Unexpected phenyl group rearrangement during an intramolecular Scholl reaction leading to an alkoxy-substituted hexa-peri-hexabenzocoronene

A simple dimethoxy-substituted hexa-peri-hexabenzocoronene (m-dimethoxy HBC) was unexpectedly obtained along with a bis-spirocyclic dienone during an intramolecular Scholl reaction of its para isomer.     

Structure-based design of conformationally constrained cyclic peptidomimetics to target the MLL1-WDR5 protein–protein interaction as inhibitors of the MLL1 methyltransferase activity

We described herein structure-based design,synthesis and evaluation of conformationally constrained,cyclic peptidomimetics to block the MLL1-WDR5 protein–protein interaction as inhibitors of the MLL1 histone methyltransferase activity.Our study has yielded cyclic peptidomimetics with very high binding affinities to WDR5(Kivalues 1 nmol/L) and function as antagonists of the MLL1 histone methyltransferase activity.     

β-Elemene-loaded polymeric micelles intensify anti-carcinoma efficacy and alleviate side effects

β-Elemene is a volatile oil used for the treatment of cancer,but poor solubility,low bioavailability,and various adverse reactions limit its application.For amelio rating risks of the venous toxicity ofβ-elemene,intravenously injectable micelle ofβ-elemene was prepared using the thin-film hydration method.The results pointed out the micelles were uniformly spherical with about 20.96±0.1966 nm in average diameter and exhibited high entrapment efficiency(99.02%±0.88%).As revealed by drug release studies in vitro,β-elemene micelles had sustained drug release.Compared with freeβ-elemene,the micelles increased the drug cellular uptake and enhanced the anti-tumor effect in vitro through retarding cell cycle and inducing apoptosis.Meanwhile,the elevated se rum stability o fβ-elemene micelles implied less drug leakage and reduced toxicity.The wound healing and tube formation assay in vitro demonstrated the anti-metastasis and anti-angiogenesis effects ofβ-elemene micelles.Moreover,the pharmacokinetics study showed the AUC and T1/2 ofβ-elemene in micelle group were 1.79 and 1.62 times of that in free fi-elemene group,suggesting the circulation time ofβ-elemene in the blood had been prolonged.In addition,β-elemene micelles showed a favorable antitumor response compared with theβ-elemene solution on C26 colon cance r-bearing mice model.Local irritation study investigated in rabbits indicated that theβ-elemene micelles strikingly mitigated the irritation to the injection sites compared with freeβ-elemene.These results proved that the micelle could be a good candidate as an auspicious drug delivery system ofβ-elemene for the prospective clinical treatment of carcinoma.     

Magnetic phase diagrams based on static and dynamic magnetic behaviour in Ru-based superconducting ferromagnets

In this work, we present magnetic phase diagrams of a RuSr(2)Eu(1.5)Ce(0.5)Cu(2)O(10-δ) (Ru-1222) superconducting ferromagnet derived from its static and dynamic magnetic responses, measured by temperature and field dependences of dc magnetization and nonlinear ac susceptibility in both low and high magnetic fields. Comparison of magnetic phase diagrams of phase pure and impure samples singles out the intrinsic and extrinsic magnetic features, naturally proposing a unified model of Ru-1222 magnetic behaviour. The results considered within the proposed interpretation indicate full agreement between static and dynamic properties which, if measured in combination, effectively complement each other, uncovering existing ambiguities.     

Synthesis, characterization, and reactivity of the stable iron carbonyl complex [Fe(CO)(N4Py)](ClO4)2: photoactivated carbon monoxide release, growth inhibitory activity, and peptide ligation

Photoactivated carbon monoxide (CO) release by the iron carbonyl complex [Fe(II)(CO)(N4Py)](ClO(4))(2) (1) is described. Compound 1 is a low-spin ferrous complex that is highly stable and soluble in aerobic aqueous solutions. CO release was studied by the substitution of MeCN for CO, which displays saturation kinetics, and by the transfer of CO to deoxymyoglobin, which is slow in the dark but fast upon irradiation with UV light (365 nm). Compound 1 is active against PC-3 prostate cancer cells and shows potent photoinduced cytotoxicity. In addition, the iron carbonyl complex was attached to a short peptide toward the goal of tissue or cell-specific delivery.     

Disruption of <Emphasis Type="BoldItalic">Chlorella vulgaris</Emphasis> Cells for the Release of Biodiesel-Producing Lipids: A Comparison of Grinding,Ultrasonication, Bead Milling,Enzymatic Lysis,and Microwaves

A comparative evaluation of different cell disruption methods for the release of lipids from marine Chlorella vulgaris cells was investigated. The cell growth of C. vulgaris was observed. Lipid concentrations from different disruption methods were determined, and the fatty acid composition of the extracted lipids was analyzed. The results showed that average productivity of C. vulgaris biomass was 208 mg L⁻¹ day⁻¹. The lipid concentrations of C. vulgaris were 5%, 6%, 29%, 15%, 10%, 7%, 22%, 24%, and 18% when using grinding with quartz sand under wet condition, grinding with quartz sand under dehydrated condition, grinding in liquid nitrogen, ultrasonication, bead milling, enzymatic lysis by snailase, enzymatic lysis by lysozyme, enzymatic lysis by cellulose, and microwaves, respectively. The shortest disruption time was 2 min by grinding in liquid nitrogen. The unsaturated and saturated fatty acid contents of C. vulgaris were 71.76% and 28.24%, respectively. The extracted lipids displayed a suitable fatty acid profile for biodiesel [C16:0 (~23%), C16:1 (~23%), and C18:1 (~45%)]. Overall, grinding in liquid nitrogen was identified as the most effective method in terms of disruption efficiency and time.     

Development and applications of fluorescent indicators for Mg2+ and Zn2+

In a study of the spectroscopic behavior of two Schiff base derivatives, salicylaldehyde salicylhydrazone (1) and salicylaldehyde benzoylhydrazone (2), Schiff base 1 has high selectivity for Zn(2+) ion not only in abiotic systems but also in living cells. The ion selectivity of 1 for Zn(2+) can be switched for Mg(2+) by swapping the solvent from ethanol-water to DMF (N,N-dimethylformamide)-water mixtures. Imine 2 is a good fluorescent probe for Zn(2+) in ethanol-water media. Many other ions tested, such as Li(+), Na(+), Al(3+), K(+), Ca(2+), Cr(3+), Mn(2+), Fe(3+), Co(2+), Ni(2+), Cu(2+), Ag(+), Cd(2+), Sn(2+), Ba(2+), Hg(2+), and Pb(2+), failed to induce any spectral change in various solvents. The selectivity mechanism of 1 and 2 for metal ions is based on a combinational effect of proton transfer (ESPT), C═N isomerization, and chelation-enhanced fluorescence (CHEF). The coordination modes of the complexes were investigated.     

Efficient quantum private comparison protocol based on one direction discrete quantum walks on the circle

We propose an efficient quantum private comparison protocol firstly based on one direction quantum walks. With the help of one direction quantum walk, we develop a novel method that allows the semi-honest third party to set a flag to judge the comparing result, which improves the qubit efficiency and the maximum quantity of the participants' secret messages. Besides, our protocol can judge the size of the secret messages, not only equality. Furthermore, the quantum walks particle is disentangled in the initial state. It only requires a quantum walks operator to move, making our proposed protocol easy to implement and reducing the quantum resources. Through security analysis, we prove that our protocol can withstand well-known attacks and brute-force attacks. Analyses also reveal that our protocol is correct and practical.     

Efficient incorporation of quantum dots into porous microspheres through a solvent-evaporation approach

Quantum dot (QD)-encoded microspheres play an important role in suspension arrays by acting as supports for various reactions between biomolecules. With regard to QD-encoded microspheres utilized in suspension arrays, three key requirements are controllable size, abundant surface functional groups, and especially excellent fluorescence properties. In this paper, narrowly dispersed poly(styrene-co-divinylbenzene-co-methylacrylic acid) (PSDM) microspheres with specific size, surface carboxyl groups, and porous structures were synthesized by seeded copolymerization. In order to improve the incorporation efficiency of QDs within microspheres, we developed a swelling-evaporation approach in which the swelling process was combined with gradual evaporation of the solvent and thus gradual concentration of QDs in the dispersion solution. This approach was demonstrated to be an efficient method for improving the fluorescence intensity of resultant microspheres compared with the use of swelling alone. Moreover, the porous structure was shown to aid the penetration of QDs into the interiors of the microspheres. Through this approach, microspheres encoded with either single or multiple wavelength-emitting QDs were fabricated effectively. The suspension immunoassays were then founded based on the QD-encoded microspheres, by coating mouse antihuman chorionic gonadotropin as the probe for goat antimouse IgG detection. The positive results determined by Luminex 100 and the low cytotoxicity of the QD-encoded microspheres demonstrated their great potential in suspension arrays.