Antileukemia Activity and Mechanism of Platinum(II)-Based Metal Complexes

Pietro, Maria Letizia Di; Stagno, Claudio; Efferth, Thomas; Omer, Ejlal A.; D’Angelo, Valeria; Germanò, Maria Paola; Cacciola, Anna; Gaetano, Federica De; Iraci, Nunzio; Micale, Nicola

doi:10.3390/molecules27249000

Cited by 6 publications

(9 citation statements)

References 47 publications

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“…In other studies, complexes have been identified which act as intercalating agents because they have the capacity to be introduced between nitrogenous bases of DNA. This intercalation mechanism has mainly been reported for complexes with planar ligands and aromatic systems [ 14 , 18 ]. Furthermore, complexes that interact with DNA through the major and minor grooves have also been reported [ 54 ].…”

Section: Recent Studies On Platinum(ii) and Copper(ii) Complexes And ...mentioning

confidence: 85%

“…Such characteristics include increased solubility, specificity, effectiveness and stability. Ligands such as phosphines [ 11 , 12 , 13 , 14 , 15 , 16 ], dithiocarbamates [ 17 , 18 ], triazoles [ 19 ], saccharinates [ 11 , 15 ], terpyridines [ 20 ], benzothiazoles [ 21 , 22 ], Schiff bases [ 23 ], benzimidazoles [ 24 ], imides [ 25 , 26 , 27 , 28 ] and others [ 10 , 29 ], as well as metal ions such as palladium, ruthenium, nickel, rhodium, iridium, gold and copper, have all been used in the development of new coordination compounds or metal complexes by researchers taking a biological approach [ 5 , 30 , 31 , 32 ]. At the same time, functionalization processes have also been developed for the controlled administration of drugs from existing complexes; these include liposome encapsulation [ 33 ], macrocycles, metal nanoparticles and carbo nanotubes [ 34 , 35 ], as well as bioconjugation [ 35 ].…”

Section: Introductionmentioning

confidence: 99%

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Recently Reported Biological Activities and Action Targets of Pt(II)- and Cu(II)-Based Complexes

Maciel-Flores,

Lozano-Alvarez,

Bivián-Castro

2024

Molecules

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Most diseases that affect human beings across the world are now treated with drugs of organic origin. However, some of these are associated with side effects, toxicity, and resistance phenomena. For the treatment of many illnesses, the development of new molecules with pharmacological potential is now an urgent matter. The biological activities of metal complexes have been reported to have antitumor, antimicrobial, anti-inflammatory, anti-infective and antiparasitic effects, amongst others. Metal complexes are effective because they possess unique properties. For example, the complex entity possesses the effective biological activity, then the formation of coordination bonds between the metal ions and ligands is controlled, metal ions provide it with extraordinary mechanisms of action because of characteristics such as d-orbitals, oxidation states, and specific orientations; metal complexes also exhibit good stability and good physicochemical properties such as water solubility. Platinum is a transition metal widely used in the design of drugs with antineoplastic activities; however, platinum is associated with side effects which have made it necessary to search for, and design, novel complexes based on other metals. Copper is a biometal which is found in living systems; it is now used in the design of metal complexes with biological activities that have demonstrated antitumoral, antimicrobial and anti-inflammatory effects, amongst others. In this review, we consider the open horizons of Cu(II)- and Pt(II)-based complexes, new trends in their design, their synthesis, their biological activities and their targets of action.

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Section: Recent Studies On Platinum(ii) and Copper(ii) Complexes And ...mentioning

confidence: 85%

Section: Introductionmentioning

confidence: 99%

Recently Reported Biological Activities and Action Targets of Pt(II)- and Cu(II)-Based Complexes

Maciel-Flores,

Lozano-Alvarez,

Bivián-Castro

2024

Molecules

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“…Then, 20 μL of 0.01% resazurin (Promega) was added to each well. The fluorescence of resazurin was measured after 4 h of incubation using an Infinite M2000 Pro plate reader (Tecan) at an Ex/Em = 550 nm/590 nm wavelength . The viability of the cells was calculated in comparison to the DMSO control.…”

Section: Methodsmentioning

confidence: 99%

Synthesis and Bioactivity of Isoflavones from Ficus carica and Some Non-Natural Analogues

et al. 2023

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Ficucaricone D (1) and its 4′-demethyl congener 2 are isoflavones isolated from fruits of Ficus carica that share a 5,7-dimethoxy-6-prenyl-substituted A-ring. Both natural products were, for the first time, obtained by chemical synthesis in six steps, starting from 2,4,6-trihydroxyacetophenone. Key steps are a microwave-promoted tandem sequence of Claisen-and Cope-rearrangements to install the 6-prenyl substituent and a Suzuki−Miyaura cross coupling for installing the B-ring. By using various boronic acids, non-natural analogues become conveniently available. All compounds were tested for cytotoxicity against drug-sensitive and drug-resistant human leukemia cell lines, but were found to be inactive. The compounds were also tested for antimicrobial activities against a panel of eight Gram-negative and two Gram-positive bacterial strains. Addition of the efflux pump inhibitor phenylalanine-arginine-β-naphthylamide (PAβN) significantly improved the antibiotic activity in most cases, with MIC values as low as 2.5 μM and activity improvement factors as high as 128-fold.

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“…With this in mind, and given the polyanionic nature of DNA, the use of cationic compounds capable of sliding along the surface of the target once in immediate proximity, establishing a second type of interaction with it, could prove very important. Moreover, several Pt (II) intercalating compounds have been developed over the years, and their cytotoxicity against different tumor cell lines has been demonstrated 28–30 . Recently, several types of metal complexes have also shown promising results in antiviral and antimicrobial research 31–34 .…”

Section: Introductionmentioning

confidence: 99%

“…Moreover, several Pt (II) intercalating compounds have been developed over the years, and their cytotoxicity against different tumor cell lines has been demonstrated. [28][29][30] Recently, several types of metal complexes have also shown promising results in antiviral and antimicrobial research. [31][32][33][34] Herein, in this paper, we report the biological activity results of sixteen Pt (II) compounds, capable of intercalating between DNA nucleobases, evaluated against three cancerous cell lines, namely, MDA-MB 231 (breast adenocarcinoma), U87 (glioblastoma), and U2-OS (osteosarcoma), which have been selected as they are known to express DNA G-quadruplex (G-4) secondary structures.…”

Section: Introductionmentioning

confidence: 99%

Anticancer activity and morphological analysis of Pt (II) complexes: Their DFT approach, docking simulation, and ADME‐Tox profiling

Rossi,

Stagno,

Piperno

et al. 2024

Applied Organom Chemis

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A consistent series of Pt (II) polypyridyl complexes (i.e., LDP‐10–25), previously obtained and characterized by our research group, underwent extensive biological investigations to verify their activity profile as target‐based anticancer agents. Preliminary in vitro screening at 10 μM against three tumor cell lines known to overexpress DNA G‐4 (MDA‐MB 231, U87, and U2‐OS) pointed out that four of them, namely, LDP‐15, LDP‐16, LDP‐24, and LDP‐25, had promising cytotoxic activity compared with cisplatin. Therefore, these four compounds were selected for continuous assays against the same three cell lines and morphological analyses on U2‐OS cells that showed IC50 values in the micromolar range and remarkable changes in nuclei shape and cytoskeleton integrity, respectively. Docking studies supported the idea that the antiproliferative activity of the complexes could be attributed to their interaction via a hybrid binding mode with the intended molecular target, DNA G‐4. In addition, in silico ADME‐Tox profiling studies showed no risk of tumorigenic, irritant, or reproductive effects for the title compounds. DFT calculations were used to verify the structural characteristics of the four selected compounds and to investigate their electronic behavior. Overall, the results obtained, both experimentally and theoretically, indicate that LDP‐15, LDP‐16, LDP‐24, and LDP‐25 complexes could be useful for further study as potential therapeutic agents.

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Antileukemia Activity and Mechanism of Platinum(II)-Based Metal Complexes

Cited by 6 publications

References 47 publications

Recently Reported Biological Activities and Action Targets of Pt(II)- and Cu(II)-Based Complexes

Recently Reported Biological Activities and Action Targets of Pt(II)- and Cu(II)-Based Complexes

Synthesis and Bioactivity of Isoflavones from Ficus carica and Some Non-Natural Analogues

Anticancer activity and morphological analysis of Pt (II) complexes: Their DFT approach, docking simulation, and ADME‐Tox profiling

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