ArticleJournal of cellular and molecular medicine2021
A novel naphthalimide derivative reduces platelet activation and thrombus formation via suppressing GPVI.
Article in Journal of cellular and molecular medicine, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 10 citations in OpenAlex.
- Costunolide, a Sesquiterpene Lactone, Protects Against Platelet Activation and Thrombus Formation.Cells · 2026Article
- Abnormal activation of platelets and inflammation in smoking-induced rheumatoid arthritis is alleviated by 3,3'-diindolylmethane.Genes and immunity · 2025Article
- A naphthalimide derivative exerts potent antiplatelet and antithrombotic activities without a bleeding tendency.Frontiers in pharmacology · 2025Article
- Novel 1,8-Naphthalimide Derivatives Inhibit Growth and Induce Apoptosis in Human Glioblastoma.International journal of molecular sciences · 2024Article
- An Overview of Naphthylimide as Specific Scaffold for New Drug Discovery.Molecules (Basel, Switzerland) · 2024Review
- Article
- A novel naphthalimide derivative reduces platelet activation and thrombus formation via suppressing GPVI.Journal of cellular and molecular medicine · 2021Article
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Naphthalimide derivatives have multiple biological activities, including antitumour and anti-inflammatory activities. We previously synthesized several naphthalimide derivatives; of them, compound 5 was found to exert the strongest inhibitory effect on human DNA topoisomerase II activity. However, the effects of naphthalimide derivatives on platelet activation have not yet been investigated. Therefore, the mechanism underlying the antiplatelet activity of compound 5 was determined in this study. The data revealed that compound 5 (5-10 μM) inhibited collagen- and convulxin- but not thrombin- or U46619-mediated platelet aggregation, suggesting that compound 5 is more sensitive to the inhibition of glycoprotein VI (GPVI) signalling. Indeed, compound 5 could inhibit the phosphorylation of signalling molecules downstream of GPVI, followed by the inhibition of calcium mobilization, granule release and GPIIb/IIIa activation. Moreover, compound 5 prevented pulmonary embolism and prolonged the occlusion time, but tended to prolong the bleeding time, indicating that it can prevent thrombus formation but may increase bleeding risk. This study is the first to demonstrate that the naphthalimide derivative compound 5 exerts antiplatelet and antithrombotic effects. Future studies should modify compound 5 to synthesize more potent and efficient antiplatelet agents while minimizing bleeding risk, which may offer a therapeutic potential for cardiovascular diseases.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.