Vanilloid‐Like Agents: Potential Therapeutic Targeting of Platelets?

Abstract

Capsaicinoids are the "hot" compounds present in placental tissues of Capsicum fruits that are responsible for capsicum's pungency. Capsaicinoids belong to the broader class of vanilloids that activate the nonselective cation channel, transient receptor potential vanilloid-1 (TRPV1). Endogenous vanilloids include arachidonic acid derivatives that have different affinities for TRPV1 and are increasingly recognized as an important group of signaling molecules affecting tissue injury, pain, and inflammation. Furthermore, some endogenous vanilloids have high affinity for cannabinoid receptors (CB1 and CB2), which are present in platelets. The most well-known and widely studied plant-derived vanilloid, capsaicin, is reported to have antiplatelet properties, but the mechanism of action is uncertain. This article will briefly review the mechanisms involved in platelet activation and aggregation, discuss the properties of vanilloids and their receptor, TRPV1, and discuss whether the effects of vanilloids, and particularly capsaicinoids, on platelets may be exploited for therapeutic benefit. Drug Dev Res 74 : 450-459, 2013.

Inhibition of Ca2+ entry by capsazepine analog CIDD-99 prevents oral squamous carcinoma cell proliferation

“…They are usually gated and transduce signals from outside the cell and induce a response via cation signaling. Many TRP channels play a role in cancer proliferation and metastasis ( Adams et al, 2013 ; Samanta et al, 2018 ). Capsaicin (CAP) is known to activate the transient receptor potential cation channel subfamily V member 1 (TRPV1) channels and inhibit cancer growth ( Clark and Lee, 2016 ).…”