Capsaicin-Induced Death of Human Haematological Malignant Cell Lines Is Independent of TRPV1 Activation

• Published in: Pharmacology Vol. 98; no. 1-2; p. 79
• Main Authors: Omari, Sofia A, Adams, Murray J, Kunde, Dale A, Geraghty, Dominic P
• Format: Journal Article
• Language: English
• Published: Switzerland 01.06.2016
• Subjects: Cannabinoid Receptor Antagonists - pharmacology; Capsaicin - pharmacology; Cell Death - drug effects; Cell Line, Tumor; Hematologic Neoplasms - metabolism; Humans; Indoles - pharmacology; Oxazines - metabolism; Piperidines - pharmacology; Pyrazoles - pharmacology; TRPV Cation Channels - antagonists & inhibitors; Xanthenes - metabolism
• ISSN: 1423-0313
• DOI: 10.1159/000445437

The effect of the plant-derived vanilloid, capsaicin (CAP), on the metabolic activity of THP-1, U266B1 and U937 hematological 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) µmol/l). 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 versus 431 µmol/l, respectively, p < 0.008). Transient receptor potential vanilloid-1 (TRPV1) and CB1 antagonists (SB452533 and AM251, respectively) suppressed the CAP-induced increase in THP-1 cell metabolic activity (p < 0.001). AM251 and SB452533 appeared to act as partial agonists and displayed a synergistic effect with CAP in U937 cells. CAP inhibits the metabolic activity of malignant hematological cells through non-TRPV1-dependent mechanisms.