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
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
目的评价替罗非班联合双抗治疗进展性脑卒中(progressive ischemic stroke,PIS)的有效性及安全性。方法检索中国知网、万方数据库、维普数据库、中国生物医学文献数据库、PubMed、Web of Science、Scopus、EMbase、Cochrane图书馆数据库...目的评价替罗非班联合双抗治疗进展性脑卒中(progressive ischemic stroke,PIS)的有效性及安全性。方法检索中国知网、万方数据库、维普数据库、中国生物医学文献数据库、PubMed、Web of Science、Scopus、EMbase、Cochrane图书馆数据库,检索时间设定为自建库至2022-10-31,语种设定为中文和英文,按纳入文献和排除文献标准筛选常规治疗+替罗非班联合双抗(简称试验组)与常规治疗+双抗治疗(简称对照组)PIS患者的对照研究,采用Meta分析替罗非班联合双抗治疗PIS患者的疗效及安全性。结果共纳入15项研究,共计1302例患者,其中6项为队列研究,9项为随机对照试验(randomized controlled trial,RCT)。Meta分析结果显示,试验组美国国立卫生院卒中量表(National Institute of Health stroke scale,NIHSS)评分低于对照组(MD=-2.47,95%CI:-2.99~-1.94;P<0.01),试验组预后良好率高于对照组(OR=1.96,95%CI:1.03~3.71;P=0.04),试验组血清超敏C反应蛋白(hs-CRP)水平(MD=-0.72,95%CI:-0.95~-0.49)、血小板聚集率(MD=-2.72,95%CI:-4.82~-0.62)、纤维蛋白原水平(MD=-0.50,95%CI:-0.66~-0.34)均低于对照组(均P<0.01),而两组间脑出血发生率差异无统计学意义(OR=1.59,95%CI:0.53~4.83;P=0.41),但试验组其他系统出血发生率高于对照组(OR=1.78,95%CI:1.03~3.09;P=0.04)。结论替罗非班联合双抗治疗PIS有效,能改善PIS患者早期神经功能缺损症状及3个月时的功能预后,能降低PIS患者血清hs-CRP水平,能抑制血小板聚集,不增加脑出血的发生率,但增加其他系统出血的发生率。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
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.
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.
文摘目的评价替罗非班联合双抗治疗进展性脑卒中(progressive ischemic stroke,PIS)的有效性及安全性。方法检索中国知网、万方数据库、维普数据库、中国生物医学文献数据库、PubMed、Web of Science、Scopus、EMbase、Cochrane图书馆数据库,检索时间设定为自建库至2022-10-31,语种设定为中文和英文,按纳入文献和排除文献标准筛选常规治疗+替罗非班联合双抗(简称试验组)与常规治疗+双抗治疗(简称对照组)PIS患者的对照研究,采用Meta分析替罗非班联合双抗治疗PIS患者的疗效及安全性。结果共纳入15项研究,共计1302例患者,其中6项为队列研究,9项为随机对照试验(randomized controlled trial,RCT)。Meta分析结果显示,试验组美国国立卫生院卒中量表(National Institute of Health stroke scale,NIHSS)评分低于对照组(MD=-2.47,95%CI:-2.99~-1.94;P<0.01),试验组预后良好率高于对照组(OR=1.96,95%CI:1.03~3.71;P=0.04),试验组血清超敏C反应蛋白(hs-CRP)水平(MD=-0.72,95%CI:-0.95~-0.49)、血小板聚集率(MD=-2.72,95%CI:-4.82~-0.62)、纤维蛋白原水平(MD=-0.50,95%CI:-0.66~-0.34)均低于对照组(均P<0.01),而两组间脑出血发生率差异无统计学意义(OR=1.59,95%CI:0.53~4.83;P=0.41),但试验组其他系统出血发生率高于对照组(OR=1.78,95%CI:1.03~3.09;P=0.04)。结论替罗非班联合双抗治疗PIS有效,能改善PIS患者早期神经功能缺损症状及3个月时的功能预后,能降低PIS患者血清hs-CRP水平,能抑制血小板聚集,不增加脑出血的发生率,但增加其他系统出血的发生率。
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.
