Anticancer Potential of Natural Chalcones: In Vitro and In Vivo Evidence

Abstract

There is no doubt that significant progress has been made in tumor therapy in the past decades. However, the discovery of new molecules with potential antitumor properties still remains one of the most significant challenges in the field of anticancer therapy. Nature, especially plants, is a rich source of phytochemicals with pleiotropic biological activities. Among a plethora of phytochemicals, chalcones, the bioprecursors of flavonoid and isoflavonoids synthesis in higher plants, have attracted attention due to the broad spectrum of biological activities with potential clinical applications. Regarding the antiproliferative and anticancer effects of chalcones, multiple mechanisms of action including cell cycle arrest, induction of different forms of cell death and modulation of various signaling pathways have been documented. This review summarizes current knowledge related to mechanisms of antiproliferative and anticancer effects of natural chalcones in different types of malignancies including breast cancers, cancers of the gastrointestinal tract, lung cancers, renal and bladder cancers, and melanoma.

Natural 2′,4-Dihydroxy-4′,6′-dimethoxy Chalcone Isolated from Chromolaena tacotana Inhibits Breast Cancer Cell Growth through Autophagy and Mitochondrial Apoptosis

“…The induction of apoptosis by chalcones, particularly through the activation of caspase-3, is a well-documented phenomenon [ 28 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 ]. In our study, the data suggested that DDC preferentially activated caspase-3 over caspase-7 in MDA-MB-231 cells, as illustrated in Figure 5 .…”

A Novel Tri-Hydroxy-Methylated Chalcone Isolated from Chromolaena tacotana with Anti-Cancer Potential Targeting Pro-Survival Proteins

“…How ever, only a few of these natural chalcones possess both hydroxy and methoxy groups in their structures (Table 1). One well-known subgroup of these chalcones is called flavoka vains, which were originally identified in Piper methysticum (Kava) [10,11].…”

Development of Stable Amino-Pyrimidine–Curcumin Analogs: Synthesis, Equilibria in Solution, and Potential Anti-Proliferative Activity

“…In the search for new therapeutics aimed at reducing side effects and the treatment of recurrences, naturally occurring compounds have been of inspiration for their pleiotropic activities [ 6 , 7 , 8 ]. In the last two decades, curcumin [(1E,6E)-1,7-bis (4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione], the most active phytocompound extracted from the dried rhizomes of Curcuma longa L., stands out, as highlighted by the exponential increase in released scientific papers, reviews, and clinical trials.…”