Chemical and Biological Aspects of Garcinol and Isogarcinol: Recent Developments

Schobert, Rainer; Biersack, Bernhard

doi:10.1002/cbdv.201900366

Cited by 49 publications

(32 citation statements)

References 86 publications

(251 reference statements)

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“…Chemically, garcinol is polyisoprenylated benzophenone (Figure 1) mainly found in Garcinia indica (Kokum) and Garcinia cambogia (Malabar tamarind) of the Mangosteen and Clusiaceae families, respectively [22]. Methanol extraction of dried G. indica plums resulted in the promising extraction of garcinol [9]. Further, re-dissolution of the above prepared extract in ethyl acetate followed column chromatography on silica gel.…”

Section: Chemistry Of Garcinolmentioning

confidence: 99%

“…Further, re-dissolution of the above prepared extract in ethyl acetate followed column chromatography on silica gel. From hexane elute, yellow needle-like crystals of garcinol with a melting point of 132 • C have been reported [9,23]. Another method comprises the initial removal of hydroxycitric acid from plant fruits.…”

Section: Chemistry Of Garcinolmentioning

confidence: 99%

“…Then, methanol extract was prepared and adsorbed on Celite and extracted with hexane. Finally, the hexane extract was purified by column chromatography [9].…”

Section: Chemistry Of Garcinolmentioning

confidence: 99%

“…Garcinol is one of such important phytochemicals with several anticancer properties. Garcinol belongs to the group of polyisoprenylated benzophenones obtained from the fruits and leaves of diverse 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].…”

Section: Introductionmentioning

confidence: 99%

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Garcinol Exhibits Anti-Neoplastic Effects by Targeting Diverse Oncogenic Factors in Tumor Cells

et al. 2020

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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.

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Section: Chemistry Of Garcinolmentioning

confidence: 99%

Section: Chemistry Of Garcinolmentioning

confidence: 99%

“…Then, methanol extract was prepared and adsorbed on Celite and extracted with hexane. Finally, the hexane extract was purified by column chromatography [9].…”

Section: Chemistry Of Garcinolmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Garcinol Exhibits Anti-Neoplastic Effects by Targeting Diverse Oncogenic Factors in Tumor Cells

et al. 2020

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“…Extracts of the pericarp, epicarp, and seeds of Garcinia have demonstrated antioxidant, anti-inflammatory, leishmanicidal, and antiprotozoal activities [ 21 , 22 , 23 ]. Another study also reported the presence of the bioflavonoids volkensiflavone, fukugetin [ 24 ], and prenylated xanthones [ 25 ]. These compounds have been associated with biological activities such as free-radical scavenging, antiulcer effects [ 26 ], cytotoxicity, inhibition of nitric oxide synthase [ 27 ], chemoprevention of cancer [ 28 ], induction of apoptosis [ 29 ], anti-HIV [ 30 ], and trypanocidal effects [ 31 ].…”

Section: Introductionmentioning

confidence: 99%

Medicinal Potential of Garcinia Species and Their Compounds

et al. 2020

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Garcinia is a genus of Clusiaceae, distributed throughout tropical Asia, Africa, New Caledonia, Polynesia, and Brazil. Garcinia plants contain a broad range of biologically active metabolites which, in the last few decades, have received considerable attention due to the chemical compositions of their extracts, with compounds which have been shown to have beneficial effects in several diseases. Our work had the objective of reviewing the benefits of five Garcinia species (G. brasiliensis, G. gardneriana, G. pedunculata, G. cambogia, and G. mangstana). These species provide a rich natural source of bioactive compounds with relevant therapeutic properties and anti-inflammatory effects, such as for the treatment of skin disorders, wounds, pain, and infections, having demonstrated antinociceptive, antioxidant, antitumoral, antifungal, anticancer, antihistaminic, antiulcerogenic, antimicrobial, antiviral, vasodilator, hypolipidemic, hepatoprotective, nephroprotective, and cardioprotective properties. This demonstrates the relevance of the genus as a rich source of compounds with valuable therapeutic properties, with potential use in the prevention and treatment of nontransmissible chronic diseases.

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Garcinol from Garcinia indica inhibits HIV‐1 reverse transcriptase‐associated ribonuclease H

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et al. 2021

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The bioactive components of Garcinia indica, garcinol (camboginol), and isogarcinol (cambogin), are suitable drug candidates for the treatment of various human diseases. HIV‐1‐RNase H assay was used to study the RNase H inhibition by garcinol and isogarcinol. Docking of garcinol into the active site of the enzyme was carried out to rationalize the difference in activities between the two compounds. Garcinol showed higher HIV‐1‐RNase H inhibition than the known inhibitor RDS1759 and retained full potency against the RNase H of a drug‐resistant HIV‐1 reverse transcriptase form. Isogarcinol was distinctly less active than garcinol, indicating the importance of the enolizable β‐diketone moiety of garcinol for anti‐RNase H activity. Docking calculations confirmed these findings and suggested this moiety to be involved in the chelation of metal ions of the active site. On the basis of its HIV‐1 reverse transcriptase‐associated RNase H inhibitory activity, garcinol is worth being further explored concerning its potential as a cost‐effective treatment for HIV patients.

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Chemical and Biological Aspects of Garcinol and Isogarcinol: Recent Developments

Cited by 49 publications

References 86 publications

Garcinol Exhibits Anti-Neoplastic Effects by Targeting Diverse Oncogenic Factors in Tumor Cells

Garcinol Exhibits Anti-Neoplastic Effects by Targeting Diverse Oncogenic Factors in Tumor Cells

Medicinal Potential of Garcinia Species and Their Compounds

Garcinol from Garcinia indica inhibits HIV‐1 reverse transcriptase‐associated ribonuclease H

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