X-ray repair cross-complementing 2 (XRCC2), a critical protein in homologous recombination (HR), plays a significant role in the occurrence, progression, and drug resistance of colorectal cancer (CRC). In this study, a series of xanthohumol C derivatives were synthesized, and their anticancer activity was evaluated. The results revealed that A33 demonstrated the potent anticancer activity and effectively inhibited the proliferation of CRC cells in vitro. Mechanistic investigations revealed that A33 suppressed the transcription and expression of XRCC2, resulting in cell cycle delay and the accumulation of DNA damage, ultimately leading to cell proliferation inhibition. Furthermore, A33 displayed high safety, favorable bioavailability (F = 37.51 %), and potent tumor growth inhibition in vivo, which highlighting its potential as a candidate for the development of novel anti-CRC therapies.
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http://dx.doi.org/10.1016/j.bmc.2024.118048 | DOI Listing |
Bioorg Med Chem
December 2024
State Key Laboratory of Macromolecular Drugs and Large-scale Manufacturing, School of Pharmaceutical Sciences, Wenzhou Medical University, 1210 University Town, Wenzhou, Zhejiang 325035, China. Electronic address:
X-ray repair cross-complementing 2 (XRCC2), a critical protein in homologous recombination (HR), plays a significant role in the occurrence, progression, and drug resistance of colorectal cancer (CRC). In this study, a series of xanthohumol C derivatives were synthesized, and their anticancer activity was evaluated. The results revealed that A33 demonstrated the potent anticancer activity and effectively inhibited the proliferation of CRC cells in vitro.
View Article and Find Full Text PDFAntioxidants (Basel)
July 2024
Department of Food and Drug, University of Parma, Viale Parco Area delle Scienze 27/A, 43124 Parma, Italy.
The demand for bioactive secondary metabolites of natural origin is increasing every day. Micropropagation could be a strategy to respond more quickly to market demands, regardless of seasonality. This research aims to evaluate in vitro-grown plants of two hop varieties, namely Columbus and Magnum, as a potential source of bioactive compounds.
View Article and Find Full Text PDFNat Prod Res
July 2024
College of Pharmacy, Chonnam National University, Gwangju, Korea.
Xanthohumol (XTH, ), a major prenylated chalcone in hops, has attracted considerable interests because of its pharmaceutical potency. To explore more related derivatives of XTH, its biotransformation was performed using the microbial model. Fungus sp.
View Article and Find Full Text PDFCancer Prev Res (Phila)
July 2024
European Institute of Oncologi IEO, Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS), Milan, Italy.
Cancer growth is dependent on angiogenesis, the formation of new blood vessels, which represents a hallmark of cancer. After this concept was established in the 1970s, inhibition of tumor development and metastases by blocking the neoangiogenic process has been an important approach to the treatment of tumors. However, antiangiogenic therapies are often administered when cancer has already progressed.
View Article and Find Full Text PDFInt J Mol Sci
March 2024
Chair and Department of the Pharmaceutical Chemistry and Biomaterials, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Str., 02-097 Warsaw, Poland.
Xanthohumol (Xn), a prenylated chalcone found in Hop ( L.), has been shown to have potent anti-aging, diabetes, inflammation, microbial infection, and cancer properties. Unfortunately, this molecule has undesirable characteristics such as inadequate intake, low aqueous solubility, and a short half-life.
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