Title:Polypharmacological Properties and Therapeutic Potential of β-Caryophyllene: A Dietary Phytocannabinoid of Pharmaceutical Promise
Volume: 22
Issue: 21
Author(s): Charu Sharma, Juma M. Al Kaabi, Syed M. Nurulain, Sameer N. Goyal, Mohammad Amjad Kamal and Shreesh Ojha
Affiliation:
Keywords:
β-Caryophyllene, CB2 receptor agonist, AM630, dietary phytocannabinoids, trans-Caryophyllene, phytochemicals, PPAR
isoforms, CB2 receptors.
Abstract: Background: β-Caryophyllene (BCP) is a natural bicyclic sesquiterpene abundantly found in essential
oils from various spices, fruits and medicinal as well as ornamental plants. It is approved by United States Food
and Drug Administration and European agencies as food additive, taste enhancer and flavoring agent and termed as
a phytocannabinoid. Methods: All the available literature on BCP and its synonyms were collected through different literature databases.
Results: BCP was found to elicit a full agonist action on cannabinoid type 2 (CB2) receptors, a G-protein coupled receptor representing
important therapeutic target in several diseases. Activation of CB2 receptors notably appeared devoid of psychotropic adverse effect of
cannabinoids contrary to the CB1 receptors. In addition, it activates peroxisome proliferated activator receptors (PPARs) isoforms;
PPAR-α &-γ and inhibits pathways triggered by the activation of toll like receptor complex; CD14/TLR4/MD2, reduce immuneinflammatory
processes and exhibit synergy with µ-opioid receptor dependent pathways. Additionally, it found as potent antagonist of
homomeric nicotinic acetylcholine receptors (α7-nAChRs) and devoid of effects mediated by serotonergic and GABAergic receptors. It
also modulates numerous molecular targets by altering their gene expression, signaling pathways or through direct interaction. Various
pharmacological activities such as cardioprotective, hepatoprotective, gastroprotective, neuroprotective, nephroprotective, antioxidant,
anti-inflammatory, antimicrobial and immune-modulator have been reported in experimental studies. It has shown potent therapeutic
promise in neuropathic pain, neurodegenerative and metabolic diseases. Conclusion: The present review provides a comprehensive insight
of pharmacological and therapeutic potential of BCP, its molecular mechanism and signaling pathways in different pathological
conditions. The review also examines the possibility of its further development as a novel candidate for various pathologies considering
the polypharmacological and multifaceted therapeutic properties potential along with favorable oral bioavailability, lipophilicity and
physicochemical properties.
