新疆尉犁县牲畜常见毒草中毒的探讨

本文主要论述了新疆尉犁县牲畜因误食小花棘豆中毒引起死亡的原因、病理变化、诊断要点、用药指南以及防治措施。     

特比萘芬的合成

目的：研究抗真菌药特比萘芬的合成路线及工艺。方法：以频哪酮为起始原料,经氯代,脱所化氢,格氏反应得6,6－二甲基－1－庚烯－4－炔－3－醇（5）,溴代后与N－甲基－1－萘甲胺反应得标题化合物。结果：合成了目标化合物,其结构经IR,^1HNMR,MS,元素分析得以确正。结论：合成路线及工艺较适用于工业化生产。     

Determination and Pharmacokinetic Study of Nitidine Chloride in Rat Plasma after Intragastrical Administration by LC-ESI-MS/MS Method

Objective To study the pharmacokinetics of nitidine chloride(NC) in rat plasma after intragastrical(i.g.) administration. Methods A liquid chromatography-electrospray ionization-mass/mass sprectrometry(LC-ESI-MS/MS) was used and carbamazepine was used as an intermal standard(I.S.). The rat plasma samples were deproteinized with acetonitrile and the resultant supernatant was assayed on an analytical Diamonsil ~(TM)ODS C_(18) column(2.1 mm × 150 mm) equipped with a C_(18) guard column(4 mm × 20 mm) with a mobile phase of acetonitrile–10 mM ammonium acetate buffer–formic acid(35: 65: 0.2, v/v/v) at the flow rate of 0.25 mL/min. The LC–MS was carried out on a triple-quadrupole mass spectrometry equipped with an ESI and positive selected-ion monitoring. Target ions were monitored at [M-Cl]~+ m/z 348.2 for NC and [M + H]~+ m/z237.2 for I.S., respectively. Results The simple one step deproteinize and rapid analysis method were successfully used in pharmacokinetic study on NC after i.g. administration. The linear relationship was good over the range of 2.5 – 1000.0 ng/ml(r~2 = 0.999 2) in rat plasma. The lower limit of quantification and detection were 2.5 and 1.6 ng/ml, respectively. The extraction recovery was in the range of 86.54 – 98.60%. The intra-and inter-day precisions(relative standard deviation) were less than 6.00%, with accuracies deviation between 89.40 to 95.57%. A two-compartment pharmacokinetic open model was proposed and validated to explain the apparent biphasic disposition of NC in rat plasma after i.g. administration. Conclusion This study was successfully applied to a pharmacokinetic study of NC in rats plasma following i.g. administration and could be used for preclinical and clinical pharmacokinetic evaluation of NC.     

红果樫木叶中1个新的三萜类化合物

目的 研究红果樫木Dysoxylum binectariferum的化学成分及抗肿瘤活性。方法 采用多种色谱方法结合进行化合物分离纯化，根据1D和2D核磁共振及质谱数据鉴定结构。采用MTT法对化合物进行肿瘤细胞增殖毒性评价。结果 从红果樫木叶提取物中得到2个具有由C₂-C₃碳键断裂C₂-C₆碳键闭环产生的双环[3，2，1]辛烷环骨架结构的三萜类化合物，分别为2，3-seco-2，6-cyclo-2a，29-dihydroxytirucalla-7，24-dien-23-oxo-3，9b-olide（1 ）、aphanamgrandiol A（2 ）。化合物1 对人肺癌H1975细胞和人结肠癌HCT116细胞的半数抑制浓度（half inhibitory concentration，IC₅₀）分别为（48.8±2.4）、（28.7±1.6）μmol/L，化合物2 对2种肿瘤细胞的IC₅₀值分别为（44.4±2.1）、（32.5±1.8）μmol/L。结论 化合物1 为新化合物，命名为大叶山楝三萜B。化合物2 首次从樫木属植物中分离得到。化合物1 和2 对肿瘤细胞具有一定的增殖抑制作用。