Molecular Mechanisms of Antiproliferative Effects of Natural Chalcones

Abstract

Although great progress has been made in the treatment of cancer, the search for new promising molecules with antitumor activity is still one of the greatest challenges in the fight against cancer due to the increasing number of new cases each year. Chalcones (1,3-diphenyl-2-propen-1-one), the precursors of flavonoid synthesis in higher plants, possess a wide spectrum of biological activities including antimicrobial, anti-inflammatory, antioxidant, and anticancer. A plethora of molecular mechanisms of action have been documented, including induction of apoptosis, autophagy, or other types of cell death, cell cycle changes, and modulation of several signaling pathways associated with cell survival or death. In addition, blockade of several steps of angiogenesis and proteasome inhibition has also been documented. This review summarizes the basic molecular mechanisms related to the antiproliferative effects of chalcones, focusing on research articles from the years January 2015–February 2021.

Chemical Composition and Antiproliferative Activity of the Ethanolic Extract of Cyperus articulatus L. (Cyperaceae)

“…Currently there is a great need to look for new anticancer drugs with the ability to perform selective cytotoxicity on cancer cells with low toxicity in healthy cells [28]. Natural products from plants can be a source of molecules with antiproliferative activity, with several recent reports worldwide [29][30][31][32][33]. In our study the EECA was first tested against human tumor lines.…”

Programmed Cell Death Alterations Mediated by Synthetic Indole Chalcone Resulted in Cell Cycle Arrest, DNA Damage, Apoptosis and Signaling Pathway Modulations in Breast Cancer Model

“…In our recent review [ 35 ] we described pleiotropic mechanisms of antiproliferative effect of chalcones at molecular level. As documented, antiproliferative effect of several chalcones was associated with arrest of cell cycle, mostly at the G2/M phase [ 14 , 30 , 36 , 37 ].…”

Zanthoxylum Species: A Review of Traditional Uses, Phytochemistry and Pharmacology in Relation to Cancer, Infectious Diseases and Sickle Cell Anemia

“…Most anticancer natural products act by blocking different mechanisms through which cancer cells grow, multiply and invade other cells, as well as resist the immune system. These mechanisms include the induction of cell cycle arrest, apoptosis and oxidative stress, as well as inhibition of angiogenesis, metastasis and growth signaling pathways in cancer cells ( Ahmad et al, 2003 ; Michalkova et al, 2021 ). As shown in Figure 1 , extracts of Z. species have been demonstrated to elicit anticancer properties via inhibition of angiogenesis Harahap et al (2018) and DNA synthesis, induction of apoptosis Alam et al (2017) and cell cycle arrest at Go/G1 Pieme et al (2014) and G2-M phases, and suppression of cyclooxygenase (COX)-2 and vascular endothelial growth factor receptor type-2 (VEGFR-2) expression ( Harahap et al, 2018 ); Table 1 presents the anticancer properties of crude extracts of Z. species whose anticancer constituents are unknown.…”

“…Most anticancer natural products act by blocking different mechanisms through which cancer cells grow, multiply and invade other cells, as well as resist the immune system. These mechanisms include the induction of cell cycle arrest, apoptosis and oxidative stress, as well as inhibition of angiogenesis, metastasis and growth signaling pathways in cancer cells (Ahmad et al, 2003;Michalkova et al, 2021). As shown in Figure 1, extracts of Z. species have been demonstrated to elicit anticancer properties via inhibition of angiogenesis Harahap et al (2018) and DNA synthesis, FIGURE 1 | Proposed mechanism of anticancer activities of natural products from Zanthoxylum species.…”