,N末端氨基酸的改变使其在酸碱稳定性方面得到了增强,中碱性条件下仍能保持较佳活性。C端和N端可塑性的研究对于漆酶新性状的获得具有重要意义。     

Playtime

Three installation projects take tropes such as the labyrinth, the lumberjack culture and the neighbor's fence, and turn them into spaces of gathering and play.