术前经动脉化疗栓塞治疗婴儿肾母细胞瘤的疗效观察

目的探讨术前经动脉化疗栓塞治疗婴儿肾母细胞瘤的可行性。方法2009年6月至2014年5月收治6例婴儿单侧肾母细胞瘤,术前评估肿瘤手术一期切除困难,所有婴儿均行经导管肾动脉化疗栓塞,术后4周内行肿瘤根治性手术切除,记录并分析6例婴儿的治疗结果、并发症及随访结果。结果6例婴儿介入后肿瘤体积均缩小,平均缩小39.03%（23.95%~61.8%）,介入治疗总有效率达83.33%（5/6）;手术中瘤体完整切除率为100%,无肿瘤破溃及污染腹腔情况。手术后随访时间平均为42.8个月,无肿瘤复发、远处转移及死亡。结论术前经动脉化疗栓塞治疗婴儿巨大肾母细胞瘤是安全、有效的,能为一期手术切除困难的肾母细胞瘤患儿提供一种新的治疗模式。     

超声萃取结合超高效液相色谱法测定皮革中10种防霉剂

建立了皮革样品中10种防霉剂(氨基苯磺酰胺、苯并咪唑、BIT、MBT、IPBC、PCMC、水杨酰苯胺、OPP、TCMTB和OIT)的超高效液相色谱(UPLC)检测方法。样品经甲醇超声萃取,T3色谱柱分离后,甲醇和0.1%甲酸水为流动相梯度洗脱,二极管阵列检测器测定。在优化条件下,10种防霉剂在一定的浓度范围内线性关系良好,相关系数(r~2)均不小于0.999 3,除IPBC的方法定量下限(S/N=10)为190.0 mg/kg外,其余9种防霉剂的方法定量下限为4.0~8.0 mg/kg,平均回收率为81.3%~104.9%,相对标准偏差(RSD,n=6)为4.7%~11.2%。该方法前处理简单、分离效果好,适用于皮革样品中10种防霉剂的同时测定。     

超高效液相色谱-串联质谱法同时测定纺织品中4种苯并三唑类紫外稳定剂

建立了快速同时测定纺织品中UV-350,UV-320,UV-328和UV-327 4种苯并三唑类紫外稳定剂(BUVSs)的超声提取/超高效液相色谱-串联质谱(USE-UPLC-MS/MS)分析方法。样品经正己烷饱和的乙腈超声波提取后,采用Eclipse Plus C18柱(2.1 mm×50 mm,1.8μm)分离,甲醇-0.01 mol/L甲酸铵水溶液为流动相梯度洗脱,电喷雾离子源电离,正离子多反应监测模式进行定性和定量分析,外标法定量。结果表明,4种BUVSs的线性相关系数(r2)均大于0.99,检出限为0.006 3~0.024 mg/kg,定量下限为0.021~0.081 mg/kg。加标回收率为80.0%~102.9%,相对标准偏差(RSD)为1.2%~9.9%。将该方法应用于纺织品中BUVSs的分析测定,结果令人满意。     

Nucleophilic Aromatic Substitution on Pentafluorophenyl‐Substituted Dipyrranes and Tetrapyrroles as a Route to Multifunctionalized Chromophores for Potential Application in Photodynamic Therapy

The application of porphyrinoids in biomedical fields, such as photodynamic therapy (PDT), requires the introduction of functional groups to tune their solubility for the biological environment and to allow a coupling to other active moieties or carrier systems. A valuable motif in this regard is the pentafluorophenyl (PFP) substituent, which can easily undergo a regiospecific nucleophilic replacement (S_NAr) of its para‐fluorine atom by a number of nucleophiles. Here, it is shown that, instead of amino‐substitution on the final porphyrinoid or BODIPY (boron dipyrromethene), the precursor 5‐(PFP)‐dipyrrane can be modified with amines (or alcohols). These dipyrranes were transformed into amino‐substituted BODIPYs. Condensation of these dipyrranes with aldehydes gave access to trans‐A₂B₂‐porphyrins and trans‐A₂B‐corroles. By using pentafluorobenzaldehyde, it was possible to introduce another para‐fluorine atom, which enabled the synthesis of multifunctionalized tetrapyrroles. Furthermore, alkoxy‐ and amino‐substituted dipyrranes were applied to the synthesis of A₃B₃‐hexaphyrins. The polar porphyrins that were prepared by using this method exhibited in vitro PDT activity against several tumor cell lines.     

La(OTf)3-catalyzed,three-component synthesis of spiro[Indolo-3,10′-indeno[1,2-b]quinolin]-2,4,11′-triones in PEG-400 under conventional heating and ultrasonic irradiation

An efficient La(OTf)₃-catalyzed three-component reaction has been developed for the synthesis of highly substituted spiro[indolo-3,10′-indeno[1,2-b]quinolin]-2,4,11′-triones in polyethylene glycol (PEG-400) under conventional heating and ultrasonic irradiation. The most exciting feature of this methodology is its mechanism involving the unusual ring opening of an isatin moiety followed by recyclization. All the reactions resulted in good yield of products. The important features of this reaction are use of green solvent, good yields, less reaction times, and recyclability of the catalyst.     

A Smart Photosensitizer–Manganese Dioxide Nanosystem for Enhanced Photodynamic Therapy by Reducing Glutathione Levels in Cancer Cells

Photodynamic therapy (PDT) has been applied in cancer treatment by utilizing reactive oxygen species to kill cancer cells. However, a high concentration of glutathione (GSH) is present in cancer cells and can consume reactive oxygen species. To address this problem, we report the development of a photosensitizer–MnO₂ nanosystem for highly efficient PDT. In our design, MnO₂ nanosheets adsorb photosensitizer chlorin e6 (Ce6), protect it from self‐destruction upon light irradiation, and efficiently deliver it into cells. The nanosystem also inhibits extracellular singlet oxygen generation by Ce6, leading to fewer side effects. Once endocytosed, the MnO₂ nanosheets are reduced by intracellular GSH. As a result, the nanosystem is disintegrated, simultaneously releasing Ce6 and decreasing the level of GSH for highly efficient PDT. Moreover, fluorescence recovery, accompanied by the dissolution of MnO₂ nanosheets, can provide a fluorescence signal for monitoring the efficacy of delivery.     

Biodegradable Inorganic Nanovector: Passive versus Active Tumor Targeting in siRNA Transportation

The biodegradable inorganic nanovector based on a layered double hydroxide (LDH) holds great promise for gene and drug delivery systems. However, in vivo targeted delivery of genes through LDH still remains a key challenge in the development of RNA interference therapeutics. Here, we describe in vivo and in vitro delivery system for Survivin siRNA (siSurvivin) assembled with passive LDH with a particle size of 100 nm or active LDH conjugated with a cancer overexpressing receptor targeting ligand, folic acid (LDHFA), conferring them an ability to target the tumor by either EPR‐based clathrin‐mediated or folate receptor‐mediated endocytosis. When not only transfected into KB cells but also injected into xenograft mice, LDHFA/siSurvivin induced potent gene silencing at mRNA and protein levels in vitro, and consequently achieved a 3.0‐fold higher suppression of tumor volume than LDH/siSurvivin in vivo. This anti‐tumor effect was attributed to a selectively 1.2‐fold higher accumulation of siSurvivin in tumor tissue compared with other organs. Targeting to the tumor with inorganic nanovector can guide and accelerate an evolution of next‐generation theranosis system.     

Ultrasound mediated green synthesis of rhodanine derivatives: Synthesis,chemical behavior,and antibacterial activity

A variety of rhodanine derivatives were synthesized via a three-component reaction of carbon disulfide, amines, and dialkyl acetylenedicarboxylate in polyethylene glycol under conventional stirring or ultrasound irradiation. The sonochemical-assisted procedure provides an improved and accelerated conversion when compared to the conventional reaction, with increased rate of reaction and quality of product obtained. The product formed, 2a, could be readily converted to bis-rhodanine under microwave conditions. Moreover, the pyranothiazoles 9a,b were prepared from the corresponding rhodanines 2a,b and malononitrile. Fifteen compounds were screened for their antibacterial activities against nine human, animal and plant pathogenic Gram-positive and Gram-negative bacteria using the agar well diffusion method. Out of these derivatives, compounds 2g and 2h were the most effective against all tested bacteria.     

Highly enhanced phototoxicity of chlorin e6‐conjugated poly(β‐cyclodextrin) with gas forming capacity at an acidic tumor extracellular pH and its in vitro evaluation

In this study, we report a novel polysaccharidic drug conjugate consisting of poly(β‐cyclodextrin) [poly(β‐CD)] with gas‐forming carbonate linkages resulting from the chemical coupling of the hydroxyl groups of poly(β‐CD) and cholesteryl chloroformate (CC) and a photosensitizing drug (chlorin e6: Ce6). This drug conjugate was self‐assembled in aqueous solution leading to the production of nanoparticles containing the poly(β‐CD) on the hydrophilic outer shell and CC and Ce6 in the hydrophobic inner core. Cleavage (i.e. the detachment of CC moieties) of the carbonate linkage at a slightly acidic pH (~pH 6.5) produced carbon dioxide bubbles. More specifically, the nanoparticles (with autoquenched Ce6 molecules in their core at pH 7.4) were destabilized at pH 6.5, thereby dequenching the Ce6 molecules. These experimental results demonstrate that under light illumination the nanoparticles increased singlet oxygen generation at pH 6.5 compared to pH 7.4 and exhibited a higher phototoxicity for KB tumor cells at pH 6.5 compared to pH 7.4. This approach represents an effective photodynamic therapy for acidic tumors. Copyright © 2015 John Wiley & Sons, Ltd.