微波消解-电感耦合等离子体质谱法测定原料药中的残留钯

建立了一种微波消解-电感耦合等离子体质谱法(ICP-MS)测定利奥西呱原料药中残留钯含量的方法。方法:对样品进行微波消解前处理,优化调谐仪器参数后,以相对稳定的铑(1 03 Rh)作在线内标校准,采用ICP-MS法对样品中的钯元素进行定量测定分析。结果表明,原料药中钯元素标准曲线的线性范围为0~60.0μg/L,相关系数r为0.9996;7次重复性测试的相对标准偏差RSD为0.85%;加标回收率为90.14%~101.3%,相对标准偏差RSD为2.17%~2.44%。表明该方法简便快速、灵敏度高,准确可靠,适用于利奥西呱原料药中残留钯含量的测定。     

细胞毒素类抗癌药物的研究进展

综述了近年来细胞毒素类抗癌药物的研究概况,根据作用机制重点介绍了几类细胞毒素类抗癌药物的合成和结构特点,并对其化学合成方法进行了评价。     

DART-Orbitrap质谱法快速筛查饲料中磺胺类药物

利用新型离子化技术--实时直接分析(DART)离子源与高分辨质谱Orbitrap联用,建立饲料中非法添加磺胺类药物的快速筛查方法。通过对DART离子化温度、样品检测模式等参数进行探索优化,最终确定饲料经过乙腈-水溶液简单提取,液体筛网模块进样,450 ℃下离子化,Orbitrap高分辨质谱在全扫描模式下定性检测,并进行相关的方法学验证,方法检出限为1.0~4.0 μg/g。该方法前处理简单、检测速度快、定性准确、样品通量大、环保无污染,能满足饲料中非法添加磺胺类药物快速筛查的要求。     

液相色谱-二极管阵列检测法同时测定血液中6种毒品及其代谢物

建立了一种同时测定血液中吗啡、苯丙胺类、氯胺酮和杜冷丁等6种常见毒品的液相色谱-二极管阵列检测器联用的定性定量方法。条件为以乙腈和0.005mol/L的磷酸二氢钾水溶液为流动相,梯度洗脱,经C18色谱柱分离,二极管阵列检测器检测,检测波长210nm。利用保留时间和紫外吸收光谱进行定性分析。血浆中6种毒品在8.0～200.0ng/mL范围内线性关系良好（r2=0.999 2）,回收率范围为68.9%～95.2%,检测限为3.3ng/mL。结果表明,该方法操作简便、快速、选择性强、灵敏度高,适于血液中6种常见毒品及其代谢物的分析,可为相关案件提供方法和技术支持。     

抗结核药物的合成及抗菌活性

采用杂合的方法合成乙酰水杨酸-吡嗪酰胺和氧氟沙星-磺胺醋酰两个抗结核药物。通过红外光谱、核磁共振氢谱、核磁共振碳谱、质谱对它们的结构对进行了表征。采用肉汤稀释法测定这2个目标化合物对标准结核杆菌的最低抑菌质量浓度,结果表明:乙酰水杨酸-吡嗪酰胺的最低抑菌质量浓度为62.5 μg/mL,氧氟沙星-磺胺醋酰的最低抑菌质量浓度为125 μg/mL,证明其具有较好的抑菌活性。     

心肌组织传感阵列在信号传导及药物分析中的应用

为了对心肌组织的搏动信号及其传导进行实时监测与分析,设计一种用于离体心肌组织电生理检测的组织传感阵列.根据组织/器件耦合原理,该传感阵列能够检测伴随心肌细胞搏动产生的场电位的变化.利用组织传感阵列,同步采集多通道的心肌信号并观察心血管药物盐酸肾上腺素和氯化乙酰胆碱对搏动信号的影响.实验结果显示：离体心肌组织及切片表现出良好的搏动和信号传导;盐酸肾上腺素和氯化乙酰胆碱对心肌组织搏动信号的幅度、频率、持续时间甚至信号的传导分别表现出兴奋和抑制作用.说明组织传感阵列技术对离体心肌组织搏动信号的提取是可行的,并且对心肌信号的传导及药物作用分析非常有用.     

鸡传染性喉气管炎的药物治疗对比试验

从流行病学、临床症状、病理变化和实验室检验四个方面对鸡传染性喉气管炎进行了诊断，并做了药物治疗对比试验．结果表明，杀病毒药(消毒王)加清热解毒、止咳平喘中草药配合治疗鸡传染性喉气管炎，效果更好，能较快地制止病鸡死亡，显著降低死亡率及减少药物治疗费用．     

Quinone‐Fused Pyrazoles through 1,3‐Dipolar Cycloadditions: Synthesis of Tricyclic Scaffolds and in vitro Cytotoxic Activity Evaluation on Glioblastoma Cancer Cells

A novel and straightforward synthesis of highly substituted isoquinoline‐5,8‐dione fused tricyclic pyrazoles is reported. The key step of the synthetic sequence is a regioselective, Ag₂CO₃ promoted, 1,3‐dipolar cycloaddition of C‐heteroaryl‐N‐aryl nitrilimines and substituted isoquinoline‐5,8‐diones. The broad functional group tolerability and mild reaction conditions were found to be suitable for the preparation of a small library of compounds. These scaffolds were designed to interact with multiple biological residues, and two of them, after brief synthetic elaborations, were analyzed by molecular docking studies as potential anticancer drugs. In vitro studies confirmed the potent anticancer effects, showing promising IC₅₀ values as low as 2.5 μm against three different glioblastoma cell lines. Their cytotoxic activity was finally positively correlated to their ability to inhibit PI3K/mTOR kinases, which are responsible for the regulation of diverse cellular processes in human cancer cells.     

Kinetic Studies of Newly Patented Aminoalkanol Derivatives with Potential Anticancer Activity as Competitive Inhibitors of Prostate Acid Phosphatase

Background: Acid phosphatase and its regulation are important objects of biological and clinical research and play an important role in the development and treatment of prostate and bone diseases. The newly patented aminoalkanol (4-[2-hydroxy-3-(propan-2-ylamino)propyl]-1,7-dimethyl-8,9-diphenyl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5,10-trione hydrochloride) (I) and (4-[3-(dimethylamino)-2-hydroxypropyl]-1,7-dimethyl-8,9-diphenyl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5,10-trione hydrochloride) (II) derivatives have potential anticancer activity, and their influence on enzymatic activity can significantly impact the therapeutic effects of acid phosphatase against many diseases. Therefore, in this study, we investigated the action of compounds (I) and (II) on acid phosphatase. Methods: Capillary electrophoresis was used to evaluate the inhibition of acid phosphatase. Lineweaver–Burk plots were constructed to compare the Km of this enzyme in the presence of inhibitors (I) or (II) with the Km in solutions without these inhibitors. Results: Compound (I) showed a stronger competitive inhibition against acid phosphatase, whereas derivative (II) showed a weaker competitive type of inhibition. The detailed kinetic studies of these compounds showed that their type and strength of inhibition as well as affinity depend on the kind of substituent occurring in the main chemical molecule. Conclusions: This study is of great importance because the disclosed inhibition of acid phosphatase by compounds (I) and (II) raises the question of whether these compounds could have any effect on the treatment possibilities of prostate diseases.