Abstract
Garcinol, a polyisoprenylated benzophenone, is the medicinal component obtained from fruits and leaves of Garcinia indica (G. indica) and has traditionally been extensively used for its antioxidant and anti-inflammatory properties. In addition, it has been also been experimentally illustrated to elicit anti-cancer properties. Several in vitro and in vivo studies have illustrated the potential therapeutic efficiency of garcinol in management of different malignancies. It mainly acts as an inhibitor of cellular processes via regulation of transcription factors NF-κB and JAK/STAT3 in tumor cells and have been demonstrated to effectively inhibit growth of malignant cell population. Numerous studies have highlighted the anti-neoplastic potential of garcinol in different oncological transformations including colon cancer, breast cancer, prostate cancer, head and neck cancer, hepatocellular carcinoma, etc. However, use of garcinol is still in its pre-clinical stage and this is mainly attributed to the limitations of conclusive evaluation of pharmacological parameters. This necessitates evaluation of garcinol pharmacokinetics to precisely identify an appropriate dose and route of administration, tolerability, and potency under physiological conditions along with characterization of a therapeutic index. Hence, the research is presently ongoing in the dimension of exploring the precise metabolic mechanism of garcinol. Despite various lacunae, garcinol has presented with promising anti-cancer effects. Hence, this review is motivated by the constantly emerging and promising positive anti-cancerous effects of garcinol. This review is the first effort to summarize the mechanism of action of garcinol in modulation of anti-cancer effect via regulation of different cellular processes.
Highlights
Despite the continuous advancements in diagnostic and therapeutic methods, cancer has still remained one of the most dreadful diseases in 21st century all over the world, with 18.1 million new cases and 9.6 million mortalities estimated by 2018 [1]
The authors showed that treatment with garcinol significantly induced apoptosis and cell cycle arrest probably mediated by downregulation of COX2 and NF-κBanalysis
The second pathway involves the interference of garcinol with lipopolysaccharide (LPS)-mediated phosphorylation of extracellular signal regulated kinases 1/2 (ERK1/2) and reduction of COX-2 products and the reduction of prostaglandins [90]
Summary
Despite the continuous advancements in diagnostic and therapeutic methods, cancer has still remained one of the most dreadful diseases in 21st century all over the world, with 18.1 million new cases and 9.6 million mortalities estimated by 2018 [1]. Many phytochemicals present in the human diet have identified as potential chemopreventive and/or chemotherapeutic substances [2,3,4,5,6,7]. Garcinia species including G. indica, a small evergreen tree found in the tropical Asia and Africa [9,10,11] This phytochemical has been shown to reveal potential therapeutic effects both in vitro and in vivo studies, including antioxidant, anti-inflammatory and anticancer activities [11]. All the anticancer activities reported so far for garcinol are compiled to highlight the promising therapeutic potential of this fascinating natural agent present its pleiotropically regulation of cellular processes in cancer. In addition to analyzing its chemopreventive and chemotherapeutic properties, the possibilities to improve the bioavailability of garcinol in the human body by applying nanotechnological approaches are under consideration in this review to further promote clinical trials with this potent phytochemical
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