Strong anticancer activity of copper(ii) and zinc(ii) complexes containing naturally occurring lapachol: cellular effects in ovarian A2780 cells.

Copper(ii) and zinc(ii) complexes with lapachol (HLap) of the composition [M(Lap)(N-N)] and [Cu(Lap)(HO)(terpy)]NO (4), where M = Cu (1-3) or Zn (for 5-7), and N-N stands for bathophenanthroline (1 and 5), 5-methyl-1,10-phenanthroline (2 and 6), 2,2'-bipyridine (3), 2,2';6',2''-terpyridine (terpy, 4) and 1,10-phenanthroline (7), were synthesised and characterised. Complexes 1-5 revealed strong antiproliferative effects against A2780, A2780R, MCF-7, PC-3, A549 and HOS human cancer lines and MRC-5 normal cells, with IC values above 0.5 μM, and reasonable selectivity index (SI), with SI > 3.

Single Atom Engineered Antibiotics Overcome Bacterial Resistance.

The outbreak of antibiotic-resistant bacteria, or "superbugs", poses a global public health hazard due to their resilience against the most effective last-line antibiotics. Identifying potent antibacterial agents capable of evading bacterial resistance mechanisms represents the ultimate defense strategy. This study shows that -the otherwise essential micronutrient- manganese turns into a broad-spectrum potent antibiotic when coordinated with a carboxylated nitrogen-doped graphene.

C-Geranylated flavanone diplacone enhances in vitro antiproliferative and anti-inflammatory effects in its copper(II) complexes.

Two copper(II) complexes containing diplacone (Hdipl), a naturally occurring C-geranylated flavanone derivative, in combination with bathophenanthroline (bphen) or 1,10-phenanthroline (phen) with the composition [Cu(bphen)(Hdipl)]⋅2HO (1) and {[Cu(phen)(Hdipl)]⋅1.25HO} (2) were prepared and characterized. As compared to diplacone, the complexes enhanced in vitro cytotoxicity against A2780 and A2780R human ovarian cancer cells (IC ≈ 0.

Dinuclear copper(II) complexes with a bridging bis(chalcone) ligand reveal considerable in vitro cytotoxicity on human cancer cells and enhanced selectivity.

A bis(chalcone) molecule (HL) was synthesized via Aldol's condensation from terephthalaldehyde and 2'-hydroxyacetophenone and it was used as bridging ligand for the preparation of five dinuclear copper(II) complexes of the composition [Cu(NN)(μ-L)Cu(NN)](NO)⋅nHO (n = 0-2) (1-5), where NN stands for a bidentate N-donor ligand such as phen (1,10-phenanthroline, 1), bpy (2,2'-bipyridine, 2), mebpy (5,5'-dimethyl-2,2'-dipyridine, 3), bphen (bathophenanthroline, 4) and nphen (5-nitro-1,10-phenanthroline, 5). The compounds were characterized by different suitable techniques to confirm their purity, composition, and structure. Moreover, the products were evaluated for their in vitro cytotoxicity on a panel of human cancer cell lines: ovarian (A2780), ovarian resistant to cisplatin (A2780R), prostate (PC3), osteosarcoma (HOS), breast (MCF7) and lung (A549), and normal fibroblasts (MRC-5), showing significant cytotoxicity in most cases, with IC ≈ 0.

Label-free detection and mapping of graphene oxide in single HeLa cells based on MCR-Raman spectroscopy.

GO is a 2D nanomaterial that has attracted attention in many industries in recent years, such as the chemical industry, electronics or medicine. Due to its unique properties such as strength, hydrophilicity and large specific surface area with the possibility of functionalization, GO is a particularly attractive material in biomedicine as a candidate for use in targeted drug delivery. In such a case, we need information on whether graphene oxide penetrates into cells and whether we are able to detect and monitor GO in these cells during and also after the treatment to evaluate possible degradation process of GO and its interaction within the cell compartements.

The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties.

Motivated by the clinical success of gold(I) metallotherapeutic in the effective treatment of both inflammatory and cancer diseases, we decided to prepare, characterize, and further study the [Au(kin)(PPh)] complex (), where Hkin = kinetin, 6-furfuryladenine, for its in vitro anti-cancer and anti-inflammatory activities. The results revealed that the complex () had significant in vitro cytotoxicity against human cancer cell lines (A2780, A2780R, PC-3, 22Rv1, and THP-1), with IC ≈ 1-5 μM, which was even significantly better than that for the conventional platinum-based drug while comparable with . Although its ability to inhibit transcription factor NF-κB activity did not exceed the comparative drug , it has been found that it is able to positively influence peroxisome-proliferator-activated receptor-gamma (PPARγ), and as a consequence of this to have the impact of moderating/reducing inflammation.

Dinuclear doubly bridged phenoxido copper(II) complexes as efficient anticancer agents.

Two cationic [Cu(L)](ClO) (1, 2), and four neutral doubly bridged-phenoxido-copper(II) complexes [Cu(L)] (3, 4) and [Cu(L)(HO)]‧2HO (5, 6) as well as 1D polymeric catena-[Cu(L)] (7), where HL and HL represent tripodal tetradentate pyridyl or aliphatic-amino groups based 2,4-disubstituted phenolates, were synthesized and thoroughly characterized by various spectroscopic methods and single crystal X-ray analysis. The molecular structures of the complexes exhibited diverse geometrical environments around the central Cu(II) atoms. The in vitro antiproliferative activity of the isolated complexes and selected parent free ligands were screened against some human cancer cell lines (A2780, A2780R, PC-3, 22Rv1, MCF-7).

Carbon dots for virus detection and therapy.

Recent experience with the COVID-19 pandemic should be a lesson learnt with respect to the effort we have to invest in the development of new strategies for the treatment of viral diseases, along with their cheap, easy, sensitive, and selective detection. Since we live in a globalized world where just hours can play a crucial role in the spread of a virus, its detection must be as quick as possible. Thanks to their chemical stability, photostability, and superior biocompatibility, carbon dots are a kind of nanomaterial showing great potential in both the detection of various virus strains and a broad-spectrum antiviral therapy.

Silver Covalently Bound to Cyanographene Overcomes Bacterial Resistance to Silver Nanoparticles and Antibiotics.

The ability of bacteria to develop resistance to antibiotics is threatening one of the pillars of modern medicine. It was recently understood that bacteria can develop resistance even to silver nanoparticles by starting to produce flagellin, a protein which induces their aggregation and deactivation. This study shows that silver covalently bound to cyanographene (GCN/Ag) kills silver-nanoparticle-resistant bacteria at concentrations 30 times lower than silver nanoparticles, a challenge which has been so far unmet.

Condensed Clustered Iron Oxides for Ultrahigh Photothermal Conversion and Multimodal Imaging.

Magnetic iron oxide nanocrystals (MIONs) are established as potent theranostic nanoplatforms due to their biocompatibility and the multifunctionality of their spin-active atomic framework. Recent insights have also unveiled their attractive near-infrared photothermal properties, which are, however, limited by their low near-infrared absorbance, resulting in noncompetitive photothermal conversion efficiencies (PCEs). Herein, we report on the dramatically improved photothermal conversion of condensed clustered MIONs, reaching an ultrahigh PCE of 71% at 808 nm, surpassing the so-far MION-based photothermal agents and even benchmark near-infrared photothermal nanomaterials.

The Differential Effect of Carbon Dots on Gene Expression and DNA Methylation of Human Embryonic Lung Fibroblasts as a Function of Surface Charge and Dose.

This study presents a toxicological evaluation of two types of carbon dots (CD), similar in size (<10 nm) but differing in surface charge. Whole-genome mRNA and miRNA expression (RNAseq), as well as gene-specific DNA methylation changes, were analyzed in human embryonic lung fibroblasts (HEL 12469) after 4 h and 24 h exposure to concentrations of 10 and 50 µg/mL (for positive charged CD; pCD) or 10 and 100 µg/mL (for negative charged CD, nCD). The results showed a distinct response for the tested nanomaterials (NMs).

Human DNA-Damage-Inducible 2 Protein Is Structurally and Functionally Distinct from Its Yeast Ortholog.

Although Ddi1-like proteins are conserved among eukaryotes, their biological functions remain poorly characterized. Yeast Ddi1 has been implicated in cell cycle regulation, DNA-damage response, and exocytosis. By virtue of its ubiquitin-like (UBL) and ubiquitin-associated (UBA) domains, it has been proposed to serve as a proteasomal shuttle factor.