miR-31调控PAX9对肺癌细胞增殖和侵袭能力的影响

目的 研究miR-31调控配对盒基因9(PAX9)对肺癌细胞侵袭和增殖能力的影响.方法 运用免疫组织化学检测肺癌组织和癌旁正常组织PAX9蛋白的表达;运用荧光定量PCR检测肺癌组织、癌旁正常组织和肺癌细胞株M14中miR-31的表达.通过转染miR-31-inhibitor下调M14细胞中miR-31的表达,双荧光素酶活性检测miR-31对PAX9转录活性的影响;Transwell侵袭实验检测miR-31对M14细胞的侵袭能力的影响;平板克隆实验检测miR-31对M14细胞的增殖能力的影响.结果 与癌旁正常组织比较,PAX9蛋白在肺癌组织中表达降低,miR-31在肺癌组织中表达明显升高(P<0.05);双荧光素酶活性检测结果显示,miR-31可以直接调控PAX9的转录活性;抑制miR-31的表达后,肺癌细胞株M14的PAX9蛋白表达水平上调,侵袭和转移能力明显降低(P<0.05).结论 miR-31靶向PAX9的表达,从而调控肺癌细胞的侵袭和增殖能力.     

2－芳基丙酸类消炎镇痛药物的研究5 羟醛缩合法合成酮基布洛芬

以环己酮为起始原料，经Ｓｔｏｒｋ烯胺反应、羟醛缩合、消除、芳构化制得酮基布洛芬，总收率４３．２％。     

替米沙坦对人脐带动脉平滑肌细胞增殖的影响

摘 要 目的： 考察替米沙坦对体外培养的人脐带动脉平滑肌细胞（HUASMCs）增殖的抑制作用及对白细胞介素 6（IL-6）表达的影响。方法: 组织块贴壁法,HUASMCs原代培养,传3代细胞实验。MTT比色法检测同一浓度替米沙坦（50 μg·ml^-1）在不同作用时间（3～96 h）和不同浓度替米沙坦（0.5～500 μg·ml^-1）在同一作用时间（48 h）,对HUASMCs增殖的抑制作用。RT PCR和ELISA法检测低、中、高3种浓度的替米沙坦（1,10,100 μg·ml^-1）对HUASMCs表达IL-6 mRNA和因子的影响。结果: 不同作用时间的替米沙坦（50 μg·ml^-1）对HUASMCs的增殖有抑制作用(P<0.05),作用时间为48 h时,抑制作用最强,抑制率为（29.12±2.89）%。其后的作用时间72 h和96 h的抑制作用与48 h比无显著变化（P>0.05）。不同浓度的替米沙坦对HUASMCs增殖有抑制作用(P<0.05),当浓度为100 μg·ml^-1时,抑制作用最强,抑制率为（41.46±3.36）%。其后各浓度的抑制作用与100 μg·ml^-1比无显著变化（P>0.05）。低、中、高3种浓度的替米沙坦对HUASMCs表达的IL-6 mRNA和IL-6 含量均有抑制作用(P<0.05),并呈浓度依赖性(P<0.05)。结论: 替米沙坦抑制体外培养的HUASMCs增殖,对HUASMCs表达的IL-6 mRNA和因子分泌均有抑制作用。     

通痹胶囊对佐剂关节炎大鼠的继发关节病变及免疫功能的影响

目的初步探讨复方中药通痹胶囊对类风湿关节炎(RA)的治疗作用及机制。方法取Wistar雄性大鼠,制成佐剂关节炎(AA)模型,设正常组、模型组、雷公藤多甙对照组、通痹胶囊治疗组,观察不同处理因素对各组实验鼠继发关节肿胀度,继发病变分级,胸腺、脾脏重量及白细胞介素(IL)-1β的影响。结果治疗后通痹胶囊组、雷公藤组的继发关节肿胀,继发病变分级以及对实验鼠的胸腺、脾脏重量、IL-1β的影响与模型组相比差异均有显著性(P<0.05);通痹胶囊组与雷公藤组相比差异无显著性(P<0.05)。结论通痹胶囊对佐剂关节炎大鼠继发病变有明显的治疗作用;对模型大鼠胸腺、脾脏重量及IL-1β的抑制说明该方有一定的免疫抑制作用,这可能是该方治疗RA的机制之一。     

奥美拉唑不同途径、不同剂量给药抑制胃酸的效果

目的 :研究不同途径、不同剂量奥美拉唑抑制胃酸的效果 ,指导临床合理用药。方法 :将 10 0例内窥镜证实为活动期消化性溃疡病人分成A组 4 0例 ,静脉推注奥美拉唑 4 0mg ,bid ;B组 36例 ,口服奥美拉唑 2 0mg ,bid ;C组 2 4例 ,口服奥美拉唑 2 0mg ,qd。监测用药后d 3～ 5胃内 2 4hpH值变化 ,对A ,B 2组中各 10例 (为A2 ,B2 组 )测定了首次给药后的药物起效时间。结果 :A ,B组的抑酸效果相仿 (P >0 .0 5) ,胃内 pH值分别为 7.0 7±s0 .15和6 .9± 0 .6 ,与C组胃内 pH值 5.8± 1.4相比 ,差异有非常显著意义 (P <0 .0 1) ;A2 组起效时间为 (0 .7± 0 .6 )h ,B2 组为 (4.8± 1.0 )h ,差异有非常显著意义 (P <0 .0 1)。结论 :不同途径 3种剂量的奥美拉唑均有良好的抑酸效果 ,A ,B组更佳 ;静脉用药起效更迅速     

Binding and Anticancer Properties of Plumbagin with Human Serum Albumin

Plumbagin has received extensive attention as a promising anticancer drug. Therefore, we investigated the binding and anticancer properties of plumbagin with human serum albumin. Fluorescence results demonstrated that plumbagin interacts with human serum albumin, although its binding affinity may be affected to various extents by different compounds. The human serum albumin–plumbagin complex structure revealed that plumbagin binds to the hydrophobic cavity in the IIA subdomain of human serum albumin through hydrogen bonding and hydrophobic interactions. The plumbagin–human serum albumin complex enhances cytotoxicity by 2‐ to 3‐fold particularly in cancer cells but has no effect on normal cells in vitro. Compared with the unbound drug, the human serum albumin–plumbagin complex promotes HeLa cell apoptosis and has a stronger capacity for cell cycle arrest at the G2/M phase of HeLa cells. In conclusion, this study contributes to the rational design and development of plumbagin‐based drugs and a drug–human serum albumin delivery system.     

消痔灵注射液治疗内痔出血疗效观察

目的 评价消痔灵注射液治疗内痔出血的临床疗效.方法 80例内痔出血患者经口服泻药或者灌肠,排便后自腔缘3、6、9点注入麻醉药,观察应用消痔灵注射液治疗80例内痔出血患者的疗效进行回顾性分析.结果 80例内痔出血患者中76例次日出血停止,4例便后偶有滴血症状,经局部换药、使用痔疮栓及局部熏洗等保守治疗后出血消失,随访6～24个月无复发.结论 消痔灵注射液治疗内痔出血是一种简单、有效、可靠的方法.

Abstract：

Objective To assess the clinical effect and safety of Xiaozhiling injection on bleeding caused by hemorrhoids.Methods A retrospective analysis was performed on 80 hemorrhoid patients treated with Xiaozhiling injection.Results Among 80 patients.76 bleeding stopped after the injection.Four bleeding had interrupted outbreak and was cured after symptomatic treatment.Conclusion Xiaozhiling is an effective medicine for treatment of hemorrhoids bleeding.     

Triptolide induced cell death through apoptosis and autophagy in murine leukemia WEHI‐3 cells in vitro and promoting immune responses in WEHI‐3 generated leukemia mice in vivo

Triptolide, a traditional Chinese medicine, obtained from Tripterygium wilfordii Hook F, has anti‐inflammatory, antiproliferative, and proapoptotic properties. We investigated the potential efficacy of triptolide on murine leukemia by measuring the triptolide‐induced cytotoxicity in murine leukemia WEHI‐3 cells in vitro. Results indicated that triptolide induced cell morphological changes and induced cytotoxic effects through G0/G1 phase arrest, induction of apoptosis. Flow cytometric assays showed that triptolide increased the production of reactive oxygen species, Ca²⁺ release and mitochondrial membrane potential (ΔΨ_m), and activations of caspase‐8, ‐9, and ‐3. Triptolide increased protein levels of Fas, Fas‐L, Bax, cytochrome c, caspase‐9, Endo G, Apaf‐1, PARP, caspase‐3 but reduced levels of AIF, ATF6α, ATF6β, and GRP78 in WEHI‐3 cells. Triptolide stimulated autophagy based on an increase in acidic vacuoles, monodansylcadaverine staining for LC‐3 expression and increased protein levels of ATG 5, ATG 7, and ATG 12. The in vitro data suggest that the cytotoxic effects of triptolide may involve cross‐talk between cross‐interaction of apoptosis and autophagy. Normal BALB/c mice were i.p. injected with WEHI‐3 cells to generate leukemia and were oral treatment with triptolide at 0, 0.02, and 0.2 mg/kg for 3 weeks then animals were weighted and blood, liver, spleen samples were collected. Results indicated that triptolide did not significantly affect the weights of animal body, spleen and liver of leukemia mice, however, triptolide significant increased the cell populations of T cells (CD3), B cells (CD19), monocytes (CD11b), and macrophage (Mac‐3). Furthermore, triptolide increased the phagocytosis of macrophage from peripheral blood mononuclear cells (PBMC) but not effects from peritoneum. Triptolide promoted T and B cell proliferation at 0.02 and 0.2 mg/kg treatment when cells were pretreated with Con A and LPS stimulation, respectively; however, triptolide did not significant affect NK cell activities in vivo. © 2016 Wiley Periodicals, Inc. Environ Toxicol 32: 550–568, 2017.     

苦碟子中的新黄酮苷(Ⅱ)

苦碟子为菊科植物抱茎苦荬菜〔Ｉｘｅｒｉｓｓｏｎｃｈｉｆｏｌｉａ(Ｂｇｅ.)Ｈａｎｃｅ〕的当年生干燥全草,具有清热解毒、消肿止痛之功效〔1〕。其主要成分为以木犀草素、芹菜素为苷元的黄酮苷.继前报〔2〕报道了两个新黄酮苷之后,又从该植物中提取分离得到一种新的黄酮苷,命名为木犀草素7ＯβＤ吡喃葡萄糖醛酸苷乙酯(ｌｕｔｅｏｌｉｎ7ＯβＤｇｌｕｃｕｒｏｎｉｄｅｅｔｈｙｌｅｓｔｅｒ,Ⅰ),此化合物为一个未见文献报道的新化合物,结构见图1.提取分离:苦碟子全草5ｋｇ,用70%的乙醇加热回流,过滤,滤液回收乙醇,经真空干燥后,浓缩液混悬于…     

美洛昔康口腔崩解片中美洛昔康含量测定方法研 究简

目的 建立测定美洛昔康口腔崩解片中美洛昔康含量的反相高效液相色谱法.方法 色谱柱为KromasilC18柱（250 mm×4.6mm,5 μm）,流动相为0.1 mol/L醋酸铵溶液-甲醇（50：50）,柱温为室温,流速为1.0 mL/min,检测波长为271 nm.结果 美洛昔康质量浓度在40 ～ 60 μg/mL范围内与峰面积呈良好线性关系（r=0.999 8）,平均回收率为100.45％,RSD为0.55％（n=9）.结论 该方法简便、灵敏、准确、专属性强、重现性好,为产品的质量标准研究提供了理论依据.