title: Garcinol: Current status of its anti-oxidative, anti-inflammatory and anti-cancer effects.
abstract: 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.
authors: Cancer Science Institute of Singapore, National University of Singapore, Singapore 117599; Department of Pharmacy, National University of Singapore, Singapore 117543.
authors: Chaoqun
authors: C
authors: Liu
authors: Department of Pharmacy, National University of Singapore, Singapore 117543.
authors: Paul Chi-Lui
authors: PC
authors: Ho
authors: Cancer Science Institute of Singapore, National University of Singapore, Singapore 117599.
authors: Fang Cheng
authors: FC
authors: Wong
authors: Department of Pharmacology, National University Health System, Singapore 117597.
authors: Gautam
authors: G
authors: Sethi
authors: Cancer Science Institute of Singapore, National University of Singapore, Singapore 117599; Department of Pharmacology, National University Health System, Singapore 117597. Electronic address: csiwl@nus.edu.sg.
authors: Ling Zhi
authors: LZ
authors: Wang
authors: Cancer Science Institute of Singapore, National University of Singapore, Singapore 117599; Department of Pharmacology, National University Health System, Singapore 117597; Department of Haematology-Oncology, National University Health System, Singapore 119228. Electronic address: phcgbc@nus.edu.sg.
authors: Boon Cher
authors: BC
authors: Goh
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000493:pharmacokinetics / Q000494:pharmacology; D000975:Antioxidants / Q000493:pharmacokinetics / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D013729:Terpenes / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000972:Antineoplastic Agents, Phytogenic; D000975:Antioxidants; D013729:Terpenes; C054597:garcinol
keywords: Garcinia indica; Garcinol; Pharmacodynamics; Pharmacokinetics; Toxicology