Semisynthesis and anti-cancer properties of novel honokiol derivatives in human nasopharyngeal carcinoma CNE-2Z cells

• Published in: Journal of enzyme inhibition and medicinal chemistry 2023-12, Vol.38 (1), p.2244694-2244694
• Main Authors: Li, Bo-Han, Ma, Hui, Zhu, Jing, Chen, Jie, Dai, Yi-Qun, Zhang, Xiao-Jing, Li, Hong-Mei, Wu, Cheng-Zhu
• Format: Article
• Language: English
• Subjects: AKT protein; Apoptosis; BAX protein; Bcl-2 protein; Cancer; Cell migration; Cytotoxicity; Gastric cancer; Gelatinase A; Gelatinase B; HIF-1α; Honokiol derivatives; Hypoxia-inducible factor 1a; invasion; migration; Nasopharyngeal carcinoma; Semisynthesis; siRNA; Testicular cancer; Throat cancer; Transfection
• ISSN: 1475-6366; 1475-6374
• DOI: 10.1080/14756366.2023.2244694

In this study, 21 new honokiol derivatives were synthesised, and their anti-cancer properties were investigated. Among these, compound exhibited the most potent cytotoxic activity against human nasopharyngeal carcinoma CNE-2Z cells, human gastric cancer SGC7901 cells, human breast cancer MCF-7 cells, and mouse leydig testicular cancer I-10 lines with IC values of 6.04, 7.17, 6.83, and 5.30 μM, respectively. Compared to the parental compound, displayed up to 5.18-fold enhancement of the cytotoxic effect on CNE-2Z cells. We further demonstrated that inhibited cell growth, suppressed migration and invasion, and induced apoptosis of CNE-2Z cells by down-regulating HIF-1α, MMP-2, MMP-9, Bcl-2, Akt and up-regulating Bax protein levels. Transfection of CNE-2Z cells with HIF-1α siRNA reduced cell migration and invasion. In addition, experiments confirmed that inhibited tumour growth in CNE-2Z cell-xenografted nude mice with low toxicity. Thus, our data suggested that was a potent and safe lead compound for nasopharyngeal carcinoma therapy.