通过非甾体抗炎药 (NSAID) 水杨酸 (SALH2) 与促线粒体药物三苯基膦的缀合制备了两种式 [Cu(SALH)(TPP)3] 的铜 (I) 多晶型物（1a 和 1b） （TPP）通过金属离子。为了进行比较，制备了同晶型[Ag(SALH)(TPP)3](2)。通过熔点（m.p.）、衰减全反射傅里叶变换红外（ATR-FTIR）光谱、紫外-可见（UV-Vis）光谱和核磁共振（1H NMR）对缀合物1a、1b和2进行表征。 1a、1b和2的晶体结构通过X射线衍射晶体学(XRD)证实。通过 UV、荧光、粘度和 DNA 热变性研究研究了 1-2 对 CT（小牛胸腺）-DNA 的离体结合亲和力。测定了它们对脂氧合酶（LOX）（一种主要位于线粒体中的酶）的抑制活性。针对人乳腺癌细胞系 MCF-7（激素依赖性（HD））和 MDA-MB 281（激素非依赖性（HI））细胞评估了 1-2 的体外活性。化合物1-2对癌细胞的抑制作用强于顺铂。通过 MCF-7 细胞形态怀疑 1-2 的分子作用机制，并通过 DNA 片段化、吖啶橙/溴化乙锭 (AO/EB) 染色和线粒体膜透化测试证实。版权所有 © 2023 Elsevier Inc. 保留所有权利。

Two copper(I) polymorphs of formula [Cu(SALH)(TPP)3] (1a and 1b) were prepared by the conjugation of the Non-Steroidal Anti-Inflammatory Drug (NSAID) salicylic acid (SALH2) with the mitochondriotropic agent triphenylphosphine (TPP) via metal ion. For comparison, the isomorph [Ag(SALH)(TPP)3] (2) was prepared. The conjugates 1a, 1b and 2 were characterized by melting point (m.p.), Attenuated total reflection Fourier-transform infrared (ATR-FTIR) spectroscopy, Ultraviolet-Visible (UV-Vis) spectroscopy and nuclear magnetic resonance (1H NMR). The crystal structures of 1a, 1b and 2 were confirmed by X-ray diffraction crystallography (XRD). The ex vivo binding affinity of 1-2 towards CT (calf thymus)-DNA was studied by UV, fluorescence, viscosity and DNA Thermal Denaturation studies. Their inhibitory activity against lipoxygenase (LOX) (an enzyme which is mainly located in the mitochondrion) was determined. The in vitro activity of 1-2 was evaluated against human breast cancer cell lines MCF-7 (hormone depended (HD)) and MDA-MB 281 (hormone independent (HI)) cells. Compounds 1-2 inhibit stronger than cisplatin the cancerous cells. The molecular mechanism of action of 1-2 was suspected by the MCF-7 cells morphology and confirmed by DNA fragmentation, Acridine Orange/Ethidium Bromide (AO/EB) Staining and mitochondrial membrane permeabilization tests.Copyright © 2023 Elsevier Inc. All rights reserved.