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1.
Pharmaceutics ; 15(6)2023 Jun 07.
Article in English | MEDLINE | ID: mdl-37376122

ABSTRACT

The therapeutic efficiency of plant extracts has been limited by their poor pharmaceutical availability. Hydrogels have promising potential to be applied as wound dressings due to their high capacity to absorb exudates and their enhanced performance in loading and releasing plant extracts. In this work, pullulan/poly (vinyl alcohol) (P/PVA) hydrogels were first prepared using an eco-friendly method based on both a covalent and physical cross-linking approach. Then, the hydrogels were loaded with the hydroalcoholic extract of Calendula officinalis by a simple post-loading immersion method. Different loading capacities were investigated in terms of the physico-chemical properties, chemical composition, mechanical properties, and water absorption. The hydrogels exhibited high loading efficiency due to the hydrogen bonding interactions between polymer and extract. The water retention capacity as well as the mechanical properties decreased with the increase in the extract amount in hydrogel. However, higher amounts of extract in the hydrogel improved the bioadhesiveness. The release of extract from hydrogels was controlled by the Fickian diffusion mechanism. Extract-loaded hydrogels expressed high antioxidant activity, reaching 70% DPPH radical scavenging after 15 min immersion in buffer solution at pH 5.5. Additionally, loaded hydrogels showed a high antibacterial activity against Gram-positive and Gram-negative bacteria and were non-cytotoxic against HDFa cells.

2.
Molecules ; 26(15)2021 Aug 02.
Article in English | MEDLINE | ID: mdl-34361832

ABSTRACT

In recent times, researchers have aimed for new strategies to combat cancer by the implementation of nanotechnologies in biomedical applications. This work focuses on developing protein-based nanoparticles loaded with a newly synthesized NIR emitting and absorbing phthalocyanine dye, with photodynamic and photothermal properties. More precisely, we synthesized highly reproducible bovine serum albumin-based nanoparticles (75% particle yield) through a two-step protocol and successfully encapsulated the NIR active photosensitizer agent, achieving a good loading efficiency of 91%. Making use of molecular docking simulations, we confirm that the NIR photosensitizer is well protected within the nanoparticles, docked in site I of the albumin molecule. Encouraging results were obtained for our nanoparticles towards biomedical use, thanks to their negatively charged surface (-13.6 ± 0.5 mV) and hydrodynamic diameter (25.06 ± 0.62 nm), favorable for benefitting from the enhanced permeability and retention effect; moreover, the MTT viability assay upholds the good biocompatibility of our NIR active nanoparticles. Finally, upon irradiation with an NIR 785 nm laser, the dual phototherapeutic effect of our NIR fluorescent nanoparticles was highlighted by their excellent light-to-heat conversion performance (photothermal conversion efficiency 20%) and good photothermal and size stability, supporting their further implementation as fluorescent therapeutic agents in biomedical applications.


Subject(s)
Indoles/administration & dosage , Nanoparticles/administration & dosage , Ovarian Neoplasms/drug therapy , Photochemotherapy/methods , Photosensitizing Agents/administration & dosage , Serum Albumin, Bovine/chemistry , Cell Proliferation , Female , Humans , Indoles/chemistry , Isoindoles , Light , Molecular Docking Simulation , Nanoparticles/chemistry , Ovarian Neoplasms/pathology , Photosensitizing Agents/chemistry , Spectroscopy, Near-Infrared , Tumor Cells, Cultured
4.
J Ethnopharmacol ; 252: 112559, 2020 Apr 24.
Article in English | MEDLINE | ID: mdl-31935497

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Crataegus leaves, flowers and fruits have been traditionally used to improve blood circulation, numerous preclinical and clinical studies supporting the cardiovascular benefits of Crataegus preparations. In this respect, there is very limited data on Crataegus pentagyna; in addition, the chemical profile of this species is still incompletely elucidated. AIM OF THE STUDY: The objective of this study was to examine the cardiovascular benefits of Crataegus pentagyna Waldst. et Kit. ex Willd. (small-flowered black hawthorn, Rosaceae) extracts (leaf, flower and fruit ethyl acetate extracts) and the underlying mechanisms. We hypothesized that C. pentagyna extracts might exert vasodilatory effects and inhibit arginase activity due, in large part, to their polyphenolic constituents. MATERIALS AND METHODS: C. pentagyna extracts induced-relaxation and the mechanisms involved were studied ex vivo in isolated aortic rings from Sprague-Dawley rats. The inhibitory effects on bovine liver arginase I were assessed by an in vitro assay. Metabolite profiling of C. pentagyna extracts was performed and the most endothelium- and nitric oxide synthase-dependent; flower extract additionally reduced Ca2+ entry and, to a lesser extent, Ca2+ release from the sarcoplasmic reticulum. C. pentagyna proved to be an important source of arginase inhibitors with potential benefits in endothelial dysfunction that remains to be explored.


Subject(s)
Aorta, Thoracic/drug effects , Arginase/antagonists & inhibitors , Plant Extracts/pharmacology , Polyphenols/pharmacology , Vasodilator Agents/pharmacology , Animals , Aorta, Thoracic/physiology , Calcium/physiology , Crataegus , Endothelium, Vascular/drug effects , Endothelium, Vascular/physiology , Flowers , Fruit , Male , Plant Leaves , Potassium Channels/physiology , Rats, Sprague-Dawley
5.
Food Chem Toxicol ; 133: 110764, 2019 Nov.
Article in English | MEDLINE | ID: mdl-31437471

ABSTRACT

The present study investigated the effects of Cornus mas, Sorbus aucuparia and Viburnum opulus fruit extracts on arginase activity and arterial vasodilation. V. opulus fruit extract exerted the highest vasorelaxant activity in phenylephrine precontracted rat aortic rings (EC50 = 6.31 ±â€¯1.61 µg/mL) and a significant inhibition of arginase (IC50 = 71.02 ±â€¯3.06 µg/mL). By contrast, S. aucuparia and C. mas fruit extracts showed no important anti-arginase activity and a significantly weaker activity in the rat aortic rings relaxation assay (EC50 = 100.9 ±â€¯11.63 and 78.52 ±â€¯8.59 µg/mL, respectively). For all extracts, the main mechanism of vasodilation was proven to be endothelium-dependent. HPLC-ESI-Q-TOF-MS/MS studies revealed a very complex metabolite profiling in all three extracts with chlorogenic acid accounting for 30.89, 0.72 and 2.03 mg/g in V. opulus, C. mas and S. aucuparia fruit extracts, respectively. All extracts were declared non-toxic in the brine shrimp acute toxicity test. Our study highlights potential benefits of V. opulus fruit extract in diseases associated with endothelial dysfunction and impaired vasodilation.


Subject(s)
Arginase/antagonists & inhibitors , Enzyme Inhibitors/pharmacology , Fruit/chemistry , Plant Extracts/pharmacology , Vasodilator Agents/pharmacology , Animals , Aorta/drug effects , Artemia/drug effects , Chromatography, High Pressure Liquid , Cornus/chemistry , Endothelium/drug effects , Enzyme Inhibitors/toxicity , Male , Metabolome , Plant Extracts/toxicity , Rats, Sprague-Dawley , Sorbus/chemistry , Tandem Mass Spectrometry , Vasodilator Agents/toxicity , Viburnum/chemistry
6.
PLoS One ; 13(8): e0202441, 2018.
Article in English | MEDLINE | ID: mdl-30153262

ABSTRACT

Young wheat plantlets (wheatgrass), represent a significant source of minerals, enzymes, vitamins, while also rich in phenolics and chlorophylls, with considerable bioactivities. As the biosynthesis of such compounds may be influenced by growth conditions, the current research assesses wheatgrass composition in soil based and hydroponic systems, using water with different elemental composition. FTIR spectroscopy did not reveal significant variations between juice and extracts cultivated in different setups. Surface elemental composition indicated higher Na, P, Si concentrations in hydroponic plants, while AAS analyses showed increased Ca and Mn in soil presence. HPLC-MS of extracts showed that soil and spring water increased chlorophyll and hydroxychlorophyll a concentrations. Phenolic contents were higher in hydroponic plants, while maximum values were recorded for spring water. Radical scavenging activity was stimulated by the use of spring water. Results indicate that wheatgrass with improved mineral and macromolecular composition may be obtained using accessible cultivation setups.


Subject(s)
Phosphorus/metabolism , Polyphenols/metabolism , Silicon Dioxide/metabolism , Sodium/metabolism , Triticum/growth & development
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