Chronic obstructive pulmonary disease(COPD)has garnered increased attention as a result of its persistent symptoms,which undermine patientsʼquality of life.Fudosteine has substantial advantages in the treatment of COP...Chronic obstructive pulmonary disease(COPD)has garnered increased attention as a result of its persistent symptoms,which undermine patientsʼquality of life.Fudosteine has substantial advantages in the treatment of COPD due to its high efficacy and low adverse effects.In this study,Fudosteine sulfonamide derivatives Series I and amine derivatives Series II were designed and synthesized,and their biological activities were evaluated.The results showed that compound 6f had outstanding anti-inflammatory action with an IC_(50) of 1.08 mmol/L,and a higher antioxidant capacity than the lead molecule.At the same time,molecular docking investigations have revealed that compound 6f establishes hydrogen bonds and hydrophobic contacts with the MUC5AC protein.Furthermore,derivative 1f inhibited PDE4A1 enzyme activity five times more than Fudosteine.2,2-Diphenyl-1-picrylhydrazyl(DPPH)free radical scavenging tests demonstrated that all examined substances had higher antioxidant activity than Fudosteine.This study established a solid foundation for further research into COPD drug therapy.展开更多
目的探讨苏黄止咳胶囊联合福多司坦片治疗支气管扩张对患者血清肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、α1-抗胰蛋白酶(α1-antitryp sin,α1-AT)、白细胞介素-37(interleukin-37,IL-37)水平的影响。方法选取支气管扩张患...目的探讨苏黄止咳胶囊联合福多司坦片治疗支气管扩张对患者血清肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、α1-抗胰蛋白酶(α1-antitryp sin,α1-AT)、白细胞介素-37(interleukin-37,IL-37)水平的影响。方法选取支气管扩张患者63例,用随机数字表法分为观察组(n=32)和对照组(n=31)。对照组采用福多司坦片治疗,观察组在对照组治疗的基础上联合苏黄止咳胶囊。比较2组患者的治疗疗效、中医证候积分、肺功能指标、TNF-α、α1-AT、IL-37、呼吸状况和不良反应。结果治疗后,观察组的总有效率(96.88%)高于对照组(80.65%),P<0.05;观察组的中医证候积分低于对照组,P<0.05;观察组的第1秒用力呼气容积(forced expiratory volume in one second,FEV1)、用力肺活量(forced vital capacity,FVC)、一氧化碳弥散量占预计值百分比(carbon monoxide diffusion capacity as a percentage of predicted value,DLCO%pred)均高于对照组,P<0.05;观察组的IL-37水平高于对照组,P<0.05,观察组的TNF-α、α1-AT水平低于对照组,P<0.05;观察组的圣乔治呼吸问卷(St.George’s respiratory questionnaire,SGRQ)各维度评分均低于对照组,P<0.05;观察组不良反应发生率低于对照组,P<0.05。结论采用苏黄止咳胶囊联合福多司坦片治疗支气管扩张能有效提高患者的治疗疗效,改善其中医证候,改善TNF-α、α1-AT、IL-37水平、肺功能指标和呼吸功能。展开更多
文摘Chronic obstructive pulmonary disease(COPD)has garnered increased attention as a result of its persistent symptoms,which undermine patientsʼquality of life.Fudosteine has substantial advantages in the treatment of COPD due to its high efficacy and low adverse effects.In this study,Fudosteine sulfonamide derivatives Series I and amine derivatives Series II were designed and synthesized,and their biological activities were evaluated.The results showed that compound 6f had outstanding anti-inflammatory action with an IC_(50) of 1.08 mmol/L,and a higher antioxidant capacity than the lead molecule.At the same time,molecular docking investigations have revealed that compound 6f establishes hydrogen bonds and hydrophobic contacts with the MUC5AC protein.Furthermore,derivative 1f inhibited PDE4A1 enzyme activity five times more than Fudosteine.2,2-Diphenyl-1-picrylhydrazyl(DPPH)free radical scavenging tests demonstrated that all examined substances had higher antioxidant activity than Fudosteine.This study established a solid foundation for further research into COPD drug therapy.
文摘目的探讨苏黄止咳胶囊联合福多司坦片治疗支气管扩张对患者血清肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、α1-抗胰蛋白酶(α1-antitryp sin,α1-AT)、白细胞介素-37(interleukin-37,IL-37)水平的影响。方法选取支气管扩张患者63例,用随机数字表法分为观察组(n=32)和对照组(n=31)。对照组采用福多司坦片治疗,观察组在对照组治疗的基础上联合苏黄止咳胶囊。比较2组患者的治疗疗效、中医证候积分、肺功能指标、TNF-α、α1-AT、IL-37、呼吸状况和不良反应。结果治疗后,观察组的总有效率(96.88%)高于对照组(80.65%),P<0.05;观察组的中医证候积分低于对照组,P<0.05;观察组的第1秒用力呼气容积(forced expiratory volume in one second,FEV1)、用力肺活量(forced vital capacity,FVC)、一氧化碳弥散量占预计值百分比(carbon monoxide diffusion capacity as a percentage of predicted value,DLCO%pred)均高于对照组,P<0.05;观察组的IL-37水平高于对照组,P<0.05,观察组的TNF-α、α1-AT水平低于对照组,P<0.05;观察组的圣乔治呼吸问卷(St.George’s respiratory questionnaire,SGRQ)各维度评分均低于对照组,P<0.05;观察组不良反应发生率低于对照组,P<0.05。结论采用苏黄止咳胶囊联合福多司坦片治疗支气管扩张能有效提高患者的治疗疗效,改善其中医证候,改善TNF-α、α1-AT、IL-37水平、肺功能指标和呼吸功能。
