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Anti-leishmanial activity and cytotoxicity of a series of tris-aryl Sb(V) mandelate cyclometallate complexes.
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2019-11-23 , DOI: 10.1016/j.jinorgbio.2019.110932 Rebekah N Duffin 1 , Victoria L Blair 1 , Lukasz Kedzierski 2 , Philip C Andrews 1
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2019-11-23 , DOI: 10.1016/j.jinorgbio.2019.110932 Rebekah N Duffin 1 , Victoria L Blair 1 , Lukasz Kedzierski 2 , Philip C Andrews 1
Affiliation
A series of ten cyclometallates and two μ2-peroxo bridged tris-aryl Sb(V) complexes derived from R/S-mandelic acid (= R/S-ManH2) were synthesised and characterised. As confirmed by X-ray crystallography the complexes 1Sr/s, [Sb(o-tol)3(man)], 2Sr/s, [Sb(m-tol)3(man)], 4Sr/s, [Sb(o-PhOMe)3(man)], 5Sr/s, [Sb(Mes)3(man)] and 6Sr/s, [Sb(p-tert-BuPh)3(man)] are all cyclometallates. Complexes 3Sr/s, [(Sb(p-tol)3(manH)2O2], contain a bridging O22- anion in the solid-state but convert to the cyclometallates in DMSO solution with concomitant release of H2O2 and formation of complexes [Sb(p-tol)3(man)], 3Sr'/s'. All complexes underwent initial testing against both human fibroblasts and L. major V121 promastigotes. IC50 values were found to range from 2.07 (6Sr) to >100 (4Sr) μM and 0.21 (5Ss) to >100 (4Ss) μM for fibroblasts and parasites respectively. Two of the complexes were found to be ineffective, displaying no toxicity (4S/r). Despite the degree of mammalian toxicity, the selectivity of most complexes exceeded an SI of three and so were assessed for their anti-amastigote activity. Excellent anti-amastigote activity was observed for complexes at both 10 μM and 5 μM, with percentage infection value ranging from 0.15-3.00% for those tested at 10 μM and 0.25-2.50% for those at 5 μM.
中文翻译:
一系列三芳基Sb(V)扁桃酸盐环金属酸盐配合物的抗Leishmanial活性和细胞毒性。
合成和表征了一系列十个环金属盐和两个μ2-过氧桥接的R / S-扁桃酸(= R / S-ManH2)形成的三芳基Sb(V)配合物。通过X射线晶体学证实,配合物1Sr / s,[Sb(o-tol)3(man)],2Sr / s,[Sb(m-tol)3(man)],4Sr / s,[Sb( o-PhOMe)3(man),5Sr / s,[Sb(Mes)3(man)]和6Sr / s,[Sb(p-tert-BuPh)3(man)]均为环金属盐。络合物3Sr / s [[(Sb(p-tol)3(manH)2O2])在固态中包含桥接的O22-阴离子,但在DMSO溶液中转化为环金属盐,同时释放出H2O2和形成络合物[Sb (p-tol)3(man)],3Sr'/ s'。所有复合物均已针对人成纤维细胞和主要V121前鞭毛体进行了初步测试,IC50值范围从2.07(6Sr)到> 100(4Sr) μM和0.21(5Ss)至 成纤维细胞和寄生虫分别为100(4Ss)μM。发现其中两种复合物无效,没有毒性(4S / r)。尽管具有哺乳动物毒性,但大多数复合物的选择性都超过了3的SI,因此评估了它们的抗寄生虫活性。在10μM和5μM的复合物中均观察到出色的抗鞭毛虫活性,对于10μM的复合物,感染百分比范围为0.15-3.00%,对于5μM的复合物,感染百分比范围为0.25-2.50%。
更新日期:2019-11-26
中文翻译:
一系列三芳基Sb(V)扁桃酸盐环金属酸盐配合物的抗Leishmanial活性和细胞毒性。
合成和表征了一系列十个环金属盐和两个μ2-过氧桥接的R / S-扁桃酸(= R / S-ManH2)形成的三芳基Sb(V)配合物。通过X射线晶体学证实,配合物1Sr / s,[Sb(o-tol)3(man)],2Sr / s,[Sb(m-tol)3(man)],4Sr / s,[Sb( o-PhOMe)3(man),5Sr / s,[Sb(Mes)3(man)]和6Sr / s,[Sb(p-tert-BuPh)3(man)]均为环金属盐。络合物3Sr / s [[(Sb(p-tol)3(manH)2O2])在固态中包含桥接的O22-阴离子,但在DMSO溶液中转化为环金属盐,同时释放出H2O2和形成络合物[Sb (p-tol)3(man)],3Sr'/ s'。所有复合物均已针对人成纤维细胞和主要V121前鞭毛体进行了初步测试,IC50值范围从2.07(6Sr)到> 100(4Sr) μM和0.21(5Ss)至 成纤维细胞和寄生虫分别为100(4Ss)μM。发现其中两种复合物无效,没有毒性(4S / r)。尽管具有哺乳动物毒性,但大多数复合物的选择性都超过了3的SI,因此评估了它们的抗寄生虫活性。在10μM和5μM的复合物中均观察到出色的抗鞭毛虫活性,对于10μM的复合物,感染百分比范围为0.15-3.00%,对于5μM的复合物,感染百分比范围为0.25-2.50%。