Evaluation of sapogenin isolated from the defatted seeds of Camellia oleifera and its derivative as anti-breast cancer agents

IF 2.9 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia Pub Date : 2026-03-01 Epub Date: 2025-12-27 DOI:10.1016/j.fitote.2025.107075

Lu Li , Chuanqing Huang , Yunong Tian , Ying Wen , Meng Zhang , Yulin Liu , Shuhong Lin , Xianchun Hu , Yong Ye

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Abstract

The defatted seeds of Camellia oleifera are an underutilized resource that leads to poor economy. Saponins extracted from these seeds exhibit anti-breast cancer effects. To augment their anticancer efficacy, the saponins were structurally modified by the incorporation of a thiosemicarbazone moiety to yield the Camellia sapogenin thiosemicarbazone (CST). CST was subsequently complexed with zinc to form Zn-CST. This zinc complex demonstrated markedly enhanced antiproliferative and cytotoxic activity in ER+ / PR+ MCF-7 cells (IC₅₀ = 3.21 ± 0.44 μM) and HER2- T47D cells (IC₅₀ = 9.80 ± 1.31 μM), demonstrating greater potency than erlotinib. In MCF-7 cells, Zn-CST induced cell cycle arrest at the G₀ / G₁ phase and resulted in a 27-fold increase in apoptosis. Additionally, Zn-CST exhibited more potent inhibitory activity against EGFR kinase, with an IC₅₀ value of 0.25 ± 0.02 μM, compared to erlotinib. Molecular docking analysis confirmed Zn-CST's superior binding affinity for EGFR with a binding energy of −102.7 kcal/mol, predominantly due to a strong electrostatic interaction with Asp831. Collectively, these findings suggest that Zn-CST could be developed as anti ER+ / PR+ breast cancer candidate.

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油茶籽皂苷元及其衍生物抗乳腺癌作用的评价。

油茶的脱脂种子是一种未充分利用的资源，导致经济状况不佳。从这些种子中提取的皂苷具有抗乳腺癌的作用。为了增强其抗癌作用，我们对这些皂苷进行了结构修饰，加入了硫代氨基脲部分，得到了山茶皂苷基硫代氨基脲（CST）。CST随后与锌络合形成Zn-CST。这锌复杂了明显增强的抗增殖和细胞毒性活动ER + / PR + MCF-7细胞(IC₅₀ = 3.21 ±0.44  μM)和HER2 - T47D细胞(IC₅₀ = 9.80 ±1.31  μM),证明比埃罗替尼更大的力量。在MCF-7细胞中，Zn-CST诱导细胞周期阻滞在G 0 / G 1期，导致细胞凋亡增加27倍。此外，与厄洛替尼相比，Zn-CST对EGFR激酶表现出更强的抑制活性，IC₅₀值为0.25 ± 0.02 μM。分子对接分析证实，Zn-CST对EGFR具有较强的结合亲和力，结合能为-102.7 kcal/mol，这主要是由于与Asp831的强静电相互作用。总之，这些发现表明Zn-CST可以作为抗ER+ / PR+乳腺癌的候选药物。

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来源期刊

Fitoterapia 医学-药学

CiteScore

5.80

自引率

2.90%

发文量

198

审稿时长

1.5 months

期刊介绍： Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.