乳腺癌是当今世界发病率和死亡率极高的癌症之一，目前，毒性小、副作用低、多靶点治疗且效果好的天然产物成为乳腺癌药物开发热点。红景天中存在两种具有良好的生物活性单体红景天苷及酪醇，该研究采用ORAC法确定其抗氧化能力，以三阴性乳腺癌细胞MDA-MB-231为实验模型，考察其抗增殖效果，通过细胞划痕实验、流式细胞仪检测细胞凋亡及周期以及RT-qPCR进一步探究相关机制。结果表明，红景天苷及酪醇均能够显著抑制MDAMB-231的增殖，其EC50值分别为63.55、127.35 μmol/L；细胞划痕实验表明它们能显著抑制细胞迁移，在36 h时高浓度组红景天苷和酪醇分别将细胞愈合率从72.16%降低至27.86%和32.69%；细胞周期和凋亡实验表明红景天苷和酪醇将细胞周期绝大部分阻滞在G2期并促进细胞凋亡；RT-qPCR实验发现红景天苷主要通过上调p53、p21基因，下调Bcl-2、Bcl-xL、CDK6基因发挥抗MDA-MB-231增殖效果，酪醇主要通过上调p53、p21、Bax基因发挥作用。上述结果为单体红景天苷和酪醇的生物活性研究提供理论支持，并为将来抗乳腺癌药物的开发提供理论依据。

The high morbidity and mortality rates that are associated with breast cancer worldwide render the discovery of new drugs critical, and natural products with low toxicity, minimal side effects, multiple targeting, and good efficacy are hot topics in the development of such drugs. Two monomers derived from Rhodiola rosea L., salidroside and tyrosol, have shown good bioactivity. Thus, the ORAC method was used to determine the antioxidant capacity of these compounds, with the triple-negative breast cancer cell line, MDA-MB-231, used as an experimental model to investigate the anti-proliferation effects of the monomers. Cell scratch assay and flow cytometry were performed to detect cell apoptosis and cell cycle stage, and RT-qPCR was employed to further explore related mechanisms. The results showed that salidroside and tyrosol can significantly inhibit the proliferation of MDA-MB-231, with EC50 values of 63.55 and 127.35 μmol/L, respectively. Cell scratch assays showed significantly inhibited cell migration, and after 36 h, salidroside and tyrosol were shown to reduce the cell healing rate from 72.16 % to 27.86 % and 32.69 %, respectively, in the high-concentration groups, while cell cycle and apoptosis assays showed that both salidroside and tyrosol arrest the cell cycle at the G2 phase, promoting apoptosis. RT-qPCR showed that the anti-proliferation effects observed for salidroside are mainly due to up-regulation of the p53 and p21 genes and down-regulation of the Bcl-2, Bcl-xL, and CDK6 genes, whereas the efficacy of tyrosol is associated with up-regulation of the p53, p21, and Bax genes. These results provide theoretical support for further study into the bioactivity of salidroside and tyrosol and provide a theoretical basis for the development of anti-breast cancer drugs in the future.

广东省自然科学基金资助项目（2021A1515012110）