A novel approach to the synthesis of ozagrel is described. The target compound is conveniently prepared from the commercially available material, 1,1-carboxyldiimidazole （CDI） through the condensation and hydrolyzat...A novel approach to the synthesis of ozagrel is described. The target compound is conveniently prepared from the commercially available material, 1,1-carboxyldiimidazole （CDI） through the condensation and hydrolyzation.展开更多
BACKGROUND The main pathological factor of cerebral infarction is atherosclerosis,which is the pathological process of chronic inflammatory diseases such as vascular smooth muscle hyperplasia,inflammatory cell infiltr...BACKGROUND The main pathological factor of cerebral infarction is atherosclerosis,which is the pathological process of chronic inflammatory diseases such as vascular smooth muscle hyperplasia,inflammatory cell infiltration,extracellular matrix increase,and thrombosis.At present,the focus of clinical treatment is anti-platelet aggregation and improving blood status,and current research is limited to improving symptoms only.AIM To observe the effect of sodium ozagrel and atorvastatin on type 2 diabetes patients with lacunar cerebral infarction.METHODS Eighty-two patients with type 2 diabetes and lacunar cerebral infarction admitted to our hospital from January 2018 to February 2020 were equally categorized into two groups according to their treatment method.The control group was administered atorvastatin,and the observation group was administered sodium ozagrel combined with atorvastatin.The National Institutes of Health stroke scale(NIHSS)score,activities of daily living(ADL)score,blood glucose,lipid levels,inflammatory factors,high-mobility group box 1(HMGB1)levels,paraoxonase-1(PON-1)levels,erythrocyte sedimentation rate(ESR),and macrophage migration inhibitory factor(MIF)levels were recorded before and after treatment.The total effective rate and adverse reaction rate of the two groups were analyzed.RESULTS The total effective rate of the observation group(94.00%)was significantly higher than that of the control group(80.00%)(χ2=3.998;P=0.046).The blood glucose indexes,total cholesterol levels,triglyceride levels,low-density lipoprotein cholesterol levels,high-sensitivity C-reactive protein levels,interleukin-1βlevels,tumor necrosis factor-αlevels,HMGB1 Levels,ESR,MIF levels,platelet aggregation rates,and plasma viscosity of the two groups decreased after treatment;however,high-density lipoprotein cholesterol and PON-1 Levels increased after treatment.After treatment,the blood glucose indexes;blood lipid indexes;inflammatory factors;HMGB1,PON-1,and MIF levels;ESR;platelet aggregation rate;and plasma viscosity of the observation group were better than those of the control group(P<0.05).After treatment,all patients in the observation group had higher ADL scores and lower NIHSS scores than those in the control group(P<0.05).CONCLUSION Sodium ozagrel with atorvastatin can reduce inflammatory reactions;regulate ESR and HMGB1,PON-1,and MIF levels;control blood glucose and lipid indexes;and alleviate nerve injury without increasing adverse effects of atorvastatin alone.展开更多
A three-dimensional cobalt coordination polymer [Co（IMPAA）2]n（1, HIMPAA =（2E）-3-[4-（1H-imidazol-1-ylmethyl）phenyl]acrylic acid） was synthesized with ozagrel and structurally characterized by element analysis, ...A three-dimensional cobalt coordination polymer [Co（IMPAA）2]n（1, HIMPAA =（2E）-3-[4-（1H-imidazol-1-ylmethyl）phenyl]acrylic acid） was synthesized with ozagrel and structurally characterized by element analysis, IR, PXRD, TGA and X-ray diffraction. Complex 1 is of monoclinic system, space group P21 with a = 5.136（4）, b = 25.577（19）, c = 8.174（6） A, V = 1078.6（14） A3, Mr = 513.41, Z = 2, Dc = 1.581 g/cm3, F（000） = 686, μ = 0.840 mm-1, S = 1.119, Rint = 0.0637 and w R = 0.1456. In complex 1, four IMPAA- and four Co（II） ions form a S-shaped 52-membered macrocycle [Co4（IMPAA）4]4＋. Two carboxlate oxygen atoms link the macrocycles to form a one-dimensional chain. IMPAA- ligands bridge one-dimensional chains to yield a novel three-dimensional metal-organic framework（MOFs）. The complex is stable up to 350 ℃.展开更多
Objective:To study the effect of danhong injection combined with sodium ozagrel on serum IL-8, TNF-α, VEGF, TBIL and NSE in old patients with acute cerebral infarction.Methods:A total of 100 old patients with acute c...Objective:To study the effect of danhong injection combined with sodium ozagrel on serum IL-8, TNF-α, VEGF, TBIL and NSE in old patients with acute cerebral infarction.Methods:A total of 100 old patients with acute cerebral infarction in our hospital from August 2014 to December 2016 were enrolled in this study. The subjects were divided into the control group (n=50) and the treatment group (n=50) randomly. The control group was treated with sodium ozagrel, the treatment group was treated with danhong injection combined with sodium ozagrel, and both the two groups were treated for 14 days. The serum IL-8, TNF-α, VEGF, TBIL and NSE of the two groups before and after treatment were compared.Results:There were no significantly differences of the serum IL-8, TNF-α, VEGF, TBIL and NSE of the two groups before treatment. The serum IL-8, TNF-α, NSE levels of the two groups after treatment were significantly lower than before treatment, the serum VEGF, TBIL levels of the two groups after treatment were significantly higher than before treatment, and that of the treatment group after treatment were significantly better than the control group.Conclusion:Danhong injection combined with sodium ozagrel can significantly reduce the serum IL-8, TNF-α, NSE levels, improve the serum VEGF, TBIL levels, and reduce inflammation, promote the nerve functional recovery of the old patients with acute cerebral infarction, and it was worthy clinical application.展开更多
To reduce the first-pass effect and increase the targeting of ozagrel(OZ),the ozagrel -magnetoliposomes(OZ-MLs)were prepared in this study.Here,we described the preparation and characterization of OZ-MLs.It had a diam...To reduce the first-pass effect and increase the targeting of ozagrel(OZ),the ozagrel -magnetoliposomes(OZ-MLs)were prepared in this study.Here,we described the preparation and characterization of OZ-MLs.It had a diameter of around 0.2μm.To prevent the aggregation of particles,the magnetite was treated with a surfactant,resulting in a stable ferrofluid suspension. The cumulative release of OZ from OZ-MLs could be up to 64.5%in 30 min in vitro under AC-magnetic field.However,it was only 24.0%for OZ-MLs without AC-magnetic field.展开更多
文摘A novel approach to the synthesis of ozagrel is described. The target compound is conveniently prepared from the commercially available material, 1,1-carboxyldiimidazole （CDI） through the condensation and hydrolyzation.
文摘BACKGROUND The main pathological factor of cerebral infarction is atherosclerosis,which is the pathological process of chronic inflammatory diseases such as vascular smooth muscle hyperplasia,inflammatory cell infiltration,extracellular matrix increase,and thrombosis.At present,the focus of clinical treatment is anti-platelet aggregation and improving blood status,and current research is limited to improving symptoms only.AIM To observe the effect of sodium ozagrel and atorvastatin on type 2 diabetes patients with lacunar cerebral infarction.METHODS Eighty-two patients with type 2 diabetes and lacunar cerebral infarction admitted to our hospital from January 2018 to February 2020 were equally categorized into two groups according to their treatment method.The control group was administered atorvastatin,and the observation group was administered sodium ozagrel combined with atorvastatin.The National Institutes of Health stroke scale(NIHSS)score,activities of daily living(ADL)score,blood glucose,lipid levels,inflammatory factors,high-mobility group box 1(HMGB1)levels,paraoxonase-1(PON-1)levels,erythrocyte sedimentation rate(ESR),and macrophage migration inhibitory factor(MIF)levels were recorded before and after treatment.The total effective rate and adverse reaction rate of the two groups were analyzed.RESULTS The total effective rate of the observation group(94.00%)was significantly higher than that of the control group(80.00%)(χ2=3.998;P=0.046).The blood glucose indexes,total cholesterol levels,triglyceride levels,low-density lipoprotein cholesterol levels,high-sensitivity C-reactive protein levels,interleukin-1βlevels,tumor necrosis factor-αlevels,HMGB1 Levels,ESR,MIF levels,platelet aggregation rates,and plasma viscosity of the two groups decreased after treatment;however,high-density lipoprotein cholesterol and PON-1 Levels increased after treatment.After treatment,the blood glucose indexes;blood lipid indexes;inflammatory factors;HMGB1,PON-1,and MIF levels;ESR;platelet aggregation rate;and plasma viscosity of the observation group were better than those of the control group(P<0.05).After treatment,all patients in the observation group had higher ADL scores and lower NIHSS scores than those in the control group(P<0.05).CONCLUSION Sodium ozagrel with atorvastatin can reduce inflammatory reactions;regulate ESR and HMGB1,PON-1,and MIF levels;control blood glucose and lipid indexes;and alleviate nerve injury without increasing adverse effects of atorvastatin alone.
基金supported by the National Natural Foundation of China(No.31060213)the Research Foundation of Educational Department of Jiangxi Province(No.GJJ13261)
文摘A three-dimensional cobalt coordination polymer [Co（IMPAA）2]n（1, HIMPAA =（2E）-3-[4-（1H-imidazol-1-ylmethyl）phenyl]acrylic acid） was synthesized with ozagrel and structurally characterized by element analysis, IR, PXRD, TGA and X-ray diffraction. Complex 1 is of monoclinic system, space group P21 with a = 5.136（4）, b = 25.577（19）, c = 8.174（6） A, V = 1078.6（14） A3, Mr = 513.41, Z = 2, Dc = 1.581 g/cm3, F（000） = 686, μ = 0.840 mm-1, S = 1.119, Rint = 0.0637 and w R = 0.1456. In complex 1, four IMPAA- and four Co（II） ions form a S-shaped 52-membered macrocycle [Co4（IMPAA）4]4＋. Two carboxlate oxygen atoms link the macrocycles to form a one-dimensional chain. IMPAA- ligands bridge one-dimensional chains to yield a novel three-dimensional metal-organic framework（MOFs）. The complex is stable up to 350 ℃.
文摘Objective:To study the effect of danhong injection combined with sodium ozagrel on serum IL-8, TNF-α, VEGF, TBIL and NSE in old patients with acute cerebral infarction.Methods:A total of 100 old patients with acute cerebral infarction in our hospital from August 2014 to December 2016 were enrolled in this study. The subjects were divided into the control group (n=50) and the treatment group (n=50) randomly. The control group was treated with sodium ozagrel, the treatment group was treated with danhong injection combined with sodium ozagrel, and both the two groups were treated for 14 days. The serum IL-8, TNF-α, VEGF, TBIL and NSE of the two groups before and after treatment were compared.Results:There were no significantly differences of the serum IL-8, TNF-α, VEGF, TBIL and NSE of the two groups before treatment. The serum IL-8, TNF-α, NSE levels of the two groups after treatment were significantly lower than before treatment, the serum VEGF, TBIL levels of the two groups after treatment were significantly higher than before treatment, and that of the treatment group after treatment were significantly better than the control group.Conclusion:Danhong injection combined with sodium ozagrel can significantly reduce the serum IL-8, TNF-α, NSE levels, improve the serum VEGF, TBIL levels, and reduce inflammation, promote the nerve functional recovery of the old patients with acute cerebral infarction, and it was worthy clinical application.
文摘To reduce the first-pass effect and increase the targeting of ozagrel(OZ),the ozagrel -magnetoliposomes(OZ-MLs)were prepared in this study.Here,we described the preparation and characterization of OZ-MLs.It had a diameter of around 0.2μm.To prevent the aggregation of particles,the magnetite was treated with a surfactant,resulting in a stable ferrofluid suspension. The cumulative release of OZ from OZ-MLs could be up to 64.5%in 30 min in vitro under AC-magnetic field.However,it was only 24.0%for OZ-MLs without AC-magnetic field.
文摘目的探究奥扎格雷钠治疗急性缺血性脑卒中(acute ischemic stroke,AIS)的疗效及对脑侧支循环、纤溶-凝血指标及外周血CD34阳性细胞(cluster of differentiation 34-positive cells,CD34^(+))、KDR阳性细胞(kinase insert domain receptor-positive cells,KDR^(+))水平的影响。方法选取2023年4月—2024年4月符合纳入标准的72例AIS患者作为研究对象,按照区组随机化分组均分为对照组(阿司匹林肠溶片治疗)和观察组(奥扎格雷钠联合阿司匹林肠溶片治疗),每组36例。比较2组的治疗效果,脑侧支循环情况,纤溶-凝血指标[组织型纤溶酶原激活物-抑制剂复合物(tissue plasminogen activator-inhibitor complex,t-PAIC)、血栓调节蛋白(thrombomodulin,TM)、凝血酶-抗凝血酶复合物(thrombin-antithrombin complex,TAT)],外周CD34^(+)、KDR^(+)细胞水平及2组用药不良反应的发生情况。结果治疗2周后,对照组的总有效率为77.78%,低于观察组的94.44%(P<0.05);观察组的美国国立卫生研究院卒中量表(National Institute of Health Stroke Scale,NIHSS)评分低于对照组(P<0.05);对照组脑侧支循环改善情况较观察组差(P<0.05);对照组的t-PAIC、TM、TAT水平较观察组均高(P<0.05);对照组的外周血CD34^(+)、KDR^(+)细胞水平较观察组均低(P<0.05);2组不良反应发生率比较,差异无统计学意义(P>0.05)。结论奥扎格雷钠联合阿司匹林治疗AIS,可以提高治疗效果,改善神经功能,促进脑侧支循环改善,有助于调节纤溶-凝血功能,改善血管内皮功能,且安全性良好。
