本草古籍中化学教学资源的开发与利用*

历代本草,世代相传,距今已发展了两千多年,蕴藏着深厚的人文底蕴和科学精神,将其融入中学化学教学有利于实现化学学科的育人功能。挖掘提炼出本草古籍中与中学化学知识相契合的内容,结合药物化学、药理学等方面的知识,举例说明本草古籍在无机化学、有机化学及试题编制等方面的应用,探索将本草古籍融入中学化学教学的有效途径。     

大学生化学竞赛对实验教学改革与创新人才培养的促进作用*

大学生的化学竞赛是课内实验教学的有效延伸,也是从学生视角对实验教学效果的有效检验。通过分析和比较学生参加化学实验竞赛的过程和效果,能有效促进化学实验教学改革、课程建设及创新人才的培养。近年来吉林大学化学学院学生实验竞赛的成绩显著提高,一方面通过化学竞赛激发本科生喜爱化学和开展化学研究的热情,增加学习的主观能动性;另一方面通过竞赛发现问题,在解决问题的过程中促进实验教学改革和课程建设,学院“三阶段”模式的竞赛活动开展,更加有利于培养学生的创新意识和创新能力,促进了化学创新人才的培养。     

A pseudotargeted method based on sequential window acquisition of all theoretical spectra mass spectrometry acquisition and its application in quality assessment of traditional Chinese medicine preparation-Yuanhu Zhitong tablet

Quality control plays a key role in the application of Chinese materia medica, especially in the preparation of traditional Chinese medicine. A pseudotargeted analysis method using an ultra-high-performance liquid chromatography-quadrupole-time-of-flight-mass spectrometry that was operated in the sequential window acquisition of all theoretical spectra mode was proposed to explore the chemical markers of traditional Chinese medicine preparation. Full-scan-based untargeted analysis was applied to extract the target ions. After data preprocessing, 302 target ions were extracted and used for the subsequent sequential window acquisition of all theoretical spectra analyses. The established sequential window acquisition of all theoretical spectra-based pseudotargeted approaches exhibited good repeatability and a wide linear range. The established method was successfully applied to discover analytical markers for the Yuanhu Zhitong tablet. After multivariate statistical analysis, 94 potential markers were identified. Ten markers were annotated by matching accurate m/z and product ion information obtained from previous reports. It is clearly indicated that the pseudotargeted analysis could make a great contribution to the quality assessment of traditional Chinese medicine preparation as a newly emerging technique.     

Facile synthesis of a novel magnetic covalent organic frameworks for extraction and determination of five fungicides in Chinese herbal medicines

A novel magnetic covalent organic framework was synthesized via a one-step coating approach with solvothermal reaction employing 2,4,6-tris(4-aminophen-yl)-1,3,5-triazine and 2,4,6-triformylphloroglucinol as two building blocks by covalent bonding. The prepared magnetic covalent organic frameworks were properly characterized by different techniques and employed as adsorbents of magnetic solid-phase extraction. An analytical method was developed for the simultaneous determination of five fungicides in two Chinese herbal medicine samples via magnetic solid-phase extraction coupled to ultra high performance liquid chromatography with tandem mass spectrometry analysis. Under optimized magnetic solid-phase extraction conditions, the method exhibited satisfactory recoveries (74.0−109.6%) with relative standard deviations of 0.4−4.6%, low limits of detection (0.003−0.015 μg/kg), and good linearity (R² > 0.9960). Compared with the traditional extraction method, the proposed method required a lower amount of adsorbent (3 mg) and extraction time (5 min). The adsorbent also had favorable reusability (not less than eight times). Therefore, the magnetic covalent organic frameworks could be a promising adsorbent for the extraction and quantitation of fungicides in Chinese herbal medicines.     

Enhanced stability designs of cell membrane chromatography for screening drug leads

Cell membrane chromatography is an effective method for screening bioactive components acting on specific receptors in complex systems, which maintains the biological activity of the membrane receptors and improves screening efficiency. However, traditional cell membrane chromatography suffers from poor stability, resulting in a limited life span and low reproducibility, greatly limiting the application of this method. To address this problem, cyanuric chloride-decorated silica gel was used for the covalent immobilization of the cell membranes. Cyanuric chloride reacts with amino groups on the cell membranes and membrane receptors to form covalent bonds. In this way, the cell membranes are not easy to fall off. The column life of the cyanuric chloride-decorated epidermal growth factor receptor/cell membrane chromatography column was extended to more than 8 days, whereas the column life of the normal cell membrane chromatography column dropped sharply in the first 3 days. A cyanuric chloride-decorated epidermal growth factor receptor/cell membrane chromatography online HPLC-IT-TOF-MSn system was applied for screening drug leads from Trifolium pratense L. One potential drug lead, formononetin, which acts on the epidermal growth factor receptor, was screened. Our strategy of covalently immobilizing cell membrane receptors also improved the stability of cell membrane chromatography.     

Develop a stepwise integrated method to screen biomarkers of Baihe-Dihuang Tang on the treatment of depression in rats applying with composition screened,untargeted, and targeted metabolomics analysis

Baihe-Dihuang Tang is a commonly prescribed remedy for depression. In this study, component screening with untargeted and targeted metabolomics was used to identify potential biomarkers for depression in chronic unpredictable mildly stressed rats. Using this novel identification method, the screening of organic acids, lily saponins, iridoids, and other ingredients formed the basis for subsequent metabolomics research. Baihe-Dihuang Tang supplementation in chronic unpredictable mild-stress-induced depression models, increased their body weight, sucrose preference, brain-derived neurotrophic factor deposition, and spatial exploring. Untargeted metabolomics revealed that Baihe-Dihuang Tang exerts its antidepressant effects by regulating the levels of lipids, organic acids, and its derivatives, and benzenoids in the brain, plasma, and urine of the depressed rats. Moreover, it also modulates the d -glutamine and d -glutamate metabolism and purine metabolism. Targeted metabolomics demonstrated significant reduction in l -glutamate levels in the brains of depressed rats. This could be a potential biomarker for depression. Baihe-Dihuang Tang alleviated depression by regulating the levels of l -glutamate, xanthine, and adenine in the brains of depressed rats. Together, these findings conclusively established the promising therapeutic effect of Baihe-Dihuang Tang on depression and also unraveled the underlying molecular mechanism of its potential antidepressant function.     

Pharmacokinetics,hepatic disposition,and heart tissue distribution of 14 compounds in rat after oral administration of Qi-Li-Qiang-Xin capsule via ultra-high-performance liquid chromatography coupled with triple quadrupole tandem mass spectrometry

In the present study, a specific and sensitive approach using ultra-high-performance liquid chromatography coupled with triple quadrupole tandem mass spectrometry was developed and validated for the quantitative analysis of 14 constituents in rat plasma, liver, and heart. The method was fully validated and successfully applied to pharmacokinetic, hepatic disposition, and heart tissue distribution studies of 14 compounds after the oral administration of Qi-Li-Qiang-Xin capsule. Ginsenoside Rb1, alisol A, astragaloside IV, and periplocymarin were found to be highly exposed in rat plasma, while toxic components such as hypaconitine, mesaconitine, and periplocin had low circulation levels in vivo. Moreover, sinapine thiocyanate, neoline, formononetin, calycosin, and alisol A exhibited significant liver first-pass effects. Notably, high levels of alisol A, periplocymarin, benzoylmesaconine, and benzoylhypaconine were observed in the heart. Based on high exposure and appropriate pharmacokinetic features in the systemic plasma and heart, astragaloside IV, ginsenoside Rb1, periplocymarin, benzoylmesaconine, benzoylhypaconine, and alisol A can be considered as the main potentially effective components. Ultimately, the results provide relevant information for discovery of effective substances, as well as further anti-heart failure action mechanism investigations of Qi-Li-Qiang-Xin capsule.     

An emerging strategy for tracing the anti-erectile dysfunction components of raw and salt-processed semens of Astragali Complanati by combinatory liquid chromatography–mass spectrometry-based quantitative analysis,efficacy assessment on impotent rats,and partial least squares regression

Semens of Astragali Complanati own anti-erectile dysfunction effect; however, the components which contribute to the anti-erectile dysfunction effect remain unclear. This work raised a strategy that integrates liquid chromatography coupled mass spectrometry-based quantitative analysis, anti-erectile dysfunction assessment on impotent rats, and their relationship analysis for pinpointing anti-erectile dysfunction components from semens of Astragali Complanati. For simultaneous quantification of seven major components in raw and salt-processed semens of Astragali Complanati, an accurate and reliable liquid chromatography–mass spectrometry method was developed under multiple reaction monitoring mode. Of note, chloramphenicol was employed as the internal standard. The method showed good linearity and repeatability, where the recovery rates of each component ranged from 98.1 to 104.7%, and the precisions of intra- and interday were all within 3.4%. The method has been used for quantification of the seven major components in 10 batches of raw and salt-processed semens of Astragali Complanati. Then, the anti-erectile dysfunction effects of raw and salt-processed semens of Astragali Complanati were evaluated on impotent rats. Gray relationship analysis and partial least squares regression were combined for elucidating the relationship. As a result, complanatuside, astragalin, complanatoside B, and kaempferol were found to be responsible for anti-erectile dysfunction effect of Astragali Complanati.     

Spectrochemical analysis using LIBS and ICP-OES techniques of herbal medicine (Tinnevelly Senna leaves) and its anti-cancerous/antibacterial applications

Tinnevelly senna leaves are being applied to cure many diseases especially in developing countries and sub-Saharan region due to many bioactive compounds such as sennosides, phenols, and flavonoids. The conventional methods to isolate and analyze plant extracts biomolecules are not very effective as well cost effective as they require hazardous chemical solvents and reagents, which are time-consuming processes. The major objective of the present study is to investigate the feasibility of the Laser induced breakdown spectroscopy (LIBS) technique for rapid, eco-friendly, and multi-elemental analysis of Senna leaves extracts and study their antibacterial and anticancer potentials. The elegant LIBS technique was applied as a qualitative and quantitative method for Senna leaves sample’s elemental analysis and their biological activities were measured by evaluating anti-cancer and anti-bacterial analysis. The quantitative analysis of Senna leaves extracts was done using the calibration-free laser-induced breakdown spectroscopy (CF-LIBS) algorithm showing their appreciable content of several nutrient elements, and the obtained results were in close conformity with these achieved by using the standard analytical ICP OES technique. We studied the bactericidal efficacy of the Senna leaves extract against Staphylococcus aureus (S. aureus) by AWD assays and morphogenesis by scanning electron microscopy (SEM) and the anticancer activity was also investigated where different concentrations of Senna leaves extract were tested on cancer cells (HCT-116 and HeLa) and normal cells (HEK-293) using the cell metabolic activity MTT assay and Propidium iodide (PI) staining. We have also calculated the inhibitory concentration (IC50) value for the various extracts concentrations (25 µg/ml, 50 µg/ml, 100 µg/ml, 150 µg/ml, 200 µg/ml, and 225 µg/ml). We have found that IC₅₀ value for HCT-116 cells were 13.5 µg/ml, 17.5 µg/ml, 21.5 µg/ml, 22.5 µg/ml, 26 µg/ml and 33.5 µg/ml and for HeLa cells 15.25 µg/ml, 21.25 µg/ml, 23.5 µg/ml, 262.5 µg/ml, 36.25 µg/ml, and 39.50 µg/ml. The bactericidal efficacy of the Senna leaves extract showed significant inhibition against Gram-positive bacterium. Both MTT and PI analysis showed that Senna leaves extract induced profound inhibition on HCT-116 growth and proliferation. Additionally, Senna leaves extract did not exert an inhibitory influence on normal (HEK-293), which is non-cancerous cells. We suggest that the extract specifically targets the cancerous cells, which could be highly beneficial for the development of future safe anticancer and antibacterial drugs using these extracts.     

Advances in nucleic acid architectures for electrochemical sensing

Nucleic acid–based electrochemical sensors are ideally suited to the detection of molecular targets for which enzymatic detection or direct electrochemical oxidation – reduction reactions are not possible. Moreover, the versatility of nucleic acids in their ability to bind a great variety of target types, from small molecules to single-entity mesoscopic targets, makes them attractive receptors for the development of electrochemical biosensors. In this brief opinion piece, we discuss field advances from the past two years. We hope the works highlighted here will inspire the community to pursue creative designs enabling the detection of larger and more complex targets with a specific focus on analytical validation and translation into preclinical or clinical applications.