环磺酮原药中3个杂质结构的确定及其合成

采用文献中报道的环磺酮的合成工艺合成了环磺酮原药,通过高效液相色谱分析,发现其原药中含有3个质量分数分别大于0.1%的杂质;通过核磁共振氢谱 (1H NMR) 及高分辨质谱 (HRMS) 对3个杂质的结构进行了确证,同时进行了合成。根据合成工艺路线,对该杂质产生的途径进行了分析。     

Cover Image,Volume 75, Issue 6

The cover image is based on Research Article Field evaluation of an unmanned aerial vehicle (UAV) sprayer: effect of spray volume on deposition and the control of pests and disease in wheat by Guobin Wang et al., DOI: 10.1002/ps.5321 . Illustration Credit: Guobin Wang, Yubin Lan, and Yuxing Han.

     

Effect of FGFR1 expression knock-down on biological characteristics of infantile hemangioma endothelial cells

AIM: To study the effect of fibroblast growth factor receptor 1 (FGFR1) expression knock-down on the viability, apoptosis, invasion and migration of infantile hemangioma endothelial cells (HemECs). METHODS: FGFR1 was down-regulated by FGFR1 small interfering RNA (si-FGFR1) transfection. The viability of the cells was measured by CCK-8 assay. The apoptotic rate was analyzed by flow cytometry and the invasion and migration abilities were determined by Transwell assay. The protein levels of phosphatidylinositol 3-kinase (PI3K), protein kinase B (AKT), and phosphorylated AKT (p-AKT) were examined by Western blot. RESULTS: Transfection of si-FGFR1 into HemECs had significant effects on inhibiting cell viability (P<0.05), promoting apoptosis (P<0.05), and decreasing cell invasion and migration abilities (P<0.05). The results of Western blot showed that knockdown of FGFR1 gene expression in the cells reduced the protein levels of PI3K and p-AKT (P<0.05), and had no significant effect on AKT protein level. CONCLUSION: Knock-down of FGFR1 expression changes the biological characteristics of endothelial cells in infantile hemangiomas by regulating PI3K/AKT signaling pathway.     

Role of cytokeratin 8 on changes of intestinal epithelial permeability induced by corticotropin-releasing factor

AIM: To investigate the role of cytokeratin 8 (CK8) on the change of intercellular permeability of intestinal epithelial cells induced by corticotropin-releasing factor (CRF). METHODS: The expression levels of CRF receptor 1 (CRFR1) and CRFR2 on human colon adenocarcinoma HT29 cell surface were determined by immunofluorescence staining. After treatment with 100 nmol/L CRF for 72 h, the translocation of FITC-labelled dextran was measured in a Transwell chamber. The structural changes of tight junctions were observed under transmission electron microscope. The expression levels of CK8, and tight junction proteins ZO-1 and occludin were determined by Western blot. The activity of protein kinase C (PKC) was detected by ELISA. Furthermore, the effects of CRF on intestinal epithelial permeability were examined in CK8-silencing HT29 cells, which were constructed by infection with sh-CK8 lentivirus. RESULTS: CRF treatment increased the permeability of FITC-labelled dextran (P<0.05), caused the opening of tight junctions, and induced increased fluorescence intensity of CK8. The expression levels of occludin and ZO-1 were down-regulated (P<0.05). PKC activity was decreased at 1 h after CRF treatment (P<0.05). CRF-induced increase in the permeability and down-regulation of occludin were not blocked by CK8 silencing. Nevertheless,CK8 silencing blocked the effects of CRF regarding the decrease in the expression levels of ZO-1 and the increase in PKC activity (P<0.05). CONCLUSION: CK8 may be involved in CRF-induced increase in intestinal epithelial permeability by inhibiting the activity of PKC, and there may be other signaling pathways involved.     

Ethanol extract from Cortex Albiziae attenuates mouse acute liver injury induced by carbon tetrachloride via modulation of NF-κB pathway

AIM:To investigate the protective effect of ethanol extract from Cortex Albiziae on acute liver injury, and to explore its possible mechanism. METHODS:Acute liver injury in mice was induced by single intraperitoneal injection of 25% carbon tetrachloride (olive oil solubilization). The effective parts of ethanol extract from Cortex Albizziae against acute liver injury were screened. The pathological changes of the liver tissues were examined by pathological sections with HE staining. The activity of total superoxide dismutase (T-SOD) and the content of malondialdehyde (MDA) of the liver tissues were detected, the serum levels of interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) were mea-sured by ELISA, and the protein expression levels of NF-κB p65, Bcl-2 and Bax in the liver cells of the mice in each group were determined by Western blot. RESULTS:Compared with model group, the serum levels of AST and ALT in low-dose n-butanol phase of ethanol extract from Cortex Albiziae (AB-L, 4 mg·kg^-1·d^-1) group and high-dose n-butanol phase of ethanol extract from Cortex Albiziae (AB-H, 8 mg·kg^-1·d^-1) group were significantly decreased. The necrosis extent and degree of the hepatocytes and infiltration of inflammatory cells were significantly lower than that in model group. Compared with model group, the serum levels of TNF-α and IL-6 in AB-H group and AB-L group were significantly decreased (P<0.05). The protein level of NF-κB p65 in the nuclei of mouse liver cells in AB-H group and AB-L group were also decreased significantly (P<0.05). Compared with model group, the protein expression of Bax was decreased, the protein expression of Bcl-2 was increased, and the Bcl-2/Bax ratio was increased in AB-L group and AB-H group. CONCLUSION:The n-butanol phase of ethanol extract from Cortex Albiziae may protect the liver by reducing the activation of NF-κB p65, inhibiting the excessive release of inflammatory cytokines IL-6 and TNF-α, and decreasing hepatocyte apoptosis via regulating Bcl-2 and Bax expression.     

Cigarette dust particles induced lung function injury of chronic obstructive pulmonary disease in mice

AIM: To investigate the pathogenesis of chronic obstructive disease (COPD) in mice by using nasal drip of cigarette dust particles (DSP) induced pulmonary function damage model.METHODS: BALB/c mice were randomly divided into control group, LPS 100 mg/L group, DSP 0.75 mL/L group, DSP 1.5 mL/L group and DSP 3 mL/L group for 30 days. The method of nasal drip was used for 30 days to establish the COPD model. Rrs, Ers, Crs, Est, Cst, P-3/8Rn, P-3/8G and P-3/8H were measured for evaluating lung function of the mice in each group by the method of FlexiVent. The effect on the increase of airway resistance induced by methacholine (Mach) was determined using main bronchial rings by Myograph method. The HE, Masson and Resorcinol fuchsin staining of mouse tracheas and lung tissues were conducted. RESULTS: Continuous nasal drip with DSP for 30 days increased Rrs, Ers, Est, P-3/8Rn and decreased Crs, Cst, P-3/8G and P-3/8H in the mice. DSP significantly shifted the dose-effect curve of tracheal contraction induced by Mach to the left, increased the sensitivity of the airway to Mach, and significantly increased the maximal contractile airway effect of Mach. Exposure to DSP caused fibrosis of airway subepithelial, deposition of collagen in the airway basement membrane under the reticular plate, induced reticular plate thickening, pulmonary bronchial lumen serious deformation, and the inflammatory cell infiltration in the lung of mice. Significantly increased alveolar wall muscle fibers and collagen fibers were also observed. CONCLUSION: The lung function and pathomorphological changes of COPD mice induced by 30 days nasal drip of cigarette dust particles were similar to those of human COPD.     

张掖市塑料大棚春茬西瓜品种筛选试验

为获得张掖市塑料大棚春茬西瓜种植的最适品种,通过田间随机区组排列试验,对6个不同西瓜品种进行了比较试验。结果表明:在所有品种中,凯旋2012的光合速率与667m~2产量最高,分别为1.28μmol/(m~2·s)和6.91 t;不同品种产量的高低顺序为凯旋2012特大丰抗88天福2号西农8号丰抗八号(CK)好梦1号;各参试品种可溶性糖含量的大小顺序为丰抗八号(CK)西农8号凯旋2012特大丰抗88天福2号好梦1号;各参试品种番茄红素含量的大小顺序为丰抗八号(CK)凯旋2012特大丰抗88西农8号好梦1号天福2号。凯旋2012产量最高,可溶性糖和番茄红素含量较高,综合品质较好,适宜在河西走廊地区推广。     

紫斑牡丹种子发育期油脂合成积累的源汇基因协同表达

为研究紫斑牡丹种子油脂合成积累与相关基因(GPD1, DGAT1和DGAT2)表达间的关系,以四个不同发育期(6月20日, 7月7日, 7月17日和7月27日)的种子为材料,氯仿甲醇法测定种子含油率,实时荧光定量PCR方法分析基因的表达模式,分析相关基因在不同发育期种子中的表达差异及其对油脂合成积累的影响。结果表明:(1)不同发育期紫斑牡丹种子含油率呈不断升高趋势,在6月20日至7月27日的38 d内,从4.21%上升到18.38%;(2)调控油脂合成的源基因GPD1和汇基因DGAT1与DGAT2在发育前期的紫斑牡丹种子中的表达呈快速上升趋势,且表达量均在7月7日达到最高值;随后源汇基因的表达均不断降低。紫斑牡丹发育前期种子中源(GPD1)汇(DGAT1和DGAT2)基因的协同高表达,既促进合成了更多的TAG前体G3P,又促进了TAG积累。源基因GPD1表达量增加了2.44倍,汇基因DGAT1和DGAT2分别增加5.16倍和3.83倍,促成种子含油量增加了2.77倍。这可为深入理解紫斑牡丹种子油脂合成积累提供理论依据,对后续开展高油紫斑牡丹的分子育种具有重要意义。