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In vitro Biological Activities of Gold(I) and Gold(III) Bis (N-Heterocyclic Carbene) Complexes

机译:黄金(I)和黄金(III)bis(N-杂环卡宾)复合物的体外生物学活性

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The aim of this research is to evaluate for the first time the in vitro leishmanicidal activity and inhibition of a-glucosidase and b-glucuronidase of new gold(I) and gold(III) complexes involving N-heterocyclic carbene (NHC) ligands, with the general formula [Au(X)n(NHC)R2][BF4] (X=Cl, OAc, R=various aromatic and aliphatic substituents). The Au(III) complexes were shown to have a significant antileishmanial activity, and were also found to be more potent inhibitors of α-glucosidase and β-glucuronidase enzymes than the standard drugs. Some complexes were also identified as potent anti-inflammatory agents with activity comparable to that of tested standard drugs, allopurinol and ibuprofen. These gold complexes were also evaluated for their in vitro cytotoxic activity against HeLa (cervical cancer), MCF-3 (breast cancer), and 3T3 (mouse fibroblast) cell lines.
机译:这项研究的目的是首次评估新黄金(I)和黄金(III)络合物的A-葡萄糖苷酶和B-葡萄糖醛酸酶的体外利什曼酶活性以及涉及N-杂环碳(NHC)配体的B-葡萄糖醛酸苷酶, 通用公式[au(x)n(nhc)r2] [bf4](x = cl,oac,r =各种芳族和脂肪族取代基)。 AU(III)复合物被证明具有显着的抗抗精性活性,并且还发现比标准药物更有效地抑制α-葡萄糖苷酶和β-葡萄糖醛酸苷酶酶。 一些复合物也被鉴定为有效的抗炎剂,其活性与测试的标准药物,别嘌醇和布洛芬相当。 还评估了这些金复合物针对HELA(宫颈癌),MCF-3(乳腺癌)和3T3(小鼠成纤维细胞)细胞系的体外细胞毒性活性。

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