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Anticoagulant effects of an antidiabetic drug on monocytes in vitro
C E Henriksson1, M Hellum, K B F Haug
1Blood cell research group, Section for research, Department of Medical Biochemistry, Oslo University Hospital, Ullevaal, Oslo, Norway. carola.henriksson@medisin.uio.no
Introduction:
Monocyte- and microparticle (MP)-associated tissue factor (TF) is upregulated in diabetes. Lipopolysaccharide (LPS) induces expression of TF and alternatively spliced TF (asTF) and increases MP release from monocytes. Using LPS-stimulated TF-bearing human monocytes, we examined whether glibenclamide, a sulfonylurea used to treat diabetes type 2, might possess anticoagulant properties.
Methods:
We studied the effects of glibenclamide on cell- and supernatant-associated procoagulant activity (Factor Xa-generating assay and clot formation assay), on expression of TF and asTF (flow cytometry, RT-qPCR, western blot) and on cell viability and MP release (flow cytometry).
Results:
Glibenclamide dose-dependently decreased procoagulant activity of cells and supernatants. The reduction in cellular procoagulant activity coincided with reduced expression of TF and asTF in cells, whereas cell viability remained almost unchanged. The glibenclamide-induced reduction in procoagulant activity of supernatants appeared to be associated with a decreased number of released MPs.
Conclusions:
Reduction of monocyte- and supernatant-associated procoagulant activity by glibenclamide is associated with decreased expression of TF and asTF and possibly with a reduced MP number. Our data indicate that glibenclamide reduces the prothrombotic state in LPS-stimulated monocytes in vitro. Glibenclamide might therefore also have an anticoagulant effect in vivo, but this needs to be further evaluated.
Insights
Glibenclamide, a diabetes drug, reduces blood clotting factors in monocytes. This study shows it lowers tissue factor (TF) and microparticle release, suggesting potential anticoagulant benefits.
Area of Science:
- Cardiovascular Research
- Endocrinology
- Hematology
Background:
- Monocyte- and microparticle (MP)-associated tissue factor (TF) are elevated in diabetes.
- Lipopolysaccharide (LPS) stimulates TF, alternatively spliced TF (asTF), and MP release from monocytes.
- Glibenclamide is a sulfonylurea used for type 2 diabetes.
Purpose of the Study:
- To investigate the anticoagulant properties of glibenclamide in LPS-stimulated human monocytes.
- To assess glibenclamide's effect on TF and asTF expression and MP release.
Main Methods:
- Assessed procoagulant activity using Factor Xa generation and clot formation assays.
- Measured TF and asTF expression via flow cytometry, RT-qPCR, and Western blot.
- Evaluated cell viability and MP release using flow cytometry.
Main Results:
- Glibenclamide dose-dependently reduced monocyte and supernatant procoagulant activity.
- This reduction correlated with decreased TF and asTF expression, with minimal impact on cell viability.
- Supernatant procoagulant activity decrease was linked to reduced MP numbers.
Conclusions:
- Glibenclamide decreases monocyte-associated procoagulant activity by reducing TF and asTF expression and potentially MP release.
- The findings suggest glibenclamide mitigates the prothrombotic state in LPS-stimulated monocytes.
- Further in vivo studies are warranted to confirm glibenclamide's anticoagulant potential.
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