Novel erbium complex with anticancer activity against radiation resistant lung adenocarcinoma cells

IF 3.2 2区化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Journal of Inorganic Biochemistry Pub Date : 2025-03-19 DOI:10.1016/j.jinorgbio.2025.112902

Hao Wang , Guozhu Ren , Yue Xu , Ruiping Deng , Rui Wang , Liang Zhou

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Abstract

In this work, novel erbium complex with anticancer activity against radiation resistant lung adenocarcinoma cells was obtained and demonstrated. Firstly, stronger inhibitory effect of Er³⁺ on non-small cell lung cancer (NSCLC) cells and NSCLC- radiation resistant (RR) cells was experimentally confirmed. Then, by selecting highly biocompatible porphyrins as ligands, a novel erbium complex tetraphenylporphyrin erbium acetylacetonate (Er(acac)TPP) was synthesized and purified. Compared with Cisplatin, notably, Er(acac)TPP exhibits relatively higher inhibitory efficiency on NSCLC-RR cells. Moreover, the toxicities of Er(acac)TPP to normal cells are much lower than that of cancer cells. Subsequently, cell expansion, increased apoptosis, a decline in mitochondrial membrane potential (MMP), an accumulation of intracellular reactive oxygen species (ROS), increased Caspase-9 protein level and G2/M arrest were seen. These data all pointed to Er(acac)TPP as a possible candidate for more research and development as a chemotherapeutic drug.

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新型铒复合物对耐辐射肺腺癌细胞具有抗癌活性

本研究获得并证实了新型铒配合物对耐辐射肺腺癌细胞具有抗癌活性。首先，实验证实Er3+对非小细胞肺癌（NSCLC）细胞和NSCLC-耐辐射（RR）细胞有较强的抑制作用。然后，选择具有高度生物相容性的卟啉作为配体，合成并纯化了新型的四苯基卟啉乙酰丙酮铒（Er(acac)TPP）。值得注意的是，与顺铂相比，Er(acac)TPP对NSCLC-RR细胞的抑制效率相对较高。此外，Er(acac)TPP对正常细胞的毒性远低于癌细胞。随后出现细胞扩增、凋亡增加、线粒体膜电位（MMP）下降、细胞内活性氧（ROS）积累、Caspase-9蛋白水平升高和G2/M阻滞。这些数据都表明，作为一种化疗药物，Er(acac)TPP有可能成为进一步研究和开发的候选药物。

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阿拉丁

Xylene

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Benzaldehyde

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P-nitrobenzoic acid

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Pyrrole

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Imidazole

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Erbium acetylacetonate (Er(acac)3)

来源期刊

Journal of Inorganic Biochemistry 生物-生化与分子生物学

CiteScore

7.00

自引率

10.30%

发文量

336

审稿时长

41 days

期刊介绍： The Journal of Inorganic Biochemistry is an established international forum for research in all aspects of Biological Inorganic Chemistry. Original papers of a high scientific level are published in the form of Articles (full length papers), Short Communications, Focused Reviews and Bioinorganic Methods. Topics include: the chemistry, structure and function of metalloenzymes; the interaction of inorganic ions and molecules with proteins and nucleic acids; the synthesis and properties of coordination complexes of biological interest including both structural and functional model systems; the function of metal- containing systems in the regulation of gene expression; the role of metals in medicine; the application of spectroscopic methods to determine the structure of metallobiomolecules; the preparation and characterization of metal-based biomaterials; and related systems. The emphasis of the Journal is on the structure and mechanism of action of metallobiomolecules.