Cholesterol-Based Nucleolipid-Ruthenium Complex Stabilized by Lipid Aggregates for Antineoplastic Therapy

Simeone, Luca; Mangiapia, Gaetano; Vitiello, Giuseppe; Irace, Carlo; Colonna, Alfredo; Ortona, Ornella; Montesarchio, Daniela; Paduano, Luigi

doi:10.1021/bc200565v

Cited by 63 publications

(106 citation statements)

References 37 publications

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“…Aiming at improving the stability of the ruthenium(III)-based drugs in biological environments, as well as their suitability for biomedical applications, we have recently proposed an innovative strategy for their transport in vivo incorporating them within liposomial aggregates. Starting from a core molecular scaffold based on a ruthenium complex inspired to NAMI-A, named AziRu showing per se higher in vitro cytotoxicity than NAMI-A2223, we have developed a mini-library of highly functionalized amphiphilic ruthenium(III) complexes, including differently decorated nucleolipids (see Fig. 1).…”

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confidence: 99%

Antiproliferative effects of ruthenium-based nucleolipidic nanoaggregates in human models of breast cancer in vitro: insights into their mode of action

Irace

Misso

Capuozzo

et al. 2017

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101

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Looking for new metal-based anticancer treatments, in recent years many ruthenium complexes have been proposed as effective and safe potential drugs. In this context we have recently developed a novel approach for the in vivo delivery of Ru(III) complexes, preparing stable ruthenium-based nucleolipidic nanoaggregates endowed with significant antiproliferative activity. Herein we describe the cellular response to our ruthenium-containing formulations in selected models of human breast cancer. By in vitro bioscreens in the context of preclinical studies, we have focused on their ability to inhibit breast cancer cell proliferation by the activation of the intrinsic apoptotic pathway, possibly via mitochondrial perturbations involving Bcl-2 family members and predisposing to programmed cell death. In addition, the most efficient ruthenium-containing cationic nanoaggregates we have hitherto developed are able to elicit both extrinsic and intrinsic apoptosis, as well as autophagy. To limit chemoresistance and counteract uncontrolled proliferation, multiple cell death pathways activation by metal-based chemotherapeutics is a challenging, yet very promising strategy for targeted therapy development in aggressive cancer diseases, such as triple-negative breast cancer with limited treatment options. These outcomes provide valuable, original knowledge on ruthenium-based candidate drugs and new insights for future optimized cancer treatment protocols.

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confidence: 99%

Antiproliferative effects of ruthenium-based nucleolipidic nanoaggregates in human models of breast cancer in vitro: insights into their mode of action

Irace

Misso

Capuozzo

et al. 2017

Sci Rep

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101

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“…The electrical conductivity of solutions of prepared derivatives can be determined by taking about 0.1 g from derivatives (1)(2)(3)(4)(5) and dissolved in 100 mL ethanol, then put the electrode inside a sample solution with 0.002 M concentration in the experiment [25].…”

Section: The Electrical Conductivitymentioning

confidence: 99%

“…The values of entropy (ΔS) were calculated by free Gipps relationship (ΔG) [31] at every degree of thermal transition in crystal phase, mesophase and isotropic phase as in Equations (1)(2)(3)(4)(5)(6).…”

Section: Differential Scanning Calorimetry (Dsc) Studymentioning

confidence: 99%

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Synthesis, characterization, physical and biological properties of some cholesterol derivatives

2016

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A series of new cholesterol derivatives have been prepared via Mitsunobu reaction. The reaction was monitored by thin-layer chromatography (TLC) technique. All new compounds were characterized by melting points, elemental analysis, FT-IR, 1 H, 13 C and 2D-NMR spectroscopy. The antibacterial and antifungal activity of these derivatives was also determined. The phase transitions of the prepared derivatives were measured with the aid of differential scanning calorimetry. The textures of the mesophases have been determined with a hot stage equipped polarizing microscope, also the electrical conductivity of the solutions of these liquid crystals measured by electrical conductivity meter. The analysis showed that these prepared derivatives were liquid crystals.

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“…These were derivatives of estradiol [8], cholesterol [9], betulinic acid [10], and the diterpenoid phorbol [11]. They all exhibited one type of biological activity or another.…”

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confidence: 99%

Open-Chain and Macrocyclic Polyethyleneglycol Esters of the Diterpenoid Isosteviol

et al. 2014

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in which two isosteviol molecules were connected by polyethyleneglycol spacers were synthesized for the first time.The number of publications on chemical transformations of the ent-beyerane diterpenoid isosteviol (1, 16-oxo-entbeyeran-19-oic acid), which is obtained by acid hydrolysis of Stevia rebaudiana glycosides, has risen dramatically during the last five years [1]. Greater than 150 isosteviol derivatives have been reported [2]. We previously synthesized open-chain dinuclear isosteviol derivatives in which two ent-beyerane moieties were connected by polymethylene spacers with terminal esters via the reactions of isosteviol chloride with diols and of 16-dihydroisosteviol (8) with dibasic carboxylic acid chlorides [3,4]. Recently, two of these dinuclear derivatives, i.e., diacids 11 and 12, were transformed into dinuclear macrocycles in which two isosteviol ent-beyerane moieties were connected by diester spacers of different polymethylene chain lengths via reactions with diol ditosylates [5].

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Cholesterol-Based Nucleolipid-Ruthenium Complex Stabilized by Lipid Aggregates for Antineoplastic Therapy

Cited by 63 publications

References 37 publications

Antiproliferative effects of ruthenium-based nucleolipidic nanoaggregates in human models of breast cancer in vitro: insights into their mode of action

Antiproliferative effects of ruthenium-based nucleolipidic nanoaggregates in human models of breast cancer in vitro: insights into their mode of action

Synthesis, characterization, physical and biological properties of some cholesterol derivatives

Open-Chain and Macrocyclic Polyethyleneglycol Esters of the Diterpenoid Isosteviol

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