FRu（phen）2（3，8—2R—phen）-]^2＋（R=OH，H，F）电子结构与抗癌活性研究

用密度泛函(DFT)法，对配合物[Ru(phen)2(3，8-2R—phen)^2 (R=OH，H，F)进行了理论计算研究。探讨了配合物的电子结构与其抗癌活性的关系：主配体上3，8位上F原子的取代有利于配合物与DNA的作用，增加配合物的抗癌活性。计算结果能较好地预测配合物与DNA的作用强度、抗癌活性及指导具有较高抗癌活性配合物的合成。     

苄胺衍生物的Cu（Ⅱ）配合物研究

设计了合成了以苄胺的缩氨基硫脲衍生物为配体的两种Ｃｕ配合物，通过元素分析，红外光谱确证了其结构，并对两种配合物的抑制活性进行了测试，结果表明，两种配合物对所试细菌都有不同程度的抑制活性。     

双取代乙二胺金属配合物的合成及抗菌活性

目的 设计合成一系列双取代乙二胺过渡金属配合物并寻找抗菌活性药物。方法以N，N’-双取代乙二胺为配体合成过渡金属配合物，并进行体外抑菌活性筛选。结果合成了6个(Ⅲ1-6)新配合物，其结构经红外光谱、元素分析确证。结论初步抑菌实验表明，合成的配合物对多种菌株有明显的抑制活性，有进一步研究的价值。     

二叔丁基二氯化锡配合物的合成,表征和抗癌活性研究

本文合成了三种未见文献报道的二叔丁基二氯化锡配合物，利用红外光谱、核磁共振氢谱等对这些配合物进行了表征，体外抗癌活性筛选表明这些配合物抗Ｅｈｒｌｉｃｈ腹水癌活性优于阿克拉霉素Ａ。     

2-乙酰噻吩吖嗪及其过渡金属配合物的合成与活性

目的 研究2-乙酰噻吩吖嗪及其过渡金属Cu^2 ，Fe^3 配合物的合成与生物活性。方法 从2-乙酰噻吩和水合肼出发合成2-乙酰噻吩吖嗪，进而合成了其过渡金属Cu^2 ，Fe^3 的配合物。用MS，^1H—NMR对配体进行了确认。通过元素分析、摩尔电导率、红外光谱、紫外光谱等手段对配合物进行了表征。用NBT法研究了配合物对超氧阴离子自由基的抑制作用；并利用MTT法和SRB法对其进行了抗肿瘤活性体外筛选实验。结果 发现配体和配合物都具有一定的生物活性，且Cu配合物活性较好。结论 配合物的生物活性可能与中心离子的最外层d轨道的电子结构有关。     

橙皮素微量元素配合物的合成及其生物活性研究

目的 合成橙皮素钙、铁、硒、锌、铬配合物5种中药新药，并研究其抗菌、抗肿瘤活性和清除自由基的能力。方法 在碱性条件下通过合成得到橙皮素钙、铁、硒、锌、铬配合物，采用倍比稀释法测定橙皮素及其配合物对大肠杆菌等8种菌的抑制活性，采用MTT法测定橙皮素及其配合物对Tca-8113等6种肿瘤细胞增殖的影响，采用超氧阴离子自由基清除法测定橙皮素及其配合物对超氧阴离子自由基的清除能力。结果 合成的5种配合物配位比均为2∶1（橙皮素∶微量元素），产率均>70%，小鼠急性毒性试验显示5种配合物均无明显毒性，5种配合物最小抑菌浓度均低于橙皮素，抗菌活性至少提升至1~4倍；5种配合物对肿瘤细胞的IC₅₀均小于橙皮素，抗肿瘤活性至少提升至1.19~2.41倍；橙皮素及其配合物对超氧阴离子自由基均有一定的清除作用，且均呈浓度依赖性，配合物对超氧阴离子自由基的清除率均高于橙皮素。结论 5种橙皮素微量元素配合物的抗菌、抗肿瘤活性和自由基清除能力均强于橙皮素。     

姜黄素-钌配合物的合成和抗氧化活性研究

目的合成和表征了姜黄素-钌金属配合物,并对其抗氧化活性进行初步的研究。方法以姜黄素为配体合成其钌的配合物,用红外光谱、紫外光谱、元素分析对配合物进行了表征,并进行抗氧化活性初步筛选。结果合成了姜黄素-钌的金属配合物,并确定其结构。结论活性筛选结果表明,配合物对自由基清除活性好于姜黄素。     

反式构型铂配合物抗癌药物研究进展

人们一直认为反式构型铂配合物无抗癌活性,但是,近来研究发现,一些反式构的铂型配合物显示了良好的抗癌活性。本文综述了这些配合物的结构、活性以及抗癌机理。     

炔基膦金（Ⅰ）配合物抗肿瘤活性研究进展

顺铂抗肿瘤活性的发现促使人们寻找新的金属配合物作为潜在的抗癌药物，其中金配合物作为抗癌药物的研究受到广泛关注。炔基膦金（Ⅰ）配合物引起的明显抗增殖作用源于其新的作用机制，同时由于其独特的化学性质和相关的配位方式，炔基膦金（Ⅰ）配合物作为未来以金为基础的抗癌药物成为该领域研究的热点之一。综述近年来炔基膦金（Ⅰ）配合物的抗肿瘤活性研究进展，包括炔基膦金（Ⅰ）配合物的结构特点、优化设计、协同药效和诊疗活性等，以期为相关研究和应用提供参考。     

稀土盐及其配合物对芽孢菌的抑菌活性的影响

目的 以稀土氧化物为原料，合成系列稀土盐及其配合物，并研究它们对芽孢菌的抑菌作用规律。方法 采用了滤纸片法、稀释法考察了多种稀土盐及其配合物对多种芽孢菌、普通革兰氏阳性细菌及普通革兰氏阴性细菌的抑菌活性；并用透射电镜观察了芽孢的形态及超微结构变化。结果 稀土盐类及其配合物抑菌性强、抑菌谱广，对生命力强的芽孢菌显示了比对普通革兰氏阳性及阴性细菌更好的强抑菌效果；稀土配合物的抑菌效果较稀土盐更好；各种稀土盐类及其配合物对多种芽孢菌的抑菌活性差别不大；重稀土（Gd）抑菌效果略优于轻稀土(La,Nd,Eu）；不同配体合成的配合物对同一菌株的抑菌效果存在显著差异，这是由于抑菌活性与配合物的稳定性有关；采用透射电镜的负染色及超薄切片术，观测到稀土配合物对芽孢休眠体有直接的溶菌作用。结论 稀土配合物是一类对芽孢菌有特效的抑菌剂。     

2-羟基-4-甲氧基二苯甲酮合钴（Ⅲ）的合成及光谱性质

目的：羟基二苯甲酮类配合物的合成及光谱性质。方法：利用2-羟基-4-甲氧基二苯甲酮（HMBP）与氯化钴在乙醇—水体系中合成了2-羟基-4-甲氧基二苯甲酮合钴（）配合物M（MBP）3,利用元素分析、激光解析飞行时间质谱等进行了表征,并研究了配合物的红外光谱性质。结果：HMBP配体通过羰基氧及羟基氧原子与中心金属以3：1的比例形成配合物,与配合物红外特征吸收谱相比,配体的征吸收有明显改变,同时确定了Mk O的特征峰位置。结论：得到了稳定的配合物。     

Finding of polysaccharide-peptide complexes in Cordyceps militaris and evaluation of its acetylcholinesterase inhibition activity

Acetylcholinesterase (AChE) inhibition enhances learning and cognitive ability for treatment of Alzheimer’s disease. Polysaccharide–peptide complexes were identified in Cordyceps militaris (CPSPs) and characterized for their AChE inhibitory properties. Three polymers (CPSP-F1, -F2, and -F3) were extracted and separated by ultrasound-assisted extraction and dieth-ylaminoethanol (DEAE)–Sepharose CL-6B column chromatography. Polysaccharide–peptide complexes were identified by DEAE–Sepharose CL-6B column chromatography and high-performance gel-filtration chromatography, Fourier transform infrared spectra, amino sugar composition analysis, and β-elimination reaction to identify polysaccharide–peptide bond categories. Separation of CPSP can increase AChE inhibitory activity from the crude poly-saccharide of C. militaris. CPSP-F1 and CPSP-F2 exhibited half maximal inhibitory concentrations of 32.2 ± 0.2 mg/mL and 5.3 ± 0.0 mg/mL. Thus, we identified polysaccharide–peptide complexes from C. militaris and suggest CPSP has great potential in AChE inhibition bioassay.     

Binding studies of phloridzin with human serum albumin and its effect on the conformation of protein

In this study, the binding mode of phloridzin with human serum albumin (HSA) was established under physiological condition. The binding study is important to understand the pharmacokinetics and toxicity of phloridzin. The results proved the mechanism of fluorescence quenching of HSA by phloridzin was due to the formation of HSA-phloridzin complex. The binding constants, the number of binding sites and thermodynamic parameters were calculated. In addition, the alterations of HSA secondary structure in the presence of phloridzin were confirmed by the evidences from Fourier transform infrared (FT-IR), UV-visible absorption, circular dichroism (CD), synchronous and three-dimensional fluorescence spectroscopy. Alterations of protein conformation were observed with reduction of α-helix from 54% (free HSA) to 50% in the HSA-phloridzin complexes, indicating a partial protein unfolding. The distance between phloridzin and HSA was 3.74 nm according to fluorescence resonance energy transfer theory. In addition, the effects of common ions on the constants of HSA-phloridzin complex were also discussed.     

姜黄素金属配合物的合成、表征和抗肿瘤活性研究

目的:合成和表征了4个姜黄素的金属配合物,并对其抗肿瘤活性进行初步的研究.方法:以姜黄素为配体合成其乙酰丙酮氧钒、锌、铜、锡的配合物,用红外光谱、紫外光谱、元素分析对配合物进行了表征,并进行体外抗肿瘤活性初步筛选.结果:合成了4个姜黄素的金属配合物,并确定其结构.结论:药理活性筛选结果表明,多个配合物对肿瘤K562,HL-60细胞有效,部分配合物显示了较强的抗癌活性.     

胆舒软胶囊的振动光谱分析

目的:建立鉴别中药材及其制剂中组分的分子振动光谱方法.方法:采用拉曼光谱法和红外光谱法鉴别胆舒软胶囊及对照品,测定胆舒胶囊中的薄荷素油的量,结果与气相法进行比较.结果:无论红外光谱还是拉曼光谱,胆舒软胶囊所呈现的峰均比对照品峰为多,但不干扰薄荷素油峰的鉴别,比较胆舒软胶囊和薄荷素油光谱,可快速鉴别胆舒软胶囊真伪.结论:建立的鉴别方法简便、快速、专属性强,灵敏度高.     

芍药苷磷脂复合物的制备及表征

目的制备芍药苷磷脂复合物并对复合物进行表征。方法采用溶剂法制备芍药苷磷脂复合物,以复合物的得率为指标,采用单因素法优化制备工艺;并以紫外、红外光谱分析表征复合物的形成。结果采用无水乙醇为反应溶剂,药物与磷脂的比例为1∶2,溶剂用量为反应物质的质量浓度为100 g/L,40℃,反应4 h,为复合物的最佳制备工艺,复合物的平均得率为(89.42±2.24)%(n=3);紫外光谱,红外光谱表征新复合物的形成。结论芍药苷与磷脂发生相互作用,反应生成了新的复合物。     

Antitumoral activity of non-platinum xanthate complexes

To establish structure-activity relationships, derivatives of bis(O-alkyldithiocarbonato)platinum(II) complexes were analyzed. Eighteen bis(O-alkyldithiocarbonato) metal complexes were synthesized, and their cytotoxic activity on two human cancer cell lines was compared with the corresponding platinum bis(O-alkyldithiocarbonato) complexes and cisplatin. Complexes were synthesized with palladium, gold, nickel, copper, rhodium, and bismuth. Palladium and bismuth complexes were found to display significant cytotoxic activity. Palladium complexes were most active with up to 10-fold lower IC50 values as compared with the corresponding platinum complexes. The other complexes were only poorly active. Palladium, bismuth, and nickel complexes were more active at pH 6.8 than at pH 7.4. This difference in activity was most pronounced with palladium complexes. A pH of 6.8 and lower has been frequently found in solid tumors. Drugs with such pH dependent activity are supposed to have an improved therapeutic index as compared to drugs that are active irrespective of pH.     

醛酮类药用辅料的振动光谱分析

目的:建立醛酮类药用辅料的拉曼光谱分析方法。方法:采集了几种醛酮类药用辅料的红外光谱和拉曼光谱,分别归属其振动光谱峰并分析比较光谱差异与结构之间的关系。结果:和红外光谱一样,拉曼光谱可以给出关于化合物结构的指纹信息,并可和红外光谱相互补充佐证。结论:建立的方法快速、简便、专属性强,可用于醛酮类药用辅料的鉴别。     

Enhancement of polyethylene glycol (PEG)-modified cationic liposome-mediated gene deliveries: effects on serum stability and transfection efficiency

In this study, we modified cationic liposomes either by polyethylene glycol (PEG)-grafting or PEG-adding methods, and compared the physical properties of transfection complexes and transfection efficiency in-vitro and prolonged circulation in-vivo. The PEG-grafted transfection complexes were prepared by mixing plasmid DNA with PEG-grafted cationic liposomes, which were composed of DSPE-PEG 2000 and cationic lipids. The PEG-added transfection complexes were prepared by adding DSPE-PEG 2000 to the mixture of cationic liposomes and plasmid DNA. The particle sizes of the PEG-modified transfection complexes (approximately 200 nm) changed a little over 4 weeks compared with the conventional transfection complexes. In the presence of serum, the transfection efficiency of the conventional transfection complexes was lowered whereas the transfection efficiency of the PEG-modified transfection complexes was maintained. Moreover, the transfection efficiency of the conventional transfection complexes was significantly reduced when they were stored. However, the transfection efficiency was stable for the PEG-modified transfection complexes, even after two weeks of storage. Of the in-vitro transfection efficiencies, there was no difference between PEG-grafted and PEG-added transfection complexes. When the conventional, PEG-grafted, and PEG-added transfection complexes were administered into mice by the tail vein, the PEG-added transfection complexes showed a prolonged circulation of plasmid DNA compared with other transfection complexes. These results suggest that the PEG-added transfection complexes could be a useful non-viral vector because of their simplicity in preparation, enhanced stability and prolonged circulation compared with the conventional transfection complexes.