Effects of novel taxanes SB-T-1213 and IDN5109 on tubulin polymerization and mitosis

SB-T-1213 and IDN5109 are semisynthetic, orally available taxanes that are up to 400-fold more active than paclitaxel against drug-resistant cells. IDN5109 is in clinical trials. We investigated the primary target for SB-T-1213 and IDN5109 and whether the compounds interact with microtubules differently than paclitaxel. Unlike paclitaxel, at 1-10 microM both novel taxanes initiate microtubule polymerization in vitro with no lag. They enhance polymerization equally or more potently than paclitaxel. SB-T-1213 induces unusual microtubules with attached extra protofilaments or open sheets, and IDN5109 induces large protofilamentous sheets. Both inhibit HeLa cell proliferation, block mitosis at the metaphase/anaphase transition, bundle microtubules at high drug concentrations, and induce abnormal metaphase spindles and apoptosis. They target microtubules but alter their polymerization and structure differently than paclitaxel. These differences may play a role in their enhanced cytotoxicity and efficacy.     

The 2-Extendability of Graphs on the Projective Plane, the Torus and the Klein Bottle

A graph is said to be k-extendable if any independent set of k edges extends to a perfect matching. We shall show that every 5-connected graph of even order embedded on the projective plane and every 6-connected one embedded on the torus and the Klein bottle is 2-extendable and characterize the forbidden structures for 5-connected toroidal graphs to be 2-extendable.     

Zeta functions and complexities of a semiregular bipartite graph and its line graph

We treat zeta functions and complexities of semiregular bipartite graphs. Furthermore, we give formulas for zeta function and the complexity of a line graph of a semiregular bipartite graph. As a corollary, we present the complexity of a line graph of a complete bipartite graph.     

Transient thermal lensing measurement in a laser diode pumped NdxY1−xAl3(BO3)4 laser using a holographic shearing interferometer

A new technique for measuring a thermal lens, using a holographic shearing interferometer is presented. This technique was used to measure transient thermal lensing in a laser diode pumped NYAB laser. The measured thermal lensing power was proportional to the pumping laser diode intensity, with a gradient of 1.1 × 10⁻¹ m⁻¹ mm²/W. The transient response time of the thermal lens was 1.5 s, this value being consistent with the temporal decline of the second harmonic power.     

Fluorescence response mechanism of D-glucose selectivity for supramolecular probes composed of phenylboronic-acid-modified beta-cyclodextrin and styrylpyridinium dyes.

Supramolecular complex formation of phenylboronic-acid-modified beta-cyclodextrin (1) with 1-methyl-4-(4-dimethylaminostyryl)pyridinium (C1SP) in aqueous solutions containing saccharides was fully clarified to gain an insight into the observed D-glucose (D-glc) selectivity of a supramolecular fluorescent probe composed of 1 and the 1-heptyl analogue of C1SP (Chem. Commun., 2006, 4319). At pH 9.6, where 1 was in its anionic form, both the stability and the fluorescence of the 1/C1SP complex were reduced by the formation of boronate esters of 1 with saccharides. Among the saccharides, D-glc had the smallest effect on destabilization of the 1/C1SP complex, almost completely retaining the fluorescence of the 1/C1SP complex that was reduced by other saccharides by approximately 2/3. Under neutral conditions, D-glc enhanced the fluorescence of the 1/C1SP complex by increasing the fraction of anionic 1 while minimally decreasing the stability and fluorescence of the 1/C1SP complex. Although other saccharides also increased the fraction of the anionic 1, their relatively large effects on the destabilization and reduction of fluorescence of the 1/C1SP complex limited the enhancement of the fluorescence of the 1-C1SP system under neutral conditions.     

FIVE-MEMBERED RING COMPOUNDS IN ORGANOMETALLIC INTRAMOLECULAR-COORDINATION COMPOUNDS

Organometallic intramolecular-coordination five-membered ring compounds show high reactivity and high selectivity. Therefore, these many compounds have been synthesized since around mid 1960s. More than 50 kinds of metals are found as the metal elements, and these compounds are very widely used as intermediates and catalysts for organic syntheses.     

Surface chemical approach to single-step measurement of antibody in human serum using localized surface plasmon resonance biosensor on microtiter plate system

In clinical settings, serum antibody levels serve as markers of pathology. For example, antibodies related to autoimmune diseases are among the conventional targets in laboratory tests. Simple clinical tests can improve the efficacy of laboratory practice. This study describes a single-step, wash-free technique for optically detecting antibodies in human serum through the localized surface plasmon resonance (LSPR) of gold nanoparticles. As a proof-of-concept experiment, the amount of antibiotin dissolved in human serum was measured with a LSPR-based biosensor in a wash-free manner using a conventional 96-well microtiter plate and a plate reader. For an efficient surface modification of biosensors, zwitterionic copolymer was used as a scaffold on the gold nanoparticle surface to immobilize antigen and blocking reagent. Single-step, wash-free measurement of antibiotin in human serum was successfully achieved. In addition, nonspecific responses from serum contents were significantly reduced because both the copolymer and hydrophilic antigen reagent that we employed were composed of poly(ethylene oxide) spacer. Comparative experiments of the antigen-antibody reaction in serum to that in buffered solution revealed that serum is a favorable environment for the biological reaction. In conclusion, our gold-nanoparticle-based LSPR method may provide a rapid and simple way to measure the amount of antibody in serum quantitatively in clinical practice.

Zeta functions of line, middle, total graphs of a graph and their coverings

We consider the (Ihara) zeta functions of line graphs, middle graphs and total graphs of a regular graph and their (regular or irregular) covering graphs. Let L(G), M(G) and T(G) denote the line, middle and total graph of G, respectively. We show that the line, middle and total graph of a (regular and irregular, respectively) covering of a graph G is a (regular and irregular, respectively) covering of L(G), M(G) and T(G), respectively. For a regular graph G, we express the zeta functions of the line, middle and total graph of any (regular or irregular) covering of G in terms of the characteristic polynomial of the covering. Also, the complexities of the line, middle and total graph of any (regular or irregular) covering of G are computed. Furthermore, we discuss the L-functions of the line, middle and total graph of a regular graph G.     

Electrochemistry of xanthine oxidase and its interaction with nitric oxide.

With the help of nanocrystalline TiO2, the direct electrochemistry of xanthine oxidase (XOD) was achieved and two pairs of redox waves were observed. The interaction between XOD and nitric oxide (NO) was also investigated. The experimental results reveal that NO can be reduced at a XOD-nano TiO2 film modified electrode. When the NO concentration was low, the reduced product, HNO, would inactivate the protein. However, when the NO concentration was high, HNO would continue to react with NO to form N2O2- and N3O3-, which would not inhibit XOD, and thus the amount of active protein did not decrease any further.