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Comparative stability, cytotoxicity and anti-leishmanial activity of analogous organometallic Sb(V) and Bi(V) acetato complexes: Sb confirms potential while Bi fails the test
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2018-09-01 , DOI: 10.1016/j.jinorgbio.2018.08.015
Rebekah N. Duffin , Victoria L. Blair , Lukasz Kedzierski , Philip C. Andrews

A series of sixteen triphenyl Bi(V) and Sb(V) acetato complexes of general formula [MPh3(O2CCR)2] and one oxido-bridge antimony complex [(SbPh3(O2COC(O)Me))2O], have been synthesised and characterised, thirteen of which are novel. The solid-state structures of fifteen of the complexes have been successfully authenticated by single crystal X-ray diffraction. All structures, excluding the oxido-bridge antimony complex, adopt a typical trigonal bipyramidal confirmation with the phenyl rings in a propeller-like orientation in the equatorial plane. Fourteen of the complexes were screened for their anti-leishmanial activity and cytotoxicity towards mammalian cells. The Bi(V) complexes were found to be unstable in DMEM culture media and to be severely toxic towards mammalian cells, with IC50 values in the range 11.4 μM–19.8 μM. In contrast, the Sb(V) complexes demonstrated a high degree of stability and selectivity, with IC50 values 6.18–19.1 μM for the promastigote assay, and of 73.8–≤100 μM for the human fibroblasts. Assessment of the Sb(V) complexes against the clinically relevant amastigote form of these parasites at 10 μM showed all but the oxido-bridged complex to be effective, with % infection values ranging from 7.0 ± 1.7–40.5 ± 2.0.



中文翻译:

相似的有机金属Sb(V)和Bi(V)乙酰复合物的比较稳定性,细胞毒性和抗Leishmanial活性:Sb证实了潜力,而Bi未能通过测试

一系列十六种通式为[MPh 3(O 2 CCR)2 ]的三苯基Bi(V)和Sb(V)醋酸盐配合物和一个氧化桥锑配合物[(SbPh 3(O 2 C O C(O)Me ))2O],已经合成和表征,其中13种是新颖的。15种配合物的固态结构已通过单晶X射线衍射成功鉴定。除氧化桥锑络合物外,所有结构均采用典型的三角双锥体确认,其苯环在赤道平面内呈螺旋桨状。筛选了十四种复合物的抗leishmanial活性和对哺乳动物细胞的细胞毒性。发现Bi(V)复合物在DMEM培养基中不稳定,对哺乳动物细胞有严重毒性,IC 50值在11.4 μM–19.8μM范围内。相比之下,Sb(V)配合物表现出高度的稳定性和选择性,IC 50假前鞭毛虫的检测值为6.18–19.1μM,人成纤维细胞的检测值为73.8–≤100μM。对这些寄生虫的临床相关的鞭毛体形式的Sb(V)复合物进行评估,其浓度为10μM,除氧化桥复合物外,其他所有复合物均有效,%感染值范围为7.0±1.7–40.5±2.0。

更新日期:2018-09-01
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