Aim To study the most stable pH value of endomorphin-1 solution and toestimate the shelf-life of EM-1 solution. Methods The content of EM-1 in its solution was determinedby HPLC, and stability was studied by accelerat...Aim To study the most stable pH value of endomorphin-1 solution and toestimate the shelf-life of EM-1 solution. Methods The content of EM-1 in its solution was determinedby HPLC, and stability was studied by accelerated tests. Results The most stable pH value of EM-1solution was observed. By the accelerated tests we obtained the Arrhe-nius relationship and thepharmacokinetic parameters. Conclusion The most stable pH value of EM-1 solution is 4.5 -4.8. Thet_(1/2)(25℃) is 45 d.展开更多
Endomorphin-1 is an endogenous opioid peptide that mediates pain relief through interaction with the μ-opioid receptor in the central nervous system. To enhance the metabolic stability of this tetrapeptide, cyclisati...Endomorphin-1 is an endogenous opioid peptide that mediates pain relief through interaction with the μ-opioid receptor in the central nervous system. To enhance the metabolic stability of this tetrapeptide, cyclisation through the formation of a disulfide bridge between the side chains of cysteine residues added to the sequence was explored. A further increase in stability was achieved through N-terminal modification with lipoamino acid and lactose succinamic acid, and the inclusion of D-amino acids. The latter also provided an alternative spatial arrangement of the aromatic side chains. The lipidated cyclic derivatives were insoluble in aqueous buffer, however, the cyclic peptides and glycopeptides showed greatly improved stability towards enzymatic degradation in human plasma.展开更多
目的探究纤维蛋白原样蛋白1(fibrinogen-like protein 1,FGL1)和膜联蛋白A11(annexin A11,ANXA11)对肺癌手术患者效用评估价值及与预后的相关性。方法将本院2020年1月至2023年12月接诊的98例肺癌患者纳入肺癌组,另选取98例健康人作为对...目的探究纤维蛋白原样蛋白1(fibrinogen-like protein 1,FGL1)和膜联蛋白A11(annexin A11,ANXA11)对肺癌手术患者效用评估价值及与预后的相关性。方法将本院2020年1月至2023年12月接诊的98例肺癌患者纳入肺癌组,另选取98例健康人作为对照组。受试者入院后分别于空腹状态下采取6 mL肘静脉血,采用ELISA法检测血清ANXA11水平,采用实时荧光定量PCR技术检测ANXA11表达水平。根据术后1个月肿瘤标志物变化、影像学表现和免疫功能指标变化情况分为治疗有效组(n=68)和无效组(n=30)。患者出院后均行12~36个月的随访,根据患者预后情况分为预后良好组(n=63)和预后不良组(n=35)。对比对照组和肺癌组/有效组和无效组/预后FGL1、ANXA11表达差异;ROC分析FGL1、ANXA11单一及联合检测对肺癌手术患者临床效用评估价值;Spearman分析FGL1、ANXA11表达与预后的关系。结果肺癌组FGL1和ANXA11表达水平明显高于对照组(均P<0.05);无效组FGL1和ANXA11表达水平明显高于有效组(均P<0.05);ROC结果显示FGL1、ANXA11单独及联合检测对肺癌手术患者效用评估的曲线线下面积分别为0.928,并且联合检测具有较高的特异性(95.59%)以及敏感度(90.00%),诊断价值显著高于单独检测ROC曲线线下面积(均P<0.05);预后不良组FGL1和ANXA11表达水平明显高于预后良好组(均P<0.05);Spearman相关性结果显示FGL1、ANXA11与肺癌手术患者预后呈显著正相关(r=0.771、0.793,均P<0.05)。结论肺癌患者的FGL1与ANXA11表达水平高于健康人,治疗无效者高于有效者,预后不良者高于良好者,二者单独及联合检测对患者手术治疗效用评估均有价值,且其与预后相关性显著。展开更多
文摘Aim To study the most stable pH value of endomorphin-1 solution and toestimate the shelf-life of EM-1 solution. Methods The content of EM-1 in its solution was determinedby HPLC, and stability was studied by accelerated tests. Results The most stable pH value of EM-1solution was observed. By the accelerated tests we obtained the Arrhe-nius relationship and thepharmacokinetic parameters. Conclusion The most stable pH value of EM-1 solution is 4.5 -4.8. Thet_(1/2)(25℃) is 45 d.
文摘Endomorphin-1 is an endogenous opioid peptide that mediates pain relief through interaction with the μ-opioid receptor in the central nervous system. To enhance the metabolic stability of this tetrapeptide, cyclisation through the formation of a disulfide bridge between the side chains of cysteine residues added to the sequence was explored. A further increase in stability was achieved through N-terminal modification with lipoamino acid and lactose succinamic acid, and the inclusion of D-amino acids. The latter also provided an alternative spatial arrangement of the aromatic side chains. The lipidated cyclic derivatives were insoluble in aqueous buffer, however, the cyclic peptides and glycopeptides showed greatly improved stability towards enzymatic degradation in human plasma.
文摘目的探究纤维蛋白原样蛋白1(fibrinogen-like protein 1,FGL1)和膜联蛋白A11(annexin A11,ANXA11)对肺癌手术患者效用评估价值及与预后的相关性。方法将本院2020年1月至2023年12月接诊的98例肺癌患者纳入肺癌组,另选取98例健康人作为对照组。受试者入院后分别于空腹状态下采取6 mL肘静脉血,采用ELISA法检测血清ANXA11水平,采用实时荧光定量PCR技术检测ANXA11表达水平。根据术后1个月肿瘤标志物变化、影像学表现和免疫功能指标变化情况分为治疗有效组(n=68)和无效组(n=30)。患者出院后均行12~36个月的随访,根据患者预后情况分为预后良好组(n=63)和预后不良组(n=35)。对比对照组和肺癌组/有效组和无效组/预后FGL1、ANXA11表达差异;ROC分析FGL1、ANXA11单一及联合检测对肺癌手术患者临床效用评估价值;Spearman分析FGL1、ANXA11表达与预后的关系。结果肺癌组FGL1和ANXA11表达水平明显高于对照组(均P<0.05);无效组FGL1和ANXA11表达水平明显高于有效组(均P<0.05);ROC结果显示FGL1、ANXA11单独及联合检测对肺癌手术患者效用评估的曲线线下面积分别为0.928,并且联合检测具有较高的特异性(95.59%)以及敏感度(90.00%),诊断价值显著高于单独检测ROC曲线线下面积(均P<0.05);预后不良组FGL1和ANXA11表达水平明显高于预后良好组(均P<0.05);Spearman相关性结果显示FGL1、ANXA11与肺癌手术患者预后呈显著正相关(r=0.771、0.793,均P<0.05)。结论肺癌患者的FGL1与ANXA11表达水平高于健康人,治疗无效者高于有效者,预后不良者高于良好者,二者单独及联合检测对患者手术治疗效用评估均有价值,且其与预后相关性显著。
