Evidence map›Paper›PMID 34448532›Full record

ArticleJournal of cellular and molecular medicine2021

A novel naphthalimide derivative reduces platelet activation and thrombus formation via suppressing GPVI.

Tzenge-Lien Shih, Kuan-Hung Lin, Ray-Jade Chen, Ting-Yu Chen, Wei-Ting Kao, Jen-Wei Liu, Hsueh-Hsiao Wang, Hsien-Yu Peng, Yu-Yo Sun, Wan-Jung Lu

Open access · goldAbstract read
In one paragraph

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.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.0field-weighted citation impact, top 23% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed, 10 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 5 institutions in 2 countries.

Tzenge-Lien ShihDepartment of Chemistry, Tamkang University, New Taipei City, Taiwan.
Kuan-Hung LinTraditional Herbal Medicine Research Center, Taipei Medical University Hospital, Taipei, Taiwan.
Ray-Jade ChenDivision of General Surgery, Department of Surgery, Taipei Medical University Hospital, Taipei, Taiwan.
Ting-Yu ChenDepartment of Pharmacology, School of Medicine, College of Medicine, Taipei Medical University, Taipei, Taiwan.
Wei-Ting KaoDepartment of Chemistry, Tamkang University, New Taipei City, Taiwan.
Jen-Wei LiuDepartment of Chemistry, Tamkang University, New Taipei City, Taiwan.
Hsueh-Hsiao WangDepartment of Medicine, Mackay Medical College, New Taipei City, Taiwan.
Hsien-Yu PengDepartment of Medicine, Mackay Medical College, New Taipei City, Taiwan.
Yu-Yo SunDepartment of Neuroscience, Center for Brain Immunology and Glia (BIG), University of Virginia School of Medicine, Charlottesville, VA, USA.
Wan-Jung LuTraditional Herbal Medicine Research Center, Taipei Medical University Hospital, Taipei, Taiwan.ORCID 0000-0001-7664-4740
Taipei Medical University Hospital · TWTamkang University · TWMackay Medical University · TWTaipei Medical University · TWUniversity of Virginia · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

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.

Indexed as

Adenosine TriphosphateAnimalsBlood PlateletsCalciumDisease Models, AnimalDose-Response Relationship, DrugHumansImmunohistochemistryMaleMiceMicrovesselsMolecular StructureNaphthalimidesPlatelet ActivationPlatelet AggregationPlatelet Aggregation InhibitorsAdenosine TriphosphateCalciumNaphthalimidesPlatelet Aggregation InhibitorsPlatelet Membrane Glycoproteinsplatelet membrane glycoprotein VIantiplatelet activitybleeding riskcollagennaphthalimide derivativesplatelet activationthrombus formation

Identifiers

PMID34448532
PMCPMC8500964
OpenAlexW3196122007

What Socratic holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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.