Structure−Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents

Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub-tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogues and their structure-activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure-dependent manner. Detailed analysis revealed a key role of the substitution pattern on the aromatic ring and a marked effect of the side chain on the activity against these two parasites. The high antileishmanial potency and remarkable selectivity of the nitro-aromatic derivatives suggested them as promising candidates for further studies. On the other hand, the high in vitro potency of catechol-type compounds against T. brucei could not be extrapolated to an in vivo mouse model.     

Influence of Different Additives on the Interaction of Quinolone Antibiotic Drug with Surfactant: Conductivity and Cloud Point Measurement Study

Conductometric and cloud point (CP) measurement studies have been performed to investigate the interaction of tetradecyltrimethylammonium bromide (TTAB) and Triton® X-100 (TX-100) with ciprofloxacin hydrochloride (CFH) in different solvents over the temperature range of 295.15–315.15 K. CFH is used for the treatment of various bacterial infections. The observed critical micelle concentration (CMC) values of TTAB were found to be reduced in the presence of electrolytes (Na₂SO₄/Na₃PO₄), and this reduction proceeds with the elevation of salt concentration. The order of the CMC of TTAB follows the trend: > >. The observed CMC values of TTAB were found to increase with increasing temperature and decrease with increasing concentration of CFH in aqueous medium. The values of Gibbs free energy of micellization () for the TTAB/TTAB + CFH mixture were found to be negative, implying spontaneous micellization. The estimated CP of TX-100 decreases with increasing concentration of TX-100 in aqueous medium. The CP values first decrease with increasing concentration of CFH and then increase at higher concentration of CFH almost in all cases investigated. The values of free energy of clouding were found to be positive in all cases studied implying that phase separation of TX-100 was nonspontaneous. The other thermodynamic parameters associated with the micellization of TTAB and the phase separation of TX-100 were estimated and explained.     

Role of Co in formation of Ni-Ti clusters in maraging stainless steel

The effect of Co addition on the formation of Ni-Ti clusters in maraging stainless steel was studied by three dimensional atom probe (3DAP) and first-principles calculation. The cluster analysis based on the maximum separation approach showed an increase in size but a decrease in density of Ni-Ti clusters with increasing the Co content. The first-principles calculation indicated weaker Co-Ni (Co-Ti) interactions than Co-Ti (Fe-Ti) interactions, which should be the essential reason for the change of distribution characteristics of Ni-Ti clusters in bcc Fe caused by Co addition.     

Imaging of two-dimensional unsaturated moisture flows in uncracked and cracked cement-based materials using electrical capacitance tomography

The development of visualizing tools to monitor unsaturated moisture flow in cement-based materials is of great importance, as most degradation processes in cement-based materials are connected to and take place in the presence moisture. This paper investigates the ability of electrical capacitance tomography (ECT) to image two-dimensional (2D) unsaturated moisture flow in cement-based materials. In ECT, the electrical permittivity distribution within an object is reconstructed based on measured capacitances between electrodes attached on the object’s surface. In a series of experiments, mortar specimens with and without discrete cracks were imaged with ECT during a 2D moisture ingress. The results show that ECT is able to monitor the evolution of the moisture flow, and to approximate the shape and position of the moisture front. These findings indicate that ECT is a viable method for monitoring and visualizing 2D unsaturated moisture flow in cement-based materials in the presence and absence of discrete cracks.     

碱蓬多糖SSP1-1的分离纯化及其抗肿瘤活性

目的:本实验对水溶性碱蓬(Suaeda salsa)多糖SSP1-1进行分离纯化并对其抗肿瘤活性进行初步研究。方法:采用水提醇沉法提取碱蓬粗多糖,通过DEAE-52纤维素柱和Sephadex G-75葡聚糖凝胶柱分离纯化碱蓬粗多糖,得到单一碱蓬多糖SSP1-1,利用高效凝胶渗透色谱法(HPGPC)对其纯度及分子量进行分析,利用MTT、Hoechst 33342染色,Western blot方法对碱蓬多糖SSP1-1的抗肿瘤活性进行研究。结果:SSP1-1分子量为60.32 kDa;SSP1-1具有时间-剂量依赖性抑制肿瘤细胞增殖作用,当SSP1-1浓度为500 μg/mL时,HepG2细胞在24和48 h的细胞活力分别为52.8%和50.2%,Hoechst 33342染色实验观察到SSP1-1可引起HepG2细胞核出现典型的细胞凋亡特征;Western blot证明SSP1-1可以降低Bcl-2的蛋白表达,提高Bax和Caspase-3的蛋白表达,各组蛋白含量与对照组相比均具有显著性(P<0.05)。结论:SSP1-1为均一组分多糖,并对肿瘤细胞具有显著的抑制作用,为进一步开发利用碱蓬多糖奠定了基础。     

Hit to Leads with Cytotoxic Effect in Leukemic Cells: Total Synthesis Intermediates as a Molecule Treasure Chest

A previously designed and developed 12-step total synthesis that includes [1,1′-biphenyl]-2-amine and carbazole intermediates and that ultimately produces the carbazole alkaloid carbazomycin G was exploited as a screening compound library with the goal of identifying potential lead compound(s) with cytotoxic effect. These compounds were investigated by using in-vitro tests involving the two human cell lines HL-60 and MOLM-13, which both model acute myeloid leukaemia (AML). The in-vitro biological test results were used together with the molecular structures of the various intermediates in a concise SAR analysis. Several of the intermediates revealed cytotoxicity (IC₅₀<10⁻⁴ M), although the final natural product carbazomycin G did not reveal cytotoxicity versus the two said human cell lines.     

Tuning of ferrimagnetic nature and hyperfine interaction of Ni2+ doped cobalt ferrite nanoparticles for power transformer applications

Ferrites may contain single domain particles which gets converted into super-paramagnetic state near critical size. To explore the existence of these characteristic feature of ferrites, we have performed magnetization(M-H loop) and Mössbauer spectroscopic studies of Ni²⁺ substitution effect in Co_1-xNi_xFe₂O₄ (where x?=?0, 0.25, 0.5, 0.75 and 1) nanoparticles were fabricated by solution combustion route using mixture of carbamide and glucose as fuels for the first time. As prepared samples exhibit spinel cubic structure with lattice parameters which decreases linearly with increase in Ni²⁺ concentration. The M-H loops reveals that saturation magnetization(M_s), coercive field(H_c) remanence magnetization(M_r) and magnetron number(η_B) decreases significantly with increasing Ni²⁺ substitution. The variation of saturation magnetization has been explained on the basis of Neel's molecular field theory. The coercive field(H_c) is found strongly dependent on the concentration of Ni²⁺ and decrease of coercivity suggests that the particles have single domain and exhibits superparamagnetic behavior. The Mössbauer spectroscopy shows two ferrimagnetically relaxed Zeeman sextets distribution at room temperature. The dependence of Mössbauer parameters such as isomer shift, quadru pole splitting, line width and hyperfine magnetic field on Ni²⁺ concentration have been discussed. Hence our results suggest that synthesized materials are potential candidate for power transformer application.