Luteolin is an active ingredient found early from Fofium perillae and Flos Ionicerae, and has a specific inhibition on phosphodiesterase 4 （PDE4） activity in vitro. Researches show luteolin has pharmacological effec...Luteolin is an active ingredient found early from Fofium perillae and Flos Ionicerae, and has a specific inhibition on phosphodiesterase 4 （PDE4） activity in vitro. Researches show luteolin has pharmacological effects of anti-inflammation, anti-anaphylaxis, antitumor, antioxidant, protection of nervous system and so on, and has mainly been used for the treatment of respiratory inflammatory diseases, cancer and cardiovascular disease in clinic. PDE4, specific to hydrolyze cyclic AMP （cAMP）, is considered to be a new anti-inflammatory target due to the decisive role on cAMP signal in inflammatory cells such as neutrophils. In order to explore the anti-inflammatory mechanism, we further studied the effects of luteolin on the activity and expression of PDE4, the expression of lymphocyte function-associated antigen-1 （LFA-1） and macrophage-1 （MAC-l） in neutrophils, and the adhesion of neutrophils and endothelial cells. The results showed that luteolin had a dose-dependent inhibition on both bare PDE4 activity and PDE4 in cultured neutrophils, and had an obviously promotive effect on gene expressions of PDE4A, 4B and 4D in later period. Luteolin had a significant inhibitory effect on neutrophils adhesion and LFA-1 expression in early stage, and had no obvious effect on MAC-1 expression. Therefore, luteolin can inhibit LFA-1 expression of neutrophils, then inhibit the adhesion of neutrophils and endothelial cells, and the mechanism is at least related with the inhibition of PDE4 activity.展开更多
Objective: To investigate the effect and safety of Guanxinning Tablet(冠心宁片, GXN) for the treatment of stable angina pectoris patients with Xin(Heart)-blood stagnation syndrome(XBSS). Methods: One hundred and sixty...Objective: To investigate the effect and safety of Guanxinning Tablet(冠心宁片, GXN) for the treatment of stable angina pectoris patients with Xin(Heart)-blood stagnation syndrome(XBSS). Methods: One hundred and sixty stable angina pectoris patients with XBSS were randomly assigned to receive GXN(80 cases) or placebo(80 cases, Guanxinning simulation tablets, mainly composed of lactose), 4 tablets(0.38 g/tablet), thrice daily for 12 weeks. After treatment, an exercise stress test(treadmill protocol), Chinese medicine(CM) syndrome score, electrocardiogram(ECG), and nitroglycerin withdrawal rate were evaluated and compared in the patients between the two groups. Meanwhile, adverse events(AEs) were evaluated during the whole clinical trial. Results: Compared with the control group, the time extension of exercise duration in the GXN group increased 29.28±17.67 s after treatment(P>0.05);moreover, the change of exercise duration in the GXN group increased 63.10±96.96 s in subgroup analysis(P<0.05). The effective rates of angina pectoris, CM syndrome and ECG as well as nitroglycerin withdrawal rate were 81.33%, 90.67%, 45.76%, and 70.73%, respectively in the GXN group, which were all significantly higher than those in the control group(40.58%, 75.36%, 26.92%, 28.21%, respectively, P<0.05). Conclusion: GXN was a safe and effective treatment for stable angina pectoris patients with XBSS at a dose of 4 tablets, thrice daily.展开更多
基金financial support of the Beijing Natural Science Foundation, China (6112007)the National Natural Science Foundation of China (31101851)+1 种基金the Funding Project for Academic Human Resources Development in Institutions of Higher Learning under the Jurisdiction of Beijing Municipality, China (PHR201107134)the Comprehensive Reforming Project to promote talents training of Beijing University of Agriculture, China (BNRC&GG201404)
文摘Luteolin is an active ingredient found early from Fofium perillae and Flos Ionicerae, and has a specific inhibition on phosphodiesterase 4 （PDE4） activity in vitro. Researches show luteolin has pharmacological effects of anti-inflammation, anti-anaphylaxis, antitumor, antioxidant, protection of nervous system and so on, and has mainly been used for the treatment of respiratory inflammatory diseases, cancer and cardiovascular disease in clinic. PDE4, specific to hydrolyze cyclic AMP （cAMP）, is considered to be a new anti-inflammatory target due to the decisive role on cAMP signal in inflammatory cells such as neutrophils. In order to explore the anti-inflammatory mechanism, we further studied the effects of luteolin on the activity and expression of PDE4, the expression of lymphocyte function-associated antigen-1 （LFA-1） and macrophage-1 （MAC-l） in neutrophils, and the adhesion of neutrophils and endothelial cells. The results showed that luteolin had a dose-dependent inhibition on both bare PDE4 activity and PDE4 in cultured neutrophils, and had an obviously promotive effect on gene expressions of PDE4A, 4B and 4D in later period. Luteolin had a significant inhibitory effect on neutrophils adhesion and LFA-1 expression in early stage, and had no obvious effect on MAC-1 expression. Therefore, luteolin can inhibit LFA-1 expression of neutrophils, then inhibit the adhesion of neutrophils and endothelial cells, and the mechanism is at least related with the inhibition of PDE4 activity.
基金Supported by the National Major Scientific and Technological Special Project for Significant New Drugs Development(No.2012ZX09303-010-002),China
文摘Objective: To investigate the effect and safety of Guanxinning Tablet(冠心宁片, GXN) for the treatment of stable angina pectoris patients with Xin(Heart)-blood stagnation syndrome(XBSS). Methods: One hundred and sixty stable angina pectoris patients with XBSS were randomly assigned to receive GXN(80 cases) or placebo(80 cases, Guanxinning simulation tablets, mainly composed of lactose), 4 tablets(0.38 g/tablet), thrice daily for 12 weeks. After treatment, an exercise stress test(treadmill protocol), Chinese medicine(CM) syndrome score, electrocardiogram(ECG), and nitroglycerin withdrawal rate were evaluated and compared in the patients between the two groups. Meanwhile, adverse events(AEs) were evaluated during the whole clinical trial. Results: Compared with the control group, the time extension of exercise duration in the GXN group increased 29.28±17.67 s after treatment(P>0.05);moreover, the change of exercise duration in the GXN group increased 63.10±96.96 s in subgroup analysis(P<0.05). The effective rates of angina pectoris, CM syndrome and ECG as well as nitroglycerin withdrawal rate were 81.33%, 90.67%, 45.76%, and 70.73%, respectively in the GXN group, which were all significantly higher than those in the control group(40.58%, 75.36%, 26.92%, 28.21%, respectively, P<0.05). Conclusion: GXN was a safe and effective treatment for stable angina pectoris patients with XBSS at a dose of 4 tablets, thrice daily.
