P6A was able to increase coronary blood flow and improve hemodynamics in the coronary thrombosis model of dogs In the binding of fibrinogen to GP IIb/IIIa,RGD is the key sequence In the present paper the effects of th...P6A was able to increase coronary blood flow and improve hemodynamics in the coronary thrombosis model of dogs In the binding of fibrinogen to GP IIb/IIIa,RGD is the key sequence In the present paper the effects of the coupling compounds of P6A and its derivatives,QP6A with RGDS,RGDV and RGDF were tested The effects of the coupling compounds so obtained on carotid thrombosis in rats were investigated At the dose of 5 μmol/kg,RGDS and RGDV exhibited no antithrombotic effects,whereas at 2.5μmol/kg RGDF decreased the dry-weight ofthrombus significantly On the other hand,P6A(5μmol/kg)and QP6A(2.5μmol/kg)showed significant antithrombosis activities.All of the coupling compounds,except P6A-RGDF and QP6A-RGDF,had potent antithrombosis effects.展开更多
Based on the structure-activity relationships of RGD-containing peptides, a series of 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. All of them were first reported. Their structures were confirmed b...Based on the structure-activity relationships of RGD-containing peptides, a series of 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. All of them were first reported. Their structures were confirmed by spectral data and elemental analysis. Their ability to inhibit angiogenesis were evaluated in the chick embryo chorioallantoic membrane assay at 10-5 mol/L. Compounds 5b and 5e displayed obviously antiangiogenic activity.展开更多
Ischemic stroke has become an important cause of death and disability for residents worldwide.At present,the main treatment methods are thrombolysis and embolectomy.However,a large number of patients miss the window p...Ischemic stroke has become an important cause of death and disability for residents worldwide.At present,the main treatment methods are thrombolysis and embolectomy.However,a large number of patients miss the window period of thrombolysis and embolectomy or have other conditions that are not suitable for thrombolysis.Therefore,cerebral protective drugs or bioactive substances are needed to protect neural tissue and improve the prognosis.However,there is still a lack of strong and effective drugs or bioactive substances for selection.Osteopontin(OPN)is a phosphorylated glycoprotein that plays an important role in cell adhesion,differentiation,survival and repair by binding to cellular integrin receptors and inducing signal transmission.Numerous studies have shown that osteopontin can protect brain tissue and reduce brain injury caused by ischemic stroke by various means such as promoting angiogenesis,and promoting neural stem cell migration in the pathogenesis of ischemic stroke.展开更多
Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characte...Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characterized by ^1H NMR, MS and elementary analysis. There ability to inhibit angiogenesis were evaluated by chick embryo chorioallantoic membrane assay at 10^-5 mol/L. Compounds 7a and 7b displayed obvious antiangiogenic activity.展开更多
文摘P6A was able to increase coronary blood flow and improve hemodynamics in the coronary thrombosis model of dogs In the binding of fibrinogen to GP IIb/IIIa,RGD is the key sequence In the present paper the effects of the coupling compounds of P6A and its derivatives,QP6A with RGDS,RGDV and RGDF were tested The effects of the coupling compounds so obtained on carotid thrombosis in rats were investigated At the dose of 5 μmol/kg,RGDS and RGDV exhibited no antithrombotic effects,whereas at 2.5μmol/kg RGDF decreased the dry-weight ofthrombus significantly On the other hand,P6A(5μmol/kg)and QP6A(2.5μmol/kg)showed significant antithrombosis activities.All of the coupling compounds,except P6A-RGDF and QP6A-RGDF,had potent antithrombosis effects.
文摘Based on the structure-activity relationships of RGD-containing peptides, a series of 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. All of them were first reported. Their structures were confirmed by spectral data and elemental analysis. Their ability to inhibit angiogenesis were evaluated in the chick embryo chorioallantoic membrane assay at 10-5 mol/L. Compounds 5b and 5e displayed obviously antiangiogenic activity.
基金Youth Project of the National Natural Science Foundation of China(No.81701301)Innovative Training Program for College Students-National(No.20022901043)。
文摘Ischemic stroke has become an important cause of death and disability for residents worldwide.At present,the main treatment methods are thrombolysis and embolectomy.However,a large number of patients miss the window period of thrombolysis and embolectomy or have other conditions that are not suitable for thrombolysis.Therefore,cerebral protective drugs or bioactive substances are needed to protect neural tissue and improve the prognosis.However,there is still a lack of strong and effective drugs or bioactive substances for selection.Osteopontin(OPN)is a phosphorylated glycoprotein that plays an important role in cell adhesion,differentiation,survival and repair by binding to cellular integrin receptors and inducing signal transmission.Numerous studies have shown that osteopontin can protect brain tissue and reduce brain injury caused by ischemic stroke by various means such as promoting angiogenesis,and promoting neural stem cell migration in the pathogenesis of ischemic stroke.
文摘Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characterized by ^1H NMR, MS and elementary analysis. There ability to inhibit angiogenesis were evaluated by chick embryo chorioallantoic membrane assay at 10^-5 mol/L. Compounds 7a and 7b displayed obvious antiangiogenic activity.
