Antimicrobial Activity of Novel C2-Substituted 1,4-Dihydropyridine Analogues

The antimicrobial activity of 3-methyl-5-isopropyl (or ethyl) 6-methyl-4-nitrophenyl-1,4-dihydropyridine-3,5-dicarboxylate derivatives was evaluated. Prokaryotes (bacteria) appeared to be more sensitive to their antimicrobial activity than were eukaryotes (filamentous fungi). The best antibacterial activity was shown by derivative 33, which was able to inhibit the growth of Mycobacterium smegmatis (MIC₃₃ = 9 μg.ml⁻¹), Staphylococcus aureus (MIC₃₃ = 25 μg.ml⁻¹), and Escherichia coli (MIC₃₃ = 100 μg.ml⁻¹). In addition, derivative 4 demonstrated its antibacterial power on the acid-fast bacterial species M. smegmatis and on Gram-positive S. aureus. Focusing on the structure-activity relationship, it appears that the increase in the substituent bulk at the C2 position improved the antibacterial activity of the set of compounds studied. Derivatives 33 and 4, carrying 2-cyano-3-oxo-3-phenylprop-1-en-1-yl and allyliminomethyl groups, respectively, showed significantly higher inhibition activities on all tested microorganisms in comparison with the rest of the derivatives. This enhancement was also in good correlation with different log P values (lipophilicity parameter).     

Protective Effect of Wheat Peptides against Indomethacin-Induced Oxidative Stress in IEC-6 Cells

Recent studies have demonstrated that wheat peptides protected rats against non-steroidal anti-inflammatory drugs-induced small intestinal epithelial cells damage, but the mechanism of action is unclear. In the present study, an indomethacin-induced oxidative stress model was used to investigate the effect of wheat peptides on the nuclear factor-κB(NF-κB)-inducible nitric oxide synthase-nitric oxide signal pathway in intestinal epithelial cells-6 cells. IEC-6 cells were treated with wheat peptides (0, 125, 500 and 2000 mg/L) for 24 h, followed by 90 mg/L indomethacin for 12 h. Wheat peptides significantly attenuated the indomethacin-induced decrease in superoxide dismutase and glutathione peroxidase activity. Wheat peptides at 2000 mg/L markedly decreased the expression of the NF-κB in response to indomethacin-induced oxidative stress. This study demonstrated that the addition of wheat peptides to a culture medium significantly inhibited the indomethacin-induced release of malondialdehyde and nitrogen monoxide, and increased antioxidant enzyme activity in IEC-6 cells, thereby providing a possible explanation for the protective effect proposed for wheat peptides in the prevention of indomethacin-induced oxidative stress in small intestinal epithelial cells.     

The Protective Effect of Rhizoma Dioscoreae Extract against Alveolar Bone Loss in Ovariectomized Rats via Regulating Wnt and p38 MAPK Signaling

Aim: The aim of this study was to evaluate the osteoprotective effect of aqueous Rhizoma Dioscoreae extract (RDE) on the alveolar bone of rats with ovariectomy-induced bone loss. Methods: Female Wistar rats were subjected to either ovariectomy or a sham operation (SHAM). The ovariectomized (OVX) rats were treated with vehicle (OVX) or RDE by oral gavage or with 17β-estradiol (E2) subcutaneously. After treatments, the bone mineral density (BMD), the three-dimensional bone architecture of the alveolar bone and the plasma biomarkers of bone turnover were analyzed to assess bone metabolism, and the histomorphometry of the alveolar bone was observed. Microarrays were used to evaluate gene expression profiles in alveolar bone from RDE-treated and OVX rats. The differential expression of genes was further analyzed using Ingenuity Pathway Analysis (IPA). The key findings were verified using real-time quantitative RT-PCR (qRT-PCR). Results: Our results showed that RDE inhibited alveolar bone loss in OVX rats. Compared to the OVX rats, the RDE-treated rats showed upregulated expression levels of 207 genes and downregulated expression levels of 176 genes in the alveolar bone. The IPA showed that several genes had the potential to code for proteins that were involved in the Wnt/β-catenin signaling pathway (Wnt7a, Fzd2, Tcf3, Spp1, Frzb, Sfrp2 and Sfrp4) and the p38 MAPK signaling pathway (Il1rn and Mapk14). Conclusion: These experiments revealed that RDE could inhibit ovariectomy-induced alveolar bone loss in rats. The mechanism of this anti-osteopenic effect in alveolar bone may be involved in the reduced abnormal bone remodeling, which is associated with the modulation of the Wnt/β-catenin and the p38 MAPK signaling pathways via gene regulation.     

Resveratrol Increases Nephrin and Podocin Expression and Alleviates Renal Damage in Rats Fed a High-Fat Diet

Resveratrol is well known for its anti-inflammation and anti-oxidant properties, and has been shown to be effective in alleviating the development of obesity. The purpose of this investigation was to analyze the effect of resveratrol on renal damage in obese rats induced by a high-fat diet (HFD) and its possible mechanisms. Male Sprague-Dawley rats were divided into three groups: control, HFD, and HFD plus resveratrol (treated with 100 mg/kg/day resveratrol). Body weight, serum and urine metabolic parameters, and kidney histology were measured. Meanwhile, the activities of nuclear factor-κB (NF-κB) and superoxide dismutase (SOD), the content of malondialdehyde (MDA), and the protein levels of tumor necrosis factor (TNF-α), monocyte chemotactic protein-1 (MCP-1), nephrin and podocin in kidney were detected. Our work showed that resveratrol alleviated dyslipidemia and renal damage induced by HFD, decreased MDA level and increased SOD activity. Furthermore, the elevated NF-κB activity, increased TNF-α and MCP-1 levels, and reduced expressions of nephrin and podocin induced by HFD were significantly reversed by resveratrol. These results suggest resveratrol could ameliorate renal injury in rats fed a HFD, and the mechanisms are associated with suppressing oxidative stress and NF-κB signaling pathway that in turn up-regulate nephrin and podocin protein expression.     

特发性肺纤维化的发病机制及凝血指标与肺功能关系的研究

目的：探讨特发性肺纤维化（IPF）的发病机制以及 IPF 患者凝血指标与肺功能的相关性。方法将32例特发性肺纤维化患者设为观察组,32例健康人设为对照组,检查两组研究对象的血凝指标、肺高分辨率 CT 及肺功能,并进行比较和相关性分析。结果 IPF 患者血液中 D‐二聚体、血浆纤维蛋白原含量升高;血浆纤维蛋白原水平与肺一氧化碳弥散量（DLCO）水平呈显著负相关性。结论 IPF 患者体内处于血液高凝状态,血浆纤维蛋白原（FIB）含量检测能够反映肺弥散能力,进一步判断肺纤维化的病情轻重。     

热熔挤出技术制备穿心莲提取物固体分散体

目的:采用热熔挤出技术(HME)制备穿心莲提取物的固体分散体,并对其进行体外评价。方法:以穿心莲内酯和脱水穿心莲内酯含量为指标,采用单因素试验,分别对亲水性载体种类、穿心莲提取物与载体用量比例进行筛选,确定最优穿心莲提取物热熔挤出固体分散体的制备方法,并对形成的固体分散体进行体外溶出度试验和差式扫描量热分析、电镜扫描、X-射线衍射等物相鉴别。结果:穿心莲提取物热熔挤出固体分散体的最优制备工艺为:以Soluplus为载体,穿心莲提取物∶Soluplus=1∶2(m/m)混合,热熔挤出区段升温程序为130→135→140→130℃,螺杆转速为27 r/min,加料速度为15 g/min。物相鉴别试验显示穿心莲提取物在热熔挤出分散体中以无定形态分散。结论:HME能使穿心莲提取物以无定形状态分散,提高穿心莲提取物的溶解度。     

应用PDCA循环改进我院药房调配人员工作量分配不均

目的:寻求解决药房调配人员工作量分配不均的方法。方法:采用PDCA循环管理方法。总结并归纳引起调配人员工作量不均的主要原因,并寻求措施进行改进,通过比较改进前、后各2个月分药、调剂人员月工作量及其标准偏差进行效果评价。结果与结论:查方与分药人员的分配比例不当是影响工作量分配不均的主要因素。通过采取调整各时间段各班次的调剂、查方和分药人员人数的排班方案,有效缩小了各岗位人员工作量的差距,改进前与改进后2个月分药剂数±标准偏差分别为5 760.00±1 569.48、5 719.30±1 558.02与5 568.20±835.36、5 456.20±639.63,调剂剂数±标准偏差分别为5 747.00±865.51、6 208.30±1287.74与5 909.30±726.79、5441.70±574.55,改进后与改进前比较标准偏差明显降低,表明采取的措施行之有效。     

新生儿神经行为评分的围产期影响因素研究

目的 探讨新生儿神经行为能力及其相关围产期影响因素.方法 应用鲍秀兰等建立的新生儿神经行为评定法（neonatal behavioral neurological assessment,NBNA）对298例足月儿进行新生儿神经行为能力评定,使用自编的“基本资料调查问卷”收集新生儿及其家庭资料.以NBNA总分为因变量,19项围产期影响因素为自变量,采用Logistic回归分析筛选影响因素.结果 新生儿NBNA评分的合格率为99.33％,孕周及孕期情绪为新生儿NBNA得分的有利因素,偏回归系数分别为-0.41和-0.33,而孕妇年龄则为新生儿NBNA得分的不利因素.结论 孕周长和孕期情绪好可促进新生儿神经行为发育,而孕妇年龄大则对其神经行为发育造成影响.