温敏性凝胶的合成与药物缓释模拟

通过自由基聚合法合成了聚（N－异丙基丙烯酰胺）一无水凝胶和聚（N－异丙基丙烯酰胺－丙烯酸）二元水凝胶，用溶胀法探讨了温度，pH有原料组分等因素对凝胶性能的影响，实现发现：一元水凝胶体系与其线性聚合物一样，具有明显的相转变温度（LCST), 与差示扫描量热法（DSC）结果一致；二元水凝胶的LCST随丙烯酸的含量的增加而上升，而碱性条件下的溶胀性能远远优于酸性条件，Lin选出一适合配方并在模拟人体体温（37℃）和胃肠液pH值的条件下进行了药物（阿司匹林）缓释实验，发现以凝胶颗粒为药物载体，能更好地达到药物长期有效释放的目的。     

流体动力粘度对液封液桥内Marangoni对流的影响

建立了具有液封的液桥(不相溶混的双层同轴液柱)内的Marangoni对流的物理模型和数学模型.采用涡量-流函数法用有限差分格式对微重力条件下具有液封的液桥内Marangoni对流进行了数值模拟,得到了双层液柱主流区的温度场和流场,找出了内、外层流体动力粘度之比对双层同轴液柱内的热毛细对流的作用规律.     

LSP1抑制万珂诱导的多发性骨髓瘤细胞凋亡(英文)

淋巴细胞特异性蛋白-1(LSP1)在部分多发性骨髓瘤中表达升高,但其在肿瘤中的作用仍知之甚少.研究了LSP1在多发性骨髓瘤中抗新型抗肿瘤药物万珂(Bortezomib)诱导细胞凋亡的作用及机制.筛选LSP1高表达和低表达的多发性骨髓瘤细胞IM9和KAS6作为实验模型.应用RNA干扰基因沉默IM9细胞中的LSP1,或在KAS6细胞中转染LSP1表达质粒,用Bortezomib等化疗药物处理细胞后,PI/Annexin V染色并用流式细胞仪检测和分析细胞凋亡率.同时RT-PCR方法检测和分析被LSP1所影响的重要细胞凋亡相关基因的变化.结果发现,LSP1在多发性骨髓瘤细胞IM9和KAS6中差异性表达高和低,与Bortezomib诱导的细胞凋亡效率密切相关.利用RNA干扰敲低IM9细胞中LSP1,可显著增强IM9对Bortezomib的敏感性,同时在KAS6中转染LSP1表达质粒,可降低Bortezomib诱导的细胞凋亡.对部分重要凋亡基因的RT-PCR检测发现,LSP1可诱导BCL-xl基因表达,同时抑制p53表达.因此,发现LSP1可通过调节凋亡基因的表达促进肿瘤的抗药性.     

中国稀土药物研究进展

综述了近10年来中国在稀土药物合成和药理作用方面的研究进展及发展趋向。研究现状反映出：参与药物合成的配体以杂环化合物类为主，稀土元素以镧、镨、钕、钐为多；药理作用研究主要表面在抗肿瘤、抗突变、抗菌、抗病毒以及对消化系统和内分泌系统的影响等方面。     

红细胞作为吗啡载体延长吗啡镇痛时效的研究

探讨用高渗法制备红细胞包蔽吗啡溶液(RBG—M)的可行性。对RBC—M制备过程中红细胞(RBC)的体积和形态的变化、RBG—M溶液内外的吗啡(M)浓度及含量的变化以及择期上腹部手术患应用RBC—M溶液术后镇痛的时效和吗啡的血药浓度进行了研究。研究发现：(1)用高渗法制备红细胞包蔽吗啡溶液是可行的。(2)RBG—M溶液与单纯M溶液相比其术后镇痛作用显延长；其药代动力学指标消除半衰期(T1／2)延长3倍多。曲线下面积(AUC0→∞)增加约11倍。而清除率(CL)明显减小约9倍。(3)用RBGM溶液行术后镇痛的患其时效明显优于单纯用吗啡的患。     

Anti-Inflammatory Effects of Spiramycin in LPS-Activated RAW 264.7 Macrophages

Drug repurposing is a simple concept with a long history, and is a paradigm shift that can significantly reduce the costs and accelerate the process of bringing a new small-molecule drug into clinical practice. We attempted to uncover a new application of spiramycin, an old medication that was classically prescribed for toxoplasmosis and various other soft-tissue infections; specifically, we initiated a study on the anti-inflammatory capacity of spiramycin. For this purpose, we used murine macrophage RAW 264.7 as a model for this experiment and investigated the anti-inflammatory effects of spiramycin by inhibiting the production of pro-inflammatory mediators and cytokines. In the present study, we demonstrated that spiramycin significantly decreased nitric oxide (NO), interleukin (IL)-1β, and IL-6 levels in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Spiramycin also inhibited the expression of NO synthase (iNOS), potentially explaining the spiramycin-induced decrease in NO production. In addition, spiramycin inhibited the phosphorylation of mitogen-activated protein kinases (MAPKs); extracellular signal-regulated kinase (ERK) and c-Jun N terminal kinase (JNK) as well as the inactivation and subsequent nuclear translocation of nuclear factor κB (NF-κB). This indicated that spiramycin attenuates macrophages’ secretion of IL-6, IL-1β, and NO, inducing iNOS expression via the inhibition of the NF-κB and MAPK signaling pathways. Finally, we tested the potential application of spiramycin as a topical material by human skin primary irritation tests. It was performed on the normal skin (upper back) of 31 volunteers to determine whether 100 μM and μM of spiramycin had irritation or sensitization potential. In these assays, spiramycin did not induce any adverse reactions. In conclusion, our results demonstrate that spiramycin can effectively attenuate the activation of macrophages, suggesting that spiramycin could be a potential candidate for drug repositioning as a topical anti-inflammatory agent.     

A Novel Gelatin-Based Sustained-Release Molluscicide for Control of the Invasive Agricultural Pest and Disease Vector Pomacea canaliculata

Pomacea canaliculata, one of the 100 most destructive invasive species in the world, and it is an important intermediate host of Angiostrongylus cantonensis. The molluscicides in current use are an effective method for controlling snails. However, most molluscicides have no slow-release effect and are toxic to nontarget organisms. Thus, these molluscicides cannot be used on a large scale to effectively act on snails. In this study, gelatin, a safe and nontoxic substance, was combined with sustained-release molluscicide and was found to reduce the toxicity of niclosamide to nontarget organisms. We assessed the effects of gelatin and molluscicide in controlling P. canaliculata snails and eggs. The results demonstrated that the niclosamide retention time with 1.0% and 1.5% gelatin sustained-release agents reached 20 days. Additionally, the mortality rate of P. canaliculata and their eggs increased as the concentration of the niclosamide sustained-release agents increased. The adult mortality rate of P. canaliculata reached 50% after the snails were exposed to gelatin with 0.1 mg/L niclosamide for 48 h. The hatching rate of P. canaliculata was only 28.5% of the normal group after the treatment was applied. The sustained-release molluscicide at this concentration was less toxic to zebrafish, which means that this molluscicide can increase the safety of niclosamide to control P. canaliculata in aquatic environments. In this study, we explored the safety of using niclosamide sustained-release agents with gelatin against P. canaliculata. The results suggest that gelatin is an ideal sustained-release agent that can provide a foundation for subsequent improvements in control of P. canaliculata.     

聚乳酸-聚扁桃酸共聚物的合成与表征

合成乳酸OCA和扁桃酸OCA单体,用DMAP引发乳酸OCA和扁桃酸OCA开环共聚合成可生物降解的聚乳酸-聚扁桃酸共聚物,通过调节聚合共聚单体的比例,可得到分子量从3 620¹1 800 g/mol不等的共聚物,实现了分子量可控的目的.使用1H NMR、GPC、DSC、TEM、XRD等手段对共聚物进行了表征,所得共聚物的热力学性能、降解性能等均得到改善.并对轮状病毒进行负载制备成载药微球,对其降解行为进行研究,为药物控制释放提供一类新的载体材料.     

自组装膜电极上烟酸的电化学行为及其分析应用

报道了烟酸在 2 -巯基苯并噻唑自组装膜修饰金电极 (MBT/SAM/Au)上的电化学行为 ,建立了新的测定烟酸的电分析方法。在 p H1 1 .92 B-R溶液中 ,烟酸在 MBT/SAM/Au上出现了两对氧化还原峰 ,对应的氧化还原峰电位为 Epa,1=-0 .0 40 V、Epa,2 =0 .5 0 9V、Epc,1=-0 .1 87V、Epc,2 =0 .1 66V;Epc,2 处的还原峰电流与烟酸的浓度在 2 .44× 1 0 -2 ～ 2 .44× 1 0 -7mol/L的范围内呈线性 ,检测限达 1 .2 2× 1 0 -7mol/L,方法用于片剂中烟酸含量的测定 ,结果令人满意