A series of novel ligustrazine derivatives were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H NMR and ESI-MS. The preliminary antiplatelet a...A series of novel ligustrazine derivatives were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H NMR and ESI-MS. The preliminary antiplatelet aggregation screening results demonstrated that the compounds 7a, 7b and 7c showed higher potency than ligustrazine.展开更多
A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inh...A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.展开更多
A series of arylsulfonamide and arylamide derivatives have been prepared from anisole in good yields. The structures of those compounds were confirmed by 1H-NMR and MS analysis. Their activities against platelet aggre...A series of arylsulfonamide and arylamide derivatives have been prepared from anisole in good yields. The structures of those compounds were confirmed by 1H-NMR and MS analysis. Their activities against platelet aggregation were tested in vitro by using the Born test on rabbits.展开更多
OBJECTIVE: To evaluate the anti-platelet aggregation effects of extracts from 31 Traditional Chinese Medicines(TCM) with the property of activating blood and resolving stasis in terms of TCM theory.METHODS: The 31 TCM...OBJECTIVE: To evaluate the anti-platelet aggregation effects of extracts from 31 Traditional Chinese Medicines(TCM) with the property of activating blood and resolving stasis in terms of TCM theory.METHODS: The 31 TCMs extracts were prepared using water, 90% ethanol and ethyl acetate., and the effects on anti-platelet aggregation were tested on a platelet aggregation analyzer in vitro with adenosine 5'-diphosphate, bovine thrombin and arachi-donic acid(AA) as aggregation inducers, respectively. Aspirin was the positive control.RESULTS: Lots of the tested TCMs had inhibitory effects with concentration-dependent manner on platelet aggregations induced by various agonists.Especially, some of the TCMs such as Chuanxiong(Rhizoma Chuanxiong), Yanhusuo(Rhizoma Corydalis Yanhusuo) and Danshen(Radix Salviae Miltiorrhizae) showed good anti-platelet aggregation effect similar or higher than that in positive control group.CONCLUSION: The study provided scientific references that several TCMs such as Chuanxiong(Rhizoma Chuanxiong), Yanhusuo(Rhizoma Corydalis Yanhusuo) and Danshen(Radix Salviae Miltiorrhizae),possess the property of anti-platelet aggregation.展开更多
In addition to esterasic activity, phospholipase A<sub>2</sub> （PLA<sub>2</sub>） from snake venom possesses various physiological activities and toxicities, such as hemolysis, anticoagulation...In addition to esterasic activity, phospholipase A<sub>2</sub> （PLA<sub>2</sub>） from snake venom possesses various physiological activities and toxicities, such as hemolysis, anticoagulation, platelet function, presynaptic toxicity, muscular toxicity. It has been found that the venom from Agkistrodon halys Pallas has three homologous PLA<sub>2</sub>, which are quite different from each other in enzymatic activity, presynaptic toxicity, platelet function, hemolysis and anticoagulation. For example, the neutral PLA<sub>2</sub> has strong presynaptic toxicity, but no platelet function. On the contrary, the acidic PLA<sub>2</sub> can inhibit the platelet aggregation,展开更多
Objective:This study was devoted to identifying natural thrombin inhibitors from traditional Chinese medicine(TCM)and evaluating its biological activity in vitro and binding characteristics.Methods:A combination strat...Objective:This study was devoted to identifying natural thrombin inhibitors from traditional Chinese medicine(TCM)and evaluating its biological activity in vitro and binding characteristics.Methods:A combination strategy containing molecular docking,thrombin inhibition assay,surface plasmon resonance(SPR)and molecular dynamics simulation were applied to verify the study result.Results:Gallic acid was confirmed as a direct thrombin inhibitor with IC;of 9.07μmol/L and showed a significant inhibitory effect on thrombin induced platelet aggregation.SPR-based binding studies demonstrated that gallic acid interacted with thrombin with a KDvalue of 8.29μmol/L.Molecular dynamics and binding free energy analysis revealed that thrombin-gallic acid system attained equilibrium rapidly with very low fluctuations,the calculated binding free energies was-14.61 kcal/mol.Ala230,Glu232,Ser235,Gly258 and Gly260 were the main amino acid residues responsible for thrombin inhibition by gallic acid,providing a mechanistic basis for further optimization.Conclusion:This study proved that gallic acid is a direct thrombin inhibitor with platelet aggregation inhibitory effect,which could provide a basis for the follow-up research and development for novel thrombin inhibitors.展开更多
OBJECTIVE: Low or moderate consumption of red wine has a greater benefit than the consumption of other beverages in the prevention of atherosclerosis and coronary heart disease and this is increasingly attributed to t...OBJECTIVE: Low or moderate consumption of red wine has a greater benefit than the consumption of other beverages in the prevention of atherosclerosis and coronary heart disease and this is increasingly attributed to the polyphenol compounds in red wine, such as resveratrol. In the present study, we investigated the effect of resveratrol on platelet aggregation in vitro and in vivo. METHODS: Platelet aggregation in rabbits and normal subjects was measured using Born's method. RESULTS: Resveratrol, at 10 - 1000 micromol/L, significantly inhibited platelet aggregation in vitro induced by collagen, thrombin, and ADP in healthy subjects. The inhibitory effect was concentration-dependent. Hypercholesterolemia induced by high-cholesterol diet enhanced ADP-induced platelet aggregation. Resveratrol 4 mg x kg(-1) x d(-1) inhibited ADP-induced platelet aggregation in vivo despite no changes in serum lipid levels. CONCLUSIONS: Resveratrol inhibits platelet aggregation both in vitro and in vivo. This may be one of the mechanisms by which resveratrol prevents atherosclerosis.展开更多
基金This project was supported by Shandong Natural Science Foundation （Y2003C11）Shandong Science ＆ Technology Bureau Foundation and Jinan Excellent Young Scientist Program.
文摘A series of novel ligustrazine derivatives were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H NMR and ESI-MS. The preliminary antiplatelet aggregation screening results demonstrated that the compounds 7a, 7b and 7c showed higher potency than ligustrazine.
文摘A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.
基金KZ acknowledges supports from the National Young Scholar Award of the NSFC(#30125043)from the Chung Kong Scholars Program administered by the Ministry of Education,PRC and the Li Ka Shing Foundation,Hong Kong.
文摘A series of arylsulfonamide and arylamide derivatives have been prepared from anisole in good yields. The structures of those compounds were confirmed by 1H-NMR and MS analysis. Their activities against platelet aggregation were tested in vitro by using the Born test on rabbits.
基金the National Natural Science Foundation of China(Magnetic Nanoparticles-based Cell Affinity Capillary Electrochromatography and Its Applications,No.21275169Screening of Bioactive Compounds From Typical Huoxue Huayu Medicine by Platelet Based Capillary Electrochromatography,No.81202886)+1 种基金the Fundamental Research Funds for the Central Universities(Study on the Quality Control Method for the Animal Glue Medicine,No.CQDXWL-2012-028)the Chongqing Postdoctoral Funds(No.RC20120027)
文摘OBJECTIVE: To evaluate the anti-platelet aggregation effects of extracts from 31 Traditional Chinese Medicines(TCM) with the property of activating blood and resolving stasis in terms of TCM theory.METHODS: The 31 TCMs extracts were prepared using water, 90% ethanol and ethyl acetate., and the effects on anti-platelet aggregation were tested on a platelet aggregation analyzer in vitro with adenosine 5'-diphosphate, bovine thrombin and arachi-donic acid(AA) as aggregation inducers, respectively. Aspirin was the positive control.RESULTS: Lots of the tested TCMs had inhibitory effects with concentration-dependent manner on platelet aggregations induced by various agonists.Especially, some of the TCMs such as Chuanxiong(Rhizoma Chuanxiong), Yanhusuo(Rhizoma Corydalis Yanhusuo) and Danshen(Radix Salviae Miltiorrhizae) showed good anti-platelet aggregation effect similar or higher than that in positive control group.CONCLUSION: The study provided scientific references that several TCMs such as Chuanxiong(Rhizoma Chuanxiong), Yanhusuo(Rhizoma Corydalis Yanhusuo) and Danshen(Radix Salviae Miltiorrhizae),possess the property of anti-platelet aggregation.
文摘In addition to esterasic activity, phospholipase A<sub>2</sub> （PLA<sub>2</sub>） from snake venom possesses various physiological activities and toxicities, such as hemolysis, anticoagulation, platelet function, presynaptic toxicity, muscular toxicity. It has been found that the venom from Agkistrodon halys Pallas has three homologous PLA<sub>2</sub>, which are quite different from each other in enzymatic activity, presynaptic toxicity, platelet function, hemolysis and anticoagulation. For example, the neutral PLA<sub>2</sub> has strong presynaptic toxicity, but no platelet function. On the contrary, the acidic PLA<sub>2</sub> can inhibit the platelet aggregation,
基金Independent Project of Minzu University of China(No.2020QNPY95)Open Project from Beijing Key Lab of Traditional Chinese Medicine Collateral Disease Theory Research in 2021+1 种基金Key Laboratory of Ethnomedicine(Minzu University of China),Ministry of Education(No.KLEMZZ202005)National and Local Joint Engineering Research Center for Mongolian Medicine(No.MDK2020004)。
文摘Objective:This study was devoted to identifying natural thrombin inhibitors from traditional Chinese medicine(TCM)and evaluating its biological activity in vitro and binding characteristics.Methods:A combination strategy containing molecular docking,thrombin inhibition assay,surface plasmon resonance(SPR)and molecular dynamics simulation were applied to verify the study result.Results:Gallic acid was confirmed as a direct thrombin inhibitor with IC;of 9.07μmol/L and showed a significant inhibitory effect on thrombin induced platelet aggregation.SPR-based binding studies demonstrated that gallic acid interacted with thrombin with a KDvalue of 8.29μmol/L.Molecular dynamics and binding free energy analysis revealed that thrombin-gallic acid system attained equilibrium rapidly with very low fluctuations,the calculated binding free energies was-14.61 kcal/mol.Ala230,Glu232,Ser235,Gly258 and Gly260 were the main amino acid residues responsible for thrombin inhibition by gallic acid,providing a mechanistic basis for further optimization.Conclusion:This study proved that gallic acid is a direct thrombin inhibitor with platelet aggregation inhibitory effect,which could provide a basis for the follow-up research and development for novel thrombin inhibitors.
文摘OBJECTIVE: Low or moderate consumption of red wine has a greater benefit than the consumption of other beverages in the prevention of atherosclerosis and coronary heart disease and this is increasingly attributed to the polyphenol compounds in red wine, such as resveratrol. In the present study, we investigated the effect of resveratrol on platelet aggregation in vitro and in vivo. METHODS: Platelet aggregation in rabbits and normal subjects was measured using Born's method. RESULTS: Resveratrol, at 10 - 1000 micromol/L, significantly inhibited platelet aggregation in vitro induced by collagen, thrombin, and ADP in healthy subjects. The inhibitory effect was concentration-dependent. Hypercholesterolemia induced by high-cholesterol diet enhanced ADP-induced platelet aggregation. Resveratrol 4 mg x kg(-1) x d(-1) inhibited ADP-induced platelet aggregation in vivo despite no changes in serum lipid levels. CONCLUSIONS: Resveratrol inhibits platelet aggregation both in vitro and in vivo. This may be one of the mechanisms by which resveratrol prevents atherosclerosis.
