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Capsaicin-induced death of human haematological malignant cell lines is independent of TRPV1 activation


Omari, SAM and Adams, MJ and Kunde, DA and Geraghty, DP, Capsaicin-induced death of human haematological malignant cell lines is independent of TRPV1 activation, Pharmacology, 98, (1-2) pp. 79-86. ISSN 0031-7012 (2016) [Refereed Article]

Copyright Statement

Copyright 2016 Karger AG, Basel

DOI: doi:10.1159/000445437


The effect of the plant-derived vanilloid, capsaicin (CAP), on the metabolic activity of THP-1, U266B1, U937 haematological malignancy cells was determined. CAP reduced metabolic activity in a concentration-dependent manner in the three cell lines. A biphasic effect was observed on THP-1 cells [EC50, IC50 (95% CI) = 32.9(19.9-54.3)/219(144-246)然]. U266B1 cells were more resistant to CAP than THP-1 and U937. Metabolic activity was significantly inhibited by CAP in U937 compared to U266B1 cells (IC50: 197 vs. 431然, respectively, P<0.008). AM251 and SB452533 appeared to act as partial agonists and displayed a synergistic effect with CAP in U937 cells. TRPV1 and CB1 antagonists (SB452533 and AM251, respectively) suppressed the CAP-induced increase in THP-1 cell metabolic activity (P<0.001). CAP inhibits the metabolic activity of malignant haematological cells through non TRPV1-dependent mechanisms. (CB1 and CB2) receptors in presence of other agonists, including collagen and arachidonic acid. Incubation of platelets with each of the individual vanilloids, or with receptor antagonists of TRPV1 (SB452533), CB1 (AM251) and CB2 (AM630), for up to 2 h did not signicantly affect the platelet count. Similarly, the effect of individual vanilloids on the inhibition of platelet aggregation was not signicantly different in the presence of receptor agonists compared to control, irrespective of the agonist used, suggesting that the inhibitory effect of vanilloids on platelet aggregation is independent of TRPV1, CB1 and CB2 receptors. Further research on the antiplatelet activity of vanilloids should focus on mechanisms other than those associated with vanilloid receptors. Key words: cannabinoid, capsaicin, N-arachidonoyldopamine, N-oleoyldopamine, transient receptor potential vanilloid-1.

Item Details

Item Type:Refereed Article
Keywords:Vanilloids, capsaicin, platelets
Research Division:Medical and Health Sciences
Research Group:Pharmacology and Pharmaceutical Sciences
Research Field:Pharmacology and Pharmaceutical Sciences not elsewhere classified
Objective Division:Health
Objective Group:Clinical Health (Organs, Diseases and Abnormal Conditions)
Objective Field:Blood Disorders
Author:Omari, SAM (Dr Sofia Omari)
Author:Adams, MJ (Dr Murray Adams)
Author:Kunde, DA (Dr Dale Kunde)
Author:Geraghty, DP (Professor Dominic Geraghty)
ID Code:107948
Year Published:2016
Deposited By:Health Sciences
Deposited On:2016-04-01
Last Modified:2017-05-02

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