VAS2870 and VAS3947 attenuate platelet activation and thrombus formation via a NOX-independent pathway downstream of PKC.

NADPH oxidase (NOX) enzymes are involved in a various physiological and pathological processes such as platelet activation and inflammation. Interestingly, we found that the pan-NOX inhibitors VAS compounds (VAS2870 and its analog VAS3947) exerted a highly potent antiplatelet effect. 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.

Embelin as a Novel Inhibitor of PKC in the Prevention of Platelet Activation and Thrombus Formation.

Embelin is a quinone derivative and found in the fruits of Burm.f. Embelin has been identified as a small molecular inhibitor of X-chromosome-linked inhibitor of apoptosis proteins, and has multiple biological activities, including antioxidation, anti-inflammation, and antitumor effects.

An Antithrombotic Strategy by Targeting Phospholipase D in Human Platelets.

Phospholipase D (PLD) is involved in many biological processes. PLD1 plays a crucial role in regulating the platelet activity of mice; however, the role of PLD in the platelet activation of humans remains unclear. Therefore, we investigated whether PLD is involved in the platelet activation of humans.

Licochalcone A attenuates glioma cell growth in vitro and in vivo through cell cycle arrest.

Licochalcone A (LA), an active ingredient of licorice, has multiple biological activities, including antioxidative and anti-inflammatory activities. Although LA exerts antitumor effects in various cancer cells, its role in gliomas remains unclear. Therefore, this study determined whether LA inhibits glioma cell growth in vitro and in vivo.

Hinokitiol inhibits platelet activation ex vivo and thrombus formation in vivo.

Hinokitiol is a tropolone-related bioactive compound that has been used in hair tonics, cosmetics, and food as an antimicrobial agent. Recently, hinokitiol has attracted considerable interest because of its anticancer activities. Platelet activation plays a crucial role in atherothrombotic processes.

Suppression of NF-κB signaling by andrographolide with a novel mechanism in human platelets: regulatory roles of the p38 MAPK-hydroxyl radical-ERK2 cascade.

Andrographolide, a novel nuclear factor-κB (NF-κB) inhibitor, is isolated from leaves of Andrographis paniculata. Platelet activation is relevant to a variety of coronary heart diseases. Our recent studies revealed that andrographolide possesses potent antiplatelet activity by activating the endothelial nitric oxide synthase (eNOS)-NO-cyclic GMP pathway.

Potent antiplatelet activity of sesamol in an in vitro and in vivo model: pivotal roles of cyclic AMP and p38 mitogen-activated protein kinase.

Sesamol is a potent phenolic antioxidant which possesses antimutagenic, antihepatotoxic and antiaging properties. Platelet activation is relevant to a variety of acute thrombotic events and coronary heart diseases. There have been few studies on the effect of sesamol on platelets.

Comparison of the relative activities of inducing platelet apoptosis stimulated by various platelet-activating agents.

Apoptosis-like events are known to occur in anuclear platelets. Although the mechanisms responsible for these events are still not completely understood, studies suggested that some platelet agonists can activate platelet apoptosis. However, the relative activities of various platelet agonists in inducing apoptosis have not yet been investigated.