Garcinol: Current status of its anti-oxidative, anti-inflammatory and anti-cancer effects

This review summarizes current in vitro and in vivo studies of garcinol and highlights perspectives on the drug development pipeline of garcinol as a drug candidate.
• We describe the pathways and major targets of garcinol that are responsible for its pharmacodynamics effects.
• We summarize the results of both in vitro and in vivo anti-cancer studies of garcinol.
• We highlight the importance of pharmacokinetic and toxicological studies of compounds with potential therapeutic benefits, such as garcinol.

Garcinol is the main medicinal component of the dried fruit rind of Garcinia indica (G. indica), which has traditionally been extensively used to treat gastric ailments and skin irritation. In vitro studies of garcinol revealed its potential therapeutic effects, such as its anti-oxidative, anti-inflammatory and anti-cancer properties. Similarly, in vivo studies in animal models also demonstrated the efficacy of garcinol for the treatment of various inflammatory and cancerous conditions. Despite being well tolerated in preclinical studies, the toxicological profile of garcinol remains elusive. More importantly, systematic pharmacokinetics (PK) studies of garcinol to establish an appropriate route of administration and its effective concentration range under physiological conditions have not yet been performed. PK studies play an essential role in translating the preclinical findings of garcinol from cell line models and animal species to humans, thereby facilitating dose selection, the characterization of the therapeutic index, identification of a metabolic pathway, and the determination of garcinol's potency and tolerability. This paper reviews the current studies of garcinol as a potential anti-oxidant, anti-inflammatory and anti-cancer agent and highlights the importance of performing preclinical PK and toxicological studies on garcinol for its development pipeline.