Effects of suramin on human platelet aggregation and Ca2+ mobilization induced by thrombin and other agonists

Athanassia Siafaka-Kapadai; Stanislaus Svetlov; Donald J. Hanahan; Martin A. Javors

doi:10.1016/S0024-3205(98)00451-2

Effects of suramin on human platelet aggregation and Ca²⁺ mobilization induced by thrombin and other agonists

Athanassia Siafaka-Kapadai, Stanislaus Svetlov, Donald J. Hanahan, Martin A. Javors

Department of Psychiatry & Behavioral Sciences

Research output: Contribution to journal › Article › peer-review

6 Scopus citations

Abstract

The purpose of this study was to investigate the effect of suramin, a polyanionic napthalene sulfonic acid, on human platelet aggregation and Ca²⁺ mobilization induced by various agonists. Our results show that suramin completely inhibited aggregation by thrombin, platelet activating factor (PAF), alkyllysophosphatidic acid (ALPA), or arachidonic acid in a concentration-dependent manner. The IC50 values of suramin for inhibition of aggregation by PAF, arachidonic acid, and thrombin were 76.7, 239, and 1.49 μg/ml, respectively. Ca²⁺ mobilization induced by thrombin was inhibited by suramin with an approximate IC50 value of 20 μg/ml. This concentration of suramin had no effect on PAF or oleic acid-induced Ca²⁺ mobilization. The mechanism by which suramin inhibits aggregation is not clear, but our results suggest that suramin inhibits the ligand-receptor interaction.

Original language	English (US)
Pages (from-to)	1769-1777
Number of pages	9
Journal	Life Sciences
Volume	63
Issue number	20
DOIs	https://doi.org/10.1016/S0024-3205(98)00451-2
State	Published - Oct 9 1998

Keywords

ALPA
Arachidonic acid
Ca mobilization
PAF
Platelet aggregation
Suramin
Thrombin

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

Access to Document

10.1016/S0024-3205(98)00451-2

Cite this

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title = "Effects of suramin on human platelet aggregation and Ca2+ mobilization induced by thrombin and other agonists",

abstract = "The purpose of this study was to investigate the effect of suramin, a polyanionic napthalene sulfonic acid, on human platelet aggregation and Ca2+ mobilization induced by various agonists. Our results show that suramin completely inhibited aggregation by thrombin, platelet activating factor (PAF), alkyllysophosphatidic acid (ALPA), or arachidonic acid in a concentration-dependent manner. The IC50 values of suramin for inhibition of aggregation by PAF, arachidonic acid, and thrombin were 76.7, 239, and 1.49 μg/ml, respectively. Ca2+ mobilization induced by thrombin was inhibited by suramin with an approximate IC50 value of 20 μg/ml. This concentration of suramin had no effect on PAF or oleic acid-induced Ca2+ mobilization. The mechanism by which suramin inhibits aggregation is not clear, but our results suggest that suramin inhibits the ligand-receptor interaction.",

keywords = "ALPA, Arachidonic acid, Ca mobilization, PAF, Platelet aggregation, Suramin, Thrombin",

author = "Athanassia Siafaka-Kapadai and Stanislaus Svetlov and Hanahan, {Donald J.} and Javors, {Martin A.}",

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T1 - Effects of suramin on human platelet aggregation and Ca2+ mobilization induced by thrombin and other agonists

AU - Siafaka-Kapadai, Athanassia

AU - Svetlov, Stanislaus

AU - Hanahan, Donald J.

AU - Javors, Martin A.

PY - 1998/10/9

Y1 - 1998/10/9

N2 - The purpose of this study was to investigate the effect of suramin, a polyanionic napthalene sulfonic acid, on human platelet aggregation and Ca2+ mobilization induced by various agonists. Our results show that suramin completely inhibited aggregation by thrombin, platelet activating factor (PAF), alkyllysophosphatidic acid (ALPA), or arachidonic acid in a concentration-dependent manner. The IC50 values of suramin for inhibition of aggregation by PAF, arachidonic acid, and thrombin were 76.7, 239, and 1.49 μg/ml, respectively. Ca2+ mobilization induced by thrombin was inhibited by suramin with an approximate IC50 value of 20 μg/ml. This concentration of suramin had no effect on PAF or oleic acid-induced Ca2+ mobilization. The mechanism by which suramin inhibits aggregation is not clear, but our results suggest that suramin inhibits the ligand-receptor interaction.

AB - The purpose of this study was to investigate the effect of suramin, a polyanionic napthalene sulfonic acid, on human platelet aggregation and Ca2+ mobilization induced by various agonists. Our results show that suramin completely inhibited aggregation by thrombin, platelet activating factor (PAF), alkyllysophosphatidic acid (ALPA), or arachidonic acid in a concentration-dependent manner. The IC50 values of suramin for inhibition of aggregation by PAF, arachidonic acid, and thrombin were 76.7, 239, and 1.49 μg/ml, respectively. Ca2+ mobilization induced by thrombin was inhibited by suramin with an approximate IC50 value of 20 μg/ml. This concentration of suramin had no effect on PAF or oleic acid-induced Ca2+ mobilization. The mechanism by which suramin inhibits aggregation is not clear, but our results suggest that suramin inhibits the ligand-receptor interaction.

KW - ALPA

KW - Arachidonic acid

KW - Ca mobilization

KW - PAF

KW - Platelet aggregation

KW - Suramin

KW - Thrombin

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