| Antiplatelet effects of piplartine, an alkamide isolated from Piper tuberculatum: possible involvement of cyclooxygenase blockade and antioxidant activity. | |
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MedLine Citation:
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PMID: 19298699 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: The Journal of pharmacy and pharmacology Volume: 61 ISSN: 0022-3573 ISO Abbreviation: J. Pharm. Pharmacol. Publication Date: 2009 Apr |
Date Detail:
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Created Date: 2009-03-20 Completed Date: 2009-06-08 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0376363 Medline TA: J Pharm Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 511-5 Citation Subset: IM |
Affiliation:
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Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, Brazil. |
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| MeSH Terms | |
Descriptor/Qualifier:
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Adenosine Diphosphate
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pharmacology Antioxidants / pharmacology* Arachidonic Acid / pharmacology Collagen / pharmacology Cyclooxygenase Inhibitors / pharmacology* Drug Interactions Humans Piperaceae / chemistry* Piperidones / pharmacology* Plant Roots / chemistry Platelet Aggregation / drug effects* Platelet-Rich Plasma Thrombin / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Antioxidants; 0/Cyclooxygenase Inhibitors; 0/Piperidones; 0/piplartine; 506-32-1/Arachidonic Acid; 58-64-0/Adenosine Diphosphate; 9007-34-5/Collagen; EC 3.4.21.5/Thrombin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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