三种营养筛查工具对维持性血液透析患者透析相关性蛋白质能量消耗的评价比较

目的比较微型营养评价精法(MNA-SF)、营养不良炎症评分(MIS)、营养风险筛查2002(NRS 2002)三种营养筛查工具用于维持性血液透析患者透析相关性蛋白质-能量消耗(PEW)的评价差异。方法选取2016年6月至2019年7月就诊本院的维持性血液透析患者212例,分别采用MNA-SF、MIS、NRS 2002进行营养筛查,采集同期患者清蛋白、前清蛋白、胆固醇、体质量指数(BMI)、上臂围减少量、肌酐值、摄入量等指标,依据国际肾脏营养与代谢学会(ISRNM)的PEW的诊断标准,判定患者PEW情况,比较三种营养筛查工具用于PEW的诊断效能差异。结果以常规界值诊断,MNA-SF量表共准确筛查出PEW患者106例,存在误诊21例,漏诊9例;MIS量表共准确筛查出103例PEW患者,产生误诊14例、漏诊12例;NRS 2002共准确筛查PEW患者100例,产生误诊12例,漏诊15例;以分值数据测算,从曲线下面积来判断,三种筛查工具的诊断效能均处于良好水平,但MNA-SF的最佳截断点是≤11分,与常规诊断截点<11分略有不同。结论维持性血液透析患者发生透析相关性蛋白质-能量消耗可采用MNA-SF、MIS、NRS2002三种营养筛查工具,但需将MNA-SF法的诊断截点设为≤11分,达到提高诊断效能的目的。在临床护理过程中,可以依据患者临床需求,选择筛查方式。

Syntheses, Crystal Structures and Hydrogen-bonding Motif of Two Glycoluril Derivatives

The synthesis and aggregation behavior of two glycoluril derivatives were descrybed.The crystal of compound 1 belongs to the triclinic system,space group P1,with a=8.946(1),b=13.445(2),c=20.361(3)?,α=89.517(3),β=84.405(3),γ=86.325(3)°,Z=2,V=2432.1(6)?3,Dc=1.293 g·cm-3,C48H34N6O6·2DMSO,Mr=947.07,F(000)=992,μ=0.170 mm-1,the final R=0.1606 and wR=0.2410 for 4382 observed reflections(Ⅰ>2σ(Ⅰ)).The crystal of compound 2belongs to the monoclinic system,space group P21/c,with a=9.500(3),b=24.522(8),c=17.997(6)A,Z=2,V=4054(2)A^3,Dc=1.296 g·cm^-3,C48H34N6O6,Mr=790.81,F(000)=1648,μ=0.087mm-1,the final R=0.2146 and wR=0.2535 for 2878 observed reflections(Ⅰ>2σ(Ⅰ)).Unlike the highly conserved R22(8)hydrogen-bonding amide···amide homosynthon,the structural analysis indicated that compound 1 selected the C(20)hydrogen-bonding motif and 2 selected the R22(34)hydrogen-bonding motif,which revealed the competition from remote solvent molecule and the interference of the molecular hydrocarbon core in crystal packing.The supramolecular structure revealed molecule 1 is further linked into a one-dimensional chain and 2 into a two-dimensional interwoven plane by N–H···N hydrogen bonds.

Syntheses, Crystal Structures, and Biological Activities of Two Enantiomeric 2-Trifluoromethylthieno[2,3-d]pyrimidin-4-amine Derivatives

Two enantiomeric 2-trifluoromethyl-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d] pyrimidin-4-amine derivatives were synthesized by nucleophilic substitution of two chiral amines with 4-chloro-2-trifiuoromethyl-6,7-dihydro-5H-cyclopenta[4~5]thieno[2-3-d]pyrimidine, which started from 2-amino-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile, trifluoroacetic acid （TFA） and phosphoryl trichloride via one-pot procedure. Their structures were determined by single-crystal X-ray diffraction. Enantiomer （R）-3,（R）-N-（1-phenylethyl）-2-trifluoromethyl-6,7- dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-amine crystallizes in the tetragonal system, space group P43 with a = 8.6847（6）, b = 8.6847（6）, c = 22.419（2） A, V= 1690.9（3） A3, Z = 4, Dc = 1.428 g/cm^3, p = 0.228 mm-1, F（000） = 752, the final R = 0.0463 and wR = 0.1257 for 3442 observed reflections with 1〉 20（/）. Enantiomer （S）-3,（S）-N-（1-phenylethyl）-2-trifluoromethyl-6,7-dihydro- 5H-cycloperita[4,5]thieno[2,3-d]pyrimidin-4-amine crystallizes in the tetragonal system, space group P41 with a = 8.688, b = 8.688, c = 22.421 A, V = 1692.4 A3, Z = 4, Dc = 1.426 g/cm^3, μ= 0.227 mm^-1, F（000） = 752, the final R = 0.0682 and wR = 0.1806 for 3182 observed reflections with ≥20（I）. The preliminary bioassay indicated that the R-enantiomer exhibits higher antitumor activity against MCF-7 than gefitinib.

Synthesis, Crystal Structure and Antitumor Activity of 4-(5-(2,6-Difluorophenyl)-1,3,4-oxadiazol-2-ylthio)-2-(trifluoromethyl)thieno[2,3-d]pyrimidine

The title compound 4-(5-(2,6-difluorophenyl)-1,3,4-oxadiazol-2-ylthio)-2-(trifluoromethyl)thieno[2,3-d]pyrimidine(C15H5F5N4OS2, Mr = 416.35) was designed and synthesized as antitumor agent, and its structure was determined by 1H NMR, 13C NMR, MS, elemental analysis and single-crystal X-ray diffraction. The crystal belongs to monoclinic system, space group P21/c with a = 9.904(2), b = 10.057(2), c = 16.595(3) ?, β = 100.000(3)°, V = 1627.9(6) ?3, Z = 4, F(000) = 832, Dc = 1.699 g/cm3, μ = 0.395 mm-1, R = 0.0468 and wR = 0.1255 for 4726 independent reflections(Rint = 0.0336) and 2847 observed ones(I > 2σ(I)). The in vitro antitumor activity of the title compound was preliminarily evaluated by the standard MTT assay.

Synthesis, Crystal Structure and Antitumor Activity of N-(5-Aryl-1,3,4-thiadiazol-2-yl)-N?-((E)-styryl)ureas

N-(5-Aryl-1,3,4-thiadiazol-2-yl)-N?-((E)-styryl)ureas 4 a^4 i were designed and synthesized as antitumor agents, and their structures were characterized by IR, 1 H NMR, 13 C NMR,MS and elemental analysis. The single crystal of compound 4 a, C17 H13 FN4 OS, was also determined by X-ray crystallography. Crystal data: monoclinic, space group P21/n, a = 4.9401(8), b= 8.7100(15), c = 36.604(6) A,β= 93.320(3)°, V = 1572.4(5) A3, Z = 4, F(000)= 704, Dc = 1.438 g/cm3,μ= 0.228 mm-1, R = 0.0600 and wR = 0.1448 for 2743 independent reflections(Rint =0.0418) and 2174 observed ones(I > 2σ(I)). The in vitro antitumor activities of compounds 4 a^4 i were preliminarily evaluated by the standard MTT assay.

Synthesis, Crystal Structure and Antitumor Activity of 3,3-(1,4-Phenylene)-bisfuro[3,2-d]pyrimidin-4(3H)-ones

3,3-(1,4-Phenylene)-bis(polysubstituted furo[3,2-d]pyrimidin-4(3 H)-ones 3 were synthesized from the starting material of functionalized iminophosphorane 1 by aza-Wittig reaction. All of the title compounds were characterized by 1H NMR, MS and elemental analysis. Meanwhile, the single crystal of compound 3 c, C46H68N6O10, was also obtained and determined by X-ray crystallography. Crystal data: triclinic, space group P1, a = 9.0017(3), b = 10.5908(4), c = 14.0116(5) A, α = 108.582(2)°, β = 94.296(1)°, γ = 105.059(2)°, V = 1204.40(7) ?3, Z = 1, F(000) = 466, Dc = 1.193 g/cm3, μ = 0.084 mm-1, R = 0.0998 and wR = 0.2146 for 4213 independent reflections(Rint = 0.0689) and 2796 observed ones(I > 2σ(I)). The in vitro antitumor activities of compounds 3 a^3 c were preliminarily evaluated by the standard MTT assay.

紫菜多糖对脑缺血再灌注损伤小鼠血脑屏障的保护作用

目的研究紫菜多糖对小鼠脑缺血再灌注损伤后血脑屏障的影响。方法将180只雄性ICR小鼠随机分为假手术组、模型组、对照组和低、中、高剂量实验组,每组30只。模型组、对照组和实验组用线栓法制作小鼠短暂性大脑中动脉阻塞(t MCAO)模型,假手术组接受相似手术处理,但是不插入线栓。对照组在造模前腹腔注射4 mg·kg^(-1)尼莫地平,低、中、高剂量实验组在造模前分别给予100,200,400 mg·kg^(-1)紫菜多糖,连续注射7 d,每天1次;假手术组和模型组腹腔注射等量生理盐水。观察各组小鼠的脑梗死范围、脑含水量,用伊文思蓝(EB)法观察小鼠血脑屏障通透性的改变,用Western blot法检测缺血大脑皮层基质金属蛋白酶-9(MMP-9)和胞浆附着蛋白-1(ZO-1)蛋白的表达。结果模型组和低、中、高剂量实验组小鼠脑梗死体积分别为(28.45±5.32)%,(24.73±3.65)%,(22.36±4.19)%和(18.61±5.72)%;脑含水量分别为(83.23±1.56)%,(80.72±1.17)%,(80.38±1.32)%和(79.59±1.41)%;脑组织EB含量分别为(8.02±0.71),(7.18±0.66),(4.75±0.73)及(3.93±0.64)μg·g^(-1);缺血侧大脑皮层MMP-9蛋白水平为0.65±0.09,0.52±0.11,0.39±0.08和0.31±0.07;缺血侧大脑皮层ZO-1蛋白水平分别为0.18±0.07,0.24±0.06,0.37±0.08和0.51±0.10,差异均有统计学意义(均P<0.05)。结论紫菜多糖通过下调脑缺血再灌注后脑组织中MMP-9的表达,上调ZO-1的表达,降低血脑屏障通透性,这可能是紫菜多糖保护缺血再灌注后脑损伤的机制之一。

液体环氧底填料制备及球型二氧化硅对其性能影响

采用示差扫描量热法(DSC)及热重分析(TGA)研究了不同促进剂及固化剂含量的环氧树脂(E128)/甲基六氢苯酐(MHHPA)体系的固化过程及固化物的热稳定性。通过测定固化物的粘度、热膨胀系数和体系的凝胶时间研究了球型二氧化硅的用量及粒径对环氧底填料性能的影响。结果表明,最佳固化反应条件如下:MHHPA与E128质量比0.74:1,咪唑作为促进剂,添加质量分数1.02%,此时固化物的耐热性最佳。球形SiO2填料的加入对降低环氧树脂固化物的热膨胀系数效果明显。当球型二氧化硅的添加质量分数为60%,粒径为2.4μm时,体系的粘度为1800 mPa·s,固化物的热膨胀系数为3×10^-5/℃。150℃以上固化时球形SiO2的加入对体系的凝胶时间影响较小。