Recent advances in the licorice root constituent dibenzoylmethane as a potential therapeutic option for cancer

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Studies in Natural Products Chemistry



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Anticancer, Chemoprevention, Chemotherapeutic, Dibenzoylmethane, Licorice root, Transcriptional regulation


© 2019 Elsevier B.V. The search for novel, therapeutic options for cancer has led to the identification of various naturally occurring compounds, one of which is dibenzoylmethane (DBM, 1,3-diphenyl-1,3-propadinedione). A minor constituent of Glycyrrhiza glabra (licorice root), DBM is a small β-diketone, structurally related to curcumin that is widely used in sunscreens as an ultraviolet blocking agent. Dietary DBM has been reported to inhibit growth in mammary-induced 7,12-dimethylbenz[a]-anthracene (DMBA) tumors and lymphomas and leukemias, and 7,12-tetradecanoylphorbol-13-acetate (TPA)-induced skin tumors in mice. DBM has also been reported to inhibit tumor formation (polycyclic aromatic hydrocarbon (PAH)-induced tumorigenesis) in a rat mammary tumor model system. And, it has been shown to inhibit the binding of [3H] estradiol to estrogen receptor in mice, suggesting a role for DBM's inhibitory actions on murine breast tumorigenesis. Our laboratory was the first to report the antineoplastic effects of DBM in prostate cancer cells. DBM induced pronounced changes in LNCaP prostate cancer cell growth, causing an accumulation of cells in the G1 phase of the cell cycle and altered key proteins, although the underlying mechanism of DBM chemopreventive activity in carcinogenesis is unknown. However, its potential chemopreventive and chemotherapeutic activities have been demonstrated in all three stages of carcinogenesis (initiation, promotion, and progression), in both chemically and UVB-induced skin carcinogenesis in mice, as well as in various cell models of human cancers. Evidence from numerous in vitro and in vivo studies has confirmed its ability to modulate various targets and signaling pathways. With the recent news of curcumin being classified as a PAINS (pan-assay interference compounds) and an IMPS (invalid metabolic panaceas) candidate, a chemical compound with false-positive results in high-throughput screens, DBM may serve as a promising template for eliciting cytotoxicity with high potency for cancer cells. This review discusses the current mechanistic data available and assesses DBM's anticancer effects to support its potential as an anticancer agent.

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