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Pt(II) 和 Ag(I) 与乙酰磺胺酸钾配合物的晶体结构及其抗肿瘤、抗菌和抗病毒活性研究。

Pt(II) and Ag(I) complexes with acesulfame: crystal structure and a study of their antitumoral, antimicrobial and antiviral activities.

机构信息

Instituto de Química, Universidade Estadual Paulista Júlio de Mesquita Filho - UNESP, Rua Prof. Francisco Degni s/n, CEP 14801-970, Araraquara, SP, Brazil.

出版信息

J Inorg Biochem. 2010 May;104(5):533-40. doi: 10.1016/j.jinorgbio.2010.01.004. Epub 2010 Jan 18.

DOI:10.1016/j.jinorgbio.2010.01.004
PMID:20149461
Abstract

Two new complexes of platinum(II) and silver(I) with acesulfame were synthesized. Acesulfame is in the anionic form acesulfamate (ace). The structures of both complexes were determined by X-ray crystallography. For K(2)[PtCl(2)(ace)(2)] the platinum atom is coordinated to two Cl(-) and two N-acesulfamate atoms forming a trans-square planar geometry. Each K(+) ion interacts with two oxygen atoms of the S(O)(2) group of each acesulfamate. For the polymeric complex Ag(ace) the water molecule bridges between two crystallographic equivalent Ag1 atoms which are related each other by a twofold symmetry axis. Two Ag1 atoms, related to each other by a symmetry centre, make bond contact with two equivalent oxygen atoms. These bonds give rise to infinite chains along the unit cell diagonal in the ac plane. The in vitro cytotoxic analyses for the platinum complex using HeLa (human cervix cancer) cells show its low activity when compared to the vehicle-treated cells. The Ag(I) complex submitted to in vitro antimycobacterial tests, using the Microplate Alamar Blue (MABA) method, showed a good activity against Mycobacterium tuberculosis, responsible for tuberculosis, with a minimal inhibitory concentration (MIC) value of 11.6microM. The Ag(I) complex also presented a promising activity against Gram negative (Escherichia coli and Pseudomonas aeruginosa) and Gram positive (Enterococcus faecalis) microorganisms. The complex K(2)[PtCl(2)(ace)(2)] was also evaluated for antiviral properties against dengue virus type 2 (New Guinea C strain) in Vero cells and showed a good inhibition of dengue virus type 2 (New Guinea C strain) replication at 200microM, when compared to vehicle-treated cells.

摘要

合成了两个新的铂(II)和银(I)与乙酰磺胺酸钾配合物。乙酰磺胺酸钾呈阴离子形式乙酰磺胺酸盐(ace)。两个配合物的结构均通过 X 射线晶体学确定。对于 K2[PtCl2(ace)2],铂原子与两个 Cl-和两个 N-乙酰磺胺酸盐原子配位,形成反式-平面正方形几何形状。每个 K+离子与每个乙酰磺胺酸盐的 S(O)2 基团的两个氧原子相互作用。对于聚合物配合物 [Ag(ace)](n),水分子在两个结晶学等价的 Ag1 原子之间桥接,这些原子通过双重对称轴相关。两个 Ag1 原子,彼此通过对称中心相关,与两个等效的氧原子键合接触。这些键合导致沿单元胞对角线在 ac 平面上形成无限链。使用 HeLa(人宫颈癌细胞)细胞对铂配合物进行的体外细胞毒性分析表明,与载体处理的细胞相比,其活性较低。Ag(I)配合物经体外抗分枝杆菌测试,使用微孔板 Alamar Blue(MABA)法,对引起结核病的分枝杆菌结核分枝杆菌表现出良好的活性,最小抑制浓度(MIC)值为 11.6μM。Ag(I)配合物对革兰氏阴性(大肠杆菌和铜绿假单胞菌)和革兰氏阳性(粪肠球菌)微生物也表现出有希望的活性。配合物 K2[PtCl2(ace)2]也针对黄病毒 2 型(新几内亚 C 株)在 Vero 细胞中的抗病毒特性进行了评估,并与载体处理的细胞相比,在 200μM 时显示出对黄病毒 2 型(新几内亚 C 株)复制的良好抑制作用。

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