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Gold(iii) bis(dithiolene) complexes: from molecular conductors to prospective anticancer, antimicrobial and antiplasmodial agents.
Metallomics ( IF 2.9 ) Pub Date : 2020-04-27 , DOI: 10.1039/d0mt00064g Diana Fontinha 1 , Sílvia A Sousa 2 , Tânia S Morais 3 , Miguel Prudêncio 1 , Jorge H Leitão 2 , Yann Le Gal 4 , Dominique Lorcy 4 , Rafaela A L Silva 5 , Mariana F G Velho 6 , Dulce Belo 5 , M Almeida 5 , Joana F Guerreiro 5 , Teresa Pinheiro 7 , Fernanda Marques 5
Metallomics ( IF 2.9 ) Pub Date : 2020-04-27 , DOI: 10.1039/d0mt00064g Diana Fontinha 1 , Sílvia A Sousa 2 , Tânia S Morais 3 , Miguel Prudêncio 1 , Jorge H Leitão 2 , Yann Le Gal 4 , Dominique Lorcy 4 , Rafaela A L Silva 5 , Mariana F G Velho 6 , Dulce Belo 5 , M Almeida 5 , Joana F Guerreiro 5 , Teresa Pinheiro 7 , Fernanda Marques 5
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The anticancer, antimicrobial and antiplasmodial activities of six gold(III) bis(dithiolene) complexes were studied. Complexes 1–6 showed relevant anticancer properties against A2780/A2780cisR ovarian cancer cells (IC50 values of 0.08–2 μM), also being able to overcome cisplatin resistance in A2780cisR cells. Complex 1 also exhibited significant antimicrobial activity against Staphylococcus aureus (minimum inhibitory concentration (MIC) values of 12.1 ± 3.9 μg mL−1) and both Candida glabrata and Candida albicans (MICs of 9.7 ± 2.7 and 19.9 ± 2.4 μg mL−1, respectively). In addition, all complexes displayed antiplasmodial activity against the Plasmodium berghei parasite liver stages, even exhibiting better results than the ones obtained using primaquine, an anti-malarial drug. Mechanistic studies support the idea that thioredoxin reductase, but not DNA, is a possible target of these complexes. Complex 1 is stable under biological conditions, which would be important if this compound is ever to be considered as a drug. Overall, the results obtained evidenced the promising biological activity of complex 1, which might have potential as a novel anticancer, antimicrobial and antiplasmodial agent to be used as an alternative to current therapeutics.
中文翻译：
金（iii）双（二硫烯）复合物：从分子导体到预期的抗癌剂、抗菌剂和抗疟原虫剂。
研究了六种金（III）双（二硫烯）配合物的抗癌、抗菌和抗疟原虫活性。复合物1-6显示出针对 A2780/A2780cisR 卵巢癌细胞的相关抗癌特性（IC 50值为 0.08-2 μM），也能够克服 A2780cisR 细胞中的顺铂耐药性。复合物1还对金黄色葡萄球菌（最小抑制浓度 (MIC) 值为 12.1 ± 3.9 μg mL -1）以及光滑念珠菌和白色念珠菌（MIC 分别为 9.7 ± 2.7 和 19.9 ± 2.4 μg mL -1）表现出显着的抗菌活性， 分别）。此外，所有复合物都显示出对伯氏疟原虫肝脏阶段的抗疟原虫活性，甚至表现出比使用伯氨喹（一种抗疟疾药物）获得的效果更好的结果。机理研究支持硫氧还蛋白还原酶而非 DNA 是这些复合物的可能靶标的观点。复合物1在生物条件下是稳定的，如果该化合物被视为药物，这一点很重要。总体而言，获得的结果证明了复合物1的有希望的生物活性，它可能具有作为新型抗癌、抗菌和抗疟原虫药物的潜力，可用作当前疗法的替代品。
更新日期：2020-06-25
中文翻译：
金（iii）双（二硫烯）复合物：从分子导体到预期的抗癌剂、抗菌剂和抗疟原虫剂。
研究了六种金（III）双（二硫烯）配合物的抗癌、抗菌和抗疟原虫活性。复合物1-6显示出针对 A2780/A2780cisR 卵巢癌细胞的相关抗癌特性（IC 50值为 0.08-2 μM），也能够克服 A2780cisR 细胞中的顺铂耐药性。复合物1还对金黄色葡萄球菌（最小抑制浓度 (MIC) 值为 12.1 ± 3.9 μg mL -1）以及光滑念珠菌和白色念珠菌（MIC 分别为 9.7 ± 2.7 和 19.9 ± 2.4 μg mL -1）表现出显着的抗菌活性， 分别）。此外，所有复合物都显示出对伯氏疟原虫肝脏阶段的抗疟原虫活性，甚至表现出比使用伯氨喹（一种抗疟疾药物）获得的效果更好的结果。机理研究支持硫氧还蛋白还原酶而非 DNA 是这些复合物的可能靶标的观点。复合物1在生物条件下是稳定的，如果该化合物被视为药物，这一点很重要。总体而言，获得的结果证明了复合物1的有希望的生物活性，它可能具有作为新型抗癌、抗菌和抗疟原虫药物的潜力，可用作当前疗法的替代品。
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