Document Detail

Antiplatelet effects of piplartine, an alkamide isolated from Piper tuberculatum: possible involvement of cyclooxygenase blockade and antioxidant activity.
MedLine Citation:
PMID:  19298699     Owner:  NLM     Status:  MEDLINE    
OBJECTIVES: Piplartine (piperlongumine; 5,6-dihydro-1-[1-oxo-3-(3,4,5-trimethoxyphenyl]-2(1H) pyridinone) is an alkaloid amide isolated from Piper species (Piperaceae). It has been reported to show multiple pharmacological activities in vitro and in vivo. METHODS: We evaluated the in-vitro antiplatelet effect of piplartine isolated from the roots of P. tuberculatum, on human platelet aggregation induced in platelet-rich plasma by the agonists collagen, adenosine 5'-diphosphate (ADP), arachidonic acid (AA) and thrombin. KEY FINDINGS: Piplartine (100 mug/ml) caused a 30% inhibition in platelet aggregation when collagen was the agonist. At 200 mug/ml, piplartine significantly inhibited the aggregation induced by arachidonic acid (100%), collagen (59%) or ADP (52%) but not that induced by thrombin. The highest concentration of piplartine (300 mug/ml) inhibited thrombin- (37%), ADP- (71%) and collagen- (98%) induced aggregation. The inhibitory effect of piplartine on ADP-induced platelet aggregation was not modified by pretreatment with pentoxifylline (a phosphodiesterase inhibitor), L-arginine (a substrate for nitric oxide synthase) or ticlopidine (a P2Y(12) purinoceptor antagonist). However, aspirin, a well-known inhibitor of cyclooxygenase, greatly increased the inhibitory effect of piplartine on arachidonic-acid-induced platelet aggregation. CONCLUSIONS: The mechanism underlying the piplartine antiplatelet action is not totally clarified. It could be related to the inhibition of cyclooxgenase activity and a decrease in thromboxane A(2) formation, similar to that occurring with aspirin. This and other possible mechanisms require further study.
Juvenia B Fontenele; L Kalyne A M Leal; Edilberto R Silveira; F Helder Felix; Cícero F Bezerra Felipe; Glauce S B Viana
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  61     ISSN:  0022-3573     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  2009 Apr 
Date Detail:
Created Date:  2009-03-20     Completed Date:  2009-06-08     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  511-5     Citation Subset:  IM    
Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, Brazil.
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MeSH Terms
Adenosine Diphosphate / pharmacology
Antioxidants / pharmacology*
Arachidonic Acid / pharmacology
Collagen / pharmacology
Cyclooxygenase Inhibitors / pharmacology*
Drug Interactions
Piperaceae / chemistry*
Piperidones / pharmacology*
Plant Roots / chemistry
Platelet Aggregation / drug effects*
Platelet-Rich Plasma
Thrombin / pharmacology
Reg. No./Substance:
0/Antioxidants; 0/Cyclooxygenase Inhibitors; 0/Piperidones; 0/piplartine; 506-32-1/Arachidonic Acid; 58-64-0/Adenosine Diphosphate; 9007-34-5/Collagen; EC

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