International Journal of Biological Macromolecules ( IF 7.7 ) Pub Date : 2024-01-02 , DOI: 10.1016/j.ijbiomac.2023.129177 Yiwen Wang 1 , Chen Lou 2 , Siyuan Zhao 1 , Binfen Li 1 , Youli Zhang 1 , Zhecheng Yu 3 , Fangfang Wu 1 , Daqing Chen 1 , Qian Wu 1
We reported the anti-cervical cancer effect of proprietary saponin content from seeds of Impatiens balsamina L., Hosenkoside A. Our study found that Hosenkoside A significantly promotes cell apoptosis and cell cycle arrest after administration, exhibiting anti-tumor effects. Then the transcriptome sequencing results after administration showed that Hosenkoside A had a significant inhibitory effect on Histone deacetylase 3 (HDAC3). After sufficient administration time, the inhibition of HDAC3 expression level leads to a significant decrease in lysine acetylation at histone 3 sites 4 and 9, blocking the activation of Signal transducer and activator of transcription 3 (STAT3) and achieving anti-tumor effects. In addition, we encapsulated Hosenkoside A into polypeptide metal complexes (PMC) to form slow-release spheres. This material breaks down in the tumor environment, not only does it solve the problem of low drug solubility, but it also achieves targeted sustained-release drug delivery. Under the same concentration of stimulation, the PMC complex group showed better anti-tumor effects in both in vitro and in vivo experiments.
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多肽金属配合物包被的Hosenkoside A的制备及其对宫颈癌的抑制作用
我们报告了凤仙花种子中专有皂苷成分 Hosenkoside A 的抗宫颈癌作用。我们的研究发现,Hosenkoside A 给药后显着促进细胞凋亡和细胞周期停滞,表现出抗肿瘤作用。然后给药后的转录组测序结果显示Hosenkoside A对组蛋白脱乙酰酶3(HDAC3)有显着的抑制作用。给予足够时间后,抑制HDAC3表达水平导致组蛋白3位点4和9的赖氨酸乙酰化显着降低,阻断信号转导和转录激活因子3(STAT3)的激活,从而达到抗肿瘤作用。此外,我们将Hosenkoside A封装到多肽金属配合物(PMC)中形成缓释球体。这种材料在肿瘤环境中分解,不仅解决了药物溶解度低的问题,还实现了靶向缓释药物递送。在相同浓度的刺激下,PMC复合物组在体外和体内实验中均表现出更好的抗肿瘤效果。