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71.
苯并二氢吡喃腙衍生物的合成及其初步药理活性 总被引:4,自引:0,他引:4
为进一步筛选活性更强、副作用更小的抗绝经后骨质疏松症药物 ,在综合考察雷洛昔芬和异丙氧基异黄酮的基础上 ,设计合成一系列苯并二氢吡喃腙化合物 .化合物的结构均经波谱鉴定 ,并通过研究其对幼年小鼠子宫增重和血碱性磷酸酶活性的影响 ,初步考察化合物的药理活性 .结果表明 ,XY990 2具有较弱的雌激素受体激动作用和一定的雌激素受体拮抗作用 ,并有助于成骨细胞增殖 ,对治疗骨质疏松症是有利的 . 相似文献
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Adama Dnou Adiaratou Togola Kari Tvete Inngjerdingen Nastaran Moussavi Frode Rise Yuan Feng Zou Dalen G. Dafam Elijah I. Nep Abubakar Ahmed Taiwo E. Alemika Drissa Diallo Rokia Sanogo Berit Smestad Paulsen 《Pharmaceutical biology》2022,60(1):1278
ContextGlobal studies on Argemone mexicana L. (Papaveraceae) traditionally used against malaria in Mali are limited to its low-mass compounds activities, and little information on its bioactive polysaccharides is available.ObjectiveThis study determines the structure and the immunomodulatory activity of polysaccharides from aerial parts of A. mexicana.Materials and methodsAcidic polysaccharides from this plant material named HMAmA1 and HMAmA2 were isolated from water extracts. Their monosaccharide composition was determined by gas chromatography. Glycosidic linkages were determined using GC-MS. NMR was also applied. The polymers were tested for effects on the human complement system in vitro at different doses.ResultsThe monosaccharide composition showed that the two polysaccharides contained in different amounts the following monomers: arabinose, rhamnose, galactose, and galacturonic acid. Overall structural analysis showed the presence of a low ratio of 1,2-linked rhamnose compared to 1,4-linked galacturonic acid with arabinogalactans substituted on position 4 of rhamnose. NMR data showed the presence of galacturonans alternated by rhamnogalacturonans bearing arabinose and galactose units. α-Linkages were found for l-arabinose, l-rhamnose and d-galacturonic acid, while β-linkages were found for d-galactose. The two polysaccharides exhibited strong complement fixation activities, with HMAmA1 being the highest potent fraction. ICH50 value of HMAmA1 was 5 µg/mL, compared to the control BPII being 15.9 µg/mL.Discussion and conclusionsPolysaccharides form A. mexicana presented a complement fixation effect. The complement system is an important part of the immune defense, and compounds acting on the cascade are of interest. Therefore, these polymers may be useful as immunodulatory agents. 相似文献
75.
The primary plasma cell leukemia (pPCL) is a rare but aggressive variant of multiple myeloma (MM). Few studies have focused on the differences in the causes of death between pPCL and MM. This study aimed to compare and evaluate the causes of death of patients with pPCL and MM.The data were collected from the Surveillance Epidemiology, and End Results (SEER) database. The demographic characteristics, survival, and causes of death in pPCL and MM patients were evaluated and compared. The competing risk regression model was performed to predict the cause of death.Between 1975 and 2009, the overall mortality rate was 96.13% and 88.71% for pPCL and MM, and the median survival was 9 and 26 months, respectively. In pPCL, leukemia caused 45.05% of the deaths, followed by myeloma (38.83%). In MM, myeloma was the leading cause of death, accounting for 74.89% of the deaths. Older age at diagnosis was a risk factor for dying of leukemia in pPCL patients (HR = 1.49, 95% CI: 1.16–1.91), while older age at death was associated with reduced risk (HR = 0.67, 95% CI: 0.52–0.86). Although the survival of pPCL patients increased with time periods of diagnosis since 1975 to 2009, the risk of dying of leukemia increased with the periods. For MM, most of the demographic characteristics were found to have independently predicting influence on the cause of death.Patients with pPCL and MM had distinct causes of death. Leukemia was the leading and the most serious cause of death in pPCL patients. The demographic factors could not predict the causes of death in pPCL. More large-scale and multi-center studies are needed to evaluate the effect of novel agents in pPCL patients, especially for patients who have progressed to leukemia. 相似文献
76.
目的 探讨优化镇静镇痛策略指导下程序化护理在重症加强治疗病房(ICU)机械通气患者中的应用效果。方法 选取2019年1月至2021年1月广东药科大学附属第二医院云浮市中医院重症医学科ICU收治的100例行机械通气患者作为研究对象,采用随机数字表法分为研究组(50例)与对照组(50例)。对照组采用ICU常规护理,研究组采用优化镇静镇痛策略指导下程序化护理。比较两组患者的机械通气时间及ICU护理时间,观察干预前、干预3 d后的镇静镇痛状态,记录ICU治疗结束时的肌力情况及不良事件发生情况(谵妄、跌倒、坠床、非计划拔管、血氧饱和度下降)。结果 研究组的机械通气时间、ICU护理时间短于对照组,差异有统计学意义(P<0.05);干预后两组的镇静镇痛评分低于干预前(P<0.05),且研究组的镇静镇痛评分低于对照组,差异有统计学意义(P<0.05);研究组ICU治疗结束时的医学研究委员会(MRC)肌力评分、ICU获得性肌无力(ICU-AW)发生率低于对照组,差异有统计学意义(P<0.05);研究组的不良事件总发生率(4.00%)低于对照组(20.00%),差异有统计学意义(P... 相似文献
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目的探讨复方樟柳碱颞浅动脉旁皮下注射治疗视神经挫伤的疗效。方法20例(22只眼)视神经挫伤患者为治疗组,采用复方樟柳碱2ml患侧颞浅动脉旁皮下注射,每日1次,每疗程14d,3个疗程。另18例(20只眼)视神经挫伤患者为对照组,除不加用复方樟柳碱外,其他用药同治疗组疗效观察指标为视力、视野。结果治疗组总有效率为86%,对照组为45%.两组比较具有显著的统计学差异(P〈0.05)。结论颞浅动脉旁皮下注射复方樟柳碱注射液治疗视神经挫伤有明显疗效,且毒副作用小,安全性高,值得临床推广应用。 相似文献
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目的:测定脓毒血症鼠Peyer小结内滤泡辅助性T细胞(T follicular helper,Tfh)的变化,分析地塞米松(dexamethasone,Dex)对脓毒血症Tfh细胞的可能作用。方法:昆明小鼠诱导脓毒血症模型,模型诱导成功后随机分2组,脓毒血症组(SE组,n=12)、脓毒血症+Dex处理组(DE组,n=12)。另设对照组(NC组,n=12)。测定血清白介素-6(interleukin-6,IL-6)、降钙素原(procalcitonin,PCT)、中性粒细胞明胶酶相关载脂蛋白(neutrophil gelatinase-associated lipocalin,NGAL)水平。Peyer小结Ⅰ型1-磷酸鞘氨醇(Sphingosine 1-Phosphate 1,S1P1)、CXC趋化因子配体13(CXC chemokine ligand 13,CXCL13)免疫组化染色。Western blot分别检测Peyer小结IL-21、程序性死亡分子-1(programmed death 1,PD-1)、胞嘧啶脱氨酶(enzyme activation-induced cytidine deaminase,AID)蛋白的表达。流式细胞仪测定3组Peyer小结Tfh细胞占T淋巴细胞的百分率。结果:与NC组相比,SE组血清IL-6(19.7±5.20 vs 10.7±3.60 ng·L~(-1))、PCT(1.56±0.92 vs 0.31±0.09μg·L~(-1))、NGAL(0.44±0.11 vs 0.35±0.09 mg·L(-1))升高(P〈0.05或0.01),Peyer小结S1P1(0.22±0.06 vs 0.14±0.04)、CXCL13(0.25±0.07 vs 0.15±0.04)的表达增加(P〈0.01),IL-21(0.60±0.08 vs 0.35±0.08)、PD-1(0.30±0.04 vs 0.20±0.05)、AID(0.23±0.05 vs 0.18±0.03)蛋白的表达亦升高(P〈0.05或0.01),Tfh细胞占T淋巴细胞(8.30±2.00 vs 5.69 vs 1.64%)的百分率升高(P〈0.01)。Dex治疗可降低SE鼠血清IL-6(19.7±5.20 vs 12.8±3.40 ng·L~(-1))、PCT(1.56±0.92 vs 0.71±0.44μg·L~(-1))水平(P〈0.05或0.01),降低Peyer小结S1P1(0.22±0.06 vs 0.17±0.05)、CXCL13(0.25±0.07 vs 0.19±0.06)的表达(P〈0.05或0.01),下调Peyer小结IL-21(0.60±0.08 vs 0.48±0.09)、PD-1(0.30±0.04 vs 0.26±0.06)、AID(0.23±0.05 vs0.19±0.04)蛋白的表达(P〈0.05),降低Tfh细胞占T淋巴细胞(8.30±2.00 vs 6.56±1.59%)的百分率(P〈0.05)。结论:Peyer小结Tfh细胞可能参与脓毒血症的发病机制,Dex抑制Peyer小结Tfh的活化,对Peyer小结微环境起保护作用。 相似文献