A novel skeletal drug delivery system for anti-bacterial drugs using self-setting hydroxyapatite cement

To solve the problem of delivering drugs to skeletal tissue at high enough local concentrations for desirable therapeutic effects, we report a novel approach using a self-setting hydroxyapatite cement, with cephalexin and norfloxacin as model drugs. After setting, the cement was transformed into hydroxyapatite with affinity for hard bone tissue. Continuous in-vitro drug release profiles from loaded cement pellets (0.9-4.8% by weight) in phosphate buffer at pH 7.4 and 37 degrees C followed the Higuchi equation.     

A screening technique useful for testing the effectiveness of novel "self-cleaning" photocatalytic surfaces

We describe a screening methodology that can be used to quickly determine the effectiveness of newly synthesized photocatalysts. We were particularly interested in measuring the destruction of organic molecules painted onto a photocatalytic surface by spraying, with destruction proceeding in ambient air (as a model for airborne toxin destruction). Our method can utilize photocatalysts that are synthesized as powders (such as doped and undoped titanium oxide) and which are then calcined onto a glass substrate disk at 600°C. Herein, we used UV illumination of Aeroxide P-25 TiO(2), but the method is general and can accommodate any region of the light spectrum.     

Reversible, metal-free hydrogen activation by frustrated Lewis pairs

The Lewis acid cyclohexylbis(pentafluorophenyl)boron 1, which exhibits about 15% lower Lewis acidity in comparison with B(C(6)F(5))(3), activates H(2) in the presence of the bulky Lewis bases 2,2,6,6-tetramethylpiperidine (TMP), 1,2,2,6,6-pentamethylpiperidine (PMP), tri-tert-butylphosphine (t-Bu(3)P) leading in facile reactions at room temperature to heterolytic splitting of dihydrogen and formation of the salts [TMPH][CyBH(C(6)F(5))(2)] 2, [PMPH][CyBH(C(6)F(5))(2)] 3 and [t-Bu(3)PH][CyBH(C(6)F(5))(2)] 4, which could be dehydrogenated at higher temperatures. The related Lewis acid 1-phenyl-2-[bis(pentafluorophenyl)boryl]ethane 5 exhibiting about 10% lower Lewis acidity than B(C(6)F(5))(3) is also capable of splitting H(2) in a heterolytic fashion in the presence of TMP, PMP and t-Bu(3)P yielding [TMPH][PhC(2)H(4)BH(C(6)F(5))(2)] 6, [PMPH][PhC(2)H(4)BH(C(6)F(5))(2)] 7 and [t-Bu(3)PH][PhC(2)H(4)BH(C(6)F(5))(2)] 8. Under comparable conditions as for 2-4, the dehydrogenations of 6-8 were much slower. 4b and 6 were characterized by single crystal X-ray diffraction studies.     

Stable silencing of SNAP-25 in PC12 cells by RNA interference

Background  

SNAP-25 is a synaptic protein known to be involved in exocytosis of synaptic vesicles in neurons and of large dense-core vesicles in neuroendocrine cells. Its role in exocytosis has been studied in SNAP-25 knockout mice, in lysed synaptosomes lacking functional SNAP-25 and in cells after treatment with botulinum toxins A or E that specifically cleave SNAP-25. These studies have shown that SNAP-25 appears to be required for most but not all evoked secretion. In order to further study the role of SNAP-25 in catecholamine secretion from PC12 cells we have used the recently developed technique of RNA interference to generate PC12 cell lines with virtually undetectable levels of SNAP-25. RNA interference is the sequence-specific silencing or knockdown of gene expression triggered by the introduction of double-stranded RNA into a cell. RNA interference can be elicited in mammalian cells in a number of ways, one of which is by the expression of small hairpin RNAs from a transfected plasmid. Selection of stably transfected cell lines expressing a small hairpin RNA allows one-time characterization of the degree and specificity of gene silencing and affords a continuing source of well-characterized knockdown cells for experimentation.     

Desulfation and rearrangement of tigemonam to an isoxazolidin-5-one and the synthesis of the rearrangement product

The β-lactam antibiotic Tigemonam 2 undergoes desulfation to the N-hydroxyazetidinone 4 , which rearranges to the isoxazolidin-5-one 6 . The structure of the rearrangement product 6 was confirmed by synthesis.     

Fission isomerism induced by helium ions

Delayed fission events due to isomeric fission have been produced using He³ and He⁴ beams from the MP Tandem Van de Graaff accelerator. The isomeric nuclei which recoil from the target and subsequently fission in flight were detected by a square cone array of polycarbonate foil detectors mounted along the beam direction. From the distribution of fission tracks along the detector foils, half-lives in the nanosecond region were deduced.