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Mar. Drugs 2015, 13(11), 6774-6791;

The Marine-Derived Kinase Inhibitor Fascaplysin Exerts Anti-Thrombotic Activity

Institute for Clinical and Experimental Surgery, Saarland University, 66421 Homburg/Saar, Germany
Institute for Hemostasiology and Transfusion Medicine, Saarland University, 66421 Homburg/Saar, Germany
Author to whom correspondence should be addressed.
Academic Editors: Vitor H. Pomin and Paulo A.S. Mourão
Received: 8 July 2015 / Revised: 27 October 2015 / Accepted: 2 November 2015 / Published: 9 November 2015
(This article belongs to the Special Issue Marine Anticoagulants and Antithrombotics)
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Background: The marine-derived kinase inhibitor fascaplysin down-regulates the PI3K pathway in cancer cells. Since this pathway also plays an essential role in platelet signaling, we herein investigated the effect of fascaplysin on thrombosis. Methods: Fascaplysin effects on platelet activation, platelet aggregation and platelet-leukocyte aggregates (PLA) formation were analyzed by flow cytometry. Mouse dorsal skinfold chambers were used to determine in vivo the effect of fascaplysin on photochemically induced thrombus formation and tail-vein bleeding time. Results: Pre-treatment of platelets with fascaplysin reduced the activation of glycoprotein (GP)IIb/IIIa after protease-activated receptor-1-activating peptide (PAR-1-AP), adenosine diphosphate (ADP) and phorbol-12-myristate-13-acetate (PMA) stimulation, but did not markedly affect the expression of P-selectin. This was associated with a decreased platelet aggregation. Fascaplysin also decreased PLA formation after PMA but not PAR-1-AP and ADP stimulation. This may be explained by an increased expression of CD11b on leukocytes in PAR-1-AP- and ADP-treated whole blood. In the dorsal skinfold chamber model of photochemically induced thrombus formation, fascaplysin-treated mice revealed a significantly extended complete vessel occlusion time when compared to controls. Furthermore, fascaplysin increased the tail-vein bleeding time. Conclusion: Fascaplysin exerts anti-thrombotic activity, which represents a novel mode of action in the pleiotropic activity spectrum of this compound. View Full-Text
Keywords: fascaplysin; thrombosis; platelets; GPIIb/IIIa; P-selectin; leukocytes; CD11b; dorsal skinfold chamber fascaplysin; thrombosis; platelets; GPIIb/IIIa; P-selectin; leukocytes; CD11b; dorsal skinfold chamber

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Ampofo, E.; Später, T.; Müller, I.; Eichler, H.; Menger, M.D.; Laschke, M.W. The Marine-Derived Kinase Inhibitor Fascaplysin Exerts Anti-Thrombotic Activity. Mar. Drugs 2015, 13, 6774-6791.

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