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1.
Molecules ; 29(19)2024 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-39407698

RESUMO

Deep eutectic solvents (DESs) have attracted attention from researchers as novel compounds for extracting active substances because of their negligible toxicity, polarity, and ability to be tailored depending on the experiment. In this review, we discuss deep eutectic solvents as a promising medium for the extraction of adaptogenic compounds. In comparison to traditional methods, extraction with the use of DESs is a great alternative to the excessive usage of harmful organic solvents. It can be conducted in mild conditions, and DESs can be designed with different precursors, enhancing their versatility. Adaptogenic herbs have a long medicinal history, especially in Eastern Asia. They exhibit unique properties through the active compounds in their structures, including saponins, flavonoids, polysaccharides, and alkaloids. Therefore, they demonstrate a wide range of pharmaceutical effects, such as anti-inflammatory, antibacterial, and anticancer abilities. Since ancient times, many different adaptogenic herbs have been discovered and are well known, including Panax ginseng, Scutellaria baicalensis, and Schisandra chinensis. Active compounds can be extracted using standard methods, such as hydrolyzation, maceration, and conventional reflux extraction. However, due to the limitations of classical processing technologies, there has been a need to develop new and eco-friendly methods. We focus on the types of solvents, extraction efficiency, properties, and applications of the obtained active compounds. This review highlights the potential of DESs as eco-friendly alternatives for extracting bioactive compounds.


Assuntos
Solventes Eutéticos Profundos , Solventes Eutéticos Profundos/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Solventes/química , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos
2.
Int J Mol Sci ; 25(13)2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-39000045

RESUMO

Cancer remains a significant global health challenge, with millions of deaths attributed to it annually. Radiotherapy, a cornerstone in cancer treatment, aims to destroy cancer cells while minimizing harm to healthy tissues. However, the harmful effects of irradiation on normal cells present a formidable obstacle. To mitigate these effects, researchers have explored using radioprotectors and mitigators, including natural compounds derived from secondary plant metabolites. This review outlines the diverse classes of natural compounds, elucidating their roles as protectants of healthy cells. Furthermore, the review highlights the potential of these compounds as radioprotective agents capable of enhancing the body's resilience to radiation therapy. By integrating natural radioprotectors into cancer treatment regimens, clinicians may improve therapeutic outcomes while minimizing the adverse effects on healthy tissues. Ongoing research in this area holds promise for developing complementary strategies to optimize radiotherapy efficacy and enhance patient quality of life.


Assuntos
Produtos Biológicos , Neoplasias , Protetores contra Radiação , Humanos , Neoplasias/tratamento farmacológico , Neoplasias/radioterapia , Protetores contra Radiação/uso terapêutico , Protetores contra Radiação/farmacologia , Produtos Biológicos/farmacologia , Produtos Biológicos/uso terapêutico , Animais
3.
Int J Mol Sci ; 25(11)2024 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-38891938

RESUMO

Neurological disorders present a wide range of symptoms and challenges in diagnosis and treatment. Cannabis sativa, with its diverse chemical composition, offers potential therapeutic benefits due to its anticonvulsive, analgesic, anti-inflammatory, and neuroprotective properties. Beyond cannabinoids, cannabis contains terpenes and polyphenols, which synergistically enhance its pharmacological effects. Various administration routes, including vaporization, oral ingestion, sublingual, and rectal, provide flexibility in treatment delivery. This review shows the therapeutic efficacy of cannabis in managing neurological disorders such as epilepsy, neurodegenerative diseases, neurodevelopmental disorders, psychiatric disorders, and painful pathologies. Drawing from surveys, patient studies, and clinical trials, it highlights the potential of cannabis in alleviating symptoms, slowing disease progression, and improving overall quality of life for patients. Understanding the diverse therapeutic mechanisms of cannabis can open up possibilities for using this plant for individual patient needs.


Assuntos
Cannabis , Epilepsia , Doenças Neurodegenerativas , Humanos , Cannabis/química , Doenças Neurodegenerativas/tratamento farmacológico , Epilepsia/tratamento farmacológico , Transtornos Mentais/tratamento farmacológico , Animais , Dor/tratamento farmacológico , Anticonvulsivantes/uso terapêutico , Canabinoides/uso terapêutico , Canabinoides/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/química , Analgésicos/uso terapêutico , Analgésicos/química , Analgésicos/farmacologia
4.
Materials (Basel) ; 17(12)2024 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-38930158

RESUMO

The present work reports an effective method for the removal of inorganic and organic pollutants using membranes based on different carbonaceous materials. The membranes were prepared based on cellulose acetate (18 wt. %), polyvinylpyrrolidone as a pore-generating agent (2 wt. %) and activated carbon (1 wt. %). Activated carbons were developed from residues after extraction of the mushroom Inonotus obliguus using microwave radiation. It has been demonstrated that the addition of activated carbon to the membranes resulted in alterations to their physical properties, including porosity, equilibrium water content and permeability. Furthermore, the chemical properties of the membranes were also affected, with changes observed in the content of the surface oxygen group. The addition of carbon material had a positive effect on the removal of copper ions from their aqueous solutions by the cellulose-carbon composites obtained. Moreover, the membranes proved to be more effective in the removal of copper ions than iron ones and phenol. The membranes were found to show higher effectiveness in copper removal from a solution of the initial concentration of 800 mg/L. The most efficient in copper ions removal was the membrane containing urea-enriched activated carbon.

5.
Pharmaceuticals (Basel) ; 17(5)2024 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-38794188

RESUMO

Sambuci folium (elderberry leaves) have been used in traditional medicine, mainly externally, to treat skin diseases and wounds. Therefore, the aim of this study was to screen the biological activity of elderberry leaves (antioxidant potential and possibility of inhibition of tyrosinase and hyaluronidase enzymes) combined with phytochemical analysis. For this purpose, a phytochemical analysis was carried out. Elderberry leaves of 12 varieties ("Sampo", "Obelisk", "Dwubarwny", "Haschberg", "Haschberg 1", "Koralowy", "Sambo", "Black Beauty", "Black Tower", "Golden hybrid", "Samyl", "Samyl 1") in two growth stages. The compounds from the selected groups, phenolic acids (chlorogenic acid) and flavonols (quercetin), were chromatographically determined in hydroalcoholic leaf extracts. All tested elderberry leaf extracts showed antioxidant effects, but the most promising potential: very high compounds content (TPC = 61.85 mg GAE/g), antioxidant (e.g., DPPH IC50 = 1.88 mg/mL; CUPRAC IC0.5 = 0.63 mg/mL) and optimal anti-inflammatory (inhibition of hyaluronidase activity 41.28%) activities were indicated for older leaves of the "Sampo" variety. Additionally, the extract obtained from "Sampo" and "Golden hybrid" variety facilitated the treatment of wounds in the scratch test. In summary, the best multidirectional pro-health effect in treating skin inflammation was specified for "Sampo" leaves II extract (leaves during the flowering period); however, wound treatment was noted as rich in chlorogenic acid younger leaf extracts of the "Golden hybrid" variety.

6.
Int J Mol Sci ; 25(7)2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38612460

RESUMO

In this study, binary amorphous solid dispersions (ASDs, fisetin-Eudragit®) and ternary amorphous solid inclusions (ASIs, fisetin-Eudragit®-HP-ß-cyclodextrin) of fisetin (FIS) were prepared by the mechanochemical method without solvent. The amorphous nature of FIS in ASDs and ASIs was confirmed using XRPD (X-ray powder diffraction). DSC (Differential scanning calorimetry) confirmed full miscibility of multicomponent delivery systems. FT-IR (Fourier-transform infrared analysis) confirmed interactions that stabilize FIS's amorphous state and identified the functional groups involved. The study culminated in evaluating the impact of amorphization on water solubility and conducting in vitro antioxidant assays: 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)-ABTS, 2,2-diphenyl-1-picrylhydrazyl-DPPH, Cupric Reducing Antioxidant Capacity-CUPRAC, and Ferric Reducing Antioxidant Power-FRAP and in vitro neuroprotective assays: inhibition of acetylcholinesterase-AChE and butyrylcholinesterase-BChE. In addition, molecular docking allowed for the determination of possible bonds and interactions between FIS and the mentioned above enzymes. The best preparation turned out to be ASI_30_EPO (ASD fisetin-Eudragit® containing 30% FIS in combination with HP-ß-cyclodextrin), which showed an improvement in apparent solubility (126.5 ± 0.1 µg∙mL-1) and antioxidant properties (ABTS: IC50 = 10.25 µg∙mL-1, DPPH: IC50 = 27.69 µg∙mL-1, CUPRAC: IC0.5 = 9.52 µg∙mL-1, FRAP: IC0.5 = 8.56 µg∙mL-1) and neuroprotective properties (inhibition AChE: 39.91%, and BChE: 42.62%).


Assuntos
Adenoma , Benzotiazóis , Flavonóis , Ácidos Polimetacrílicos , Ácidos Sulfônicos , beta-Ciclodextrinas , Humanos , Acetilcolinesterase , Antioxidantes/farmacologia , Butirilcolinesterase , Simulação de Acoplamento Molecular , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier
7.
Int J Mol Sci ; 25(7)2024 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-38612575

RESUMO

Multifunctional delivery systems capable of modulating drug release and exerting adjunctive pharmacological activity have attracted particular attention. Chitosan (CS) and pomegranate seed oil (PO) appear to be attractive bioactive components framing the strategy of complex therapy and multifunctional drug carriers. This research is aimed at evaluating the potential of CS in combination with PO in studies on topical emulgels containing hydrocortisone as a model anti-inflammatory agent. Its particular goal was to distinguish alterations in anti-inflammatory action followed with drug dissolution or penetrative behavior between the designed formulations that differ in CS/PO weight ratio. All formulations favored hydrocortisone release with up to a two-fold increase in the drug dissolution rate within first 5 h as compared to conventional topical preparations. The clear effect of CS/PO on the emulgel biological performance was observed, and CS was found to be prerequisite for the modulation of hydrocortisone absorption and accumulation. In turn, a greater amount of PO played the predominant role in the inhibition of hyaluronidase activity and enhanced the anti-inflammatory effect of preparation E-3. Emulgels showed a negligible reduction in mouse fibroblasts' L929 cell viability, confirming their non-irritancy with skin cells. Overall, the designed formulation with a CS/PO ratio of 6:4 appeared to be the most promising topical carrier for the effective treatment of inflammatory skin diseases among the tested subjects.


Assuntos
Quitosana , Punica granatum , Animais , Camundongos , Humanos , Hidrocortisona/farmacologia , Anti-Inflamatórios/farmacologia , Óleos de Plantas/farmacologia
8.
Int J Mol Sci ; 25(5)2024 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-38474022

RESUMO

In this study, amorphous solid dispersions (ASDs) of pterostilbene (PTR) with polyvinylpyrrolidone polymers (PVP K30 and VA64) were prepared through milling, affirming the amorphous dispersion of PTR via X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Subsequent analysis of DSC thermograms, augmented using mathematical equations such as the Gordon-Taylor and Couchman-Karasz equations, facilitated the determination of predicted values for glass transition (Tg), PTR's miscibility with PVP, and the strength of PTR's interaction with the polymers. Fourier-transform infrared (FTIR) analysis validated interactions maintaining PTR's amorphous state and identified involved functional groups, namely, the 4'-OH and/or -CH groups of PTR and the C=O group of PVP. The study culminated in evaluating the impact of amorphization on water solubility, the release profile in pH 6.8, and in vitro permeability (PAMPA-GIT and BBB methods). In addition, it was determined how improving water solubility affects the increase in antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays) and neuroprotective (inhibition of cholinesterases: AChE and BChE) properties. The apparent solubility of the pure PTR was ~4.0 µg·mL-1 and showed no activity in the considered assays. For obtained ASDs (PTR-PVP30/PTR-PVPVA64, respectively) improvements in apparent solubility (410.8 and 383.2 µg·mL-1), release profile, permeability, antioxidant properties (ABTS: IC50 = 52.37/52.99 µg·mL-1, DPPH: IC50 = 163.43/173.96 µg·mL-1, CUPRAC: IC0.5 = 122.27/129.59 µg·mL-1, FRAP: IC0.5 = 95.69/98.57 µg·mL-1), and neuroprotective effects (AChE: 39.1%/36.2%, BChE: 76.9%/73.2%) were confirmed.


Assuntos
Antioxidantes , Benzotiazóis , Povidona , Ácidos Sulfônicos , Resveratrol , Povidona/química , Polímeros/química , Solubilidade , Difração de Raios X , Água , Varredura Diferencial de Calorimetria , Espectroscopia de Infravermelho com Transformada de Fourier
9.
Molecules ; 29(6)2024 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-38542923

RESUMO

Our research aimed to develop an amorphous solid dispersion (ASD) of myricetin (MYR) with Polyvinylpyrrolidone K30 (PVP30) to enhance its solubility, dissolution rate, antioxidant, and neuroprotective properties. Employing a combination of solvent evaporation and freeze drying, we successfully formed MYR ASDs. XRPD analysis confirmed complete amorphization in 1:8 and 1:9 MYR-PVP weight ratios. DSC thermograms exhibited a single glass transition (Tg), indicating full miscibility. FT-IR results and molecular modeling confirmed hydrogen bonds stabilizing MYR's amorphous state. HPLC analysis indicated the absence of degradation products, ensuring safe MYR delivery systems. Solubility, dissolution rate (pH 1.2 and 6.8), antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays), and in vitro neuroprotective activities (inhibition of cholinesterases: AChE and BChE) were significantly improved compared to the pure compound. Molecular docking studies revealed that MYR had made several hydrogen, hydrophobic, and π-π stacking interactions, which could explain the compound's potency to inhibit AChE and BChE. MYR-PVP 1:9 w/w ASD has the best solubility, antioxidant, and neuroprotective activity. Stability studies confirmed the physical stability of MYR-PVP 1:9 w/w ASD immediately after dissolution and for two months under ambient conditions. Our study showed that the obtained ASDs are promising systems for the delivery of MYR with the potential for use in alleviating the symptoms of neurodegenerative diseases.


Assuntos
Antioxidantes , Flavonoides , Povidona , Espectroscopia de Infravermelho com Transformada de Fourier , Antioxidantes/farmacologia , Simulação de Acoplamento Molecular , Solubilidade , Povidona/química
10.
Int J Mol Sci ; 25(5)2024 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-38473770

RESUMO

Turmeric, known for its curcuminoid-rich rhizome, particularly curcumin, exhibits notable antioxidant and antiviral properties. The likelihood of microbial contamination necessitates finding reliable techniques for subjecting the sample to radiation from this plant-based raw material. One alternative is to expose curcumin to radiation (e-beam), which was carried out as part of this research. Confirmation of the lack of curcumin decomposition was carried out using HPLC-DAD/MS techniques. Additionally, using the EPR technique, the generated free radicals were defined as radiation effects. Using a number of methods to assess the ability to scavenge free radicals (DPPH, ABTS, CUPRAC, and FRAP), a slight decrease in the activity of curcumin raw material was determined. The analysis of the characteristic bands in the FT-IR spectra allowed us to indicate changes in the phenolic OH groups as an effect of the presence of radicals formed.


Assuntos
Curcumina , Espectroscopia de Infravermelho com Transformada de Fourier , Diarileptanoides , Antioxidantes , Radicais Livres
11.
Antioxidants (Basel) ; 13(1)2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38247529

RESUMO

Photoaging is a process related to an increased level of reactive oxygen species (ROS). Polyphenols can scavenge free radicals in the body, which can delay skin aging. Therefore, our work aimed to prepare a biologically active extract from dry fruits of Vaccinium myrtillus or Vaccinium corymbosum and use it for the preparation of hydrogels for topical application. Therefore, eight different extracts (using V. myrtillus and V. corymbosum and different extraction mixtures: methanol, methanol-water 1:1, water, acetone-water 1:1) were prepared and their phytochemical (total polyphenolic content, total flavonoid content, total anthocyanin content) and biological properties (antioxidant, anti-hyaluronidase, and anti-tyrosinase activity) were assessed. Cytotoxicity towards HaCaT keratinocytes was also determined. Based on the results, the acetone-water extract from V. myrtillus was selected for further study. Using the Design of Experiments approach, chitosan-based hydrogels with bilberry fruit extract were prepared. The content of extract and chitosan were selected as independent factors. The activity of hydrogels depended on the extract content; however, the enzyme-inhibiting (anti-hyaluronidase and anti-tyrosinase) activity resulted from the presence of both the extract and chitosan. Increased concentration of chitosan in the hydrogel base led to increased viscosity of the hydrogel and, consequently, a slower release of active compounds. To get optimal hydrogel characteristics, 1% extract and 2.5% MMW chitosan were utilized. The research suggests the validity of using bilberry fruit extracts in topical preparations with anti-aging properties.

12.
Antioxidants (Basel) ; 12(9)2023 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-37760078

RESUMO

Despite the wide pharmacological action of polyphenols, their usefulness is limited due to their low oral bioavailability, which is due to their low solubility and rapid first-pass metabolism. Red vine leaf extract is an herbal medicine containing several polyphenols, with resveratrol and polydatin as the main compounds exhibiting antioxidant and anti-inflammatory properties. In the first stage of the work, using the Design of Experiment (DoE) approach, the red vine leaf extract (50% methanol, temperature 70 °C, and three cycles per 60 min) was obtained, which showed optimal antioxidant and anti-inflammatory properties. In order to circumvent the above-described limitations and use innovative technology, electrospun nanofibers containing the red vine leaf extract, polyvinylpyrrolidone (PVP), and hydroxypropyl-ß-cyclodextrin (HPßCD) were first developed. The optimization of the process involved the time of system mixing prior to electrospinning, the mixture flow rate, and the rotation speed of the collector. Dissolution studies of nanofibers showed improved resveratrol release from the nanofibers (over five-fold). Additionally, a PAMPA-GIT assay confirmed significantly better buccal penetration of resveratrol from this nanofiber combination (over ten-fold). The proposed strategy for electrospun nanofibers with the red vine leaf extract is an innovative approach to better use the synergy of the biological action of active compounds present in extracts that are beneficial for the development of nutraceuticals.

13.
Int J Mol Sci ; 24(18)2023 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-37762460

RESUMO

As secondary plant metabolites, polyphenols are abundant in fruits and vegetables. They are in high demand because of their many health benefits. However, their low bioavailability makes them complex compounds to use for therapeutic purposes. Due to the limited solubility of phytocompounds, dietary supplements made from them may only be partially effective. Such molecules include fisetin, found in strawberries, and have shown great promise in treating Alzheimer's disease and cancer. Unfortunately, because of their limited water solubility, low absorption, and poor bioavailability, the assistance of nanotechnology is required to allow them to fulfil their potential fully. Here, we provide evidence that nanodelivery methods and structure modifications can improve fisetin bioavailability, which is linked to improvements in therapeutic efficacy. An open question remains as to which nanocarrier should be chosen to meet the abovementioned requirements and be able to enhance fisetin's therapeutic potential to treat a particular disease.


Assuntos
Doença de Alzheimer , Humanos , Disponibilidade Biológica , Suplementos Nutricionais , Flavonóis
14.
Molecules ; 28(13)2023 Jun 24.
Artigo em Inglês | MEDLINE | ID: mdl-37446627

RESUMO

Plants are commonly used in folk medicine. Research indicates that the mechanisms of biological activity of plant extracts may be essential in the treatment of various diseases. In this respect, we decided to test the ethanolic extracts of Bidens tripartita herb (BTH), Galium verum herb (GVH), and Rumicis hydrolapathum root (RHR) on angiogenic, anti-inflammatory, and antioxidant properties and their total polyphenols content. In vitro studies using endothelial cells were used to see tested extracts' angiogenic/angiostatic and anti-inflammatory properties. The DPPH assay and FRAP analysis were used to detect antioxidant properties of extracts. The Folin-Ciocalteu analysis was used to determine the content of total polyphenols. The results of gas chromatography-mass spectrometry analysis was also presented. In vitro study demonstrated that BTH, GVH, and RHR ethanolic extracts significantly increased cell invasiveness, compared with the control group. Increased endothelial proangiogenic invasiveness was accompanied by reduced metalloproteinase inhibitor 1 (TIMP-1) and raised in metalloproteinase 9 (MMP-9). Only BTH and GVH significantly reduced cell proliferation, while BTH and RHR facilitated migration. Additionally, tested extracts reduced the production of proangiogenic platelet-derived growth factor (PDGF) and hepatocyte growth factor (HGF). The most potent anti-inflammatory capacity showed BTH and GVH, reducing proinflammatory interleukin 8 (CXCL8) and interleukin 6 (Il-6), compared to RHR extract that has slightly less inhibited CXCL8 production without affecting IL-6 production. Moreover, we confirmed the antioxidant properties of all examined extracts. The highest activity was characterized by RHR, which has been correlated with the high content of polyphenols. In conclusion, the modifying influence of examined extracts can be promising in disorders with pathogenesis related to angiogenesis, inflammation and free radicals formation. BTH is the best choice among the three tested extracts with its antiangiogenic and anti-inflammatory properties.


Assuntos
Galium , Rumex , Antioxidantes/farmacologia , Antioxidantes/química , Galium/química , Células Endoteliais , Interleucina-6 , Polifenóis/farmacologia , Extratos Vegetais/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Etanol
15.
Molecules ; 28(13)2023 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-37446841

RESUMO

Red clover is a raw material of interest primarily due to its isoflavone content. However, other groups of compounds may affect the pleiotropic biological effects of this raw material. It is used to alleviate menopausal symptoms, but the fact that there are many varieties of this plant that can be grown makes it necessary to compare the biological activity and phytochemical composition of this plant. Also of interest are the differences between the leaves and flowers of the plant. The aim of this study was to evaluate the properties of the leaves and flowers of six clover varieties-'Tenia', 'Atlantis', 'Milena', 'Magellan', 'Lemmon' and 'Lucrum'-with respect to their ability to inhibit α-glucosidase, lipase, collagenase and antioxidant activity. Therefore, the contents of polyphenols and the four main isoflavones-genistein, daidzein, biochanin and formononetin-were assessed. The study was complemented by testing for permeability through a model membrane system (PAMPA). Principal component analysis (PCA) identified a relationship between activity and the content of active compounds. It was concluded that antioxidant activity, inhibition of glucosidase, collagenase and lipase are not correlated with isoflavone content. A higher content of total polyphenols (TPC) was determined in the flowers of red clover while a higher content of isoflavones was determined in the leaves of almost every variety. The exception is the 'Lemmon' variety, characterized by high isoflavone content and high activity in the tests conducted.


Assuntos
Isoflavonas , Trifolium , Trifolium/química , Antioxidantes/farmacologia , Isoflavonas/farmacologia , Isoflavonas/análise , Polifenóis/farmacologia , Menopausa
16.
Molecules ; 28(13)2023 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-37446871

RESUMO

Hesperidin is a polyphenol derived from citrus fruits that has a broad potential for biological activity and the ability to positively modify the intestinal microbiome. However, its activity is limited by its low solubility and, thus, its bioavailability-this research aimed to develop a zein-based hesperidin system with increased solubility and a sustained release profile. The study used triple systems enriched with solubilizers to maximize solubility. The best system was the triple system hesperidin-zein-Hpß-CD, for which the solubility improved by more than six times. A significant improvement in the antioxidant activity and the ability to inhibit α-glucosidase was also demonstrated, due to an improved solubility. A release profile analysis was performed in the subsequent part of the experiments, confirming the sustained release profile of hesperidin, while improving the solubility. Moreover, the ability of selected probiotic bacteria to metabolize hesperidin and the effect of this flavonoid compound on their growth were investigated.


Assuntos
Citrus , Hesperidina , Zeína , Hesperidina/farmacologia , Prebióticos , Preparações de Ação Retardada , Excipientes
17.
Int J Mol Sci ; 24(9)2023 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-37175671

RESUMO

Orange peel, which is a rich source of polyphenolic compounds, including hesperidin, is produced as waste in production. Therefore, optimization of the extraction of hesperidin was performed to obtain its highest content. The influence of process parameters such as the kind of extraction mixture, its temperature and the number of repetitions of the cycles on hesperidin content, the total content of phenolic compounds and antioxidant (DPPH scavenging assay) as well as anti-inflammation activities (inhibition of hyaluronidase activity) was checked. Methanol and temperature were key parameters determining the efficiency of extraction in terms of the possibility of extracting compounds with the highest biological activity. The optimal parameters of the orange peel extraction process were 70% of methanol in the extraction mixture, a temperature of 70 °C and 4 cycles per 20 min. The second part of the work focuses on developing electrospinning technology to synthesize nanofibers of polyvinylpyrrolidone (PVP) and hydroxypropyl-ß-cyclodextrin (HPßCD) loaded with hesperidin-rich orange peel extract. This is a response to the circumvention of restrictions in the use of hesperidin due to its poor bioavailability resulting from low solubility and permeability. Dissolution studies showed improved hesperidin solubility (over eight-fold), while the PAMPA-GIT assay confirmed significantly better transmucosal penetration (over nine-fold). A DPPH scavenging assay of antioxidant activity as well as inhibition of hyaluronidase to express anti-inflammation activity was established for hesperidin in prepared electrospun nanofibers, especially those based on HPßCD and PVP. Thus, hesperidin-rich orange peel nanofibers may have potential buccal applications to induce improved systemic effects with pro-health biological activity.


Assuntos
Hesperidina , Nanofibras , Hesperidina/química , Solubilidade , Metanol/química , Nanofibras/química , 2-Hidroxipropil-beta-Ciclodextrina , Hialuronoglucosaminidase , Extratos Vegetais/farmacologia , Antioxidantes/farmacologia , Antioxidantes/química , Povidona , Permeabilidade
18.
Pharmaceutics ; 15(4)2023 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-37111543

RESUMO

In recent years, there has been a significant surge in reports on the health-promoting benefits of winter cherry (Withania somnifera), also known as Ashwagandha. Its current research covers many aspects of human health, including neuroprotective, sedative and adaptogenic effects and effects on sleep. There are also reports of anti-inflammatory, antimicrobial, cardioprotective and anti-diabetic properties. Furthermore, there are reports of reproductive outcomes and tarcicidal hormone action. This growing body of research on Ashwagandha highlights its potential as a valuable natural remedy for many health concerns. This narrative review delves into the most recent findings and provides a comprehensive overview of the current understanding of ashwagandha's potential uses and any known safety concerns and contraindications.

19.
Molecules ; 28(6)2023 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-36985686

RESUMO

The influence of ionizing radiation on the physicochemical properties of quercetin and rutin in the solid state was studied. Quercetin and rutin were irradiated with the standard recommended radiation dose (25 kGy) according to EN 522 standard. The samples were irradiated by electron beam radiation. EPR studies indicate the formation of a small number of free radicals due to irradiation. Moreover, some radicals recombined with the mean lifetime of 1200 and 93 h, and a stable radical concentration reached only 0.29 and 0.90 ppm for quercetin and rutin, respectively. The performed spectroscopic study (FT-IR) confirmed the radiostability of the flavonoids tested. Chromatographic tests (HPLC, HPLC-MS) showed that irradiation of quercetin and rutin with a 25 kGy dose did not change the physicochemical properties of the tested compounds. Degradation products were not observed. The antioxidant activities were determined by the 2,2-diphenyl-1-pycrylhydrazyl (DPPH) free radical scavenging activity assay, ABTS Radical Scavenging Assay (ABTS), Ferric Reducing Antioxidant Power Assay (FRAP), Cupric Ion Reducing Antioxidant Capacity Assay (CUPRAC). The conducted research confirmed that exposure to ionizing radiation does not change the chemical structure of tested flavonoids and their antioxidant properties.


Assuntos
Quercetina , Rutina , Antioxidantes/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Flavonoides/química
20.
Materials (Basel) ; 15(22)2022 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-36431484

RESUMO

Biochars that are the subjects of this report have been obtained from the residue of supercritical extraction of common nettle seeds with CO2. The residue was subjected to direct activation with carbon(IV) oxide as an activator. The obtained biochars were found to have a specific surface area inthe range of 888-1024 m2/g and a basic surface. They were used for the adsorption of a liquid organic pollutant (methylene blue) and a gas inorganic pollutant (NO2). As follows from the test results, the biochars were able to adsorb 150-239 mg of the dye. The Langmuir model was found to better describe the adsorption experimental data, while the kinetics of the process was better described by the pseudo-second-order model. From the thermodynamic analysis, it was inferred that the adsorption of methylene blue from a water solution was an endothermic and spontaneous reaction. It was established that elevated temperature of activation and the presence of air stream during adsorption had a positive impact on the adsorption of NO2 by the biochars studied. The greatest sorption capacity of the biochars towards NO2 was 59.1 mg/g.

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