Chalcones and Gastrointestinal Cancers: Experimental Evidence

Abstract

Colorectal (CRC) and gastric cancers (GC) are the most common digestive tract cancers with a high incidence rate worldwide. The current treatment including surgery, chemotherapy or radiotherapy has several limitations such as drug toxicity, cancer recurrence or drug resistance and thus it is a great challenge to discover an effective and safe therapy for CRC and GC. In the last decade, numerous phytochemicals and their synthetic analogs have attracted attention due to their anticancer effect and low organ toxicity. Chalcones, plant-derived polyphenols, received marked attention due to their biological activities as well as for relatively easy structural manipulation and synthesis of new chalcone derivatives. In this study, we discuss the mechanisms by which chalcones in both in vitro and in vivo conditions suppress cancer cell proliferation or cancer formation.

A Promising Therapeutic Scaffold Fusing Chalcone/Coumarin Targeting Colorectal Cancer: Design, Synthesis, Biological and ADME‐tox Modelling

“…These results could be explained by the fact that both, coumarin and chalcone, involve many anticancer mechanisms, including cell cycle arrest, ROS production and apoptosis. [31,[58][59][60] This is also in accordance with those previous reports made by Wang and colleagues [46] who showed a coumarin-chalcone hybrid which efficiently delivered to cells to induce apoptosis through the generation of intracellular ROS in a colorectal carcinoma cell line HCT116. Besides, in other study, Singh and colleagues [61] had demonstrated that a coumarin-chalcone hybrid caused cell cycle arrest at G2/M phase and induced intrinsic caspase-dependent apoptosis mediated by alterations in the cellular levels of Bcl-2 family proteins in cervical cancer cell lines (HeLa and C33A).…”

The effects and mechanisms of natural products on Helicobacter pylori eradication

“…Among the polyphenol family, flavonoids are one of the most important and vast groups of compounds with a basic skeleton comprising two benzene rings linked through a heterocyclic ring, involving over 9000 species of molecules ( Gonzalez et al., 2021 ). Many flavonoids have been shown to possess promising antimicrobial capacity against H. pylori , including kaempferol, chalcone, myricetin, taxifolin, and other compounds with proven validity ( Krzyżek et al., 2021 ; Stenger Moura et al., 2021 ; Yang et al., 2022 ; Michalkova et al., 2023 ). Flavonoids contribute to several antibacterial mechanisms, such as the inhibition of crucial enzymes for colonization, survival, and reproduction ( Asha et al., 2013 ; Steinmann et al., 2013 ; Egas et al., 2018 ), and interference with the fluidity and stability of the cytoplasmic membrane ( Tsuchiya and Iinuma, 2000 ; Yang et al., 2022 ).…”

Natural Chalcones and Derivatives in Colon Cancer: Pre-Clinical Challenges and the Promise of Chalcone-Based Nanoparticles

“…This unique structure allows them to interact with specific molecular targets within the cancer cells. They have demonstrated significant anticancer properties, making them attractive candidates for targeted therapeutics in the fight against colon cancer [3]. This review will focus on utilizing natural chalcones and some derivatives (such as curcumin) as targeted therapeutics for colon cancer, exploring their intriguing anticancer properties and mechanisms of action.…”

“…In recent years, one promising avenue in colon cancer treatment has emerged in the form of chalcones, a class of compounds with diverse pharmacological activities. Chalcones have garnered attention for their potential to modulate the multiple signaling pathways implicated in CRC development and progression [ 3 ]. Chalcones (except for curcumin, which may be considered a bis-chalcone derivative) are characterized by their chemical structure, which consists of two aromatic rings linked by a three-carbon α,β-unsaturated carbonyl system [ 4 ] ( Figure 1 ).…”

“…This unique structure allows them to interact with specific molecular targets within the cancer cells. They have demonstrated significant anticancer properties, making them attractive candidates for targeted therapeutics in the fight against colon cancer [ 3 ].…”