PLGA-based nanocarriers for combined delivery of colchicine and purpurin 18 in cancer therapy: Multimodal approach employing cancer cell spheroids.

Improving the anticancer efficacy of chemotherapeutic drugs and photosensitizers requires innovative multifunctional nanoplatforms. This study introduces a chemo- and phototherapeutic drug delivery system (DDS) based on poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs), both PEGylated and non-PEGylated, with a mean size of 200 ± 75 nm. Colchicine (Colch) and purpurin18 (P18) were co-encapsulated into these NPs, and their in vitro drug release profiles were investigated. The anticancer potential of these systems was evaluated across various cell lines (i.e., CaCo-2, PC-3, MCF-7, and MRC-5 cells), demonstrating enhanced NP uptake by cancer cells compared to free drugs. Co-administration of Colch and P18 in 2D and 3D cell line models exhibited a synergistic effect, harnessing both chemotherapeutic and photodynamic effects, leading to higher cancer cell elimination efficacy. This newly developed multifunctional DDS presents a promising platform for combined chemo- and photodynamic therapy in cancer treatment.

Open-tubular capillary electrochromatography with bare gold nanoparticles-based stationary phase applied to separation of trypsin digested native and glycated proteins.

In this work, open-tubular capillary electrochromatography (OT-CEC) method with bare gold nanoparticles (GNPs)-based stationary phase has been developed and applied for separation of tryptic peptide fragments of native and glycated proteins, bovine serum albumin (BSA), and human transferrin (HTF). The GNPs-based stationary phase was prepared by immobilization of bare GNPs, freshly reduced from tetrachloroaurate(III) ions by citrate reduction, on the sol-gel pretreated inner wall of the fused silica capillary. The separation efficiency, peak capacity, and peptide recovery of this open-tubular capillary column were investigated by varying the experimental parameters such as type and concentration of the buffering constituent and pH of the background electrolyte (BGE), temperature, and separation voltage. The best separations of the above tryptic peptides were achieved in the BGE composed of aqueous 100 mmol/L sodium phosphate buffer, pH 2.5, at separation voltage 10 kV per 47-cm long, 50 µm inside diameter capillary thermostated at 25°C. OT-CEC with bare GNPs stationary phase is shown to be a suitable technique for separation of complex peptide mixtures arising from tryptic digestion of native and glycated BSA and HTF, and for investigation of glycation (nonenzymatic glycosylation) of these proteins.

Application of bare gold nanoparticles in open-tubular CEC separations of polyaromatic hydrocarbons and peptides.

In this study, bare gold nanoparticles (GNPs) immobilized in the sol-gel-pretreated fused-silica (FS) capillary as a stationary phase for open-tubular capillary electrochromatography (OT-CEC) are for the first time shown to be able to separate both hydrophobic polyaromatic hydrocarbons (PAHs) as well as hydrophilic cationic antimicrobial peptides. Model mixture of four PAHs, naphthalene, fluorene, phenanthrene, and anthracene, was resolved by OT-CEC in the GNP-modified FS capillaries using the hydro-organic background electrolyte (BGE) composed of 20 mmol/L sodium phosphate buffer, pH 7, modified with ACN at 8:2 v/v ratio. On the other hand, three synthetic analogues of an antimicrobial peptide mastoparan PDD-B, basic tetradecapeptides INWKKLGKKILGAL-NH(2), INSLKLGKKILGAL-NH(2) and NWLRLGRRILGAL-NH(2), were separated in aqueous acidic BGEs, pH 2.1-3.1, composed of weak acids (formic and acetic) or amphoteric amino or imino acids (aspartic or iminodiacetic), utilizing the advantage of a slow reversed (anodic) EOF and slightly positive charge of the GNP-modified FS capillary suppressing the adsorption of cationic peptides on the inner capillary wall and improving their resolution.

Modified porphyrin-brucine conjugated to gold nanoparticles and their application in photodynamic therapy.

Two porphyrin-brucine quaternary ammonium salts were immobilized on gold nanoparticles and their suitability for both in vitro and in vivo photodynamic therapy (PDT) was assayed using the basaloid squamous cell carcinoma PE/CA-PJ34 cell line. In vitro PDT experiments revealed that the gold nanoparticle-bound conjugates were less effective than unbound conjugates in killing cells. However, the same conjugates were more effective in reducing tumor size in vivo, with complete tumor regression observed.

Glycosides of arylnaphthalene lignans from Acanthus mollis having axial chirality.

Glycosides of arylnaphthalene lignans having axial chirality were isolated from Acanthus mollis. Owing to the axial chirality, their structure, including absolute configuration, was determined by means of extensive spectroscopic data such as UV, IR, MS, 1D and 2D NMR spectra, and computational chiroptical methods. A compound, 2',4-dihydroxyretrohelioxanthin (2'-hydroxy-justirumalin), has a structure containing two aromatic moieties with substituents hindering rotation about the biaryl axis. The aglycone was connected to a saccharide moiety linked at C-4 or C-2' and made up of one or four sugars (rhamnose or quinovose, and tetrasaccharide 4-O-beta-D-xylopyranosyl-(1'''''-6'')-O-[beta-D-rhamnopyranosyl-(1''''-3'')]-O-beta-D-apiofuranosyl-(1''''-2'')-O-beta-D-glucopyranoside and quinovose). Two mono- and one tetraglycoside gave positive results in the sea urchin eggs test (Paracentrotus lividus) of cytotoxicity and in a crown gall tumor on potato disks test (Agrobacterium tumefaciens).

A biaryl xanthone derivative having axial chirality from Penicillium vinaceum.

A new xanthone derivative having axial chirality was isolated from Penicillium vinaceum. Owing to the axial chirality, its structure, including absolute configuration, was determined by means of extensive spectroscopic data, such as UV, IR, MS, and 1D and 2D NMR spectra, and computational chiroptical methods. The new compound, (a R)-2'-methoxyvinaxanthone, has a structure containing two aromatic moieties with substituents hindering rotation about the biaryl axis. The compound gave positive results in a sea urchin egg test ( Paracentrotus lividus) and a crown gall tumor on potato disks test (Agrobacterium tumefaciens).