Novel 2(3H)-Benzothiazolones as Highly Potent and Selective Sigma-1 Receptor Ligands

In an effort to produce a new pharmacological probe with high affinity and selectivity for the sigma-1 receptor, we have synthesized a series of original 2(3H)-benzothiazolones utilizing compound 4 [3-(1-piperidinoethyl)-6-propylbenzothiazolin-2-one] as a lead. Receptor binding affinities were determined at sigma-1 and sigma-2 receptors. The best ligand (9, sigma-1 K_i = 0.56 nM, selectivity ratio >1000) was obtained with an azepine side-chain. When tested on a wide battery of receptors, including 5HT_2A(h), 5HT₃(h), α₁, α ₂, β₁, β₂, H₁, H₂, opioids, D₁(h), D₂(h), 5HT uptake, and DOPA uptake, compound 9 showed submicromolar affinity only for α₂ (K_i = 205 nM) and H₁ (K_i = 311 nM).     

Anti-inflammatory effects of fructose-1,6-bisphosphate on carrageenan-induced pleurisy in rat.

In the present study, we evaluated the effect of fructose-1,6-bisphosphate (FBP), a high energy intermediate metabolite of glycolysis, in an acute model of lung injury. Injection of carrageenan into the pleural cavity of rats elicited an acute inflammation response characterized by a fluid accumulation in the pleural cavity which contained a large number of polymorphonuclear neutrophils. FBP (500mg/kg) attenuated the inflammation parameters: exudate volume, total leukocytes and the number of polymorphonuclear leukocytes, but the protein concentration in the exudate was not significantly affected by treatment with FBP. The precise site and mechanism of the anti-inflammatory effect was not addressed, considering the diverse pharmacological actions of FBP. This drug has anti-inflammatory actions suggesting that it may represent a novel strategy for the modulation of inflammatory response.     

用血清药理学方法观察毛茛提取液对家兔主动脉平滑肌细胞内钙的影响

目的:观察毛茛提取液含药血清对培养家兔主动脉平滑肌细胞内游离钙浓度的影响.方法:体外培养家兔主动脉平滑肌细胞(VSMC),用荧光指示剂INDO-AM负载细胞,灌胃给予不同浓度药物,观察不同稀释浓度含药血清及不同时相药物血清对由NE诱导细胞内游离钙浓度([Ca2 ]i)增加的影响.结果:毛茛提取液各含药血清组均能降低由NE诱发的细胞内[Ca2 ]i的升高.结论:毛茛提取液含药血清能减少VSMC细胞内[Ca2 ]i.     

Psoas abscess: diagnostic and therapeutic considerations in six patients

Psoas abscess (PA) is an infrequent clinical entity and presents diagnostic and therapeutic challenges. Six cases are reported concerning diagnostic and therapeutic considerations. Clinical diagnosis is difficult because of non-specific symptoms. The primary psoas abscess has no definite etiology and is spread by hematogeneous route from a distant occult site. The PA can also be secondary to gastrointestinal pathology through direct infection of adjacent structures. The most common causes are Crohn's disease, appendicitis, diverticulitis and carcinoma. Routine laboratory evaluation is seldom useful for localizing the disease process. Conventional radiological techniques are often unhelpful. Modern imaging diagnosis techniques such as ultrasound and computerized tomography have allowed for a refinement in both the etiologic diagnosis and the treatment by means of CT-guided or ultrasound-guided percutaneous drainage of the abscess, thus avoiding surgical drainage in many cases. Immediately on diagnosis of PA prompt treatment is necessary. Percutaneous drainage should be performed whenever possible and in case of failure, surgical drainage should be practiced as well as intestinal resection, whenever indicated.     

粪便自诱导分子-2在新生儿坏死性小肠结肠炎临床病情监测中的价值

目的初步探讨粪便自诱导分子-2(AI-2)监测新生儿坏死性小肠结肠炎(NEC)病情变化的价值。方法以2017年10月至2018年4月收治的12例NEC患儿为研究对象,并按照胎龄、日龄、生产方式、喂养方式、抗生素使用等选择12例与NEC组患儿匹配的非NEC新生儿为对照组。NEC诊断时定为急性期,再次开奶3天后定为恢复期。采集NEC急性期、恢复期和对照组的粪便标本,以BB170生物荧光检测法检测粪便AI-2浓度,采用16s rDNA高通量测序分析粪便菌群。结果在菌门水平,拟杆菌门比例在NEC组急性期、恢复期和对照组之间差异有统计学意义(P0.05),其中NEC恢复期比例最低。在菌属水平,肠球菌属、拟杆菌属比例在三组之间差异均有统计学意义(P0.05),其中NEC急性期肠球菌属比例最低,恢复期拟杆菌属比例最低。三组粪便AI-2浓度差异有统计学意义(P0.05),以NEC急性期为最低。结论 AI-2在监测NEC病情变化方面具有潜在临床应用价值。     

晚期肺癌患者免疫功能的系统评价及临床意义

背景与目的真实评价免疫功能对明确肿瘤的发生发展及给予适时治疗具有重要意义。本研究旨在系统评价晚期肺癌患者免疫功能及意义。方法计数晚期肺癌患者和健康人外周血免疫细胞数;用流式细胞仪测定免疫细胞亚群比例和细胞内IL-4、INF-γ及穿孔素、颗粒酶水平;用MTT法评价淋巴细胞对肿瘤细胞株的抑制率及其增殖活性。结果晚期肺癌患者组T、B、NK细胞绝对数及亚群比例均显著低于健康组(P<0.05);但患者组的调节性T细胞(4.00±1.84)%明显高于健康组(1.27±0.78)%(P<0.05)。患者组的CD8+T细胞中IFN-γ、穿孔素及颗粒酶阳性率均显著低于健康组(P<0.05);而IL-4正好相反。患者组的免疫细胞增殖能力、PPD阳性率及对瘤细胞株的抑制率显著低于健康组(P<0.05)。结论晚期肺癌患者免疫功能较健康人明显低下。     

Effect of Brazilian green propolis on the production of reactive oxygen species by stimulated neutrophils

The activity of a crude ethanol extract of green propolis and its fractions obtained by partition with hexane, chloroform and n-butanol was assessed on luminol- and lucigenin- enhanced chemiluminescence (CL) produced by rabbit neutrophils (PMNs) stimulated with particles of serum-opsonized zymosan (OZ). The total production of reactive oxygen species (ROS) by PMNs was measured by the luminol-enhanced CL (LumCL) assay and the production of the superoxide anion (O2*-) by the lucigenin-enhanced CL (LucCL) assay. All evaluated propolis samples had inhibitory effect on the LumCL and LucCL, which was concentration dependent. The n-butanol and chloroform fractions displayed the highest inhibitory effect on the LumCL produced by PMNs stimulated with OZ, in comparison with both the ethanol extract and the hexane fraction. Besides, the hexane fraction was the one which presented the highest effect for the LucCL assay. Some isolated compounds from both n-butanol and chloroform fractions were also assessed, including kaempferide, isosakuranetin, aromadendrine-4'-methyl-ether and 3-prenyl-p-coumaric acid. Kaempferide presented the highest inhibitory effect on the LumCL in comparison with the other compounds. Moreover, under the conditions assessed, the studied green propolis samples and isolated compounds were not toxic to the rabbit PMNs.     

中药及提取物抑制肿瘤血管生成抗转移的研究进展

转移是恶性肿瘤的基本生物学特征,是临床上绝大多数肿瘤病人的致死因素^[1]。1971年Folkman^[2]就提出恶性肿瘤的一大特性是无限制地侵袭性生长和远处转移,这一特性依赖于肿瘤血管的生成,因此抑制血管生成能显著抑制肿瘤的生长和转移。目前抑制肿瘤血管生成抗转移的途径主要有：①阻断或抑制促血管生成因子通路。     

莪术醇通过降解ECM改变细胞周期抑制A549细胞增殖

目的:探讨莪术醇抑制A549细胞增殖作用及分子机理。方法:MTT法观察莪术醇对A549细胞增殖的抑制作用;天狼猩红染色法检测莪术醇对A549细胞层分泌胶原的影响;流式细胞术检测细胞周期阻滞。结果:莪术醇对A549细胞增殖有抑制作用,并能抑制细胞胶原分泌;细胞周期分析显示,莪术醇作用细胞24h,主要通过增加G1期细胞比例来抑制细胞增殖,作用48h主要影响了细胞的G2期。结论莪术醇能抑制肺腺癌A549细胞增殖,其机制可能是与莪术醇抑制ECM中胶原的分泌、诱导细胞周期阻滞有关。