Scientific Name(s): Garcinia spp., Garcinia indica.
Common Name(s): Camboginol, Garcinol
Garcinol is primarily present in family Clusiaceae and genus Garcinia. Although Garcinia indica is commonly referenced in the scientific literaturePadhye 2009 it is found in other plant species.Yamaguchi 2000 The genus Garcinia includes 200 species located throughout Asia and Africa. G. indica, also known as kokum, is a slow-growing, mid-sized dioecious tree.Deodhar 2008 Its leaves are elliptic, oblong, and deep green. The flowers are dark pink, and the dried fruit rind contains the medicinal component of garcinol. The fruit is about the size of an orange and usually contains 6 to 8 seeds. The tree has the potential of bearing hundreds of fruits during the summer.
G. indica is used in culinary, pharmaceutical, and industrial applications.Padhye 2009 The dried fruit rind of G. indica is used as a garnish in Indian curries.Deodhar 2008, Sang 2001, Sang 2002 The oils from the seeds are used in preparing chocolates, medicines, and cosmetics. Kokum butter is extracted from the seeds and used in the cosmetic industry for preparing lotions, creams, lip balms, and soaps.Padhye 2009 Garcinol is claimed to inhibit skin glycation, thus reducing inflammation and injury to the extracellular matrix.Lodén 2007 The fruit rind has also been utilized as a pink and purple food coloring agent and as a culinary spice to provide a sour and sweet taste to foods.Hong 2007 In Indian Ayurvedic medicine, the extract of the fruit rind is used to treat inflammatory and infectious disease.Hong 2007, Koeberle 2009Garcinia is also used in central African traditional medicine for infectious disease.Khanum 2005
Garcinol is also known as camboginol and is commonly found in the dried fruit rind of G. indica as a yellow oil or pigment.Ciochina 2006 Mass spectral analysis of garcinol has been performed.Padhye 2009 Garcinol is an example of a prenylated chalcone, which has many beneficial effects in human health and disease.Padhye 2009
Uses and Pharmacology
Inhibition of cholinesterase activity increases acetylcholine availability for nerve cell communication. Garcinol has anticholinesterase activity toward acetyl cholinesterase (AChE) and butylcholinesterase. The IC50 value of garcinol (0.66 mcM) versus the reference compound galanthamine (0.50 mcM) against AChE was comparable.Lenta 2007
Aberrant arachidonic acid metabolism and nitric oxide synthesis are involved with inflammatory and carcinogenic processes. Garcinol and its derivatives inhibited release of arachidonic acid metabolites in human colon adenocarcinoma cells. Several key proteins involved in inflammation were inhibited, and the inhibitory effect on nitric oxide synthesis was concentration dependent. The proposed molecular mechanism of action of garcinol affects inflammatory processes associated with phosphorylation, inflammatory cytokines, and membrane phospholipids.Hong 2006 Garcinol is a direct and potent inhibitor of the catalytic activity of 2 crucial enzymes involved with inflammation, 5-lipoxygenase, and microsomal prostaglandin PGE2 synthase.Koeberle 2009 These 2 enzymes are often overexpressed in many tumors. Cigarette smoke extract leads to airway inflammation, which may be regulated by cyclooxygenase-2 (COX-2) expression and prostaglandin E2 (PGE2) synthesis.Yang 2009 Pretreatment of tracheal smooth muscle cells with garcinol markedly inhibited COX-2 expression stimulated by the cigarette smoke extract.
Topical application or oral administration of garcinol inhibited TPA-induced ear inflammation in a dose-dependent manner in CD-1 mice. TPA-induced expression of proinflammatory cytokine IL-6 protein was inhibited by topical application of garcinol to the ears of CD-1 mice. UVB-induced ear inflammation and proinflammatory cytokines IL-1 beta and IL-6 were inhibited in mice after oral administration of garcinol. Topical application of garcinol strongly inhibited TPA-induced skin tumor promotion in mice.Huang 2008
Garcinol has free radical scavenging activity against the hypoxanthine/xanthine oxidase system, superoxide anion, hydroxyl radical, and methyl radical.Yamaguchi 2000 The activity of emulsified garcinol was almost comparable with that of DL-alpha–tocopherol by weight but less than that of ascorbic acid. However, garcinol suppressed hydroxyl radical more strongly than that of DL-alpha–tocopherol.
The mechanism of action may be associated with garcinol reacting with peroxyl radicals followed by deprotonation of the hydroxyl group.Sang 2001, Sang 2002 Garcinol has chelating and antiglycation activity (glycation plays a role in diabetic complications) and is a lipid-soluble superoxide anion scavenger.Yamaguchi 2000
Garcinol provided a neuroprotective effect by decreasing nitric oxide production and expression of lipopolysaccharide-induced inflammatory mediators, iNOS and COX-2, in rat cortical astrocyte cultures.Liao 2005
Reviews of studies have been published.(Behera, Liu, Semwal) Garcinol showed potent inhibitory growth activity against HT-29 and HCT-116 colon cancer cells.Hong 2007 Focal adhesion kinase (FAK) is involved in protecting against apoptosis. Garcinol inhibited cell invasion by inhibiting the downstream signaling of FAK.Liao 2005 Elevation of the detoxifying enzyme glutathione S-transferase and quinine reductase in the liver, reduction of free radicals, and arachidonic acid metabolites by dietary garcinol in rats may suppress chemically induced colon carcinogenesis.Tanaka 2000 In human leukemia HL-60 cells, garcinol inhibited activity in a dose- and time-dependent manner by inducing DNA fragmentation and apoptotic cell death.Pan 2001 A similar study with human leukemia HL-60 cells documented the loss of mitochondrial membrane potential by garcinol-induced apoptosis.Matsumoto 2003 Dietary administration of garcinol in rats inhibited development of 4-nitroquinoline 1-oxide–induced tongue carcinogenesis and preneoplasms when compared with the control diet.Yoshida 2005 The mechanism of action involves garcinol suppressing cell proliferation activity in affected tissues and/or COX-2 expression in the tongue lesions. Garcinol induced caspase-mediated apoptosis in highly metastatic human breast cancer cells (MDA-MD-231) through down-regulation of NF-kappaB signaling pathway.Ahmad 2010 A chemical study examining 2 ethers of garcinol and isogarcinol documented inhibitory activity against Epstein-Barr virus early antigen activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells; the activity was comparable or stronger to that of the antitumor promoter glycyrrhetic acid.Ito 2003 Dysfunction or alteration of histone acetyl transferases (HATS) may lead to diseases such as cancer and viral infections, including HIV.Dekker 2009 Garcinol is a potent, nonspecific in vitro and in vivo inhibitor of HATS, a key regulatory step in gene expression in eukaryotic cells.Balasubramanyam 2004, Arif 2009 Garcinol is also the first reported cell-permeable HATS inhibitor.Varier 2004 Viral protein integrase is a critical protein for the integration of HIV-1 virus into the human genome. In one study, garcinol-derived molecules inhibited a critical step in this integration as well as HIV multiplication in T cells at nontoxic concentrations.Dekker 2009, Mantelingu 2007
An in vitro study documents garcinol inhibition of the growth of methicillin-resistant Staphylococcus aureus, with the activity comparable to that of the antibiotic vancomycin.Iinuma 1996, Rukachaisirikul 2005 Several concentrations of an extract from G. indica, with garcinol as the major compound, inhibited the growth of Aspergillus flavus and subsequent mycotoxin aflatoxin B1 production in a growth inhibition assay.Tamil Selvi 2003G. indica rind extracts and garcinol inhibited the growth of some foodborne gram-positive and gram-negative bacteria.Negi 2004 Garcinol has moderate antiplasmodial activity against the chloroquine-resistant strain of Plasmodium falciparum (FcB1).Marti 2009
Oral administration of garcinol to rats prevented acute ulceration induced by indomethacin. The mechanism of action may be associated with the interaction of garcinol with reactive oxygen species on the surface of gastric mucosa.Yamaguchi 2000 The in vitro bactericidal activities of clarithromycin and garcinol exerted time- and concentration-dependent effects on Helicobacter pylori. In the same study, garcinol exhibited greater bactericidal activity on H. pylori when compared with resveratrol.Chatterjee 2003, Chatterjee 2005
Garcinol is an active ingredient in various topical products for its antioxidant activity. It is also used as an additive to hydroxycitric acid, purported by some commercial manufacturers to improve lean body mass.
Toxicological studies suggest an upper limit of 2,800mg/day of Garcinia extracts or hydroxycitric acid, based on the "no observed adverse effect level."Semwal 2015
Pregnancy / Lactation
Information regarding safety and efficacy in pregnancy and lactation is lacking.
Theoretically, when used with stomach acid–reducing medications (eg, proton pump inhibitors) garcinol may provide an additive effect, but should be used cautiously with antioxidant products or cancer medications.
No clinical data were found in the medical literature. Avoid use if allergy or hypersensitivity to any of the components of garcinol exist.
Most reports suggest dietary administration of garcinol in animal studies exhibits low toxicity, with animal studies finding no histological or pathological changes in liver, kidney, lung, heart, or esophageal organ systems.(1, 22) However, toxicity towards spermatogenesis and testicular atrophy in rats from administered G. cambogia extract has been reported.Semwal 2015
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