Quantification of erythromycin in pharmaceutical formulation by transmission Fourier transform infrared spectroscopy

A simple, cost-effective and environmental friendly analytical method was developed for the quantification of erythromycin in tablet formulation using transmission Fourier Transform Infrared (FT-IR) spectroscopy for routine quality control analysis. There is no need of sample preparation except pellet formation for FT-IR analysis. Use of solvent was totally avoided in this method. Calibration was carried out by using simple Beer’s law in the FT-IR region between 1743 and 1697 cm⁻¹. The excellent coefficient of determination (R² = 0.998) was achieved with 0.0247 and 1.14 root mean square error of prediction (RMSEP) and root mean square error of cross validation (RMSECV), respectively. The results of the study revealed that the transmission FT-IR spectroscopy could be effectively used for rapid determination of active ingredients like erythromycin in pharmaceutical formulations to control the quality of finished products.     

Identification and analysis of alkaloids in cortex Phellodendron amurense by high‐performance liquid chromatography with electrospray ionization mass spectrometry coupled with photodiode array detection

Alkaloids from Cortex Phellodendron amurense Rupr. were identified to determine the material basis for the bioactivity of this herb. HPLC–ESI‐MS with photodiode array detection coupled to XCharge C₁₈ column was applied to analyze the alkaloids qualitatively and quantitatively. A total of 37 alkaloids were identified and tentatively characterized from the ethanol extract by online ESI‐MSⁿ fragmentation and UV spectral analysis. A total of ten alkaloids, including four novel natural products, were tentatively identified for the first time in P. amurense. The fragmentation pathways for certain compounds were analyzed. The contents of a pair of isomers (columbamine and jatrorrhizine) and four main alkaloids (phellodendrine, magnoflorine, berberine, and palmatine) were simultaneously quantified using the aforementioned method. Results showed that the newly discovered and known components of P. amurense were helpful in determining the material basis for the bioactivity of the herb. The application of the XCharge C₁₈ column is a suitable and practical method for the isolation of alkaloids in plants.     

Peptide prefractionation is essential for proteomic approaches employing multiple‐reaction monitoring of fruit proteomic research

Off‐gel? IEF has become a popular tool in proteomics research to fractionate peptides or proteins. We conducted a detailed investigation on the fruit proteomics of apple, banana, and strawberry fruit employing Off‐gel? electrophoresis (OGE) as a crucial step to improve the proteome coverage and quantitative proteomic workflows including multiple‐reaction monitoring (MRM). We provide technical details concerning the application of Off‐gel?IEF, nano‐LC–MS detection, and MRM optimization and analysis. Our results demonstrated that the application of OGE is an effective method for peptide fractionation and increased significantly the number of proteins identified by at least ten times, with more total peptides detected and collected. Furthermore, we developed a protocol combining OGE and MRM studies to identify and quantitatively investigate monodehydroascorbate reductase, a key enzyme in the redox and antioxidant system of apple fruit during fruit ripening. Using this method, the quantitative changes in this protein during ripening and in response to ethylene treatment was investigated. Our results provide direct and comprehensive evidence demonstrating the benefits of OGE and its application for both shotgun and quantitative proteomics research.     

钯(Ⅱ)类抗肿瘤药物研究进展

20世纪60年代,美国密执安州立大学Rosenberg发现了顺铂具有抗癌活性,开辟了金属类抗肿瘤药物研究的新领域.经过40余年的研究,已相继成功开发了卡铂、奈达铂、奥沙利铂、舒铂、洛铂和双环铂等铂类抗肿瘤药物.虽然对于铂类抗肿瘤药物研究取得了一定的成绩,但在临床使用过程中也存在一些问题,如其毒副作用和抗药性,限制了其在临床上的进一步广泛应用.为了解决这些问题,科研工作者开始寻找新的金属类抗肿瘤药物以弥补现有铂类抗肿瘤药物的不足.在金属元素中,唯有钯(II)与铂(II)配合物具有相似或相同的结构特征,进而表现出相近或相似的化学性质.因此,继铂类抗肿瘤配合物后,钯(II)配合物作为潜在抗肿瘤药物成为一个诱人的领域.本文综述了近年来钯(II)类抗肿瘤药物的研究进展,并探讨了其构效关系,这对于指导新型钯(II)类抗肿瘤药物的合成具有重要的参考价值.     

我国铝期货、铝现货与废铝价格动态关系的实证研究

利用Johansen协整检验、Granger因果检验以及向量误差修正(VEC)模型、脉冲响应分析和方差分解分析,从三个不同的角度对我国铝期货、铝现货和废铝市场价格间的动态关系进行了实证分析,研究结果表明:从引导关系看,铝期货价格与铝现货价格之间具有协整关系,并且铝期货价格对铝现货价格及废铝价格具有单向价格引导关系,铝现货价格对废铝价格具有单向价格引导关系;从冲击反应看,铝期货对铝现货的冲击比较强烈,而铝期货对废铝以及铝现货对废铝的冲击相对比较和缓;从价格发现程度看,铝期货市场具有最强的价格发现能力,铝现货价格发现能力次之,废铝的价格发现能力最弱,表明铝期货是价格发现过程的主要驱动力量.     

Complexity spaces as quantitative domains of computation

We study domain theoretic properties of complexity spaces. Although the so-called complexity space is not a domain for the usual pointwise order, we show that, however, each pointed complexity space is an ω-continuous domain for which the complexity quasi-metric induces the Scott topology, and the supremum metric induces the Lawson topology. Hence, each pointed complexity space is both a quantifiable domain in the sense of M. Schellekens and a quantitative domain in the sense of P. Waszkiewicz, via the partial metric induced by the complexity quasi-metric.     

Application of quantitative structure-activity relationship to the determination of binding constant based on fluorescence quenching

Quantitative structure-activity relationship (QSAR) model was used to predict and explain binding constant (log K) determined by fluorescence quenching. This method allowed us to predict binding constants of a variety of compounds with human serum albumin (HSA) based on their structures alone. Stepwise multiple linear regression (MLR) and nonlinear radial basis function neural network (RBFNN) were performed to build the models. The statistical parameters provided by the MLR model (R²=0.8521, RMS=0.2678) indicated satisfactory stability and predictive ability while the RBFNN predictive ability is somewhat superior (R²=0.9245, RMS=0.1736). The proposed models were used to predict the binding constants of two bioactive components in traditional Chinese medicines (isoimperatorin and chrysophanol) whose experimental results were obtained in our laboratory and the predicted results were in good agreement with the experimental results. This QSAR approach can contribute to a better understanding of structural factors of the compounds responsible for drug-protein interactions, and can be useful in predicting the binding constants of other compounds.     

A dynamic terramechanic model for small lightweight vehicles with rigid wheels and grousers operating in sandy soil

This paper presents a validated dynamic terramechanic model for rigid wheels with grousers that may be used for planetary and terrestrial mobile robots operating in loose sandy soil. The proposed model is based on established analytical terramechanic theories and incorporates two new dimensionless empirical coefficients. The additional terms in the model are based on existing soil mechanic theories that vary as a function of soil properties, slip conditions, and vehicle loading. The proposed model was able to capture and predict the dynamic oscillations observed in experimental data from a single-wheel testbed for the sinkage, drawbar pull and normal load. For the operating conditions tested in this research the simulation results using the proposed model show an improvement over traditional terramechanic models for capturing the dynamic effects of grousers.     

Recent Clinical and Preclinical Studies of Hydroxychloroquine on RNA Viruses and Chronic Diseases: A Systematic Review

The rapid spread of the new Coronavirus Disease 2019 (COVID-19) has actually become the newest challenge for the healthcare system since, to date, there is not an effective treatment. Among all drugs tested, Hydroxychloroquine (HCQ) has attracted significant attention. This systematic review aims to analyze preclinical and clinical studies on HCQ potential use in viral infection and chronic diseases. A systematic search of Scopus and PubMed databases was performed to identify clinical and preclinical studies on this argument; 2463 papers were identified and 133 studies were included. Regarding HCQ activity against COVID-19, it was noticed that despite the first data were promising, the latest outcomes highlighted the ineffectiveness of HCQ in the treatment of viral infection. Several trials have seen that HCQ administration did not improve severe illness and did not prevent the infection outbreak after virus exposure. By contrast, HCQ arises as a first-line treatment in managing autoimmune diseases such as rheumatoid arthritis, lupus erythematosus, and Sjögren syndrome. It also improves glucose and lipid homeostasis and reveals significant antibacterial activity.