Gambogic Acid as a Candidate for Cancer Therapy: A Review

Abstract

Gambogic acid (GA), a kind of dry resin secreted by the Garcinia hanburyi tree, is a natural active ingredient with various biological activities, such as anti-cancer, anti-inflammatory, antioxidant, anti-bacterial effects, etc. An increasing amount of evidence indicates that GA has obvious anti-cancer effects via various molecular mechanisms, including the induction of apoptosis, autophagy, cell cycle arrest and the inhibition of invasion, metastasis, angiogenesis. In order to improve the efficacy in cancer treatment, nanometer drug delivery systems have been employed to load GA and form micelles, nanoparticles, nanofibers, and so on. In this review, we aim to offer a summary of chemical structure and properties, anti-cancer activities, drug delivery systems and combination therapy of GA, which might provide a reference to promote the development and clinical application of GA.

Anticancer Profiling of Gambogic Acid as a Target Specific RANKL Inhibitor in Osteosarcoma Cell Line

“…Therapeutic potentials of natural compounds have been extensively evaluated against various diseases for a long time. Gambogic acid is an important member of the herbal medicine and exhibits anti-proliferative activity against in a wide variety of cancer types in experimental studies (Liu et al, 2020;Xu et al, 2012). In the present study, anti-proliferative and antimetastatic activities of gambogic acid were investigated in Saos-2 cell line by in-silico and invitro studies.…”

“…Also, IC50 value of gambogic acid was calculated as 0.88 µM at 48h in Saos-2 cells. Previous studies revealed that gambogic acid exhibited significant toxicity on various cancer types and its IC50 values is around low μM levels in cancer cells (Liu et al, 2020;Xu et al, 2012). The molecular mechanisms of the anticancer activities of gambogic acid could be determined with further biochemical experiments in Saos-2 cells.…”

Multiple Myeloma Inhibitory Activity of Plant Natural Products

“…Three studies investigated the antimyeloma potential of gambogic acid. Gambogic acid is a caged polyprenylated xanthone and the major active ingredient of gamboge secreted from Garcinia hanburryi [ 142 ]. It exhibited pronounced effects against an array of different cancers and was therefore attributed promising therapeutic potential [ 143 ].…”

“…However, poor aqueous solubility and biodistribution combined with multi-targeting capacity led to unavoidable systemic toxicity [ 144 ]. Therefore, numerous studies focused on the minimization of these side-effects by means of nanotechnology [ 142 , 144 ]. The potential of gambogic acid against MM was evaluated in three studies [ 145 , 146 , 147 ].…”

“…Although the compound’s antiproliferative effects were in the micromolar range (at least under normoxic conditions), it effectively suppressed hypoxia-activated pathways which might be important in vivo [ 147 ]. Consequently, gambogic acid was subject of additional studies evaluating its efficacy in combination therapies with bortezomib and other chemotherapeutics [ 142 , 215 , 216 ]. With regard to clinical trials, a phase IIa study comparing the efficacy and safety of different dosage schedules of gambogic acid in patients with advanced malignant tumors was reported [ 217 ].…”