结石患者和健康对照者尿微晶生长、聚集过程的比较研究

采用扫描电子显微镜(SEM)和X-射线粉末衍射仪(XRD)比较研究了5例泌尿系结石患者和5名健康对照者的尿微晶的生长动力学差异。随着生长时间(t)增加,结石患者尿微晶尺寸不断增大,粒径从t=1 h时的约(6±4)μm增加到t=48 h的(29±17)μm,但微晶数密度从(1 400±300)mm-2逐渐减少至(450±140)mm-2,表明在患者尿液中微晶的形成过程为生长控制;相比之下,在对照者尿液中,随着t从1 h增加48 h,尿微晶数密度从(850±260)mm-2减少至(610±210)mm-2,微晶尺寸从(6±5)μm增加至(15±9)μm,这表明其生长过程同时为成核控制和生长控制。上述差异归因于对照者尿液中抑制剂的浓度和活性均比结石患者的高,更能抑制尿微晶的生长和聚集。     

石榴皮单宁的超声波-半仿生法提取及抗氧化性分析

采用超声波辅助半仿生法提取石榴皮单宁。利用正交实验方法对提取工艺进行优化,并进行了红外光谱分析和研究抗氧化能力检测。在提取液的pH值分别:1.2、7.6、8.4,溶剂质量分数50%、提取时间45 min、提取温度50℃、超声波功率320 W和超声波频率25KHz的条件下,单宁提取量可达234.6 mg.g-1,远高于无超声波辅助的试样。红外光谱分析表明:石榴皮单宁中含有大量的无色花翠素-3-葡萄糖苷分子结构式类物质;抗氧化能力检测显示:采用超声波辅助半仿生法能够提高单宁对OH.、DPPH.和ABTS+.等自由基的清除能力,与水回流提取法相比,其IC50值分别降低了0.26、0.022和0.41 mg.mL-1。     

Synthesis of aromatic carbamates derivatives with a chromen-2-one fragment

Condensation of methyl N-(3-hydroxyphenyl)carbamate with ethyl trifluoromethylacetoacetate, 2-methoxyethyl acetoacetate in the presence of conc. sulfuric acid, and also with acetonedicarboxylic acid formed in situ from citric acid under the action of conc. sulfuric acid afforded chromene derivatives. The esterification of 2-{7-[(methoxycarbonyl)amino]-2-oxo-2H-chromen-4-yl}acetic acid with methanol in the presence of TsOH provided the corresponding ester. The oxidation of its α-methylene group with selenium dioxide led to the formation of methyl 2-{7-[(methoxycarbonyl)amino]-2-oxo-2H-chromen-4-yl}-2-oxo-acetate entering into a condensation with o-phenylenediamine resulting in a derivative with a dihydroquinoxaline fragment. The reaction of phenyl N-(4-formylphenyl)carbamate with 3-acetyl-2H-chromen-2-one in butanol in the presence of catalytic quantity of piperidine and acetic acid furnished 4-[(E)-3-oxo-2H-chromen-3-yl)-1-propenyl]phenyl N-phenylcarbamate.     

堆浸工艺中浸润面的牛顿迭代计算方法

为了研究堆浸工艺的机理,用牛顿迭代公式寻求浸润面的非线性方程的数值解,经过14次迭代的误差达到了10^-6,说明此算法收敛有效。     

Palladium-Catalyzed [4+2] Cycloaddition of Vinyl Benzoxazinanones with 1,3-Indanedione: Approach to Spiro-Tetrahydroquinoline Scaffolds

A palladium catalyzed decarboxylative [4+2] cycloaddition of vinyl benzoxazinanones with 2-arylidene indan-1,3-dione has been established, which afford a series of bioactive spiro-tetrahydroquinolines (27 examples) in moderate to good yield (up to 87 %) with high diastereoselectivities. The synthetic utility of this reaction was demonstrated by gram-scale synthesis. Compounds synthesized by this method potently inhibited proliferation in a panel of cancer cell lines. Particularly, the most potent compounds 3 ae , 3 ah , 3 aj and 3 fa displayed selective inhibition of MDA-MB-231 breast carcinoma cells with IC₅₀ values of 1.292, 0.6118, 0.6558, 1.656 and 2.215 μM, respectively.