Novel ether-functional spiro-tetronic acid derivatives: molecule design, convenient synthesis and biological evaluation

A novel series of ether functionalization of spiro-tetronic acid derivatives have been designed and conveniently synthesized via three steps, including esterification, one-pot heterocyclization, and etherification reactions. The target molecules have been identified on the basis of analytical spectra data. All newly synthesized compounds have been screened for their potential insecticidal activity against Heliothis armigera and Plutella xylostella compared with spirodiclofen by standard method.     

Design,Synthesis, and Cytotoxic Activity of Novel Natural Arylsulfonamide-Inspired Molecules

Primary arylsulfonamide functional groups feature prominently in diverse pharmaceuticals. However, natural arylsulfonamides are relatively infrequent. In this work, two novel arylsulfonamide natural products were first synthesized, and then a series of novel molecules derived from natural arylsulfonamides were designed and synthesized, and their in vitro cytotoxic activities against A875, HepG2, and MARC145 cell lines were systematically evaluated. The results indicate that some of these arylsulfonamide derivatives exhibit significantly good cytotoxic activity against the tested cell lines compared with the control 5-fluorouracil (5-FU), such as compounds 10l, 10p, 10q, and 10r. In particular, the potential molecule 10q, containing a carbazole moiety, exhibited the highest inhibitory activity against all tested cell lines, with IC₅₀ values of 4.19 ± 0.78, 3.55 ± 0.63, and 2.95 ± 0.78 μg/mL, respectively. This will offer the potential to discover novel drug-like compounds from the sparsely populated area of natural products that can lead to effective anticancer agents.     

The influence of KH-550 on properties of ammonium polyphosphate and polypropylene flame retardant composites

Ammonium polyphosphate (APP)/polypropylene (PP) composites were prepared by melt blending and extrusion in a twin-screw extruder. APP was first modified by a silane coupling agent KH-550 then added to polypropylene. The surface modification of APP by the coupling agent decreased its water solubility and its interface compatibility with the PP matrix. Limiting oxygen index (LOI) and thermogravimetric analysis (TGA) were used to characterize the flame retardant property and the thermal stability of the composites. The addition of APP improved the flame retardancy of PP remarkably. The crystal structures of APP/PP composites were characterized by X-ray diffraction (XRD). The results indicated that β-crystal phase PP may be formed. The structures and morphologies of APP, KH-550/APP and APP/PP composites were characterized by field-emission scanning electron microscope (FESEM). The mechanical property tests showed good mechanical properties of composite materials. Compared with unmodified one, the impact strength, tensile strength and elongation of modified APP/PP were all improved.     

Synthesis and Antifungal Activity of Substituted 2‐Aryl Benzimidazoles Derivatives

Benzimidazole fungicides were among the early systemic fungicides developed and used for controlling a wide variety of plant diseases. During the course of our screening process for active compounds, two 2‐aryl benzimidazoles derivatives bearing sulfoxide group ( 6b and 6c ) have been demonstrated to exhibit good inhibition activity against high‐resistant isolate of Botrytis cinerea compared with carbendazim, and the inhibition rates are up to 46.67% and 51.11% at the concentration of 10 μg/mL, which might be considered as the active framework for the discovery of novel fungicide to high‐resistant isolate of B. cinerea.     

Improved method to retrieve aerosol optical properties from combined elastic backscatter and Raman lidar data

Two methods to load a microtrap consisting of two concentric microwire loops of radii 300 and 660 μm carrying oppositely oriented currents are demonstrated. Atoms can be directly loaded into the microtrap from a surface magneto-optical trap or alternatively using a far-off resonance optical dipole trap (FORT) as an intermediate step. About 1 × 10^{5 87}Rb atoms can be loaded into the microtrap using either technique although the FORT achieves a lower temperature. The FORT is well suited to loading a linear array of 3 microtraps that are aligned with the propagation direction of the infrared laser. Atoms can be trapped in either the $5S_{1/2}\;F=1$ or 2 ground state hyperfine level. The position of the microtrapped atom cloud can be precisely adjusted using a bias magnetic field over a distance of 350 to slightly <50 μm from the atom chip surface.     

全光纤多模速度干涉仪的研究

针对传统全光纤单模速度干涉仪在爆炸冲击试验中,前端的单模准直器对高速运动的物体的漫反射光难以有效收集,提出了全光纤多模速度干涉仪的装置。利用超辐射发光二极管作为光源,初步验证了全光纤多模速度干涉仪的可行性。主要阐述了全光纤多模速度干涉仪的原理和结构,并将其与全光纤单模速度干涉仪在喇叭振动速度的实验中进行比较,取得了一致的结果,最后还进行霍普金森压杆撞击实验,实测的速度最大值为10.49 m/s,与理论值10 m/s符合较好。     

Noninvasive determination of human cortisol and dehydroepiandrosterone sulfate using liquid chromatography-tandem mass spectrometry

Liquid chromatography-tandem mass spectrometry (LC-MS/MS) for measurements of steroids in human saliva has garnered increased interest in the area of clinical psychoneuroendocrinological research. However, performance characteristics of LC-MS/MS methods for the analysis of steroids in saliva are limited. Human saliva samples were collected via passive drool. Cortisol and dehydroepiandrosterone sulfate (DHEA-S) in the samples were extracted together, resolved on a C18-A column, and analyzed using tandem mass spectrometry. The LC-MS/MS method had limits of quantitation of 0.03 and 0.06 ng/mL for DHEA-S and cortisol, respectively. Method evaluations showed coefficient variation (%CV) of inter-assay ranging 4.6–17.9% for DHEA-S and cortisol, recoveries of 102.4–109.5% for DHEA-S and 94.6–98.3% for cortisol, and assay linearity with R² = 0.9964 for DHEA-S (1.0–25.0 ng/mL) and R² = 0.997 (1.0–25.0 ng/mL) for cortisol. No cross contamination among samples was observed. Human saliva showed 20% and 18% ion enhancement effect for DHEA-S and cortisol assay, respectively. No interference by ten common steroids was detected. Regression analysis of method comparisons with laboratory-developed test (LDT) method revealed R² = 0.9688 (LC-MS/MS = 0.9665 LDT-LC-MS/MS − 0.7355) for cortisol, and R² = 0.9039 (LC-MS/MS = 1.0173 LDT-LC-MS/MS + 3.6797) for DHEA-S. Reference ranges for young adults were determined to be 0.3–5.9 ng/mL for females and 0.1–5.6 ng/mL for males for salivary cortisol, and 0.6–7.4 ng/mL for females and 0.6–10.1 ng/mL for males for salivary DHEA-S. An LC-MS/MS method for quantifying cortisol and DHEA-S in human saliva was developed and validated for clinical and psychoneuroendocrinological research that require noninvasive means of measuring these hormones.

     

A new family of two-dimensional triple-codeweight asymmetric optical orthogonal code for OCDMA networks

A new generation algorithm of two-dimensional triple-codeweight asymmetric optical orthogonal codes for optical code division multiple access （OCDMA） networks is proposed. The code cardinality is obtained and the error-probability performance for corresponding OCDMA system is analyzed. The codes with two constraints （i.e., auto- and cross-correlation properties） being unequal are taken into account. On the premise of fixed system resources, the code of the error-probability performance, it is shown cardinality can be significantly improved. By analysis that the codes with different parameters have different performances. Therefore, this type of codes can be applied to support diverse quality of service （QoS） and satisfy the quality requirement of different multimedia or distinct users, and simultaneously make the better use of bandwidth resources in oDtical networks.     

Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin

Cantharidin (CTD) is the main active ingredient isolated from Mylabris, and norcantharidin (NCTD) is a demethylated derivative of CTD, which has similar antitumor activity to CTD and lower toxicity than CTD. However, the clinical use of NCTD is limited due to its poor solubility, low bioavailability, and toxic effects on normal cells. To overcome these shortcomings, researchers have explored a number of strategies, such as chemical structural modifications, microsphere dispersion systems, and nanodrug delivery systems. This review summarizes the structure–activity relationship of NCTD and novel strategies to improve the solubility and bioavailability of NCTD as well as reduce the toxicity. This review can provide evidence for further research of NCTD.     

Transmittance ratio constrained retrieval technique for lidar cirrus measurements

This letter describes a lidar retrieval technique that uses the transmittance ratio as a constraint to determine an average lidar ratio as well as extinction and backscatter coefficients of transparent cirrus clouds. The cloud transmittance ratio is directly obtained from two adjacent elastic lidar backscatter signals. The technique can be applied to cirrus measurements where neither the molecular scattering dominant signals above and below the cloud layer are found nor cloudfree reference profiles are available. The technique has been tested with simulated lidar signals and applied to backscatter lidar measurements at Hampton University, Hampton, Virginia.