An Efficient Synthesis of a Hydroxyethylamine (HEA) Isostere and Its α-Aminophosphonate and Phosphoramidate Derivatives as Potential Anti-HIV Agents

HIV protease is a promising drug target for AIDS therapy, and several potent HIV‐1 protease inhibitors have been reported to date. Although existing inhibitors exhibit high selectivity, they have also been associated with severe side effects and the possible emergence of therapeutic resistance. As HIV protease cleaves the peptide bond via a tetrahedral intermediate, various transition‐state models such as hydroxyethylamine (HEA) have been designed. We therefore pursued an efficient synthesis of an HEA isostere; this was performed with a novel one‐pot reduction–transimination–reduction reaction sequence as a key step. α‐Aminophosphonate and phosphoramidate derivatives of the HEA isostere were designed and synthesized, and all of the synthesized derivatives were assayed for their anti‐HIV activities against wild‐type and mutant HIV strains. Phosphoramidate derivative 15 a was found to be the most active of all synthesized compounds against the III_B and RES056 strains. As phosphonates are known to exhibit physiological stability, good cell permeability, and other promising pharmacokinetic characteristics, our newly synthesized compounds have the potential as alternatives to existing therapeutics and diagnostics.     

Low-Temperature Processing of Dense Hydroxyapatite–Zirconia Composites

Hydroxyapatite (HA)–YTZP (2, 5, 7.5, and 10 wt% ZrO₂) composite powders prepared from inorganic precursors were characterized by FTIR, DSC/TG, XRD, and TEM. The calcined powders had HA and t / c -ZrO₂, which undergo structural changes between 650°C and 1050°C. TEM of calcined powder showed larger HA particles (100 nm) and smaller ZrO₂ particles (≤50 nm). HA and HA–2 wt% ZrO₂-sintered samples had 98% density and it was (90–95%) for HA–5, 7.5, and 10 wt% ZrO₂. The bending strength of HA–2wt% ZrO₂ composites was 72 MPa. The grain sizes of HA showed a refinement with ZrO₂ addition.     

Effect of the preparation method on the structural stability and hydrodesulfurization activity of NiMo/SBA-15 catalysts

Defined hexagonal cylindrical pore structure SBA-15 material was synthesized as support for hydrotreating catalysts. The stability of the mesoporous material under acid and basic environments commonly used to prepare hydrotreating catalysts was investigated. The effects of the acid and basic treatments on the stability of SBA-15 and NiMo/SBA-15 catalysts were evidenced by different characterization techniques such as N₂ adsorption–desorption, X-ray diffraction (XRD), Raman Spectroscopy and high resolution transmission electron microscopy (HRTEM). Supported NiMo/SBA-15 catalysts prepared by pore volume co-impregnation in acidic, neutral and basic solutions of the Ni and Mo precursor salts were characterized to evaluate the textural and structural changes caused by the method of preparation. Characterization of the support after accelerated stability tests indicates large deterioration of the SBA-15 structural order at basic pH. The characterization results of oxide and sulfided catalysts indicate, for the catalysts prepared at high pH, an increasing presence of β–NiMoO₄ phase in the oxide catalysts, and a relatively lower population of MoS₂ in the sulfided catalysts. The activity of the different catalysts evaluated in the thiophene hydrodesulfurization reaction was higher for the catalysts prepared at low pH.     

Stepwise Oxidation Mechanism of HVOF Sprayed NiCrAlY Coatings in Air

High velocity oxide fuel sprayed NiCrAlY coatings on the Superni 76 superalloy have been oxidized cyclically at 900 °C up to 200 cycles. Weight change measurements were taken after each cycle to obtain kinetics of the oxidation process. The surface and cross-section of oxidized samples have been examined by XRD, FESEM/EDS to characterize the corrosion products. The formation of Al₂O₃ at the surface as well as at the coating/scale interface as a sub-layer was observed. Other oxides such as Ni (Al, Cr)₂O₄ and Cr₂O₃ were also present above this Al₂O₃ sub-layer. An oxidation mechanism has been proposed for the oxidation of the coating for 200 cycles by correlating the results after different cycles of oxidation.     

反相硅胶纯化阿克苏“次等枣”环磷酸腺苷

采用反相硅胶对红枣环磷酸腺苷提取物进行纯化。以吸附率和解析率为指标,确定反相硅胶纯化红枣环磷酸腺苷的最佳工艺参数为:上样液流速1 m L/min、上样液浓度70μg/m L、上样液p H 6,洗脱液为体积分数60%的甲醇、洗脱液流速3 m L/min,在此条件下环磷酸腺苷的纯度由0.098%提高到44.69%。     

Bioactive peptides derived from milk proteins and their health beneficial potentials: an update

It has been well recognized that dietary proteins provide a rich source of biologically active peptides. Today, milk proteins are considered the most important source of bioactive peptides and an increasing number of bioactive peptides have been identified in milk protein hydrolysates and fermented dairy products. Bioactive peptides derived from milk proteins offer a promising approach for the promotion of health by means of a tailored diet and provide interesting opportunities to the dairy industry for expansion of its field of operation. The potential health benefits of milk protein-derived peptides have been a subject of growing commercial interest in the context of health-promoting functional foods. Hence, these peptides are being incorporated in the form of ingredients in functional and novel foods, dietary supplements and even pharmaceuticals with the purpose of delivering specific health benefits.     

Energy and flux measurements of laser-induced silver plasma ions by using Faraday cup

Silver(Ag)plasma has been generated by employing Nd∶YAG laser(532 nm,6 ns)laser irradiation.The energy and flux of ions have been evaluated by using Faraday cup(FC)using time of flight(TOF)measurements.The dual peak signals of fast and slow Ag plasma ions have been identified.Both energy and flux of fast and slow ions tend to increase with increasing irradiance from 7 GW cm-2 to 17.9 GW cm-2 at all distances of FC from the target surface.Similarly a decreasing trend of energies and flux of ions has been observed with increasing distance of FC from the target.The maximum value of flux of the fast component is 21.2×1010cm-2,whereas for slow ions the maximum energy and flux values are 8.8 keV,8.2×1012 cm-2 respectively.For the analysis of plume expansion dynamics,the angular distribution of ion flux measurement has also been performed.The overall analysis of both spatial and angular distributions of Ag ions revealed that the maximum flux of Ag plasma ions has been observed at an optimal angle of～15°.In order to confirm the ion acceleration by ambipolar field,the self-generated electric field(SGEF)measurements have also been performed by electric probe;these SGEF measurements tend to increase by increasing laser irradiance.The maximum value of 232 V m-1 has been obtained at a maximum laser irradiance of 17.9 GW cm-2.     

Physico-chemical,mechanical and electrical performance of bael fruit gum–chitosan IPN films

The gum obtained from unripe fruits of Aegle marmelos was co-processed with chitosan to improve the film forming property of the former. The results of FTIR and differential thermal analysis of films revealed maximum interaction between –COO⁻ groups of gum and –NH₃⁺ of chitosan when they were present in equal proportion in the film. These films exhibited almost negligible zeta potential and the surface remained smooth after exposure to both acidic and alkaline pH as observed under scanning electron microscope. The contact angle and swelling index of this film in both acidic and alkaline buffers were observed to be lowest as compared to other films prepared with different ratios of gum and chitosan. The work of adhesion and spreading coefficient for this film was observed to be lowest. These results could be attributed to optimum interaction between –COO⁻ groups of gum and –NH₃⁺ groups of chitosan. These results indicated the ability of this film for use in modifying drug release and processed food items.     

Cyber Attack Protection and Control of Microgrids

Recently, the smart grid has been considered as a next-generation power system to modernize the traditional grid to improve its security, connectivity, efficiency and sustainability. Unfortunately, the smart grid is susceptible to malicious cyber attacks, which can create serious technical, economical, social and control problems in power network operations. In contrast to the traditional cyber attack minimization techniques, this paper proposes a recursive systematic convolutional (RSC) code and Kalman filter (KF) based method in the context of smart grids. Specifically, the proposed RSC code is used to add redundancy in the microgrid states, and the log maximum a-posterior is used to recover the state information, which is affected by random noises and cyber attacks. Once the estimated states are obtained by KF algorithm, a semidefinite programming based optimal feedback controller is proposed to regulate the system states, so that the power system can operate properly. Test results show that the proposed approach can accurately mitigate the cyber attacks and properly estimate and control the system states.      

The Role of PEDF in Reproductive Aging of the Ovary

Reproductive aging is characterized by a decline in ovarian function and in oocytes’ quantity and quality. Pigment epithelium-derived factor (PEDF), a pivotal player in ovarian angiogenic and oxidative balance, was evaluated for its involvement in reproductive aging. Our work examines the initial stage of reproductive aging in women and mice, and the involvement of PEDF in the process. Granulosa cells from reproductively-aged (RA) women and mice (36–44 years old and 9–10 months old, respectively) indicated an increase in the level of PEDF mRNA (qPCR), with yet unchanged levels of AMH and FSHR mRNAs. However, the PEDF protein level in individual women showed an intra-cellular decrease (ELISA), along with a decrease in the corresponding follicular fluid, which reflects the secreted fraction of the protein. The in vitro maturation (IVM) rate in the oocytes of RA mice was lower compared with the oocytes of young mice, demonstrated by a reduced polar body extrusion (PBE) rate. The supplementation of PEDF improved the hampered PBE rate, manifested by a higher number of energetically-competent oocytes (ATP concentration and mtDNA copy number of individual oocytes). Our findings propose PEDF as an early marker of reproductive aging, and a possible therapeutic in vitro agent that could enhance the number of good-quality oocytes in older IVF patients.