Baicalin induces apoptosis in SW620 human colorectal carcinoma cells in vitro and suppresses tumor growth in vivo

In the United States, colorectal cancer (CRC) is the second most frequent malignancy and the fourth most common cause of cancer death. Baicalin, a flavone derivative isolated and purified from the dry root of Scutellaria, was assessed for its antitumor effects in human SW620 CRC cells. Baicalin (200 μM) inhibited proliferation of SW620 cells. Baicalin (200 μM) increased activities of caspase-3, -8, and -9 in SW620 cells. Furthermore, flow cytometric analysis of baicalin-treated SW620 cells showed an increase in sub-G1 cells, and the dihydroethidium assay showed significant enhancement of intracellular peroxide production in baicalin-treated cells. Addition of N-acetylcysteine prevented most of the baicalin-induced apoptosis, which in turn mediated cytotoxicity in human SW620 cells. In vivo, baicalin (50 mg/kg/day, i.p.) treatment inhibited 55% of tumor growth in xenografted nude mice by 4 weeks, compared to that of the vehicle control (p < 0.05). Baicalin had no noteworthy influence on body weight. Thus, we suggest the development of baicalin as a potential leading antitumor agent in CRC.     

Electrostatic assembly of gold colloidal nanoparticles on organosilane monolayers patterned by microcontact electrochemical conversion

A new approach is introduced for electrostatically guided adsorption of colloidal nanoparticles onto a patterned self-assembled monolayer (SAM) with feature sizes ranging from nm to mm. Patterning of the adsorption templates is realized by electric-field-induced anodic oxidation of aminosilane SAM using an ink-free method. In this versatile method, both "positive" and "negative" type pattern transfers are possible. The chemically converted patterns are induced by localized electrical fields on the microcontacted areas, and the patterning resolution is insensitive to the diffusion of oxidizing agents because of the self-limiting oxidation kinetics, thereby enabling high-resolution, large-scale parallel patterning.     

Surfactant-assisted hollowing of Cu nanoparticles involving halide-induced corrosion-oxidation processes

We have demonstrated a simple fabrication of hollow nanoparticles by halide-induced corrosion oxidation with the aid of surfactants. Cuprous oxide Cu2O nanoshells can be generated by simply mixing Cu nanoparticles with alkyltrimethylammonium halides at 55 degrees C for 16 min. The hollowing mechanism proposed is that absorption of surfactants onto the Cu surface facilitates the formation of the void interior through an oxidative etching process. Upon extending the reaction up to 4 h, fragmentation, oxidation, and self-assembly were observed and the CuO ellipsoidal structures were formed. The headgroup lengths of the surfactants influenced the degree of CuO ellipsoidal formation, whereby longer surfactants favored the generation of ellipsoids. Optical absorption measured by UV-visible spectroscopy was used to monitor both oxidation courses of Cu-->Cu2O and Cu2O-->CuO and to determine the band-gap energies as 2.4 eV for Cu2O nanoshells and 1.89 eV for CuO ellipsoids. For the contact-angle measurements, the wettability changed from hydrophilicity (18 degrees) to hydrophobicity (140 degrees) as the Cu2O nanoshells shifted to CuO ellipsoids.     

Simultaneous determination of adenosine and its metabolites by capillary electrophoresis as a rapid monitoring tool for 5'-nucleotidase activity

A simple and rapid capillary electrophoretic method was developed for the simultaneous determination of micro-molar adenosine, hypoxanthine and inosine in enzyme assays without using radioactive labeled substrates. Prior to electrophoretic separation, addition of acetonitrile and sodium chloride to the assay solution and brief centrifugation are recommended for the purpose of sample cleanup and sample stacking. Under the optimal condition, the good separation with high efficiency was achieved in 6 min. Using deoxyadenylate as an internal standard, the linear range of the method was 5-200 microM, and the concentration limits of detection of adenosine, hypoxanthine and inosine were 2.2, 3.6 and 1.4 microM, respectively. Application of the proposed method was demonstrated by the activity assay of 5'-nucleotidase from Hep G2 cells.     

Internal electric field distribution within a micro-cylinder-shaped particle suspended in an absorbing gaseous medium

The present study is concerned with photophoresis of a microsized long cylinder-shaped particle suspended in an absorbing gas medium. To facilitate the analysis, an infinite cylinder subjected to an intensive light beam is considered as the physical model. The electromagnetic energy can be absorbed by the particle and turned into thermal energy heating surface unevenly, which results in a net momentum transfer between gas molecules and the particle to drive particle in photophoretic motion. Effects of the governing parameters on the absorbed energy distribution in the cylindrical particle are investigated. The results demonstrate that increasing either the radius or absorptivity of the cylinder enhances the energy absorbed on the illuminated side and tends to generate positive photophoresis; while an increase in the refractivity of the particle tends to enhance the internal electric field intensity and shift the absorption peak on the shaded side toward the particle center. Increase in medium absorptivity reduces the energy reaching at the particle, which significantly degrades the level of energy absorption and therefore weakens the photophoretic mobility of the particle. It is also found that, at the same conditions, the source function peaks in long cylinder-shaped particles are generally lower than those in spheres due to the weaker light refraction of the cylindrical shape.     

4-Azapteridines. I. Covalent addition products of the pyrazino[2,3-e]-as-triazine ring system

Ring closure of 5, 6-diamino-3-methylthio-as-triazine with 40% aqueous glyoxal provided the 6, 7-dihydrate of the pyrazino[2, 3-e]-as-triazine (4-azapteridine) ring system. The C7 hydroxy group of this dihydrate underwent exchange in methanol or ethanol affording the 7-alkoxy, 6-hydroxy derivatives.     

Antiplatelet α-Methylidene-γ-butyrolactones: Synthesis and evaluation of quinoline,flavone, and xanthone derivatives

As a continuation of our previous studies on the synthesis and antiplatelet activity of coumarin derivatives of α-methylidene-γ-butyrolactones, certain quinoline, flavone, and xanthone derivatives were synthesized and evaluated for antiplatelet activity against thrombin (Thr)-, arachidonic acid (AA)-, collagen (Col)-, and platelet-activating factor (PAF)-induced aggregation in washed rabbit platelets. These compounds were synthesized from quinolin-8-ol, flavon-7-ol, and xanthon-3-ol, respectively, via alkylation and Reformatsky-type condensation (Schemes 1–3). By the comparison with comparison with coumarin α-methylidene-γ-butyrolactone 3a , flavone and xanthone derivatives, 3b and 3c , respectively, are more selective in which only AA- and collagen-induced aggregation are strongly inhibited. Most of the quinoline derivatives ( 9a–e ) exhibited broad-spectrum antiplatelet activities.     

Syntheses of ruthenium(II) quinonediimine complexes of cyclam and characterization of their DNA-binding activities and cytotoxicity

The synthesis and characterization of ruthenium(II) complexes, [Ru(cyclam)(bqdi)] x ZnCl(4) (1 x ZnCl(4); cyclam = 1,4,8,11-tetraazacyclotetradecane, bqdi = o-benzoquinonediimine), [Ru(cyclam)(nqdi)] x (ClO(4))(2) (2 x (ClO(4))(2); nqdi = 2,3-naphthoquinonediimine), and [Ru(cyclam)(phi)] x (ClO(4))(2) (3 x (ClO(4))(2); phi = 9,10-phenanthroquinonediimine), are described. The DNA binding properties and biological activity of the Ru(II) complexes were studied by various biophysical and cytological techniques. As expected, only 3 showed significant binding with DNA. The thermodynamic profile of the binding of 3 and DNA was constructed by analyzing the experimental data of absorption titration and UV melting studies with the McGhee equation, van't Hoff's equation, and the Gibbs-Helmholtz equation. Compound 3 binds double-stranded DNA with a binding constant of 5.0 x 10(4) M(-1) at 20 degrees C, and the binding mode of the complex to DNA was proved to be intercalative. Cytotoxicity and induced type of cell death of 1-3 were also investigated. Basically, metal complexes with ligands of molecular shape closely related to the structure of DNA are more likely to bind DNA and possess higher toxicity.     

A new highly oxygenated pseudoguaianolide from a collection of the flowers of Parthenium hysterophorus

A new highly oxygenated pseudoguaianolide, 8-beta-acetoxyhysterone C, along with the known compounds, parthenin, coronopilin and hysterone C, has been isolated from a collection of the flowers of Parthenium hysterophorus. The structure of the new compound was derived from the extensive studies of its spectral (mainly 1D and 2D NMR) data.