Synthesis of bis(amino)furans from biomass based 5-hydroxymethyl furfural

In this study we report a new reaction pathway in which the hydroxyl and the aldehyde groups of 5-hydroxymethyl furfural were aminated respectively. Hydroxyl group was aminated via Ritter reaction followed by direct reductive amination of aldehyde group. For the Ritter reaction of 5-hydroxymethyl furfural, mixture of trifluoromethane sulfonic acid and phosphoric anhydride showed good performance and the intermediate N-acyl-5-aminomethyl furfural with the highest yield of 89.1 wt% was obtained.Optimization of direct reductive amination of 2,5-bis（aminomethyl） furan was conducted and a yield of45.7 wt% was achieved. This study presents a simple way for preparing bis（amino）furans from renewable biomass based 5-hydroxymethyl furfural, which enriches the biorefinery concept from biomass.

Increased 5-hydroxymethylcytosine is a favorable prognostic factor of Helicobacter pylori-negative gastric cancer patients

BACKGROUND Most gastric cancer(GC)patients are diagnosed at middle or late stage because the symptoms in early stage are obscure,which causes higher mortality rates of GC.Helicobacter pylori(H.pylori)was identified as a class I carcinogen and leads to aberrant DNA methylation/hydroxymethylation.5-hydroxymethylcytosine(5-hmC)plays complex roles in gene regulation of tumorigenesis and can be considered as an activating epigenetic mark of hydroxymethylation.AIM To explore the association between 5-hmC levels and the progression and prognosis of GC patients with or without H.pylori infection.METHODS A retrospective cohort study was conducted to estimate the predicted value of 5-hmC level in the progression and prognosis of GC patients with different H.pylori infection status.A total of 144 GC patients were recruited.RESULTS The levels of 5-hmC were significantly decreased in tumor tissues(0.076±0.048)compared with the matched control tissues(0.110±0.057,P=0.001).A high level of 5-hmC was an independent significant favorable predictor of overall survival in GC patients(hazard ratio=0.61,95% confidence interval:0.38-0.98,P=0.040),the H.pylori-negative GC subgroup(hazard ratio=0.30,95% confidence interval:0.13-0.68,P=0.004)and the GC patients with TNM stage Ⅰ or Ⅱ(hazard ratio=0.32,95% confidence interval:0.13-0.77,P=0.011).CONCLUSION Increased 5-hmC is a favorable prognostic factor in GC,especially for H.pylori-negative subgroups.

校正因子法测定替硝唑葡萄糖注射液中5-羟甲基糠醛的含量

目的应用高效液相色谱法,测定5羟甲基糠醛对替硝唑的校正因子,并以该校正因子计算替硝唑葡萄糖注射液中5羟甲基糠醛的含量。方法ODS柱,以005mol·L1磷酸二氢钾溶液乙腈(75∶25)为流动相,检测波长为284nm。结果5羟甲基糠醛对替硝唑的校正因子为926;5羟甲基糠醛的平均回收率为1010%(n=5)、RSD为068%;5羟甲基糠醛对替硝唑的相对保留时间为055mol·ml-1。结论该方法简便,灵敏度高,重复性好。

Effects of 5-hydroxymethyl Furfural Extracted from Rehmannia Glutinosa Libosch on the Expression of Signaling Molecules Relevant to Learning and Memory among Hippocampal Neurons Exposed to High Concentration of Corticosterone

Objective：To determine the effects of 5-hydroxymethyl furfural（5-HMF）,an extract of Rehmannia glutinosa Libosch,on several down-regulated signaling molecules involved in learning and memory in hippocampal neurons.Methods：After cultured for 7 days,primary hippocampal neurons were divided into 5 groups：normal,corticosterone model,RU38486,5-HMF,and donepezil group.Neuron survival rates were calculated 24 h later using SYT013-P1 double-fluorescence staining and an 3-（4,5-Dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide（MTT）assay.β-galactosidase activity was also assayed.Protein expressed by the glucocorticoid receptor（GCR）,brainderived neurotrophic factor（BDNF）,and N-methyl-D-aspartate receptor 2B（NR2B）,as well as phosphorylationcyclic adenosine monophosphate（cAMP）response element binding protein（p-CREB）,phosphorylation-extracellular signal-regulated kinase（p-ERK）,and phosphorylation-synapsin（p-synapsin）were quantified with Western blot.Results：Hippocampal neuron survival rates and the above-mentioned proteins were dramatically decreased（P〈0.05）,β-galactosidase activity was significantly increased in the model group,but the effect was reversed by5-HMF,RU38486,and to a lesser extent by donepezil（P〈0.05）.Conclusion：5-HMF extracts from the Chinese herb Rehmannia glutinosa Libosch could protect hippocampal neurons from glucocorticoid injury and from down-regulated signaling molecules in the GCR-BDNF-NR2B-p-ERK-p-CREB-p-synapsin signal transduction pathway.

桂枝茯苓胶囊化学成分研究(Ⅱ)

目的对桂枝茯苓胶囊内容物正丁醇萃取部位化学成分进行研究。方法采用柱色谱技术进行分离纯化,利用理化性质及波谱方法鉴定化合物结构。结果共得到9个单体化合物,分别鉴定为5-羟甲基-糠醛(1)、芍药苷(2)、磺酸钠芍药苷(3)、芍药内酯苷(4)、1,2,3,4,6-O-五没食子酰葡萄糖(5)、野樱苷(6)、蔗糖(7)、麦芽糖(8)、去苯甲酰基芍药苷(9)。结论化合物1～9均为首次从该复方中得到。