Exploring Titanium(IV) Complexes as Potential Antimicrobial Compounds.
Exploring Titanium(IV) Complexes as Potential Antimicrobial Compounds.
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DOI：
10.3390/antibiotics11020158
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发表时间：
2022-01-26
期刊：
影响因子：
--
通讯作者：
Tinoco AD
中科院分区：
文献类型：
--
作者：
Rodríguez I;Fernández-Vega L;Maser-Figueroa AN;Sang B;González-Pagán P;Tinoco AD
由于病原微生物的快速突变，抗药性超级细菌已经进化出来。抗微生物细菌可能与其他细菌共享其抗性基因，使其无法治疗。寻找更具战斗力的抗生素化合物促使研究人员探索以金属为基础的策略，这些策略的核心是干扰微生物中必需金属的生物利用度，并研究金属络合物的治疗潜力。鉴于对钛（IV）应用的有限了解，在这项工作中，8个Ti（IV）配合物和它们的一些相应配体由开放式抗菌药物发现社区筛选抗菌活性。选择这些化合物进行评价，因为它们对人非癌细胞系的细胞毒性/抗增殖行为较低。在pH 7.4时，这些化合物在其溶液稳定性和配体交换不稳定性方面有所不同;因此，对其溶液行为的评估提供了关于金属化合物的特性对抗微生物治疗潜力的重要性的一些见解。只有一种化合物Ti（地拉罗司）2对革兰氏阳性菌耐甲氧西林金黄色葡萄球菌表现出有希望的抑制活性，对人体细胞的毒性最小。这种化合物的能力进行transmetalation与不稳定的Fe（III）源，因此，抑制铁的生物利用度和核糖核苷酸还原酶的评价作为一个可能的机制，其抗生素的作用。
Due to the rapid mutation of pathogenic microorganisms, drug-resistant superbugs have evolved. Antimicrobial-resistant germs may share their resistance genes with other germs, making them untreatable. The search for more combative antibiotic compounds has led researchers to explore metal-based strategies centered on perturbing the bioavailability of essential metals in microbes and examining the therapeutic potential of metal complexes. Given the limited knowledge on the application of titanium(IV), in this work, eight Ti(IV) complexes and some of their corresponding ligands were screened by the Community for Open Antimicrobial Drug Discovery for antimicrobial activity. The compounds were selected for evaluation because of their low cytotoxic/antiproliferative behavior against a human non-cancer cell line. At pH 7.4, these compounds vary in terms of their solution stability and ligand exchange lability; therefore, an assessment of their solution behavior provides some insight regarding the importance of the identity of the metal compound to the antimicrobial therapeutic potential. Only one compound, Ti(deferasirox)2, exhibited promising inhibitory activity against the Gram-positive bacteria methicillin-resistant Staphylococcus aureus and minimal toxicity against human cells. The ability of this compound to undergo transmetalation with labile Fe(III) sources and, as a consequence, inhibit Fe bioavailability and ribonucleotide reductase is evaluated as a possible mechanism for its antibiotic effect.
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影响因子：
4.8
作者：
Frei, Angelo
通讯作者：
Frei, Angelo
DOI：
10.1107/s1600536805021276
发表时间：
2005-08-01
期刊：
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS
影响因子：
--
作者：
Dey, R;Mukharjee, K;Roychowdhury, P
通讯作者：
Roychowdhury, P
DOI：
10.1107/s0108270193006493
发表时间：
1994-06-15
期刊：
ACTA CRYSTALLOGRAPHICA SECTION C-CRYSTAL STRUCTURE COMMUNICATIONS
影响因子：
--
作者：
FESTER, A;BENSCH, W;TROMEL, M
通讯作者：
TROMEL, M
DOI：
10.1107/s160053680502475x
发表时间：
2005-09-01
期刊：
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS
影响因子：
--
作者：
Fu, YL;Xu, ZW;Ng, SW
通讯作者：
Ng, SW
影响因子：
4.8
作者：
Ketikidis, Ioannis;Banti, Christina N.;Hadjikakou, Sotiris K.
通讯作者：
Hadjikakou, Sotiris K.