3-氨基黄酮的反式铂（II）配合物——合成、X射线晶体结构及体外生物活性

trans-Platinum(II) complex of 3-aminoflavone - synthesis, X-ray crystal structure and biological activities in vitro.

作者信息

Fabijańska Małgorzata, Studzian Kazimierz, Szmigiero Leszek, Rybarczyk-Pirek Agnieszka J, Pfitzner Arno, Cebula-Obrzut Barbara, Smolewski Piotr, Zyner Elżbieta, Ochocki Justyn

机构信息

Department of Bioinorganic Chemistry, 1 Muszyńskiego St., Medical University, 90-151 Łódź, Poland.

出版信息

Dalton Trans. 2015 Jan 21;44(3):938-47. doi: 10.1039/c4dt01501k.

DOI:10.1039/c4dt01501k

PMID:25110914

Abstract

This paper describes the synthesis of trans-bis-(3-aminoflavone)dichloridoplatinum(ii) (trans-Pt(3-af)2Cl2; TCAP) for use as a potential anticancer compound, and the evaluation of its structure by elemental and spectral analyses, and X-ray crystallography. The complex demonstrated a significant cytotoxic effect against human and murine cancer cell lines, as well as weaker toxicity towards healthy cells (human peripheral blood lymphocytes) in comparison with cisplatin. Various biochemical and morphological methods confirm that the proapoptotic activity of trans-Pt(3-af)2Cl2 is markedly higher than the reference cisplatin. Our results suggest that trans-Pt(3-af)2Cl2 may have a different antitumour specificity from that of cisplatin.

摘要

本文描述了反式双（3-氨基黄酮）二氯铂（II）（反式-Pt(3-af)2Cl2；TCAP）作为一种潜在抗癌化合物的合成，以及通过元素分析、光谱分析和X射线晶体学对其结构的评估。该配合物对人和小鼠癌细胞系表现出显著的细胞毒性作用，与顺铂相比，对健康细胞（人外周血淋巴细胞）的毒性较弱。各种生化和形态学方法证实，反式-Pt(3-af)2Cl2的促凋亡活性明显高于参比顺铂。我们的结果表明，反式-Pt(3-af)2Cl2可能具有与顺铂不同的抗肿瘤特异性。