trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity[1][2][3].
trans-Chalcone competitively inhibits porcine pancreatic α-amylase with a Ki of 48 µM[2]. trans-Chalcone (30.23-98.03 µM; 24 hours) induces cell cycle arrest and apoptosis in MCF-7 cells[1]. trans-Chalcone (20-80 µM; 24, 48 hours) reduces the expression of the apoptosis-related protein Bcl-2[1]. trans-Chalcone (58.25 µM; 6, 24 hours) has greater inhibition of Bcl-2, induction of APAF1 and BAX, and strong induction of CIDEA in 24 hours[1]. trans-Chalcone (24 hours) inhibits MCF-7 cell viability (IC20=30.23 µM; IC50=58.25 µM; IC80=98.03 µM). trans-Chalcone (48 h) has IC50s of 41.53 µM and 48.41 µM for MCF-7 and 3T3 cell lines, respectively. trans-Chalcone exhibits a pronounced cytotoxicity activity[1].
References:
[1]. Luis Felipe Buso Bortolotto, et al. Cytotoxicity of trans-chalcone and licochalcone A against breast cancer cells is due to apoptosis induction and cell cycle arrest. Biomed Pharmacother. 2017 Jan;85:425-433.
[2]. Mahmoud Najafian, et al. Trans-chalcone: a novel small molecule inhibitor of mammalian alpha-amylase. Mol Biol Rep. 2011 Mar;38(3):1617-20.
[3]. Tamires Aparecida Bitencourt, et al. Trans-chalcone and quercetin down-regulate fatty acid synthase gene expression and reduce ergosterol content in the human pathogenic dermatophyte Trichophyton rubrum. BMC Complement Altern Med. 2013 Sep 17;13:229.