Antibiotic C3368-A,a fungus-derived nucleoside transport inhibitor,potentiates the activity of antitumor drugs

Antibiotic C3368-A (CA) is produced by a fungus strain from a soil sample collected in Antarctica. CA markedly inhibited radiolabeled thymidine and uridine transport in mouse Ehrlich carcinoma cells, its 50% inhibitory concentration (IC₅₀) being 4.6 and 7.7 M, respectively. In clonogenic assay, CA displayed a synergistic effect with methotrexate (MTX), mitomycin C (MMC), 5-fluorouracil (5FU), and Adriamycin (ADR) against human oral epidermoid carcinoma KB cells. CA also markedly enhanced the inhibitory effect of 5FU and ADR on the proliferation of human hepatoma BEL-7402 cells as determined by thep-nitrophenyl-N-acetyl--d-glucosaminide (NAG) enzyme-reaction assay. 5FU or ADR cytotoxicity was not augmented by CA in human fetal lung 2BS cells. In vivo, CA significantly potentiated the inhibitory effect of MMC against colon carcinoma 26 in mice. No significant augmentation of toxicity by the combination was found in treated mice. The results suggest that CA, the newly found nucleoside-tranport inhibitor, may be useful in potentiation of the effect of antitumor drugs.     

奥替普拉诱发人肺腺癌细胞凋亡的研究

目的探讨奥替普拉（ｏｌｔｉｐｒａｚ）能否诱发人肺腺癌细胞凋亡及其机制。方法应用光镜、ＤＮＡ电泳、流式细胞仪、活细胞视频观察进行检测和分析。结果癌细胞在奥替普拉作用下,细胞分裂阻滞在分裂中期,Ｇ２／Ｍ百分比增高,出现细胞凋亡峰,凋亡细胞出现胞体固缩、核染色质凝聚或者断裂,细胞ＤＮＡ裂解片段呈现典型的“梯形”条带。奥替普拉诱导的ＧＬＣ细胞凋亡在使用浓度１２０μｇ／ｍｌ时效果明显。结论奥替普拉在适当浓度时能够诱发人肺腺癌细胞凋亡,这种作用与分裂期阻滞密切相关。     

Effect of recombinant human growth hormone on the intestinal structure of rats receiving bowel resection and parenteral nutrition

Recombinant human growth hormone (rHGH) can improve nitrogen balance and promotecell proliferation. Little is known about the relationship between rHGH and gastrointestinal mucosal structure and function after bowel resection and parenteral nutrition (PN). The aim of this study was to determine the effect of rHGH on bowel mucosal structure and barrier function in rats receiving 50% small intestinal resection and PN. Thirty Wistar rats with central vein catheterization plus 50% small bowel resection were divided into three groups: chow (chow), standard (STD) and rHGH (rHGH). The chow group received chow food; the STD group was given standard PN; the rHGH group received standard PN plus rHGH (4.8 mg/kg/day, subcutaneously). The groups were maintained on their respective diets for 8 days and then killed. Body weight, small intestinal mucosal thickness, villus height and Goblet cells in the villus were measured. Body weight loss in the STD group was significantly greater than that in the chow and rHGH groups (P< 0.01). The mucosal thickness and villus height of rHGH group were significantly greater than the STD and chow groups (mucosal thickness: 806 +/- 5.5 vs. 533 +/- 6.0 and 593 +/- 6.0 microm; Villus height: 506 +/- 6.0 vs. 295 +/- 5.5 gm and 400 +/- 6.7 lam, respectively) (P< 0.05). The number of Goblet cells in the STD group was significantly greater than the rHGH and chow groups (9.06 +/- 1.07 vs. 5.35 +/- 1.48 and 6.10 +/- 1.51/per villus) (P < 0.01). rHGH can maintain body weight and promote bowel mucosal cell growth and might improve the barrier function of the bowel in rats after 50% small intestinal resection and PN.     

Effects of Aging and Advanced Glycation on Gene Expression in Cerebrum and Spleen of Mice^1

Objective To analyze the effects of aging or advanced glycation on gene expression in the cerebrum and spleen of female C57BL/6J mice. Methods The gene expression profile wasdetermined by using cDNA expression arrays containing 588 cDNA.     

升麻地上部分化学成分研究升麻地上部分化学成分研究

目的 为开发中药升麻(Cimicifuga foetida L.)的地上部分资源,从中寻找新的天然活性成分。方法 利用多种色谱技术进行分离纯化,根据理化性质和现代波谱技术并辅以化学方法进行结构鉴定。结果 从升麻地上部分80%乙醇提取物的乙酸乙酯部分分得5个9,19-环菠萝蜜烷型三萜皂苷和1个甾醇苷。分别鉴定为:西麻苷I(1),西麻苷II(2),升麻醇半乳糖苷(3),12β-羟基升麻醇木糖苷(4),12β-羟基升麻醇阿拉伯糖苷(5),胡萝卜苷(6)。结论 1和2为新化合物,4及5为首次从该植物中分得。     

20-位酯化喜树碱衍生物的合成和抗肿瘤活性

目的寻找高效低毒的抗肿瘤新喜树碱酯衍生物。方法通过酰化反应合成了目标产物，用¹HNMR,IR,MS,和 HRMS确证了它们的结构；MTT法评价了目标产物的细胞毒活性；并用小鼠肝癌H₂₂肿瘤模型对这些化合物的体内抗肿瘤活性进行了评价。结果合成了12个新喜树碱衍生物。结论体内外抗肿瘤试验表明，对小鼠肝癌细胞H₂₂模型，新合成的喜树碱衍生物4的抗肿瘤活性与拓扑替康相近，但毒性低于拓扑替康。     

小叶石楠的化学成分研究

目的 研究小叶石楠茎的化学成分。方法 采用硅胶色谱法分离纯化，薄层色谱及波谱法进行结构鉴定。结果 从其乙醇提取物的氯仿、醋酸乙酯部分分得7个化合物，其结构鉴定为羽扇豆醇(Ⅰ)，β-谷甾醇(Ⅱ)，白桦酸(Ⅲ)，pyracrenic acid(Ⅳ)，表儿茶素(V)，胡萝卜苷(Ⅵ)，野樱苷(Ⅶ)。结论 化合物Ⅰ，Ⅲ～Ⅵ为首次从该属植物中分离得到，化合物Ⅲ和Ⅶ为首次从该植物中分离得到。化合物Ⅳ具有抗肿瘤活性。     

黄连生物碱抗糖尿病机制的研究进展

黄连为中国传统中药，药理作用广泛，应用历史悠久。现代药理学研究新发现其具有治疗糖尿病及其并发症的作用，其有效成分为多种生物碱。对黄连及其生物碱抗糖尿病整体实验和分子水平上的研究工作进行了综述。提出阐明黄连生物碱作用的分子靶点及相关机制是未来研究的方向。     

微细化工艺制备的葛根微粉溶出度和生物利用度的研究

 目的 研究葛根微粉在溶出和生物利用度方面的效果,为微细化工艺在中药中的应用提供理论依据。方法 以葛根黄酮为指标,用紫外分光光度法测定葛根微粉和葛根粉在不同时间点葛根黄酮溶出的量,计算累积释放率;采用透析袋为屏障观察葛根微粉和葛根粉的溶出情况。按葛根素100mg·kg^-1体重分别给大鼠口服葛根微粉和提取物,用HPLC测定葛根素含量,以葛根提取物为对照,计算葛根微粉的相对生物利用度。结果 用桨法测定体外溶出度时,葛根微粉累积释放度显著高于葛根粉;用透析袋作为屏障时,两者差异不明显。葛根微粉的生物利用度是葛根提取物的50％强。结论 葛根制成微粉后,能改善其有效成分的溶出,但是与提取物相比,服药量大,生物利用度低,因此微米中药的应用有待进一步评价。     

原发纵隔的弥漫大B细胞非霍奇金淋巴瘤34例临床分析

目的:探讨原发纵隔的弥漫大B细胞非霍奇金淋巴瘤(PMLBL)的临床特征及治疗策略.方法:回顾性分析34例原发纵隔的弥漫大B细胞非霍奇金淋巴瘤的临床特点和不同治疗方案对患者生存期的影响.结果:临床分期79.4%为Ⅰ～Ⅱ期,50.0%患者起病时出现上腔静脉压迫综合征,47.1%有邻近器官侵犯.采用化、放疗联合治疗29例(85.3%)、单纯化疗5例(14.7%)、自体造血干细胞移植9例(26.4%).根据寿命表法分析,全组5和10年无瘤生存率(DFS)为47.8%和41.0%,5和10年总生存率(OS)为54.4%和54.4%.自体造血干细胞移植组较常规化、放疗组5年DFS和OS均有所提高,但无显著性差异(P＞0.05).不良预后因素分析显示,具有巨大肿块及治疗后未能获得完全缓解者预后差(P＜0.05).结论:原发纵隔的弥漫大B细胞非霍奇金淋巴瘤具有独特的临床和病理特点,治疗以化、放疗为主.具有不良预后因素的患者可考虑自体外周血造血干细胞移植(APBSCT),但最佳的治疗方案尚需进一步的前瞻性随机研究证实.