三尖杉属植物中生物碱的研究——Ⅸ.三尖杉酯碱类似物的半合成及其抗白血病活性

报道三尖杉碱的十七个新的酯类化合物的半合成及其抗肿瘤作用。药理实验结果表明1,2,2+3,6和8有显著的抗癌活性,4,5,15和16有中等的抗肿瘤作用。通过化学结构和抗肿瘤活性的比较,初步探讨了此类生物碱的构效关系。     

Increased inflammatory properties of adipose tissue macrophages recruited during diet-induced obesity

Although recent studies show that adipose tissue macrophages (ATMs) participate in the inflammatory changes in obesity and contribute to insulin resistance, the properties of these cells are not well understood. We hypothesized that ATMs recruited to adipose tissue during a high-fat diet have unique inflammatory properties compared with resident tissue ATMs. Using a dye (PKH26) to pulse label ATMs in vivo, we purified macrophages recruited to white adipose tissue during a high-fat diet. Comparison of gene expression in recruited and resident ATMs using real-time RT-PCR and cDNA microarrays showed that recruited ATMs overexpress genes important in macrophage migration and phagocytosis, including interleukin-6 (IL-6), inducible nitric oxide synthase (iNOS), and C-C chemokine receptor 2 (CCR2). Many of these genes were not induced in ATMs from high-fat diet-fed CCR2 knockout mice, supporting the importance of CCR2 in regulating recruitment of inflammatory ATMs during obesity. Additionally, expression of Apoe was decreased, whereas genes important in lipid metabolism, such as Pparg, Adfp, Srepf1, and Apob48r, were increased in the recruited macrophages. In agreement with this, ATMs from obese mice had increased lipid content compared with those from lean mice. These studies demonstrate that recruited ATMs in obese animals represent a subclass of macrophages with unique properties.     

血清反复冻融对HBsAg和抗HBs抗体检测的影响

0　引言　 EL ISA技术已在乙肝标志物的检测中已普遍应用 ,一般认为收集的血清应及时检测 .而在基层单位或在流行病学调查研究中 ,由于血标本收集不集中 ,或者有些标本常需检测多个指标而持续时间较长 ,因此 ,血清必须低温贮存一定时间或反复冻融后检测 ,而血清冻融对 EL ISA检测结果是否有影响尚不清楚 .为此 ,我们对 183份血清标本冻融前、冻融 3次、冻融 6次后的 HBs Ag和抗 - HBs进行了检测和分析比较 .1　材料和方法1.1　材料　 1999- 0 5收集西京医院门诊乙肝 5项检测血清183份 ,年龄、性别、诊断不限 .1.2　方法　于初次检测 …     

有自杀行为的单、双相抑郁症患者父母育龄及胎次效应比较

目的:比较有自杀行为的单、双相抑郁症患者间父母育龄及胎次效应的差异。方法:于1983-07/2003-06选择无锡市精神卫生中心门诊和住院符合中国精神疾病分类方案与诊断标准第3版及美国精神障碍诊断和统计手册第4版心境障碍中抑郁发作标准的、无严重躯体疾病或脑器质性疾病的抑郁患者。有自杀行为的单相抑郁症患者家系59例,双相抑郁症患者家系31例。采用自行编制的精神病家系调查表(内容主要包括患者及一级亲属所有成员社会人口学资料、疾病发作特点及次数、自杀情况),由两名主治医师或以上的研究人员对每一家系进行调查,然后再由两名研究人员在互不知情的情况下对每一患者进行再诊断。对所有先症者及一级亲属中有自杀行为者进行面检(面检率>95%);对无自杀行为的一级亲属则进行信函调查(53%)及面检(47%)。已死亡及不能进行面检者的资料由一两名一级亲属提供有关情况填写调查表。用Haldance和Smith法观察有自杀行为的单相抑郁症患者及双相抑郁症患者父母育龄及胎次的效应。结果:符合入组诊断标准者共151例,完成家系调查的共122例,其中纳入分析的单相抑郁症家系59例,双相抑郁症家系31例。①单相抑郁症患者胎次为1的13例,胎次为2的15例,胎次为3的13例,胎次为4的8例,胎次为5的8例,胎次为7的2例;双相抑郁症患者胎次为1的10例,胎次为2的11例,胎次为3的7例,胎次为4的1例,胎次为5的2例,胎次为7的0例。②有自杀行为单相抑郁症患者与父母育龄及胎次的关系非常显著(C=2.4>2,P<0.01,6A>X6A);有自杀行为双相抑郁症患者与父母育龄及胎次无显著关系(C=0.74<2,P>0.05)。结论:单相抑郁症患者父母育龄越大和胎次越高者易发生自杀行为,双相抑郁症患者父母育龄和胎次自杀行为的发生无明显关系。提示适龄婚育对防止单相抑郁症自杀行为的发生具有重要意义。     

Effects of Sibutramine on Gastric Emptying, Intestinal Motility and Rectal Tone in Dogs

The aim of this study was to evaluate the effects of sibutramine on gastric emptying, small-bowel contractions, rectal tone and compliance, and gastrointestinal myoelectrical activity. The study was performed in 14 dogs. It was composed of three separate experiments: gastric emptying of liquids and gastrointestinal slow waves; small-bowel contractions; and rectal tone and rectal compliance. Each experiment included two sessions: a control session and a treatment session with sibutramine (5 mg/kg orally) administrated 2 h before the study. Sibutramine significantly accelerated liquid gastric emptying at 75 and 90 min after the meal but did not alter gastrointestinal slow waves. Gastric emptying at 75 and 90 min was 61.42 ± 7.71 and 66.32 ± 7.67% in the control session, and increased to 71.27 ± 5.14 and 75.93 ± 5.29% in the session with sibutramine (p < 0.05, vs. control). Sibutramine significantly inhibited postprandial small-bowel contractions. Sibutramine did not alter the rectal tone, but significantly increased rectal compliance. Sibutramine accelerates gastric emptying of liquids but inhibits small-bowel contractions. These findings suggest the peripheral mechanisms of sibutramine in reducing food intake and causing weight loss in obesity patients.     

Vaginal trichomoniasis among HIV patients attending primary health care centers of Jos,Nigeria

ObjectiveTo determine the prevalence of trichomonal infection in HIV/AIDS and non-HIV control group of patients in a population of women with abnormal vaginal discharge.MethodsWe conducted a simple cross-sectional study. Primary health care centers in Jos metropolis and Jos University Teaching Hospital, during December 2006 to December 2007. Seven hundred high vaginal swabs were collected; 350 from HIV positive and another 350 from HIV-negative control group of patients with abnormal vaginal discharge attending primary health care centers in Jos metropolis and analysed for microscopy and culture in Jos University Teaching Hospital. Data on epidemiologic indices from the patients, using structured interviewer-administered questionnaires were collected.ResultsThe rate of trichomoniasis among all participants in the study was 17% (n=120/700). The prevalence rate of trichomoniasis among persons with HIV was 24% while it was found to be 10.3% among HIV negative controls. The difference was statistically significant (χ² =23.172; df=1; P<0.05). The rate of co-infection of Trichomonas vaginalis (T. vaginalis) in bacterial vaginosis was 42% (n=50/120), while it was 24% (n=29/120) in candidiasis. The singles had a 35% high rate of trichomonal infection. The infected women had a median age of 26 years, and a median number of 3 intra-vaginal sex partners per week.ConclusionsThere was a significant statistical difference in prevalence of T. vaginalis between HIV/AIDS group and non-HIV(control) group of patients in the study (P<0.05). Local HIV prevention strategies should target such women with trichomonal infection for intervention efforts, especially in HIV endemic area of sub-continent of Africa to further reduce the burden of HIV in the population.     

阿霉素致兔心脏毒性心肌细胞凋亡及相关基因bcl-2，bax蛋白表达变化

目的:观察不同剂量阿霉素心脏毒性心肌细胞凋亡情况及相关基因bcl-2,bax蛋白表达变化。方法:实验于2005-06/2006-08在大连医科大学附属第二医院实验中心完成。选用健康新西兰纯种白兔42只,按随机数字表法分成4组:①对照组(n=10),给予2mL/kg的生理盐水静脉注射,1次/周,共8周。②阿霉素4mg/kg组(n=10),给予阿霉素2mg/kg,以生理盐水稀释耳缘静脉注射,1次/周,共2周。③阿霉素8mg/kg组(n=10),同样方法给予阿霉素,共4周。④阿霉素16mg/kg组(n=12),同样方法给予阿霉素,共8周。12周后麻醉处死兔,取心肌组织,应用原位末端标记法标记凋亡的心肌细胞;应用免疫组织化学法检测bcl-2,bax蛋白的表达,以平均吸光度表达。结果:阿霉素16mg/kg组兔死亡3只,最后39只兔进入结果分析。①透射电镜观察结果:对照组、阿霉素4mg/kg组未见心肌细胞凋亡;阿霉素8mg/kg组和阿霉素16mg/kg组均观察到细胞核变小、核染色质浓缩、边聚的凋亡心肌细胞。②心肌细胞凋亡指数:对照组、阿霉素4mg/kg组未见心肌细胞凋亡;阿霉素8mg/kg组和阿霉素16mg/kg组心肌细胞凋亡指数显著高于对照组(P<0.01)。③心肌bcl-2与bax蛋白表达:阿霉素8,16mg/kg组bcl-2蛋白表达显著低于对照组(P<0.01),bax蛋白表达显著高于对照组(P<0.01),bcl-2/bax显著低于对照组(P<0.01)。阿霉素16mg/kg组bcl-2蛋白表达显著低于阿霉素8mg/kg组(P<0.01),bax蛋白表达显著高于阿霉素8mg/kg组(P<0.01)。与对照组相比,阿霉素4mg/kg组bcl-2,bax蛋白表达及bcl-2/bax无明显变化(P>0.05)。结论:阿霉素4mg/kg组可能因阿霉素剂量小未出现心肌细胞凋亡,阿霉素8,16mg/kg组可见典型凋亡心肌细胞,并且呈一定的量效关系,进一步说明细胞凋亡机制参与了阿霉素心脏毒性的病理过程,其作用与下调bcl-2基因的蛋白表达、上调bax基因的蛋白表达有关。     

平痛新素丸的处方设计及制备

目的：为制备平痛新包衣微丸提供良好的底物，方法：以流动性指数为指标采用均匀设计优化平痛新素丸。结果：确定了制备平痛新素丸的最佳处方工艺。结论：淀粉量是影响产率的主要因素：转速是影响堆密度，脆碎度的主要因素；粘合剂用量是影响休止角和流动性的主要因素；滚动时间是影响喷流指数的主要因素。     

三尖杉属植物中生物碱的研究——Ⅷ.二种新的抗癌三尖杉酯碱生物碱的结构和半合成

从安徽产三尖杉(Cephalotaxusfortunei Hook f.)弱碱中分到二种新的抗癌生物碱,命名为新三尖杉酯碱(neoharringonine,1)和脱水三尖杉酯碱(anhydroharringtonine,2)。从本种植物中还首次分到二个已知生物碱:脱氧三尖杉酯碱(deoxyharringtonine,3)和异三尖杉酯碱(isoharringtonine,4)。