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以银和金基N-杂环卡宾配合物靶向克氏锥虫:对寄生虫死亡和锥虫硫醇还原酶相互作用的见解。

Targeting Trypanosoma cruzi with silver and gold-based N-heterocyclic carbene complexes: insights into parasite death and trypanothione reductase interaction.

作者信息

Bernal Yuly, Marquez Angie Melo, Rangel Hector Rafael, Goite Maria Cristina, Noguera Pedro, Fuentes Franmerly, Machado Rubén, Castro William, Velasquéz Vaneza Paola Lorett, Buendia-Atencio Cristian, Cristancho Eduvan Valencia, Rodriguez Anny Karely, Lopez-Pazos Silvio, Losada-Barragán Monica

机构信息

Facultad de Ciencias, Universidad Antonio Nariño-Sede Circunvalar, Cra. 3 Este # 47A - 15, Bogotá, D.C., Colombia.

Laboratorio de Virología Molecular, Venezuelan Institute for Scientific Research, IVIC, Caracas, Venezuela.

出版信息

Biometals. 2025 Aug 14. doi: 10.1007/s10534-025-00731-4.

DOI:10.1007/s10534-025-00731-4
PMID:40804207
Abstract

Chagas disease remains a major public health challenge, and there is a need for new therapeutic agents. N-heterocyclic carbene (NHC) complexes, particularly those linked to silver or gold, have shown significant anticancer, antimicrobial, and antiparasitic activities. This study aimed to evaluate the efficacy of four NHC compounds (QMT3, QMT4, QMT7, and QMT8) against Trypanosoma cruzi, the causative agent of Chagas disease. In vitro assays revealed that QMT3 and QMT8 exhibited the strongest antiparasitic effects, with QMT3 showing the highest potency and stability over time (IC₅₀ = 10.3 µg/mL at 24 h). Both compounds induced rapid, irreversible cell death in epimastigotes, primarily through late apoptotic-like and necrotic pathways, as evidenced by Annexin V/PI labeling. Additionally, treatment with QMT3 and QMT8 led to significant increases in intracellular reactive oxygen species (ROS), particularly superoxide (SO). Notably, both compounds displayed high specificity for the parasite with low cytotoxicity towards mammalian cells, although QMT8 was less toxic to host cells than QMT3 at short exposure times. Molecular modeling studies revealed that QMT3, and QMT8 bind to the active site of TryR, a crucial player in maintaining redox homeostasis in trypanosomatids, potentially competing with its natural ligand and disrupting its enzymatic function. These findings suggest that QMT3 and QMT8, silver- and gold-based NHC complexes, act through redox system disruption and TryR inhibition, positioning them as promising candidates for the development of new treatments for Chagas disease.

摘要

恰加斯病仍然是一项重大的公共卫生挑战,因此需要新的治疗药物。N-杂环卡宾(NHC)配合物,特别是那些与银或金相连的配合物,已显示出显著的抗癌、抗菌和抗寄生虫活性。本研究旨在评估四种NHC化合物(QMT3、QMT4、QMT7和QMT8)对恰加斯病病原体克氏锥虫的疗效。体外试验表明,QMT3和QMT8表现出最强的抗寄生虫作用,其中QMT3在一段时间内显示出最高的效力和稳定性(24小时时IC₅₀ = 10.3 μg/mL)。两种化合物均可诱导前鞭毛体快速、不可逆的细胞死亡,主要通过晚期凋亡样和坏死途径,Annexin V/PI标记证明了这一点。此外,用QMT3和QMT8处理导致细胞内活性氧(ROS)显著增加,尤其是超氧化物(SO)。值得注意的是,尽管在短暴露时间下QMT8对宿主细胞的毒性低于QMT3,但这两种化合物对寄生虫均表现出高特异性,对哺乳动物细胞的细胞毒性较低。分子模拟研究表明,QMT3和QMT8与TryR的活性位点结合,TryR是锥虫中维持氧化还原稳态的关键因子,它们可能与其天然配体竞争并破坏其酶功能。这些发现表明,基于银和金的NHC配合物QMT3和QMT8通过破坏氧化还原系统和抑制TryR发挥作用,使其成为开发恰加斯病新疗法的有希望的候选药物。

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