Exploring Mono and Bis-gold(I)-DTC Complexes Against Cancer and Leishmania

IF 3.2 3区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY Chemistry - An Asian Journal Pub Date : 2025-02-17 DOI:10.1002/asia.202401553

Thaiz Cristina Soares dos Santos, Patrícia Salvador Tessaro, Ana Luiza de Andrade Querino, Arthur Henrique Rodrigues Neto, Igor Martins Felix Evangelista, Alessandra Mara de Sousa, Jerônimo Nunes Rugani, Willian Xerxes Coelho Oliveira, Rubens Lima do Monte-Neto, Heveline Silva

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Abstract

Cancer is one of the main challenges of global public health and a leading cause of death, hindering the increase in life expectancy, and leishmaniasis occupies the second position in the number of deaths from parasitic diseases. Gold(I)-based drugs are being studied for chemotherapy and have shown promising results, leading to the search for analogs with more favorable effect profiles. This work presents the synthesis and characterization of five new gold(I) complexes, [Au^IDTCPPh₃] and [Au^I₂DTC(PPh₃)₂], using dithiocarbamate-derived ligands and triphenylphosphine, with potential biological activity. The antiproliferative activity was investigated in breast tumor cell lines (MDA-MB-231 and 4T1) and a non-tumor breast cell line (MCF-10a), showing that complexation with gold enhances cytotoxic activity. The antileishmanial activity was investigated against intracellular amastigotes of Leishmania (Viannia) braziliensis, L. (Leishmania) amazonensis, and L. (L.) infantum. All complexes demonstrated promising activity, especially the bis-gold(I) complexes, which showed higher activity in the studied cell lines and Leishmania parasites. The results show the importance of the gold atom in these compounds, supporting the development of gold-based compounds as prototypes for metallodrugs.

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探索单金和双金dtc配合物对抗癌症和利什曼原虫。

癌症是全球公共卫生面临的主要挑战之一，也是导致死亡的主要原因之一，阻碍了预期寿命的延长，而利什曼病在寄生虫病死亡人数中排名第二。基于金(I)的药物正在研究用于化疗，并已显示出有希望的结果，导致寻找具有更有利效果的类似物。本文利用二硫代氨基甲酸酯衍生配体和三苯基膦合成并表征了五种具有潜在生物活性的新型金(I)配合物[AuIDTCPPh3]和[AuI2DTC(PPh3)2]。在乳腺肿瘤细胞系MDA-MB-231和4T1和非肿瘤乳腺细胞系MCF-10a中研究了金的抗增殖活性，结果表明金的络合增强了细胞毒活性。研究了其对巴西利什曼原虫、亚马逊利什曼原虫和婴儿利什曼原虫胞内无尾线虫的抗利什曼原虫活性。所有配合物都显示出良好的活性，特别是双金(I)配合物，在所研究的细胞系和利什曼原虫中显示出较高的活性。结果表明金原子在这些化合物中的重要性，支持了金基化合物作为金属药物原型的发展。

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来源期刊

Chemistry - An Asian Journal 化学-化学综合

CiteScore

7.00

自引率

2.40%

发文量

535

审稿时长

1.3 months

期刊介绍： Chemistry—An Asian Journal is an international high-impact journal for chemistry in its broadest sense. The journal covers all aspects of chemistry from biochemistry through organic and inorganic chemistry to physical chemistry, including interdisciplinary topics. Chemistry—An Asian Journal publishes Full Papers, Communications, and Focus Reviews. A professional editorial team headed by Dr. Theresa Kueckmann and an Editorial Board (headed by Professor Susumu Kitagawa) ensure the highest quality of the peer-review process, the contents and the production of the journal. Chemistry—An Asian Journal is published on behalf of the Asian Chemical Editorial Society (ACES), an association of numerous Asian chemical societies, and supported by the Gesellschaft Deutscher Chemiker (GDCh, German Chemical Society), ChemPubSoc Europe, and the Federation of Asian Chemical Societies (FACS).