Antitumor Effect of Chalcone Derivatives against Human Prostate (LNCaP and PC-3), Cervix HPV-Positive (HeLa) and Lymphocyte (Jurkat) Cell Lines and Their Effect on Macrophage Functions

• Type: Article in International Scientific Journal
• Date: 2023

Authors

Horta, B (Author) Other; Freitas Silva, J (Author) Other; Silva, J (Author) Other; Dias, F (Author) Other; Teixeira, AL (Author) Other; Rui Medeiros (Author) ICBAS; Honorina Cidade (Author) FFUP; Pinto, M (Author) Other; Cerqueira, F (Author) Other

Journal

Title: Molecules

Vol. 95

Final page: 2159

ISSN: 1420-3049

Publisher: MDPI

Indexing

ISI Web of Knowledge - 4 Citations

Scopus - 4 Citations

Other information

Authenticus ID: P-00Y-3VN

DOI: 10.3390/molecules28052159

Abstract (EN): Chalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, the effect of chalcones 1-18 against the metabolic viability of cervical (HeLa) and prostate (PC-3 and LNCaP) tumor cell lines was tested, to compare the activity against solid and liquid tumor cells. Their effect was also evaluated on the Jurkat cell line. Chalcone 16 showed the highest inhibitory effect on the metabolic viability of the tested tumor cells and was selected for further studies. Recent antitumor therapies include compounds with the ability to influence immune cells on the tumor microenvironment, with immunotherapy being one actual goal in cancer treatment. Therefore, the effect of chalcone 16 on the expression of mTOR, HIF-1 alpha, IL-1 beta, TNF-alpha, IL-10, and TGF-beta, after THP-1 macrophage stimulation (none, LPS or IL-4), was evaluated. Chalcone 16 significantly increased the expression of mTORC1, IL-1 beta, TNF-alpha, and IL-10 of IL-4 stimulated macrophages (that induces an M2 phenotype). HIF-1 alpha and TGF-beta were not significantly affected. Chalcone 16 also decreased nitric oxide production by the RAW 264.7 murine macrophage cell line, this effect probably being due to an inhibition of iNOS expression. These results suggest that chalcone 16 may influence macrophage polarization, inducing the pro-tumoral M2 macrophages (IL-4 stimulated) to adopt a profile closer to the antitumor M1 profile.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11