PEGylation of Chrysin Improves Its Water Solubility while Preserving the In Vitro Biological Activity

OGGERO, JULIA; GASSER, FÁTIMA B.; ZACARÍAS, SILVIA M.; BURNS, PATRICIA; BARAVALLE M.E; RENNA, MARIA SOL; ORTEGA, HUGO H.; VAILLARD, SANTIAGO E.; VAILLARD, VICTORIA A.

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

AMER CHEMICAL SOC

Año: 2023 vol. 71 p. 19817 - 19831

0021-8561

Phenolic compounds present in plants have demonstrated several biological propertiessuch as antioxidant, antitumor, cardioprotective, and antiproliferative. On the other hand,doxorubicin, a chemotherapeutic widely used to treat breast cancer, usually exhibitschronic cardiotoxicity associated with oxidative stress. Therefore, we aimed to study theeffects of phenolic compound‐enriched extract (PCEE) with doxorubicin in breast cancer.To achieve this, after an SPE‐C18‐column purification process of crude extracts obtainedfrom pecan nutshells (Carya illinoinensis), the resulting PCEE was used to evaluate thecytotoxicity and antioxidant properties against the human breast cancer cell line MDAMB‐231 and the normal‐hamster ovary cell line CHO‐K1. PCEE was selectively cytotoxicagainst both cell lines, with an IC50 value (≈26.34 mg/L) for MDA‐MB‐231 lower than thatobtained for CHO‐K1 (≈55.63 mg/L). As a cytotoxic mechanism, PCEE inhibited cellgrowth by G2/M cell cycle arrest in MDA‐MB‐231 cells. Simultaneously, the study of theantioxidant activity showed that PCEE had a cytoprotective effect, evidenced by reducedROS production in cells with oxidative stress caused by doxorubicin. The results highlightPCEE as a potential antitumor agent, thus revaluing it as an agro‐industrial residue.