Terpyridine-based ruthenium complexes containing a 4,5-diazafluoren-9-one ligand with light-driven enhancement of biological activity†

IF 3.5 3区 化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR
Francisca Mayara Santos de Alencar, Florencio Sousa Gouveia, Geângela de Fátima Sousa de Oliveira, Alexandre Lopes Andrade, Mayron Alves de Vasconcelos, Alejandro Pedro Ayala, Ana Claudia Silva Gondim, Idalina Maria Moreira de Carvalho, Carlos André Ferreira Moraes, Marcos V. Palmeira-Mello, Alzir Azevedo Batista, Luiz Gonzaga de França Lopes and Eduardo Henrique Silva Sousa
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Abstract

There has been growing effort in the scientific community to develop new antibiotics to address the major threat of bacterial resistance. One promising approach is the use of metal complexes that provide broader opportunities. Among these systems, polypyridine-ruthenium(II) complexes have received particular attention as drug candidates. Here, we prepared two new ruthenium(II) complexes with the formulation [Ru(DFO)(phtpy-R)Cl](PF6), where phtpy = 4′-phenyl-2,2′:6′,2′′-terpyridine; R = –H(MPD1), –CH3(MPD2); and DFO = 4,5-diazafluoren-9-one, and investigated their chemical, biochemical and antibacterial activities. These compounds exhibit photoreactivity and produce reactive oxygen species (ROSs). Photogeneration of singlet oxygen (1O2) was measured in acetonitrile with significant quantum yields using blue light, Φ = 0.40 and 0.39 for MDP1 and MPD2, respectively. Further studies have shown that MPD1 and MPD2 can generate superoxide radicals. Antibacterial assays demonstrated a significant enhancement in MIC (minimum inhibitory concentration) upon blue light irradiation (>32-fold), with MICs of 15.6 μg mL−1 (S. aureus, ATCC 700698) and 3.9 μg mL−1 (S. epidermidis, ATCC 35984) for both metal complexes. Interestingly, an MIC of 15.6 μg mL−1 for MPD1 and MPD2 was observed against S. epidermidis ATCC 12228 under red light irradiation. The latter results are encouraging, considering that red light penetrates deeper into the skin. In addition, no significant cytotoxicity was observed in some mammalian cells, even upon light irradiation, supporting their potential safety. Altogether, these data show evidence of the potential use of these compounds as antimicrobial photodynamic therapeutic agents, enriching our arsenal to combat this worldwide bacterial threat.

Abstract Image

含4,5-二氮芴-9- 1配体的三吡啶基钌配合物与光驱动增强生物活性
科学界一直在努力开发新的抗生素,以解决细菌耐药性的主要威胁。一种有希望的方法是使用金属配合物,它提供了更广泛的机会。在这些系统中,多吡啶-钌(II)配合物作为候选药物受到了特别的关注。本文制备了两种新型钌(II)配合物,其分子式为[Ru(DFO)(phtpy- r)Cl](PF6),其中phtpy = 4′-苯基-2,2′:6′,2′-三吡啶;R= -H(MPD1), -CH3(MPD2), DFO= 4,5-二氮芴-9- 1,研究了它们的化学和生化活性,并进行了抗菌研究。这些化合物具有光反应性并产生活性氧(ROS)。在乙腈中测量了单线态氧(1O2)在蓝光下的产率,MDP1和MPD2的产率分别为0.40和0.39。进一步的研究表明MPD1可以产生超氧自由基。抑菌实验表明,蓝光照射下,两种金属配合物的MIC(最小抑制浓度)显著增强(32倍),MIC分别为15.6µg/mL(金黄色葡萄球菌ATCC 700698)和3.9µg/mL(表皮葡萄球菌ATCC 35984)。有趣的是,在红光照射下,MPD1和MPD2对表皮葡萄球菌ATCC 12228的MIC为15.6µg/mL。考虑到红光能穿透更深的皮肤,后一种结果令人鼓舞。此外,在一些哺乳动物细胞中没有观察到明显的细胞毒性,即使在光照射下,也支持其潜在的安全性。总之,这些数据显示了这些化合物作为抗菌光动力治疗剂的潜在用途的证据,丰富了我们对抗这种全球细菌威胁的武器库。
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来源期刊
Dalton Transactions
Dalton Transactions 化学-无机化学与核化学
CiteScore
6.60
自引率
7.50%
发文量
1832
审稿时长
1.5 months
期刊介绍: Dalton Transactions is a journal for all areas of inorganic chemistry, which encompasses the organometallic, bioinorganic and materials chemistry of the elements, with applications including synthesis, catalysis, energy conversion/storage, electrical devices and medicine. Dalton Transactions welcomes high-quality, original submissions in all of these areas and more, where the advancement of knowledge in inorganic chemistry is significant.
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