Princiotto Salvatore, Pinna Cecilia, Mattio Luce Micaela, Annunziata Francesca, Beretta Giovanni Luca, Pinto Andrea, Dallavalle Sabrina
Department of Food, Environmental and Nutritional Sciences (DeFENS), University of Milan, Via Celoria 2, 20133 Milan, Italy.
Molecular Pharmacology Unit, Department of Experimental Oncology, Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, 20133 Milan, Italy.
Pharmaceuticals (Basel). 2024 Aug 1;17(8):1012. doi: 10.3390/ph17081012.
Within the huge class of plant secondary metabolites, resveratrol-derived stilbenoids show wide structural diversity and mediate a great number of biological responses relevant for human health, including cancer prevention and cytotoxicity. Resveratrol is known to modulate several pathways directly linked to cancer progression, as well as its analogue pterostilbene, characterized by an increased metabolic stability and significant pharmacological activities. To study the potential anticancer activity of other stilbenoids, a home-made collection of resveratrol dimers and simplified analogues was tested on melanoma A375, non-small cell lung cancer H460 and PC3 prostate cancer cell lines. The structural determinants responsible for the antiproliferative activity have been highlighted. Moreover, to investigate the DNA damage ability of the selected molecules, the expression of the γ-H2AX after compound exposure was evaluated.
在种类繁多的植物次生代谢产物中，白藜芦醇衍生的芪类化合物具有广泛的结构多样性，并介导了大量与人类健康相关的生物学反应，包括癌症预防和细胞毒性。已知白藜芦醇可调节与癌症进展直接相关的多种途径，其类似物紫檀芪也如此，紫檀芪具有更高的代谢稳定性和显著的药理活性。为了研究其他芪类化合物的潜在抗癌活性，我们用自制的白藜芦醇二聚体和简化类似物组合对黑色素瘤A375、非小细胞肺癌H460和PC3前列腺癌细胞系进行了测试。已明确了负责抗增殖活性的结构决定因素。此外，为了研究所选分子的DNA损伤能力，我们评估了化合物暴露后γ-H2AX的表达。
