Development and applications of photo-triggered theranostic agents

Theranostics, the fusion of therapy and diagnostics for optimizing efficacy and safety of therapeutic regimes, is a growing field that is paving the way towards the goal of personalized medicine for the benefit of patients. The use of light as a remote-activation mechanism for drug delivery has received increased attention due to its advantages in highly specific spatial and temporal control of compound release. Photo-triggered theranostic constructs could facilitate an entirely new category of clinical solutions which permit early recognition of the disease by enhancing contrast in various imaging modalities followed by the tailored guidance of therapy. Finally, such theranostic agents could aid imaging modalities in monitoring response to therapy. This article reviews recent developments in the use of light-triggered theranostic agents for simultaneous imaging and photoactivation of therapeutic agents. Specifically, we discuss recent developments in the use of theranostic agents for photodynamic-, photothermal- or photo-triggered chemotherapy for several diseases.     

B3GNT2, a Polylactosamine Synthase,Regulates Glycosylation of EGFR in H7721 Human Hepatocellular Carcinoma Cells

The epidermal growth factor receptor (EGFR) is an important surface receptor with N-glycans in itsextracellular domain, whose glycosylation is essential for its function, especially in tumor cells. Here, wedemonstrated that polylactosamine is markedly increased in H7721 hepatocellular carcinoma cells after treatmentwith EGF, while it apparently declined after exposure to all-trans retinoic acid (ATRA). In the study of theenzymatic mechanism of this phenomenon, we explored changes in the expression of poly-N-acetyllactosamine(PLN) branching glycosyltransferases using RT-PCR. Among the four glycosyltransferases with alteredexpression, GnT-V was most elevated by EGF, while GnT-V and B3GNT2 were most declined by ATRA. Next,we conducted co-immunoprecipitation experiments to test whether B3GNT2 and EGFR associate with eachother. We observed that EGFR is a B3GNT2-targeting protein in H7721 cells. Taken together, these findingsindicated that the altered expression of B3GNT2 will remodel the PLN stucture of EGFR in H7721 cells, whichmay modify downstream signal transduction.     

蒙药格根滴眼剂的工艺研究

目的：对蒙药格根滴眼剂（简称GNT）进行工艺研究，并初步探讨其稳定性。方法：1．利用正交设计实验，以盐酸小檗碱和藏红花甙-1为考察指标，筛选出最佳工艺条件；2．利用ZTCl＋1天然澄清剂调节药液的澄明度；3．通过简单药理实验，筛选药液初步浓度；4．利用pH值和渗透压的检测，筛选辅料。结果：黄柏提取工艺的正交实验L9（3^4）结果分析，加10倍量蒸馏水提取3次，每次30min；藏红花提取工艺的正交实验L9（3^4）结果分析，加14倍量蒸馏水，在60℃条件下，提取2次，每次1．5h浸泡；ZTCl＋1天然澄清剂的澄清条件为，先用6％的B组份处理后，再用3％的A组份澄清剂处理；在家兔眼结膜微循环的影响实验表明，与对照组比较，GNT的大、中、小剂量组和可的松眼药水组都有显著性差异（P〈0.05），与可的松眼药水组比较，GNT的大剂量组有明显性差异（P〈0．05），与小、中剂量组无显著性差异，GNT的小、中、大剂量组之间比较，无显著性差异，根据药理实验，定为中荆量浓度，即黄柏、藏红花浓缩液各1mL，熊胆、牛黄各1g加100mL注射用水；经GNT药液的测定，pH值为6—7之间较稳定，平均渗透压的-0．24，配置等渗溶液需加5％NaCl。结论：对蒙药GNT指定出初步的工艺指标，为今后的研究奠定了基础。     

β1,3-乙酰葡萄糖胺转移酶3在非小细胞肺癌中的表达及其临床意义

目的 探讨β1,3-乙酰葡萄糖胺转移酶3（β1,3-N-acetylglucosaminyltransferase-3, B3GNT3）在非小细胞肺癌（non-small cell lung cancer, NSCLC）组织中的表达及其临床意义。方法 通过在线TCGA数据库分析B3GNT3基因的表达;Western blot法及免疫组织化学法检测60例NSCLC组织及22例正常肺组织中B3GNT3蛋白的表达情况,分析B3GNT3蛋白表达与NSCLC患者临床病理特征及预后之间的关系。结果 NSCLC患者组织中B3GNT3基因和蛋白表达明显高于正常肺组织,差异有统计学意义（P<0.01）。B3GNT3蛋白表达与NSCLC患者的年龄、性别、吸烟情况、种族、TNM分期均无明显关系（P>0.05）。B3GNT3高表达组患者生存期明显短于B3GNT3低表达组患者（P<0.05）。结论 B3GNT3蛋白在NSCLC组织中高表达,且其表达高低与NSCLC患者预后有关。     

The SPPL3-Defined Glycosphingolipid Repertoire Orchestrates HLA Class I-Mediated Immune Responses

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蒙药格根滴眼剂对兔眼刺激性的试验

目的：观察不同浓度格根滴眼剂（简称GNT）对兔眼睛的刺激反应。方法：观察3.72mg/kg、2.48mg/kg、1.24mg/kg浓度格根滴眼剂及生理盐水对正常兔眼的刺激性。20只兔随机分成4组,每组5兔10眼,4次/d滴眼,每次50μL,连续10d。于滴眼后1d、2d、4d、6d、8d、10d,用裂隙灯观察兔眼结膜、角膜、虹膜的刺激反应并评分。结果：双眼结膜无充血、水肿、分泌物,角膜透明,无浑浊,虹膜纹理清晰。眼刺激反应评分为0,属无刺激性物质。结论：格根滴眼剂对兔眼无刺激性。