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. 2024 Jul 1.
doi: 10.1007/s11030-024-10833-9. Online ahead of print.

In vitro anticancer study of novel curcumin derivatives via targeting PI3K/Akt/p53 signaling pathway

Huixian Zhou #  1 , Zhiwen Wu #  1 , Yannan Zhang  1 , Zikai Yu  1 , Zhengyang Nie  1 , Jinbiao Fan  1 , Zuchang Zhu  2 , Fenglian Chen  3 , Tao Wang  4
Affiliations

In vitro anticancer study of novel curcumin derivatives via targeting PI3K/Akt/p53 signaling pathway

Huixian Zhou et al. Mol Divers. .

Abstract

Four new series of curcumin derivatives bearing NO-donating moiety were synthesized via etherification, nucleophilic substitution, and Knoevenagel condensation etc. The cytotoxicity activity of curcumin derivatives against five human tumor cell lines (A549, Hela, HepG2, MCF-7 and HT-29) and two normal cell lines (LO-2 and HK-2) has been studied. The results showed that compound 6a could inhibit the proliferation of MCF-7 cells remarkably and exhibit low toxicity to normal cells. Also, the underlying mechanism in vitro of compound 6a on MCF-7 was investigated. It has been found that compound 6a induced G2/M arrest and apoptosis of MCF-7 in a dose-dependent manner. Compound 6a-induced the fluorescence changes of ROS in MCF-7 cells confirmed the occurrence of apoptosis. Western Blot suggested that compound 6a decreased the expression of PI3K, as well as increased the expression of p53, cleaved caspase-9 and cleaved caspase-3. Furthermore, molecular docking revealed that compound 6a could bind well at active site of PI3K (3zim) with total score 9.59. Together, compound 6a, a potential PI3K inhibitor, may inhibit the survival of MCF-7 cells via interfering with PI3K/Akt/p53 pathway.

Keywords: Antitumor; Curcumin derivatives; Knoevenagel condensation; PI3K/Akt/p53 pathway.

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