AIM： To investigate the effect of interleukin-8（IL-8） on neural retinal ganglion cells（RGCs） and whether it can be alleviated by G31P. METHODS： RGC-5 cells were exposed to IL-8 with or without its specific recep...AIM： To investigate the effect of interleukin-8（IL-8） on neural retinal ganglion cells（RGCs） and whether it can be alleviated by G31P. METHODS： RGC-5 cells were exposed to IL-8 with or without its specific receptor antagonist G31P for 24h, and the cell viability was assessed by Cell Counting Kit 8（CCK-8）. Apoptosis was measured by examining nuclear morphology and quantifying with flow cytometry. Reverse transcription quantitative real-time polymerase chain reaction（RT-qP CR） and Western blot were used to investigate the expression of apoptosis-related genes. RESULTS： CCK-8 assay showed that IL-8 significantly inhibits the viability of RGC-5 cells in a dose-dependent manner. Cell apoptosis assays exhibited higher apoptotic rate in IL-8 treatment group compared to control group. We further found that IL-8 could promote Bax and caspase-3 expressions, but decrease the level of Bcl-2 in the aspect of m RNA and protein. However, pre-treatment with G31P partly attenuated these effects in RGC-5 cells（P〈0.05）.CONCLUSION： These results indicate that anti-proliferation effects of IL-8 through induction of cell apoptosis regulated by Bcl-2, Bax and caspase-3 expressions, can be ameliorated by G31P.展开更多
The a-amino acid derivatives constitute a class of compounds of particular medicinal and synthetic attention and considerable interest has been devoted to their synthesis in recent years.In the present work,we develop...The a-amino acid derivatives constitute a class of compounds of particular medicinal and synthetic attention and considerable interest has been devoted to their synthesis in recent years.In the present work,we develop the computational study of the synthesis reaction of new pyrazolyl a-amino esters derivatives using the Gaussian 09based on the DET/B3LYP density functional theorv method,with the base 6-31G(d.p)to ensure the possibility of carrying out these reactions within the laboratory of synthesis.Indeed,this research has encouraged us to establish an economical synthesis strategy of these products in overall vields of 73.5%to 87%to have access to new active biomolecule through the O-alkvlation reaction between methyl a-azidoglycinate N-benzoylated and primary pyrazole alcohols(3,5-dimethyl-1 H-pyrazol-1-yl)methanol,(1H-pyrazol-1-yl)methanol and(3-ethoxy-5-methyl-1H-pyrazol-1yl)methanoll under different operating conditions.The structure of the prepared heterocyclic systems was characterized by conventional spectroscopic techniques,like H NMR.I3℃NMR,and MS.The results revealed that the experimental study is in good correlation with the computational one.展开更多
文摘目的:探讨CXCR1/CXCR2受体拮抗剂-G31P对人前列腺癌细胞PC-3增殖的体内外抑制作用。方法:采用CCK-8法研究不同浓度G31P对PC-3细胞体外增殖的抑制作用。建立体内绿色荧光蛋白(Green fluorescent protein,GFP)标记人雄激素非依赖性前列腺癌细胞PC-3裸鼠原位移植瘤模型,观察G31P对裸鼠前列腺癌原位移植瘤的体积、重量的影响。结果:CCK-8结果显示100 ng/ml G31P与对照组相比分别作用1、3 d和5 d差异具有统计学意义(1 d P=0.007、3 d P=0.001、5 d P=0.028,均为P<0.05)。前列腺癌PC-3细胞裸鼠模型体内实验显示,与对照组(100μl N.S)相比,G31P处理组(0.5 mg/kg)从给药第18天起能显著抑制前列腺肿瘤的体积(P=0.026,P<0.05);与对照组相比G31P处理组在抑制前列腺肿瘤重量方面有明显作用(P=0.027,P<0.05)。结论:G31P体内外实验均能抑制人雄激素非依赖性前列腺癌细胞系PC-3的增殖。
文摘AIM： To investigate the effect of interleukin-8（IL-8） on neural retinal ganglion cells（RGCs） and whether it can be alleviated by G31P. METHODS： RGC-5 cells were exposed to IL-8 with or without its specific receptor antagonist G31P for 24h, and the cell viability was assessed by Cell Counting Kit 8（CCK-8）. Apoptosis was measured by examining nuclear morphology and quantifying with flow cytometry. Reverse transcription quantitative real-time polymerase chain reaction（RT-qP CR） and Western blot were used to investigate the expression of apoptosis-related genes. RESULTS： CCK-8 assay showed that IL-8 significantly inhibits the viability of RGC-5 cells in a dose-dependent manner. Cell apoptosis assays exhibited higher apoptotic rate in IL-8 treatment group compared to control group. We further found that IL-8 could promote Bax and caspase-3 expressions, but decrease the level of Bcl-2 in the aspect of m RNA and protein. However, pre-treatment with G31P partly attenuated these effects in RGC-5 cells（P〈0.05）.CONCLUSION： These results indicate that anti-proliferation effects of IL-8 through induction of cell apoptosis regulated by Bcl-2, Bax and caspase-3 expressions, can be ameliorated by G31P.
基金Supported by the Centre National de la Recherche Scientifique et Techniques,Rabat,Morocco(No.PROTARS D13/03).
文摘The a-amino acid derivatives constitute a class of compounds of particular medicinal and synthetic attention and considerable interest has been devoted to their synthesis in recent years.In the present work,we develop the computational study of the synthesis reaction of new pyrazolyl a-amino esters derivatives using the Gaussian 09based on the DET/B3LYP density functional theorv method,with the base 6-31G(d.p)to ensure the possibility of carrying out these reactions within the laboratory of synthesis.Indeed,this research has encouraged us to establish an economical synthesis strategy of these products in overall vields of 73.5%to 87%to have access to new active biomolecule through the O-alkvlation reaction between methyl a-azidoglycinate N-benzoylated and primary pyrazole alcohols(3,5-dimethyl-1 H-pyrazol-1-yl)methanol,(1H-pyrazol-1-yl)methanol and(3-ethoxy-5-methyl-1H-pyrazol-1yl)methanoll under different operating conditions.The structure of the prepared heterocyclic systems was characterized by conventional spectroscopic techniques,like H NMR.I3℃NMR,and MS.The results revealed that the experimental study is in good correlation with the computational one.
