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Chien-Ming Wu Shu-Chun Wu Wan-Jung Chung Hsien-Cheng Lin Kun-Tze Chen Yu-Chian Chen Mei-Feng Hsu Jwu-Maw Yang Jih-Pyang Wang Chun-Nan Lin 《International journal of molecular sciences》2007,8(8):830-841
The known flavonoids ginkgetin (1), taiwanhomoflavone A (2), taiwanhomoflavone B (3), and taiwanhomoflavone C (4) and eight known lignans: justicidin B (9), justicidin C (10), justicidin D (11), chinensinaphthol methyl ether (12), procumphthalide A (13), procumbenoside A (15), and ciliatosides A (16) and B (17) were isolated from Cephalotaxus wilsoniana and Justicia species, respectively. The antiplatelet effects of the above constituents on human platelet-rich plasma (PRP) were evaluated. Of the compounds tested on human PRP, compounds 1, 4, 9, and 11 showed inhibition of secondary aggregation induced by adrenaline. Compound 1 had an inhibitory effect on cyclooxygenase-1 (COX-1). Molecular docking studies revealed that 1 and the related compounds apigenin (5), cycloheterophyllin (6), broussoflavone F (7), and quercetin (8) were docked near the gate of active site of COX-1. It indicated that the antiplatelet effect of 1, 4, 9, and 11 is partially owed to suppression of COX-1 activity and reduced thromboxane formation. Flavonoids, 1, 5, 6, 7, and 8 may block the gate of the active site of COX-1 and interfere the conversion of arachidonic acid to prostaglandin (PG) H2 in the COX-1 active site. 相似文献
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Joanna Sikora Aleksandra Karczmarska-Wdzka Joanna Bugieda Przemysaw Sobczak 《International journal of molecular sciences》2022,23(3)
Ischemic stroke is a disease related to abnormal blood flow that leads to brain dysfunction. The early and late phases of the disease are distinguished. A distinction is made between the early and late stages of the disease, and the best effect in treating an ischemic stroke is usually achieved within the first hours after the onset of symptoms. This review looked at studies platelet activity monitoring studies to determine the risks and benefits of various approaches including antiplatelet therapy. A study was conducted on recently published literature based on PRISMA. This review includes 32 research articles directly addressing the importance of monitoring platelet function during antiplatelet therapy (dual or monotherapy) after ischemic stroke. In patients with transient ischemic attack or ischemic stroke, antiplatelet therapy can reduce the risk of stroke by 11–15%, assuming that patients respond well. Secondary prevention results are dependent on platelet reactivity, meaning that patients do not respond equally to antiplatelet therapy. It is very important that aspirin-resistant patients can benefit from the use of dual antiplatelet therapy. The individualized approach to secondary stroke prevention is to administer the most appropriate drug at the correct dose and apply the optimal therapeutic procedure to the individual patient. 相似文献
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Discovery of Aporphine Analogues as Potential Antiplatelet and Antioxidant Agents: Design,Synthesis, Structure–Activity Relationships,Biological Evaluations,and in silico Molecular Docking Studies
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Vashundhra Sharma Dr. Pradeep K. Jaiswal Dr. Surendra Kumar Dr. Manas Mathur Dr. Ajit K. Swami Dr. Dharmendra K. Yadav Prof. Sandeep Chaudhary 《ChemMedChem》2018,13(17):1817-1832
To explore the potential of aporphine alkaloids, a novel series of functionalized aporphine analogues with alkoxy (OCH3, OC2H5, OC3H7) functional groups at C1/C2 of ring A and an acyl (COCH3 and COPh) or phenylsulfonyl (SO2Ph and SO2C6H4‐3‐CH3) functionality at the N6 position of ring B of the aporphine scaffold were synthesized and evaluated for their arachidonic acid (AA)‐induced antiplatelet aggregation inhibitory activity and 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) free‐radical‐scavenging antioxidant activity, with acetylsalicylic acid and ascorbic acid as standard references, respectively. The preliminary structure–activity relationship related to AA‐induced platelet aggregation inhibitory activity results showed that the aporphine analogues 1‐[1,2,9,10‐tetramethoxy‐6a,7‐dihydro‐4H‐dibenzo[de,g]quinolin‐6(5H)‐yl]ethanone and 1‐[2‐(benzyloxy)‐1,9,10‐trimethoxy‐6a,7‐dihydro‐4H‐dibenzo[de,g]quinolin‐6(5H)‐yl]ethanone to be the best compounds of the series. Moreover, the DPPH free‐radical‐scavenging antioxidant activity results demonstrated that the aporphine analogues 1,2,9,10‐tetramethoxy‐6‐(methylsulfonyl)‐5,6,6a,7‐tetrahydro‐4H‐dibenzo[de,g]quinoline, 2‐ethoxy‐1,9,10‐trimethoxy‐6‐(methylsulfonyl)‐5,6,6a,7‐tetrahydro‐4H‐dibenzo[de,g]quinoline, 1‐ethoxy‐2,9,10‐trimethoxy‐6‐(methylsulfonyl)‐5,6,6a,7‐tetrahydro‐4H‐dibenzo[de,g]quinoline, 2,9,10‐trimethoxy‐6‐(methylsulfonyl)‐1‐propoxy‐5,6,6a,7‐tetrahydro‐4H‐dibenzo[de,g]quinoline, and 1‐(benzyloxy)‐2,9,10‐trimethoxy‐6‐(methylsulfonyl)‐5,6,6a,7‐tetrahydro‐4H‐dibenzo[de,g]quinoline were the best compounds of the series. Moreover, in silico molecular docking simulation studies of the active analogues were also performed. 相似文献
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Bibian M. E. Tullemans Alicia Veninga Delia I. Fernandez Maureen J. B. Aarts Johannes A. Eble Paola E. J. van der Meijden Johan W. M. Heemskerk Marijke J. E. Kuijpers 《International journal of molecular sciences》2021,22(20)
Current antiplatelet drugs for the treatment of arterial thrombosis often coincide with increased bleeding risk. Several tyrosine kinase inhibitors (TKIs) for cancer treatment inhibit platelet function, with minor reported bleeding symptoms. The aim of this study was to compare the antiplatelet properties of eight TKIs to explore their possible repurposing as antiplatelet drugs. Samples of whole blood, platelet-rich plasma (PRP), or isolated platelets from healthy donors were treated with TKI or the vehicle. Measurements of platelet aggregation, activation, intracellular calcium mobilization, and whole-blood thrombus formation under flow were performed. Dasatinib and sunitinib dose-dependently reduced collagen-induced aggregation in PRP and washed platelets; pazopanib, cabozantinib, and vatalanib inhibited this response in washed platelets only; and fostamatinib, axitinib, and lapatinib showed no/limited effects. Fostamatinib reduced thrombus formation by approximately 50% on collagen and other substrates. Pazopanib, sunitinib, dasatinib, axitinib, and vatalanib mildly reduced thrombus formation on collagen by 10–50%. Intracellular calcium responses in isolated platelets were inhibited by dasatinib (>90%), fostamatinib (57%), sunitinib (77%), and pazopanib (82%). Upon glycoprotein-VI receptor stimulation, fostamatinib, cabozantinib, and vatalanib decreased highly activated platelet populations by approximately 15%, while increasing resting populations by 39%. In conclusion, the TKIs with the highest affinities for platelet-expressed molecular targets most strongly inhibited platelet functions. Dasatinib, fostamatinib, sunitinib, and pazopanib interfered in early collagen receptor-induced molecular-signaling compared with cabozantinib and vatalanib. Fostamatinib, sunitinib, pazopanib, and vatalanib may be promising for future evaluation as antiplatelet drugs. 相似文献
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目的:调查分析老年医学科冠心病患者不同抗血小板药物服用及其临床病情。方法:本研究为一项单中心横断面研究,选取2021年12月至2022年6月在中南大学湘雅医院老年医学科心血管亚专科住院的冠心病患者,调查分析患者单用或双联抗血小板药物服用情况和临床病情资料。结果:共纳入347例冠心病患者,年龄为(65.2±10.1)岁,氯吡格雷是服用率最高的抗血小板药物,且随着冠脉靶病变支数的增加,氯吡格雷服用率明显增加(P<0.05);双联抗血小板治疗(dual antiplatelet therapy, DAPT)方案中阿司匹林联合氯吡格雷应用最为广泛(P<0.05)。在靶血管病变支数不同的各组中,阿司匹林服用率均高于吲哚布芬(P<0.05);与服用阿司匹林的患者比较,服用吲哚布芬的患者年龄大,血肌酐水平高,合并慢性胃病比例高,血小板聚集率水平高(P<0.05)。结论:氯吡格雷在冠心病患者中是最常用的抗血小板药物;在DAPT中阿司匹林联合氯吡格雷服用率最高;与阿司匹林相比,在合并慢性胃炎、血肌酐水平高和高龄患者中吲哚布芬服用率明显增加。 相似文献
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Theoretical chemistry methods have been used to study the molecular properties of antiplatelet agents (ticlopidine, clopidogrel, prasugrel, elinogrel, ticagrelor and cangrelor) and several thiol-containing active metabolites. The geometries and energies of most stable conformers of these drugs have been computed at the Becke3LYP/6-311++G(d,p) level of density functional theory. Computed dissociation constants show that the active metabolites of prodrugs (ticlopidine, clopidogrel and prasugrel) and drugs elinogrel and cangrelor are completely ionized at pH 7.4. Both ticagrelor and its active metabolite are present at pH = 7.4 in neutral undissociated form. The thienopyridine prodrugs ticlopidine, clopidogrel and prasugrel are lipophilic and insoluble in water. Their lipophilicity is very high (about 2.5–3.5 logP values). The polar surface area, with regard to the structurally-heterogeneous character of these antiplatelet drugs, is from very large interval of values of 3–255 Å2. Thienopyridine prodrugs, like ticlopidine, clopidogrel and prasugrel, with the lowest polar surface area (PSA) values, exhibit the largest absorption. A high value of polar surface area (PSA) of cangrelor (255 Å2) results in substantial worsening of the absorption in comparison with thienopyridine drugs. 相似文献
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Svetha Chunduri Jon E. Folstad Tushar J. Vachharajani 《Hemodialysis international. International Symposium on Home Hemodialysis》2017,21(4):453-471
The delicate balance of risk vs. benefit of using antiplatelet and antithrombotic agents in the general population is well established. The decision to use these agents in the end stage renal disease (ESRD) population remains complex and difficult. The concomitant association of a prothombotic state with high risk of bleeding in the ESRD population requires individualization and careful clinical judgment before implementing such therapy. There remains a paucity of clinical trials and lack of substantial evidence in literature for safe and effective use of antithrombotic drugs in patients with advanced chronic kidney disease. The current review summarizes the pros and cons of using antiplatelet and antithrombotic agents in primary and secondary prevention of cardiovascular events, evaluate the risks with routine use of anticoagulation for cerebrovascular stroke prevention with nonvalvular atrial fibrillation and role of newer oral anticoagulants as alternate agents in the dialysis population. 相似文献