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Targeted Theranostic of Cryptococcal Encephalitis by a Novel Polypyridyl Ruthenium Complex.
Molecular Pharmaceutics ( IF 4.9 ) Pub Date : 2019-12-24 , DOI: 10.1021/acs.molpharmaceut.9b00848
Qinghua Wang 1, 2 , Chen Fu 1 , Zizhen Zhao 1 , Ailing Fu 1
Affiliation  

Cryptococcus neoformans (C. neoformans) is one of the most well-known zoonotic fungal pathogens. Cryptococcal encephalitis remains a major cause of morbidity and mortality in immunocompromised hosts. Effective and targeting killing of C. neoformans in the brain is an essential approach to prevent and treat cryptococcal encephalitis. In this study, a fluorescent polypyridyl ruthenium complex RC-7, {[phen2Ru(bpy-dinonyl)](PF6)2 (phen = 1,10-phenanthroline, bpy-dinonyl = 4,4'-dinonyl-2,2'-bipyridine)}, was screened out, which showed a highly fungicidal effect on C. neoformans. The values of minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) in antifungal activities were significantly lower than fluconazole as the control. Moreover, RC-7 was prepared as a brain-targeting nanoliposome (RDP-liposome; RDP is a peptide derived from rabies virus glycoprotein) for in vivo application. The results revealed that the liposomes could accumulate in the encephalitis brain and play an antifungal role. Compared with the cryptococcal encephalitis model mice, the RDP-liposomes remarkably prolonged the survival days of the encephalitis-bearing mice from 10 days to 24 days. Here, we introduce a polypyridyl ruthenium complex that could be used as a novel antifungal agent, and this study may have a broad impact on the development of targeted delivery based on ruthenium complex-loaded liposomes for theranostics of cryptococcal encephalitis.

中文翻译:

新型多吡啶钌复合物靶向治疗隐球菌性脑炎。

新型隐球菌(C. neoformans)是最著名的人畜共患病真菌病原体之一。隐球菌脑炎仍然是免疫功能低下宿主发病和死亡的主要原因。有效和有针对性地杀死脑中的新孢子虫是预防和治疗隐球菌性脑炎的必不可少的方法。在这项研究中,荧光聚吡啶钌钌络合物RC-7,{[phen2Ru(bpy-dinonyl)](PF6)2(phen = 1,10-菲咯啉,bpy-dinonyl = 4,4'-dinonyl-2,2' -bipyridine)},被筛选出来,这显示了对新孢梭菌的高度杀真菌作用。抗真菌活性中的最小抑菌浓度(MIC)和最小杀真菌浓度(MFC)的值显着低于作为对照的氟康唑。此外,RC-7制备为脑靶向纳米脂质体(RDP-脂质体;RDP是一种来自狂犬病病毒糖蛋白的肽,可用于体内应用。结果表明脂质体可在脑炎脑中积聚并起抗真菌作用。与隐球菌性脑炎模型小鼠相比,RDP-脂质体显着延长了携带脑炎的小鼠的存活天数从10天延长至24天。在这里,我们介绍了可以用作新型抗真菌剂的聚吡啶基钌复合物,这项研究可能对基于载有钌复合物的脂质体用于隐球菌脑炎治疗的靶向递送的发展产生广泛的影响。与隐球菌性脑炎模型小鼠相比,RDP-脂质体显着延长了携带脑炎的小鼠的存活天数从10天延长至24天。在这里,我们介绍了可以用作新型抗真菌剂的聚吡啶基钌复合物,这项研究可能对基于载有钌复合物的脂质体用于隐球菌脑炎治疗的靶向递送的发展产生广泛的影响。与隐球菌性脑炎模型小鼠相比,RDP-脂质体显着延长了携带脑炎的小鼠的存活天数从10天延长至24天。在这里,我们介绍了可以用作新型抗真菌剂的聚吡啶基钌复合物,这项研究可能对基于载有钌复合物的脂质体用于隐球菌脑炎治疗的靶向递送的发展产生广泛的影响。
更新日期:2019-12-25
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