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1.
Int J Mol Sci ; 24(24)2023 Dec 07.
Artigo em Inglês | MEDLINE | ID: mdl-38139059

RESUMO

Centella asiatica extract is a valued plant material with known anti-inflammatory and anti-microbiological properties. Using the Design of Experiment (DoE) approach, it was possible to obtain an optimized water/alcoholic extract from Centella asiatica, which allowed the preparation of the final material with biological activity in the wound healing process. Studies on the novel applications of Centella asiatica in conjunction with the multifunctional chitosan carrier have been motivated by the plant's substantial pharmacological activity and the need to develop new and effective methods for the treatment of chronic wounds. The controlled release of asiaticoside was made possible by the use of chitosan as a carrier. Based on the findings of investigations using the PAMPA skin assay, which is a model imitating the permeability of actives through skin, this compound, characterized by sustained release from the chitosan delivery system, was identified as being well able to permeate biological membranes such as skin. Chitosan and the lyophilized extract of Centella asiatica worked synergistically to block hyaluronidase, exert efficient microbiological activity and take part in the wound healing process, as proven in an in vitro model. A formulation containing 3% extract with 3% medium-molecular-weight chitosan was indicated as a potentially new treatment with high compliance and effectiveness for patients. Optimization of the chitosan-based hydrogel preparation ensured the required rheological properties necessary for the release of the bioactive from the chitosan delivery system and demonstrated a satisfactory antimicrobial activity.


Assuntos
Centella , Quitosana , Triterpenos , Humanos , Quitosana/farmacologia , Hidrogéis/farmacologia , Triterpenos/farmacologia , Triterpenos/uso terapêutico , Extratos Vegetais/farmacologia , Cicatrização
2.
Pharmaceuticals (Basel) ; 16(4)2023 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-37111336

RESUMO

This study investigated the ability of PVP/HPßCD-based electrospun nanofibers to enhance the dissolution rate of poorly soluble polydatin and resveratrol, the main active components of Polygoni cuspidati extract. To make a solid unit dosage form that would be easier to administer, extract-loaded nanofibers were ground. SEM examination was used to analyze the nanostructure of the fibers, and the results of the cross-section of the tablets showed that they had maintained their fibrous structure. The release of the active compounds (polydatin and resveratrol) in the mucoadhesive tablets was complete and prolonged in time. Additionally, the possibility of staying on the mucosa for a prolonged time has also been proven for both tablets from PVP/HPßCD-based nanofibers and powder. The appropriate physicochemical properties of the tablets, along with the proven antioxidant, anti-inflammatory, and antibacterial properties of P. cuspidati extract, highlight the particular benefits of the mucoadhesive formulation for use as a drug delivery system for periodontal diseases.

3.
Int J Mol Sci ; 24(6)2023 Mar 19.
Artigo em Inglês | MEDLINE | ID: mdl-36982908

RESUMO

Hot Melt Extrusion (HME) technology was developed to obtain blends containing lyophilized Scutellariae baicalensis root extract and chitosan in order to improve the rheological properties of the obtained blends, including tableting and compressibility properties. (Hydroxypropyl)methyl cellulose (HPMC) in 3 different ratios was used as amorphous matrix formers. The systems were characterized using X-ray powder diffraction (PXRD), Fourier Transform Infrared Spectroscopy with Attenuated Total Reflectance (FTIR-ATR), and in vitro release, permeability, and microbiological activity studies. Then, the extrudates were used to prepare tablets in order to give them the appropriate pharmaceutical form. HPMC-based systems released baicalin more slowly, resulting in delayed peaks in the acceptor fluid. This behavior can be explained by the fact that HPMC swells significantly, and the dissolved substance must have diffused through the polymer network before being released. The best tabletability properties are provided by the formulation containing the extrudate with lyophilized extract HPMC 50:50 w/w. These tablets offer a valuable baicalin release profile while maintaining good mucoadhesive properties that condition the tablet's retention in the application site and the effectiveness of therapy.


Assuntos
Química Farmacêutica , Quitosana , Química Farmacêutica/métodos , Tecnologia de Extrusão por Fusão a Quente , Solubilidade , Comprimidos , Composição de Medicamentos/métodos , Temperatura Alta
4.
Pharmaceutics ; 14(4)2022 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-35456574

RESUMO

Scutellarie baicalensis radix, as a flavone-rich source, exhibits antibacterial, antifungal, antioxidant, and anti-inflammatory activity. It may be used as a therapeutic agent to treat various diseases, including vaginal infections. In this study, six binary mixtures of chitosan with stable S. baicalensis radix lyophilized extract were obtained and identified by spectral (ATR-FTIR, XRPD) and thermal (TG and DSC) methods. The changes in dissolution rates of active compounds and the significant increase in the biological properties towards metal chelating activity were observed, as well as the inhibition of hyaluronic acid degradation after mixing plant extract with chitosan. Moreover, the combination of S. baicalensis radix lyophilized extract with a carrier allowed us to obtain the binary systems with a higher antifungal activity than the pure extract, which may be effective in developing new strategies in the vaginal infections treatment, particularly vulvovaginal candidiasis.

5.
Antioxidants (Basel) ; 11(2)2022 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-35204262

RESUMO

As a systemic disease, diabetes mellitus (DM) is characterized by the disruption of many glucose metabolic pathways. Therefore, it seems critical to study new therapies to support treatment to develop therapeutic systems that can operate across a broad metabolic spectrum. The current state of knowledge indicates an essential role of the gut microbiota in the development and course of the disease. Cornus mas fruits have demonstrated a rich biological activity profile and potential for application in the treatment of DM. As part of a preliminary analysis, the activity of four cultivars of Cornus mas fruits was analyzed. The cultivar Wydubieckij was selected as having the highest activity in in vitro conditions for further prebiotic system preparation. The study aimed to develop a unique therapeutic system based, first of all, on the mechanism of α-glucosidase inhibition and the antioxidant effect resulting from the activity of the plant extract used, combined with the prebiotic effect of inulin. The obtained system was characterized in vitro in terms of antioxidant activity and enzyme inhibition capacity, and was then tested on diabetic rats. The study was coupled with an analysis of changes in the intestinal microflora. The system of prebiotic stabilized Cornus mas L. lyophilized extract with inulin offers valuable support for the prophylaxis and treatment of DM.

6.
Antioxidants (Basel) ; 10(12)2021 Dec 04.
Artigo em Inglês | MEDLINE | ID: mdl-34943048

RESUMO

Blackberry fruits are recognized as functional foods while blackberry leaves are outside this classification and they also contain active compounds with health-promoting potential. Therefore, the aim of this study was the phytochemical analysis of blackberry leaves of varieties (Chester, Loch Ness, Loch Tay and Ruczaj) and screening of their biological activity (antioxidant potential, possibility of inhibition of enzymes, anti-inflammatory and microbial activity). The following compounds from selected groups: phenolic acids (caffeic acid, ellagic acid, gallic acid, syringic acid), flavonols (quercetin, kaempferol) and their glycosides (rutin, isoquercetin, hyperoside) and flavon-3-ols (catechin, epicatechin) were chromatographically determined in the aqueous and hydroalcoholic leaves extracts. All tested blackberry leaves extracts showed antioxidant effects, but the highest compounds content (TPC = 101.31 mg GAE/g) and antioxidant activity (e.g., DPPH IC50 = 57.37 µg/mL; ABTS IC50 = 24.83 µg/mL; CUPRAC IC50 = 62.73 µg/mL; FRAP IC50 = 39.99 µg/mL for hydroalcoholic extracts) was indicated for the Loch Tay variety. Blackberry leaf extracts' anti-inflammatory effect was also exceptionally high for the Loch Tay variety (IC50 = 129.30 µg/mL), while leaves extracts of the Loch Ness variety showed a significant potential for microbial activity against Lactobacillus spp. and Candida spp. Summarizing, the best multidirectional pro-health effect was noted for leaves extracts of Loch Tay variety.

7.
PLoS One ; 16(2): e0243871, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33556063

RESUMO

Cornelian cherry (Cornus mas L.) fruits are a valuable source of bioactive compounds that are responsible for the perception of bitter taste of chocolate products. The aim of the study was to validate the inhibitory effect of Cornus mas on the TAS2R3 and TAS2R13 bitter taste receptors and to assess the effect of masking the bitter taste of dark chocolate with the help of the sensory panel. Dark chocolate was prepared with an addition of 5% of freeze-dried cornelian cherry fruits and 108 CFU/g of Bacillus coagulans probiotic strains. Effect on the TAS2R receptors was evaluated in specially transfected HEK293T cells, and the inhibition ratio was measured using the calcium release test. Moreover, the total polyphenol content, antioxidant activity and simulated intestinal in vitro digestion were determined for the samples. The tested chocolate products were rich in chlorogenic, caffeic and sinapic acids. The addition of cornelian cherry positively affected the antioxidant activity. The phytochemicals of Cornus mas decreased the TAS2R13 activity by 132% after a 2-minute interaction and, % at the same time, inhibited the TAS2R3 activity by 11.5. Meanwhile, chocolate with the addition of fruit was less bitter according to the sensory panel.


Assuntos
Chocolate , Cornus/metabolismo , Aromatizantes/metabolismo , Probióticos , Receptores Acoplados a Proteínas G/metabolismo , Bacillus coagulans/citologia , Chocolate/análise , Cornus/química , Suplementos Nutricionais/análise , Aromatizantes/química , Liofilização , Frutas/química , Frutas/metabolismo , Células HEK293 , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/metabolismo , Probióticos/análise , Paladar , Percepção Gustatória
8.
Talanta ; 223(Pt 2): 121749, 2021 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-33298273

RESUMO

A new way of electrochemical DNA sensor using as a screening tool for the determination of phytochemicals with high genoprotective functionality is proposed. The biosensor's detection layer was prepared with double stranded deoxyribonucleic acid (ds DNA) that were subjected to oxidative stress induced by •OH radicals generated by Fenton reaction. The oxidized guanine derivative, 8-oxo-7,8-dihydro-2'-deoxyguanosine, was treated as an indicator of DNA oxidative damage. This derivative may cause mutation through its ability to pair with adenine. The abnormalities of DNA structure and DNA repair system are known to be directly related to progressive neurodegeneration. The present study showed that during oxidative stress, the 2.5% oregano extract protected guanine from undergoing oxidation to 8-oxoguanine. The results revealed that this genoprotective effectiveness can make oregano a very efficient protective barrier against oxidative stress. Due to these unique properties of oregano we propose the recipe of a functional bread with its addition. It was found that the functionality of the prepared bread was not limited to antioxidative activity but also is expressed in the inhibition of cholinesterases. These findings indicate that oregano can act as an important component in the therapeutic diet recommended in neurodegenerative disorders.


Assuntos
Doenças Neurodegenerativas , Origanum , Antioxidantes/farmacologia , Doenças Neurodegenerativas/prevenção & controle , Compostos Fitoquímicos , Extratos Vegetais/farmacologia
9.
Int J Mol Sci ; 22(1)2020 Dec 24.
Artigo em Inglês | MEDLINE | ID: mdl-33374358

RESUMO

Progressive increase in bacterial resistance has caused an urgent need to introduce new antibiotics, one of them being oxazolidinones with their representative tedizolid. Despite the broad spectrum of activity of the parent tedizolid, it is characterized by low water solubility, which limits its use. The combination of the active molecule with a multifunctional excipient, which is cyclodextrins, allows preservation of its pharmacological activity and modification of its physicochemical properties. Therefore, the aim of the study was to change the dissolution rate and permeability through the model membrane of tedizolid by formation of solid dispersions with a cyclodextrin. The research included identification of tedizolid-hydroxypropyl-ß-cyclodextrin (tedizolid/HP-ß-CD) inclusion complex by thermal method (Differential Scanning Colorimetry), spectroscopic methods (powder X-ray diffraction, Fourier-Transform Infrared spectroscopy), and molecular docking. The second part of the research concerned the physicochemical properties (dissolution and permeability) and the biological properties of the system in terms of its microbiological activity. An increase in the dissolution rate was observed in the presence of cyclodextrin, while maintaining a high permeation coefficient and high microbiological activity. The proposed approach is an opportunity to develop drug delivery systems used in the treatment of resistant bacterial infections, in which, in addition to modifying the physicochemical properties caused by cyclodextrin, we observe a favorable change in the pharmacological potential of the bioactives.


Assuntos
Antibacterianos/farmacologia , Ciclodextrinas/administração & dosagem , Sistemas de Liberação de Medicamentos , Oxazolidinonas/administração & dosagem , Tetrazóis/administração & dosagem , 2-Hidroxipropil-beta-Ciclodextrina , Varredura Diferencial de Calorimetria , Preparações de Ação Retardada , Liberação Controlada de Fármacos , Farmacorresistência Bacteriana , Concentração de Íons de Hidrogênio , Simulação de Acoplamento Molecular , Estresse Oxidativo , Permeabilidade , Pós , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X , beta-Ciclodextrinas/química
10.
Electron. j. biotechnol ; 48: 62-71, nov. 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1254807

RESUMO

BACKGROUND: A key challenge for manufacturers of pro-health food containing active probiotic microorganisms is to develop a product with attractive sensory features along with maintenance of declared number of microorganisms during storage and transfer by alimentary tract. RESULTS: The highest concentration of polyphenols was observed in snacks without an additive of probiotics as well as those with an additive of L. rhamnosus and B. animalis bacteria and concentration of these compounds increased by 9.5% during six months of storage. None of the products distinguished itself in the sensorial assessment although each was assessed positively. The number of microorganisms was stable and comparatively high during six months of storage at a room temperature and in cooling conditions (108 cfu/g). In the digestion model, an influence of aggressive digestion conditions was examined in the alimentary tract on the number of microorganisms, which allowed to arrange strains from the most resistant (S. boulardii) to the most sensitive (B. breve). It must be noted that currently on the market there is no available snack containing probiotic yeast as well as there is no literature data on works on such formulation of food. CONCLUSIONS: In the newly developed snack made of chocolate, in which sugar has been replaced with maltitol, a raw material was added in the form of raspberry, prebiotic in the form of inulin and a strain of probiotic bacteria, including the unprecedented so far S. boulardii, which stands a high chance to occupy a good place on the market of functional food.


Assuntos
Probióticos , Alimento Funcional , Chocolate/microbiologia , Álcoois Açúcares , Temperatura , Alimentos Integrais , Digestão , Armazenamento de Alimentos , Prebióticos , Simbióticos , Polifenóis , Lanches , Rubus , Maltose/análogos & derivados
11.
Molecules ; 25(19)2020 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-33003643

RESUMO

Honeys have a pleasant taste and a wide range of use. They are characterized by a relatively high consumption compared to bee pollen or beebread. Honeys are the most popular bee products. Considering health reasons, beebread exhibits the strongest properties as it has the highest nutritional value as well as strong detoxifying, antioxidant, and antiradical properties. Despite having such valuable properties, consumption of beebread is negligible; sometimes, it is limited only to supplementation in case of diseases. This paper proposes a new food product, that is, beebread caviar made from buckwheat honey. The expiry date and sensory and physicochemical quality of beebread caviar have been determined in this study. Beebread caviar, obtained by immobilization on alginate carrier, contained 0.34 mg GAE/mL extract. It remained stable until five days after preparation. Its total acidity was 33.7 mval/kg. Its extract content was 22.53%. Caviar had a high overall sensory score of 4.8 points on a 5-point scale. Beebread caviar can be successfully classified as probiotic food because beebread contains a large amount of lactic acid. In the form of caviar, a new, attractive, and convenient form of beebread consumption could become one of the products of comfortable and functional food.


Assuntos
Alginatos/química , Fagopyrum/química , Mel/análise , Própole/química , Concentração de Íons de Hidrogênio
12.
J Food Sci ; 85(10): 3003-3011, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32935860

RESUMO

Food can be a source of valuable peptides with high bioactivity, which regulate the functioning of cardiovascular and nervous systems. The aim of the study was to evaluate the possibility of usage ricotta after hydrolysis to obtain innovative chocolate desserts. It was shown that the hydrolysis of whey proteins in ricotta had insignificant effect on the texture indices of the products, except gumminess, as it declined to 16% in ricotta samples and to 7% in case of chocolate dessert samples. Confirmed was that the hydrolysis of the ricotta affected the activity of prepared desserts with respect to cholinesterases and angiotensin-converting enzyme. Enzymatic hydrolysate of ricotta may be consider as a semifinished product of high functional activity, and its further application in dessert production allows to provide novel prohealth new products. PRACTICAL APPLICATION: Study results indicate new feasibilities of ricotta application as functional ingredient of new products--chocolate desserts. The results show that ricotta after the stage of enzyme hydrolysis of proteins might have noticeable effect on product functionality. A measurable benefit for the consumer is the receipt of a new product with favorable health-promoting properties, and for the entrepreneur new possibilities to expand the range of functional products. Moreover, described technology allows to use dairy byproducts for new products developments, such as chocolate desserts, due to sustainability development strategy.


Assuntos
Inibidores da Enzima Conversora de Angiotensina/química , Queijo/análise , Chocolate , Inibidores da Colinesterase/química , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Inibidores da Colinesterase/farmacologia , Colinesterases , Hidrólise
13.
J Enzyme Inhib Med Chem ; 35(1): 1811-1821, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32967477

RESUMO

The nutraceutical system of curcumin-piperine in 2-hydroxypropyl-ß-cyclodextrin was prepared by using the kneading technique. Interactions between the components of the system were defined by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR). Application of hydroxypropyl-ß-cyclodextrin as a carrier-solubiliser improved solubility of the curcumin-piperine system, its permeability through biological membranes (gastrointestinal tract, blood-brain barrier) as well as the antioxidant, antimicrobial and enzyme inhibitory activities against acetylcholinesterase and butyrylcholinesterase.


Assuntos
2-Hidroxipropil-beta-Ciclodextrina/química , Acetilcolinesterase/metabolismo , Alcaloides/química , Benzodioxóis/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/química , Curcumina/química , Portadores de Fármacos/química , Piperidinas/química , Alcamidas Poli-Insaturadas/química , Alcaloides/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Benzodioxóis/farmacologia , Transporte Biológico , Barreira Hematoencefálica/metabolismo , Inibidores da Colinesterase/farmacologia , Curcumina/farmacologia , Suplementos Nutricionais , Composição de Medicamentos , Trato Gastrointestinal/metabolismo , Humanos , Piperidinas/farmacologia , Alcamidas Poli-Insaturadas/farmacologia , Solubilidade
14.
Molecules ; 25(15)2020 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-32752298

RESUMO

Currently, coniferous shoots are almost absent as a food ingredient despite their wide availability in many parts of the world. The aim of the study was to assess and compare the composition of selected plant metabolites, evaluate the antioxidant and antimicrobial properties of selected shoots collected in 2019 from the arboretum in Zielonka (Poland), including individual samples from Picea abies L. (PA), Larix decidua Mill (LD), Pinus sylvestris L. (PS), Pseudotsuga menziesii (PM) and Juniperus communis L. (JC). The present work has shown that aqueous extracts obtained from tested shoots are a rich source of phenols such as caffeic acid, ferulic acid, chlorogenic acid, 4-hydroxybenzoic acid and many others. Obtained extracts exhibit antioxidant and antimicrobial properties in vitro. The highest sum of the studied phenolic compounds was found in the PA sample (13,947.80 µg/g dw), while the lowest in PS (6123.57 µg/g dw). The samples were particularly rich in ferulic acid, chlorogenic acid and 4-hydroxybenzoic acid. The highest values regarding the Folin-Ciocâlteu reagent (FCR) and ferric reducing ability of plasma (FRAP) reducing ability tests, as well as the total flavonoid content assay, were obtained for the LD sample, although the LD (14.83 mg GAE/g dw) and PM (14.53 mg GAE/g dw) samples did not differ statistically in the FCR assay. With respect to free radical quenching measurements (DPPH), the PA (404.18-µM Trolox/g dw) and JC (384.30-µM Trolox/g dw) samples had the highest radical quenching ability and did not differ statistically. Generally, extracts obtained from PA and PS showed the highest antimicrobial activity against tested Gram-negative bacteria, Gram-positive bacteria and fungi.


Assuntos
Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Traqueófitas/química , Cromatografia Líquida de Alta Pressão , Alimento Funcional , Humanos , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Brotos de Planta/química , Polônia
15.
Pharmaceutics ; 12(7)2020 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-32645859

RESUMO

Calendulae flos is a valued plant material with known anti-inflammatory and antimicrobiological properties. The limitation for its use in the treatment of chronic wounds is the lack of adhesion to the required site of action. Obtaining the Calendulae flos lyophilized extract from water-ethanolic extract allowed to prepare valuable material whose biological activity in the wound healing process was confirmed by a positive result of the scratch test. The Calendulae flos lyophilized extract was standardized for the contents of the chlorogenic acid and the narcissin. The significant potency of the Calendulae flos pharmacological activity has become the reason for studies on its novel applications in combination with the multifunctional chitosan carrier, to create a new, valuable solution in the treatment of chronic wounds. The use of chitosan as a carrier allowed for the controlled release of the chlorogenic acid and the narcissin. These substances, characterized by prolonged release from the chitosan delivery system, were identified as well permeable, based on the results of the studies of the parallel artificial membrane permeability assay (PAMPA Skin) a model simulating permeability through membrane skin. The combination of the Calendulae flos lyophilized extract and the chitosan allowed for synergy of action towards hyaluronidase inhibition and effective microbiological activity. Optimization of the hypromellose hydrogel preparation ensuring the required rheological properties necessary for the release of the chlorogenic acid and the narcissin from the chitosan delivery system, as well as demonstrated antimicrobial activity allows indicating formulations of 3% Calendulae flos lyophilized extract with chitosan 80/500 in weight ratio 1:1 and 2% or 3% hypromellose as an important support with high compliance of response and effectiveness for patients suffering from chronic wounds.

16.
J Clin Med ; 9(4)2020 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-32331437

RESUMO

Chelidonium majus (also known as celandine) contains pharmacologically active compounds such as isoquinoline alkaloids (e.g., chelidonine, sanguinarine), flavonoids, saponins, carotenoids, and organic acids. Due to the presence of isoquinoline alkaloids, Chelidonii herba extracts are widely used as an antibacterial, antifungal, antiviral (including HSV-1 and HIV-1), and anti-inflammatory agent in the treatment of various diseases, while chitosan is a biocompatible and biodegradable carrier with valuable properties for mucoadhesive formulations preparation. Our work aimed to prepare mucoadhesive vaginal drug delivery systems composed of Chelidonii herba lyophilized extract and chitosan as an effective way to treat vaginitis. The pharmacological safety of usage of isoquinoline alkaloids, based on MTT test, were evaluated for the maximum doses 36.34 ± 0.29 µg/mL and 0.89 ± 1.16 µg/mL for chelidonine and sanguinarine, respectively. Dissolution rate profiles and permeability through artificial membranes for chelidonine and sanguinarine after their introduction into the chitosan system were studied. The low permeability for used save doses of isoquinoline alkaloids and results of microbiological studies allow confirmation that system Chelidonii herba lyophilized extract chitosan 80/500 1:1 (w/w) is a promising strategy for vaginal use. Ex vivo studies of mucoadhesive properties and evaluation of tableting features demonstrated that the formulation containing Chelidonii herba lyophilized extract (120.0 mg) with chitosan (80/500-100.0 mg) and polymer content (HPMC-100.0 mg, microcrystalline cellulose-50.0 mg, lactose monohydrate-30.0 mg and magnesium stearate-4.0 mg) is a vaginal dosage form with prolonging dissolution profile and high mucoadhesion properties (up to 4 h).

17.
Electron. j. biotechnol ; 37: 25-33, Jan. 2019. tab, graf, ilus
Artigo em Inglês | LILACS | ID: biblio-1051225

RESUMO

Background: Ammonium stress is a prime limiting phenomenon that occurs during methane formation from poultry manure. It is caused by elevated ammonium nitrogen concentrations that result from substrate decomposition. The amounts of methane formed depend on the activity of methanogenic microbes. Results: During the research reported in this paper, the response of a mesophilic consortium inhabiting a biogas reactor to rising load of poultry manure was investigated. The taxonomic composition of bacterial population was mostly typical, however syntrophic bacteria were not detected. This absence resulted in limitation of succession of some methanogenic microorganisms, especially obligate hydrogenotrophs. The methanogenic activity of the consortium was totally dependent on the activity of Methanosaeta. Inhibition of methanoganesis was noticed at ammonium nitrogen concentration of 3.68 g/L, total cessation occurred at 5.45 g/L. Significant amounts of acetic acid in the fermentation pulp accompanied the inhibition. Conclusions: The effectiveness of the consortium was totally dependent on the metabolic activity of the acetoclastic Methanoseata genus and lack of SAOB did not allow hydrogenotrophic methanogens to propagate and lead to cessation of biogas production at an elevated ammonium concentration at which acetoclastic methanogens were inhibited.


Assuntos
Methanosarcinaceae/metabolismo , Biocombustíveis , Microbiota , Anaerobiose , Aves Domésticas , Estresse Fisiológico , Reação em Cadeia da Polimerase , Impressões Digitais de DNA , Cromatografia Líquida de Alta Pressão , Archaea/metabolismo , Biodiversidade , Fermentação , Consórcios Microbianos , Compostos de Amônio , Esterco , Metano , Nitrogênio
18.
Electron. j. biotechnol ; 37: 1-10, Jan. 2019. tab, graf, ilus
Artigo em Inglês | LILACS | ID: biblio-1048922

RESUMO

BACKGROUND: Chia seeds are gaining increasing interest among food producers and consumers because of their prohealth properties. RESULTS: The aim of this work was to evaluate the potential of chia seeds to act as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors. The highest inhibitory activity against AChE and BChE was observed for colored seed ethanol extracts. A positive correlation was found between the presence of quercetin and isoquercetin as well as protocatechuic, hydroxybenzoic, and coumaric acids and the activity of extracts as AChE and BChE inhibitors. It has also been shown that grain fragmentation affects the increase in the activity of seeds against cholinesterases (ChE). Furthermore, seeds have been shown to be a source of substances that inhibit microbial growth. CONCLUSIONS: It was found that the chia seed extracts are rich in polyphenols and inhibit the activity of ChEs; therefore, their use can be considered in further research in the field of treatment and prevention of neurodegenerative diseases.


Assuntos
Sementes/química , Butirilcolinesterase , Inibidores da Colinesterase , Salvia/química , Anti-Infecciosos/metabolismo , Técnicas In Vitro , Flavonóis/análise , Compostos Fenólicos/análise , Polifenóis/análise , Aditivos Alimentares
19.
Biomolecules ; 10(1)2019 12 23.
Artigo em Inglês | MEDLINE | ID: mdl-31878057

RESUMO

This study aimed to investigate changes in the solubility and antimicrobial efficacy of cefuroxime axetil (CA) when incorporated into cyclodextrin (CD). While choosing the CD, the validated in silico model was used. A theoretical model based on docking and molecular mechanics/generalized born surface area was validated using a curated dataset of API (active pharmaceutical ingredient)-CD stability constants. The library of commonly used cyclodextrins was virtually screened, indicating CA -hydroxypropyl-ßCD (HPßCD) as the most thermodynamically favored system. Solid-state CA-HPßCD system was prepared and characterized by differential scanning calorimetry (DSC), Fourier-transform infrared (FT-IR), and X-ray diffraction (XRPD) methods. The dissolution profiles of the CA and its cyclodextrin system were evaluated. Microbiological activity of the CA-HPßCD inclusion system was studied based on changes in minimal inhibitory concentration (MIC) values and related to ones of the pure CA. The theoretical model was successfully validated, obtaining an average correlation with experimental data R = 0.7. The dissolution study showed significantly improved dissolution profiles of CA-HPßCD compared to CA. HPßCD increases the antimicrobial efficacy of CA up to 4-fold compared to pure CA.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Cefuroxima/análogos & derivados , Desenho Assistido por Computador , Ciclodextrinas/química , Cefuroxima/química , Cefuroxima/farmacologia , Simulação por Computador , Klebsiella pneumoniae/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Solubilidade , Relação Estrutura-Atividade
20.
Molecules ; 24(16)2019 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-31416182

RESUMO

For the first time, the influence of ionising radiation on the physicochemical properties of ertapenem in solid state was studied. During our studies, we evaluated the possibility of applying radiosterilization to obtain sterile ertapenem. Spectroscopic (Fourier Transform Infrared (FT-IR)), thermal (differential scanning calorimetry (DSC), chromatography (High-Performance Liquid Chromatography (HPLC) and HPLC-MS), and X-ray powder diffraction (XRPD) studies shown that irradiation of ertapenem with the 25 kGy, the dose required to achieve sterility, does not change the physicochemical properties of the studied compound. The antimicrobial activity of ertapenem irradiated with the dose of 25 kGy was only reduced for one species. Based on the received results, we can conclude that radiostelization is a promising alternative method of obtaining sterile ertapenem. In our studies, ertapenem was also exposed to e-beam radiation with a dose of 400 kGy. It was determined that two novel degradation products that are structurally differently to degradants formed during hydrolysis and thermolysis.


Assuntos
Antibacterianos/química , Ertapenem/química , Radiação Ionizante , Esterilização , Antibacterianos/farmacologia , Varredura Diferencial de Calorimetria , Ertapenem/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Análise Espectral , Esterilização/métodos
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