用碘取代金诺芬中的硫糖可增强卵巢癌小鼠模型中的抗癌效力。
Replacement of the Thiosugar of Auranofin with Iodide Enhances the Anticancer Potency in a Mouse Model of Ovarian Cancer.
作者信息
Marzo Tiziano, Massai Lara, Pratesi Alessandro, Stefanini Matteo, Cirri Damiano, Magherini Francesca, Becatti Matteo, Landini Ida, Nobili Stefania, Mini Enrico, Crociani Olivia, Arcangeli Annarosa, Pillozzi Serena, Gamberi Tania, Messori Luigi
机构信息
Department of Pharmacy, University of Pisa, via Bonanno Pisano 6, 56126 Pisa, Italy.
Laboratory of Metals in Medicine (MetMed), Department of Chemistry "U. Schiff", University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.
出版信息
ACS Med Chem Lett. 2019 Feb 7;10(4):656-660. doi: 10.1021/acsmedchemlett.9b00007. eCollection 2019 Apr 11.
Abstract
In recent years, a few successful attempts were made to repurpose the clinically approved antiarthritic gold drug, Auranofin (), as an anticancer agent. The present study shows that the iodido(triethylphosphine)gold(I) complex, ( hereafter)-an analogue where the thiosugar ligand is simply replaced by one iodide ligand-manifests a solution chemistry resembling that of and exerts similar cytotoxic and proapoptotic effects on A2780 human ovarian cancer cells . However, when evaluated in a preclinical orthotopic model of ovarian cancer, produces a far superior anticancer action than inducing a nearly complete tumor remission. The highly promising performances here documented for warrant its further evaluation as a drug candidate for ovarian cancer treatment.
摘要
近年来，人们成功进行了一些尝试，将临床批准的抗关节炎金药物金诺芬（）重新用作抗癌剂。本研究表明，碘（三乙膦）金（I）配合物（以下简称）——硫代糖配体简单地被一个碘配体取代的类似物——表现出与金诺芬相似的溶液化学性质，并对A2780人卵巢癌细胞产生类似的细胞毒性和促凋亡作用。然而，在卵巢癌的临床前原位模型中进行评估时，产生的抗癌作用远比金诺芬优越，可诱导几乎完全的肿瘤缓解。此处记录的的极具前景的表现，使其有理由作为卵巢癌治疗的候选药物进行进一步评估。
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