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The norpurpureine alkaloid from Annona purpurea inhibits human platelet activation in vitro

Overview of attention for article published in Cellular & Molecular Biology Letters, April 2018
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Title
The norpurpureine alkaloid from Annona purpurea inhibits human platelet activation in vitro
Published in
Cellular & Molecular Biology Letters, April 2018
DOI 10.1186/s11658-018-0082-4
Pubmed ID
Authors

Gabriela Sánchez, Omar Estrada, Giovana Acha, Alfonso Cardozo, Franshelle Peña, Marie Christine Ruiz, Fabián Michelangeli, Claudia Alvarado-Castillo

Abstract

The leaves of Annona purpurea have yielded several alkaloids with anti-aggregation activities against rabbit platelets. This is promising in the search for agents that might act against platelets and reduce the incidence of cardiovascular diseases. Since significant differences in platelet function have been reported between human and animal platelets, a study focusing on the effect of A. purpurea extracts against human platelet activation is necessary. The compounds in an A. purpurea ethanolic extract underwent bio-guided fractionation and were used for in vitro human platelet aggregation assays to isolate the compounds with anti-platelet activity. The bioactive compounds were identified by spectroscopic analysis. Additional platelet studies were performed to characterize their action as inhibitors of human platelet activation. The benzylisoquinoline alkaloid norpurpureine was identified as the major anti-platelet compound. The IC50 for norpurpureine was 80 μM against platelets when stimulated with adenosine 5'-diphosphate (ADP), collagen and thrombin. It was pharmacologically effective from 20 to 220 μM. Norpurpureine (220 μM) exhibited its in vitro effectiveness in samples from 30 healthy human donors who did not take any drugs during the 2 weeks prior to the collection. Norpurpureine also gradually inhibited granule secretion and adhesion of activated platelets to immobilized fibrinogen. At the intra-platelet level, norpurpureine prevented agonist-stimulated calcium mobilization and cAMP reduction. Structure-activity relationship analysis indicates that the lack of a methyl group at the nitrogen seems to be key in the ability of the compound to interact with its molecular target. Norpurpureine displays a promising in vitro pharmacological profile as an inhibitor of human platelet activation. Its molecular target could be a common effector between Ca2+ and cAMP signaling, such as the PLC-PKC-Ca2+ pathway and PDEs. This needs further evaluation at the protein isoform level.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 11 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 11 100%

Demographic breakdown

Readers by professional status Count As %
Student > Postgraduate 2 18%
Student > Ph. D. Student 1 9%
Other 1 9%
Student > Doctoral Student 1 9%
Lecturer 1 9%
Other 2 18%
Unknown 3 27%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 2 18%
Biochemistry, Genetics and Molecular Biology 1 9%
Physics and Astronomy 1 9%
Neuroscience 1 9%
Chemistry 1 9%
Other 0 0%
Unknown 5 45%

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 19 April 2018.
All research outputs
#10,240,380
of 12,826,501 outputs
Outputs from Cellular & Molecular Biology Letters
#85
of 195 outputs
Outputs of similar age
#203,346
of 269,690 outputs
Outputs of similar age from Cellular & Molecular Biology Letters
#1
of 1 outputs
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So far Altmetric has tracked 195 research outputs from this source. They receive a mean Attention Score of 2.3. This one is in the 18th percentile – i.e., 18% of its peers scored the same or lower than it.
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