- |||||||||| Clinical, Journal: Platelet-Reactive Antibodies in Patients after Ischaemic Stroke-An Epiphenomenon or a Natural Protective Mechanism. (Pubmed Central) - Mar 3, 2021
Antibodies from stroke sera reacted more strongly with activated platelets (p = 0.031) and inhibited platelet aggregation by up to 30.1 ± 2.8% (p < 0.001), suggesting the potential to interfere with thrombus formation. In conclusion, platelet-reactive antibodies can be found in patients soon after ischaemic stroke and correlate with better short-term outcomes, suggesting a potential novel mechanism limiting thrombosis.
- |||||||||| Review, Journal: Callicarpa nudiflora Hook. & Arn.: A comprehensive review of its phytochemistry and pharmacology. (Pubmed Central) - Feb 27, 2021
Different types of compounds in Callicarpa nudiflora were summarized as follow: a) diterpenoid compounds can inhibit the generation of nitric oxide (NO) for exerting the function of anti-inflammation; b) triterpene compounds can play a role of anti-thrombus via inhibiting platelet aggregation and oleanane type and arbutane type pentacyclic triterpenes have the hepatoprotective activities; c) iridoid glycosides have cytotoxicity to tumor cells, and phenylpropanoids compounds have an antioxidant effect and could improve the function of memory. Our group further studied the antiviral activities of Callicarpa nudiflora finding that it has significant effects on RSV, EV71, COXB5, and HSV-1.
- |||||||||| Journal: CKD Increases Carbonylation of HDL and Is Associated with Impaired Antiaggregant Properties. (Pubmed Central) - Feb 25, 2021
Our study suggests the limited benefit of systematic CT head scan as a standard practice for the management of mTBI patients under antithrombotic therapy. HDL from CKD rabbits and patients on hemodialysis exhibited an impaired ability to inhibit platelet aggregation, suggesting that altered HDL properties may contribute to the increased cardiovascular risk in this population.
- |||||||||| MitoQ (mitoquinone) / Antipodean
Journal: Mitoquinone (MitoQ) Inhibits Platelet Activation Steps by Reducing ROS Levels. (Pubmed Central) - Feb 23, 2021 Additionally, in platelets stimulated with antimycin A and collagen MitoQ significantly decreased ROS production. Our findings showed, for the first time, an antiplatelet effect of MitoQ that is probably associated with its mitochondrial antioxidant effect.
- |||||||||| Bay11-7082 / InvivoGen, MG132 / Jilin University, Dorothy M. Davis Heart and Lung Research Institute, bisindolylmaleimide IX (RO-31-8220) / Roche
Preclinical, Journal: Regulation of Human Platelet Activation and Prevention of Arterial Thrombosis in Mice by Auraptene through Inhibition of NF-κB Pathway. (Pubmed Central) - Feb 18, 2021 MG-132 (an inhibitor of proteasome) and BAY11-7082 (an inhibitor of IκB kinase; IKK), obviously inhibited platelet aggregation; however, BAY11-7082 exhibited more potent activity than MG-132 in this reaction...To investigate cellular signaling events between PLCγ2-PKC and NF-κB, we found that BAY11-7082 abolished PLCγ2-PKC activation; nevertheless, neither U73122 nor Ro31-8220 had effect on NF-κB activation...For in vivo study, auraptene prolonged the occlusion time of platelet plug in mice. In conclusion, we propose a novel inhibitory pathway of NF-κB-mediated PLCγ2-PKC activation by auraptene in human platelets, and further supported that auraptene possesses potent activity for thromboembolic diseases.
- |||||||||| Preclinical, Journal: Complement 5 Inhibition Ameliorates Hepatic Ischemia/reperfusion Injury in Mice, Dominantly via the C5a-mediated Cascade. (Pubmed Central) - Feb 9, 2021
Anti-C5 antibody significantly ameliorated hepatic IRI, predominantly via the C5a-mediated cascade, not only by inhibiting platelet aggregation during the early phase, but also by attenuating the activation of infiltrating macrophages/neutrophils and hepatocyte apoptosis in the late phase of reperfusion. Given its efficacy, clinical availability, and controllability, C5-targeted intervention may provide a novel therapeutic strategy against hepatic IRI.
- |||||||||| Integrilin (eptifibatide) / Takeda
Journal: Inhibition of platelet adhesion, thrombus formation, and fibrin formation by a potent αIIbβ3 integrin inhibitor from ticks. (Pubmed Central) - Feb 5, 2021 Whole-blood thrombus formation was investigated by perfusing blood over collagen I with and without tissue factor at a high wall-shear rate (1000 s) in the presence of disagregin, RGD-disagregin, or eptifibatide...Both αIIbβ3-blocking disagregins have a strong potential to suppress collagen-tissue factor-mediated platelet adhesion, thrombus formation, and fibrin formation. Both disagregins can be seen as potential new αIIbβ3 inhibitors.
- |||||||||| Journal: Lack of an effective drug therapy for abdominal aortic aneurysm. (Pubmed Central) - Feb 2, 2021
Past trials were noted to have a number of design issues, particularly small sample sizes and limited follow-up. Much larger trials are needed to properly test potential therapeutic approaches if a convincingly effective medical therapy for AAA is to be identified.
- |||||||||| aspirin / Generic mfg., clopidogrel / Generic mfg., prasugrel / Generic mfg.
Clinical, Journal: Bedside testing of CYP2C19 gene for treatment of patients with PCI with antiplatelet therapy. (Pubmed Central) - Jan 13, 2021 P4 The primary goal of this trial is to study the benefits of treating only those patients that cannot activate clopidogrel with an alternative that has shown to be a more effective platelet inhibitor and does not require bioactivation by the cytochrome P450 enzyme. We expect an improvement in net clinical benefit outcome in the active arm patients, thus supporting pharmacogenetic testing in PCI patients post STEMI.
- |||||||||| setanaxib (GKT831) / Genkyotex
Journal: VAS2870 and VAS3947 attenuate platelet activation and thrombus formation via a NOX-independent pathway downstream of PKC. (Pubmed Central) - Jan 2, 2021 Unlike VAS compounds, concurrent inhibition of NOX1, 2, and 4 by treatment with ML171, GSK2795039, and GKT136901/GKT137831 did not affect thrombin and U46619-induced platelet aggregation...This study is the first to demonstrate that, in addition to inhibiting NOX activity, VAS compounds reduced platelet activation and thrombus formation through a NOX-independent pathway downstream of PKC. These findings also indicate that VAS compounds may be safe and potentially therapeutic agents for treating patients with cardiovascular diseases.
- |||||||||| clopidogrel / Generic mfg., prasugrel / Generic mfg.
Retrospective data, Journal, Adverse events: Comparison of Hemorrhagic Risk between Prasugrel and Clopidogrel: a Retrospective Study using Adverse Drug Event Reporting Databases. (Pubmed Central) - Dec 30, 2020 After adjustment for known confounders including age, sex, and concomitant medications (aspirin, anticoagulants, and proton pump inhibitors), the hemorrhagic risk of prasugrel compared with clopidogrel remained significant (adjusted reporting odds ratios [95% CI] for total, intracranial, and gastrointestinal hemorrhagic events = 2.42 [1.97-2.96], 2.45 [1.85-3.24], and 2.27 [1.73-2.97] in JADER, and 2.21 [2.09-2.34], 1.21 [1.09-1.33], and 1.41 [1.29-1.54] in FAERS). The hemorrhagic risk was found to be greater with prasugrel than clopidogrel in real-world patients, including Japanese patients.
- |||||||||| Journal: The G-protein βγ subunits regulate platelet function. (Pubmed Central) - Dec 16, 2020
Our findings demonstrate, for the first time, that Gβγ subunits directly regulate GPCR-dependent platelet function, in vitro and in vivo. Moreover, these data highlight Gβγ as a novel therapeutic target for managing thrombotic disorders.
- |||||||||| deferiprone / Generic mfg.
Journal: Antiplatelet activity of deferiprone through cyclooxygenase-1 inhibition. (Pubmed Central) - Nov 27, 2020 Moreover, the results from molecular docking showed that deferiprone interacted closely with key residues in the peroxidase active site of COX-1. These results suggested that deferiprone possessed antiplatelet activity mainly through the inhibition of COX-1 activity.
- |||||||||| epinephrine / Generic mfg.
Journal: Role of Kv1.3 Channels in Platelet Functions and Thrombus Formation. (Pubmed Central) - Nov 26, 2020 We showed specific inhibition of Kv1.3 by the novel monoclonal antibody 6E12#15 suppressed platelet functions and platelet-dependent thrombosis through modulating platelet [Ca] elevation. These results indicate that Kv1.3 could act as a promising therapeutic target for antiplatelet therapies.
- |||||||||| Journal: Antiplatelet Effect of Carbon Monoxide Is Mediated by NAD and ATP Depletion. (Pubmed Central) - Nov 26, 2020
These results indicate that Kv1.3 could act as a promising therapeutic target for antiplatelet therapies. The antiplatelet effect of CO is mediated by inhibition of mitochondrial respiration-attributed to the inhibition of cytochrome c oxidase, and inhibition of glycolysis-ascribed to cytosolic NAD+ depletion.
- |||||||||| Journal: Resveratrol inhibits Ca signals and aggregation of platelets. (Pubmed Central) - Nov 26, 2020
The antiplatelet effect of CO is mediated by inhibition of mitochondrial respiration-attributed to the inhibition of cytochrome c oxidase, and inhibition of glycolysis-ascribed to cytosolic NAD+ depletion. The results suggest that resveratrol inhibits thrombin-induced platelet aggregation through decreasing Ca release from its stores and inhibiting store-operated Ca influx into platelets.
- |||||||||| Review, Journal: Mechanisms of the protective effects of nitrate and nitrite in cardiovascular and metabolic diseases. (Pubmed Central) - Nov 25, 2020
In this review, we focus on nitrate/nitrite bioactivation, as well as the potential mechanisms for nitrate/nitrite-mediated effects on cardiovascular and metabolic diseases. Understanding how dietary nitrate and nitrite induce beneficial effect on cardiovascular and metabolic diseases could open up novel therapeutic opportunities in clinical practice.
- |||||||||| aspirin / Generic mfg.
Clinical, Journal: Role of aspirin and statin therapy in patients with cerebral cavernous malformations. (Pubmed Central) - Nov 12, 2020 A GLMM showed that patients in the combined therapy group to have significantly lower odds of having an acute hemorrhage at diagnosis compared to the reference group of no therapy (OR 0.24; 95% CI 0.09-0.59; P = 0.002). Patients with a CCM receiving therapy with both aspirin and statins were less likely to present at diagnosis with acute hemorrhage.
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