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1.
Sci Rep ; 14(1): 2288, 2024 01 27.
Artigo em Inglês | MEDLINE | ID: mdl-38280925

RESUMO

Bacterial cells can form biofilm on food contact surfaces, becoming a source of food contamination with profound health implications. The current study aimed to determine some Egyptian medicinal plants antibacterial and antibiofilm effects against foodborne bacterial strains in milk plants. Results indicated that four ethanolic plant extracts, Cinnamon (Cinnamomum verum), Chamomile (Matricaria chamomilla), Marigold (Calendula officinalis), and Sage (Salvia officinalis), had antibacterial (12.0-26.5 mm of inhibition zone diameter) and antibiofilm (10-99%) activities against Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes and Salmonella Typhimurium. The tested extracts had minimum inhibitory concentration values between 0.14 and 2.50 mg/ml and minimum bactericidal concentration values between 0.14 and 12.50 mg/ml. L. monocytogenes was more sensitive for all tested ethanolic extracts; Sage and Cinnamon showed a bacteriocidal effect, while Chamomile and Marigold were bacteriostatic. The ethanolic extracts mixture from Chamomile, Sage, and Cinnamon was chosen for its antibiofilm activity against L. monocytogenes using L-optimal mixture design. Gas chromatography and mass spectrometry analysis showed that this mixture contained 12 chemical compounds, where 2-Propenal,3-phenyl- had the maximum area % (34.82%). At concentrations up to 500 µg/ml, it had no cytotoxicity in the normal Vero cell line, and the IC50 value was 671.76 ± 9.03 µg/ml. Also, this mixture showed the most significant antibacterial effect against detached L. monocytogenes cells from formed biofilm in stainless steel milk tanks. At the same time, white soft cheese fortified with this mixture was significantly accepted overall for the panelist (92.2 ± 2.7) than other cheese samples, including the control group.


Assuntos
Queijo , Listeria monocytogenes , Animais , Aço Inoxidável/farmacologia , Queijo/microbiologia , Leite , Cromatografia Gasosa-Espectrometria de Massas , Biofilmes , Extratos Vegetais/farmacologia , Antibacterianos/farmacologia , Cinnamomum zeylanicum/química , Microbiologia de Alimentos
2.
J Adv Vet Anim Res ; 10(3): 469-483, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37969796

RESUMO

Objective: This study was designed to show the effect of adding different levels of microbial (lab-produced) and commercial xanthan (CX) for 30 days on the sensory, chemical, and microbiological parameters of mozzarella cheese (MC). Materials and Methods: The production of xanthan was done in Garcia-Ochoa's medium. The sensory evaluation of the examined MC was achieved through a tabulated scorecard. The Gerber method was used for the determination of MC fat%. The mean counts of staphylococci [colony forming unit (CFU)/gm], coliforms (most probable number/gm), fungi (CFU/gm), and mesophilic bacteria (CFU/gm) were estimated in different fortified cheeses. Also, mean counts of Escherichia coli O157 and Staphylococcus aureus in artificially contaminated MC were determined. Results: The microbial xanthan (MX) had a significant (p < 0.05) effect on the sensory parameters of the examined samples with its concentration (0.0007%) after 20 days of storage. The MX (0.0005%) and CX (0.0002%) had a significant effect on moisture, fat in dry matter, and protein percentage of MC throughout the storage period. The high meltability degree of MC was observed in samples with both types of xanthan (0.0002%) at the end of storage. Conclusion: Both types of xanthan at all concentrations had a significant reducing effect on E. coli O157 and S. aureus in all samples from 10 to 30 days of storage. Xanthan has accepted attentiveness and offers beneficial and safe characteristics that improve its adaptability in MC. In the Middle East, this survival trial of E. coli O157 and S. aureus in the MC supplemented by xanthan is considered a scarce exploratory investigation.

3.
BMC Microbiol ; 23(1): 110, 2023 04 20.
Artigo em Inglês | MEDLINE | ID: mdl-37081407

RESUMO

BACKGROUND: The production of biopolymers from waste resources is a growing trend, especially in high-population countries like Egypt. Beta-glucan (ß-glucan) belongs to natural polysaccharides that are derived from plant and microbial origins. In this study, following increasing demands for ß-glucan owing to its bioactive properties, a statistical model to enhance microbial ß-glucan production was evaluated for its usefulness to the food and pharmaceutical industries. In addition, a trial to convert ß-glucan polymer to nanostructure form was done to increase its bioactivity. RESULTS: Ingredients of low-cost media based on agro-industrial wastes were described using Plackett-Burman and central composite design of response surface methodology for optimizing yeast ß-glucan. Minerals and vitamin concentrations significantly influenced ß-glucan yield for Kluyveromyces lactis and nitrogen and phosphate sources for Meyerozyma guilliermondii. The maximum predicted yields of ß-glucan recovered from K. lactis and M. guilliermondii after optimizing the medium ingredients were 407 and 1188 mg/100 ml; respectively. For the first time, yeast ß-glucan nanoparticles (ßGN) were synthesized from the ß-glucan polymer using N-dimethylformamide as a stabilizer and characterized using UV-vis spectroscopy, transmission electron microscope (TEM), dynamic light scattering (DLS) and Fourier transform infrared spectroscopy (FT-IR). The average size of ßGN was about 300 nm as determined by DLS. The quantitative variation of functional groups between ß-glucan polymer and ßGN was evaluated by FT-IR for explaining the difference in their biological activity against Normal Homo sapiens-Hela contaminant and Hepatic cancer cell lines. CONCLUSIONS: Enriching the low-cost media based on agro-industrial wastes with nutritional ingredients improves the yield of yeast ß-glucan. The present study succeeds to form ß-glucan nanoparticles by a simple method.


Assuntos
Nanopartículas , beta-Glucanas , Humanos , beta-Glucanas/química , beta-Glucanas/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Resíduos Industriais , Nanopartículas/química , Nanotecnologia
4.
Metab Brain Dis ; 38(4): 1365-1377, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-36696035

RESUMO

Malnutrition and low dietary protein intake could be risk factors for developing peripheral and central hyperammonemia, especially in pediatrics. Both curcumin and resveratrol proved to be effective against several hepatic and cerebral injuries. They were reported to be beneficial in lowering circulating ammonia levels, yet both are known for their low bioavailability. The use of pharmaceutical nano-formulations as delivery systems for these two nutraceuticals could solve the aforementioned problem. Hence, the present study aimed to investigate the valuable outcome of using a combination of curcumin and resveratrol in a nanoemulsion formulation, to counteract protein-deficient diet (PDD)-induced hyperammonemia and the consequent complications in male albino rats. Results revealed that using a nanoemulsion containing both curcumin and resveratrol at a dose of (5 + 5 mg/kg) effectively reduced hepatic and brain ammonia levels, serum ALT and AST levels, hepatic and brain nitric oxide levels, oxidative DNA damage as well as disrupted cellular energy performance. In addition, there was a substantial increase in brain levels of monoamines, and a decrease in glutamate content. Therefore, it can be concluded that the use of combined curcumin and resveratrol nanoemulsion is an effective means of ameliorating the hepatic and cerebral adverse effects resulting from PDD-induced hyperammonemia in rats.


Assuntos
Curcumina , Hiperamonemia , Criança , Humanos , Masculino , Amônia , Curcumina/farmacologia , Curcumina/uso terapêutico , Proteínas Alimentares , Hiperamonemia/tratamento farmacológico , Resveratrol/farmacologia , Resveratrol/uso terapêutico , Animais , Ratos
5.
Pharmacol Rep ; 75(1): 199-210, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36517694

RESUMO

BACKGROUND: Cisplatin is considered one of the most effective and commonly used chemotherapeutic drugs, but despite its high therapeutic effectiveness, most patients treated with cisplatin suffer from nausea and vomiting, neurotoxic side effects, and cerebral psychiatric disorders such as depression. Therefore, the aim of the current work was to explore whether a selective 5-HT3 receptor antagonist (Ondansetron) administered via the oral route or intranasally in microemulsion form would alleviate cisplatin's adverse effects. METHODS: The selected ondansetron microemulsion was characterized in vitro for particle size, polydispersity, zeta potential, morphology, and nasal permeation, and in vivo in terms of anti-emetic and antidepressant activity, with the assessment of biochemical markers in brain homogenates. RESULTS: Results revealed that both orally administered ondansetron and intranasally administered microemulsion were able to counteract the pica effect by increasing food consumption, water intake, and decreasing kaolin intake. They were also able to increase BDNF, normalize IL-6, increase serotonin, and normalize NOx, MDA, GSSH/GSH as well as 8OHdG levels in rats' brain homogenates. The intranasal ondansetron microemulsion displayed superiority compared to oral conventional ondansetron in terms of increasing food intake, reduction of stomach content, and normalization of serotonin turnover. CONCLUSION: Ondansetron microemulsion can be administered by an alternative route of administration (intranasal) rather than oral, for patients on cisplatin chemotherapy.


Assuntos
Antieméticos , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Ratos , Animais , Ondansetron/farmacologia , Ondansetron/uso terapêutico , Cisplatino/toxicidade , Serotonina , Antieméticos/farmacologia , Antieméticos/uso terapêutico , Vômito/induzido quimicamente , Vômito/tratamento farmacológico
6.
Pharm Dev Technol ; 27(9): 925-941, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36168910

RESUMO

The effectiveness of cisplatin in cancer treatment renders its use vital to clinicians. However, the accompanying side effects as cachexia, emesis and liver damage necessitate the use of a dietary supplement which is capable of hindering such undesirable complications. The branched chain amino acids as well as glutamine and arginine have been proven to be effective nutritional co-adjuvant therapeutic agents. Furthermore, new pharmaceutical approaches encompass designing organ-targeted nanoformulations to increase the medicinal efficacy. Therefore, the aim of the present study was to investigate the beneficial effects of liver-targeted amino acids-loaded nanoliposomes in counteracting the adverse hematopoietic and hepatic complications associated with cisplatin. Results revealed the use of the combination of two nanoliposomal formulations (one loading leucine + isolecuine + valine, and the other loading glutamine and arginine) given orally at a dose of 200 mg/kg for twelve days was effective against cisplatin-induced toxicities represented by improvement in the complete blood picture parameters, decrease in the serum hepatic enzymes levels, amelioration of the hepatic oxidative stress and cellular energy imbalance along with reduction in the histopathological abnormalities. It can be concluded that amino acids loaded nanoliposomes could be considered a new strategy in preventing cisplatin's adverse effects.


Assuntos
Carcinoma Hepatocelular , Ácido Glicirretínico , Neoplasias Hepáticas , Humanos , Cisplatino , Aminoácidos , Glutamina , Arginina
7.
J Food Biochem ; 46(12): e14442, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36165438

RESUMO

The relationship between the incidence of cardiovascular abnormalities and non-alcoholic fatty liver disease (NAFLD) has long been postulated. Curcumin (CUR) is a potential anti-atherosclerotic agent but its poor water solubility hinders its pharmacological use. Therefore, the present study aimed to investigate the effect of formulation of CUR nanoemulsion prepared using the spontaneous emulsification technique on high fat high fructose (HFHF)-induced hepatic and cardiac complications. Fifty Wistar rats were divided into five groups. CUR nanoemulsion at doses of 5 and 10 mg/kg and conventional powdered CUR at a dose of 50 mg/kg were orally administered daily to rats for two weeks, and compared with normal control and HFHF control. Results revealed that the high dose level of CUR nanoemulsion was superior to conventional CUR in ameliorating the HFHF-induced insulin resistance status and hyperlipidemia, with beneficial impact on rats' recorded electrocardiogram (ECG), serum aspartate aminotransferase (ALT) and alanine aminotransferase (AST) levels, leptin, adiponectin, creatine phosphokinase, lactate dehydrogenase and cardiac troponin-I. In addition, hepatic and cardiac oxidative and nitrosative stresses, oxidative DNA damage and disrupted cellular energy statuses were counteracted. Results were also confirmed by histopathological examination. PRACTICAL APPLICATIONS: The use of curcumin nanoemulsion could be beneficial in combating hepatic and cardiac complications resulting from HFHF diets.


Assuntos
Curcumina , Hepatopatia Gordurosa não Alcoólica , Ratos , Animais , Curcumina/farmacologia , Ratos Wistar , Frutose/efeitos adversos , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Hepatopatia Gordurosa não Alcoólica/etiologia
8.
Biomarkers ; 27(3): 247-257, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-34978233

RESUMO

CONTEXT: Gastric ulcer is regarded as one of the main clinical ailments with high morbidity and mortality rates. MATERIALS AND METHODS: Gastro-protective effect of Artemisia sieberi essential oil (AS-EO) in ethanol-induced rats was evaluated via biochemical, histopathological and large-scale metabolomics analyses. Glutathione (GSH), total antioxidant capacity (TAC), prostaglandin (PGE2) and tumour necrosis factor α (TNF-α) alongside with histopathological examination of gastric mucosa were analysed. Metabolites profiling coupled to Global Natural Products Social molecular networking platform (GNPS) and multivariate data analyses to reveal for changes in rats metabolome with treatments and involved action mechanisms. RESULTS: Pre-treatment with 100 and 200 mg/kg of AS-EO in EtOH-treated rats restored all parameters towards normal status compared to disease model. AS-EO alleviated the histological and pathological damage of gastric tissue caused by ethanol. Metabolites profiling revealed an increase in uracil, cholesterol and fatty acids/fatty acyl amides levels in ulcer rats and restored to normal levels post AS-EO intervention. These results indicated the efficacy of AS-EO in a dose-dependent manner, and to exert protective effects in ulcer rat model by targeting several metabolic pathways viz. lipid, energy, and nucleotide metabolisms. CONCLUSION: AS-EO adds to the known uses of genus Artemisia as anti-ulcerogenic agent by attenuating oxidative stress and inflammatory responses associated with an ulcer. Several novel biomarkers for ulcer progression in rats were identified and have yet to be confirmed in human models.


Assuntos
Antiulcerosos , Artemisia , Óleos Voláteis , Animais , Antiulcerosos/farmacologia , Etanol/farmacologia , Mucosa Gástrica , Humanos , Metabolômica , Óleos Voláteis/farmacologia , Ratos , Ratos Wistar , Úlcera/tratamento farmacológico , Úlcera/metabolismo , Úlcera/patologia
9.
J Pharm Pharmacol ; 74(2): 268-281, 2022 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-34928371

RESUMO

OBJECTIVES: Curcumin is a promising nutraceutical with reported diverse therapeutic properties, but of limited oral bioavailability. The current manuscript investigates the role of encapsulation of curcumin in nanoemulsion form in counteracting the adverse effect of chronic ingestion of a high-fat high-fructose diet (HFHF) by juvenile male rats regarding testicular abnormalities and declined spermatogenesis. METHODS: Curcumin nanoemulsion was administered orally to Wistar rats at a dose of 5 or 10 mg/kg and compared with curcumin powder, followed by a pharmacological and histological assessment. KEY FINDINGS: Results demonstrated that curcumin nanoemulsion was superior to curcumin powder, particularly in enhancing the percentage progressive motility of spermatozoa, normalization of essential and non-essential amino acids in semen, normalization of serum leptin and testosterone levels, as well as normalization of oxidative and nitrosative parameters. It was also proven to reduce testicular DNA fragmentation, while elevating testicular cellular energy. In addition, curcumin nanoemulsion administered at a dose of 10 mg/kg induced the highest level of spermatogenesis, delineated by histological examination of the seminiferous tubules. CONCLUSIONS: It can be concluded that curcumin nanoemulsion administered at a dose of 10 mg/kg successfully ameliorates the adverse effects of a HFHF on spermatogenesis.


Assuntos
Curcumina/farmacologia , Nanopartículas , Espermatogênese/efeitos dos fármacos , Espermatozoides/efeitos dos fármacos , Administração Oral , Animais , Curcumina/administração & dosagem , Fragmentação do DNA/efeitos dos fármacos , Dieta Hiperlipídica/efeitos adversos , Relação Dose-Resposta a Droga , Emulsões , Frutose/efeitos adversos , Masculino , Ratos , Ratos Wistar
10.
Molecules ; 26(19)2021 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-34641376

RESUMO

Different parts of Araucaria bidiwillii (bunya pin) trees, such as nuts, seeds, bark, and shoots, are widely used in cooking, tea, and traditional medicines around the world. The shoots essential oil (EO) has not yet been studied. Herein, the chemical profile of A. bidiwillii shoots EO (ABSEO) was created by GC-MS analysis. Additionally, the in vivo oral and topical anti-inflammatory effect against carrageenan-induced models, as well as antipyretic potentiality of ABSEO and its nanoemulsion were evaluated. Forty-three terpenoid components were identified and categorized as mono- (42.94%), sesqui- (31.66%), and diterpenes (23.74%). The main compounds of the ABSEO were beyerene (20.81%), α-pinene (16.21%), D-limonene (14.22%), germacrene D (6.69%), ß-humulene (4.14%), and sabinene (4.12%). The ABSEO and its nanoemulsion exhibited significant inflammation suppression in carrageenan-induced rat paw edema model, in both oral (50 and 100 mg/kg) and topical (5% in soyabean oil) routes, compared to the control and reference drugs groups. All the results demonstrated the significant inflammation reduction via the inflammatory cytokines (IL-1ß and IL8), nitrosative (NO), and prostaglandin E2 (PGE2) supported by the histopathological studies and immunohistochemical assessment of MMP-9 and NF-κß levels in paw tissues. Moreover, the oral administration of ABSEO and its nanoemulsion (50 and 100 mg/kg) exhibited antipyretic activity in rats, demonstrated by the inhibition of hyperthermia induced by intramuscular injection of brewer's yeast. These findings advised that the use of ABSEO and its nanoemulsion against numerous inflammatory and hyperthermia ailments that could be attributed to its active constituents.


Assuntos
Anti-Inflamatórios/farmacologia , Antipiréticos/farmacologia , Araucaria/química , Edema/tratamento farmacológico , Febre/tratamento farmacológico , Inflamação/tratamento farmacológico , Óleos Voláteis/farmacologia , Animais , Carragenina/efeitos adversos , Edema/induzido quimicamente , Edema/patologia , Emulsões , Inflamação/induzido quimicamente , Inflamação/patologia , Masculino , Dor/tratamento farmacológico , Extratos Vegetais/farmacologia , Brotos de Planta/química , Ratos , Ratos Wistar
11.
Biomolecules ; 11(8)2021 08 21.
Artigo em Inglês | MEDLINE | ID: mdl-34439913

RESUMO

Different species belonging to the genus Nephthea (Acyonaceae) are a rich resource for bioactive secondary metabolites. The literature reveals that the gastroprotective effects of marine secondary metabolites have not been comprehensively studied in vivo. Hence, the present investigation aimed to examine and determine the anti-ulcer activity of 4α,24-dimethyl-5α-cholest-8ß,18-dihydroxy,22E-en-3ß-ol (ST-1) isolated from samples of a Nephthea species. This in vivo study was supported by in silico molecular docking and protein-protein interaction techniques. Oral administration of ST-1 reduced rat stomach ulcers with a concurrent increase in gastric mucosa. Molecular docking calculations against the H+/K+-ATPase transporter showed a higher binding affinity of ST-1, with a docking score value of -9.9 kcal/mol and a pKi value of 59.7 nM, compared to ranitidine (a commercial proton pump inhibitor, which gave values of -6.2 kcal/mol and 27.9 µM, respectively). The combined PEA-reactome analysis results revealed promising evidence of ST-1 potency as an anti-ulcer compound through significant modulation of the gene set controlling the PI3K signaling pathway, which subsequently plays a crucial role in signaling regarding epithelialization and tissue regeneration, tissue repairing and tissue remodeling. These results indicate a probable protective role for ST-1 against ethanol-induced gastric ulcers.


Assuntos
Antozoários/metabolismo , Antiulcerosos/farmacologia , Esteróis/química , Animais , Simulação por Computador , Etanol/metabolismo , Feminino , Mucosa Gástrica/efeitos dos fármacos , Glicoproteínas/metabolismo , Inflamação , Espectroscopia de Ressonância Magnética , Simulação de Acoplamento Molecular , Fosfatidilinositol 3-Quinases/metabolismo , Mapeamento de Interação de Proteínas , Ratos , Ratos Wistar , Transdução de Sinais , Úlcera Gástrica/metabolismo , Úlcera/metabolismo
12.
Heliyon ; 7(6): e07159, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34159266

RESUMO

Fibrosis represents a common outcome of almost all chronic liver diseases and leads to an impairment of liver function that requires medical intervention. The current study aimed to evaluate the potential anti-fibrotic effect of Saccharomyces cervisciae cell wall extract (SCCWE) against thioacetamide (TAA)-induced liver fibrosis in rats (200mg/kg b.w. i.p. twice weekly for 6 weeks) using Ursodeoxycholic acid (UDCA) as a reference anti-fibrotic product. SCCWE at two doses (50 and 100 mg/kg) significantly ameliorated the rise in serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma glutamide transferase (GGT) activities, total bilirubin and direct bilirubin, increased total protein and albumin. SCCWE significantly reduced glutathione depletion (GSH), Nitric oxide (NOx) and malondialdehyde (MDA), thioredoxin (Trx) contents and elevated nuclear factor erythroid 2-related factor 2 (Nrf-2) content. Its anti-inflammatory effects were confirmed by observing a decrease in nuclear factor-κB (NF- κß), interleukin-1b (IL-1ß) and inducible nitric oxide synthase (iNOS) content. The anti-fibrotic effects of SCCWE were explored by assessing fibrosis related markers as it significantly reduced transform growth factor-ß (TGF-ß) and autotaxin (ATX) contents. Administration of SCCWE significantly decreased matrix metalloproteinase-3 and 9 (MMP-3 and -9). Furthermore, it also decreased alpha smooth muscle actin (α-SMA) and caspase-3 as assessed immunohistochemically those results were similar to that of the standard drug UDCA. This study shows that SCCWE protects against TAA-induced liver fibrosis in rats, through attenuating oxidative stress, and inflammation, ameliorating MMPs, combating apoptosis and thereby fibrotic biomarkers in addition to improving histopathological changes.

13.
Plants (Basel) ; 10(4)2021 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-33807147

RESUMO

Plants belonging to the Asteraceae family are widely used as traditional medicinal herbs around the world for the treatment of numerous diseases. In this work, the chemical profiles of essential oils (EOs) of the above-ground parts of Pluchea dioscoridis (L.) DC. and Erigeron bonariensis (L.) were studied in addition to their cytotoxic and anti-aging activities. The extracted EOs from the two plants via hydrodistillation were analyzed by gas chromatography-mass spectroscopy (GC-MS). GC-MS of EO of P. dioscoridis revealed the identification of 29 compounds representing 96.91% of the total oil. While 35 compounds were characterized from EO of E. bonariensis representing 98.21%. The terpenoids were found the main constituents of both plants with a relative concentration of 93.59% and 97.66%, respectively, including mainly sesquiterpenes (93.40% and 81.06%). α-Maaliene (18.84%), berkheyaradulen (13.99%), dehydro-cyclolongifolene oxide (10.35%), aromadendrene oxide-2 (8.81%), ß-muurolene (8.09%), and α-eudesmol (6.79%), represented the preponderance compounds of EO of P. dioscoridis. While, trans-α-farnesene (25.03%), O-ocimene (12.58%), isolongifolene-5-ol (5.53%), α-maaliene (6.64%), berkheyaradulen (4.82%), and α-muurolene (3.99%), represented the major compounds EO of E. bonariensis. A comparative study of our results with the previously described data was constructed based upon principal component analysis (PCA) and agglomerative hierarchical clustering (AHC), where the results revealed a substantial variation of the present studied species than other reported ecospecies. EO of P. dioscoridis exhibited significant cytotoxicity against the two cancer cells, MCF-7 and A-549 with IC50 of 37.3 and 22.3 µM, respectively. While the EO of the E. bonariensis showed strong cytotoxicity against HepG2 with IC50 of 25.6 µM. The EOs of P. dioscoridis, E. bonariensis, and their mixture (1:1) exhibited significant inhibitory activity of the collagenase, elastase, hyaluronidase, and tyrosinase comparing with epigallocatechin gallate (EGCG) as a reference. The results of anti-aging showed that the activity of mixture (1:1) > P. dioscoridis > E. bonariensis against the four enzymes.

14.
Molecules ; 26(4)2021 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-33668635

RESUMO

Launaea nudicaulis is used in folk medicine worldwide to treat several diseases. The present study aimed to assess the antidiabetic activity of L. nudicaulis ethanolic extract and its effect on diabetic complications in streptozotocin-induced hyperglycemic rats. The extract was orally administrated at 250 and 500 mg/kg/day for 5-weeks and compared to glibenclamide as a reference drug at a dose of 5 mg/kg/day. Administration of the extract exhibited a potential hypoglycemic effect manifested by a significant depletion of serum blood glucose concurrent with a significant elevation in serum insulin secretion. After 5-weeks, extract at 250 and 500 mg/kg/day decreased blood glucose levels by about 53.8 and 68.1%, respectively, compared to the initial values (p ≤ 0.05). The extract at the two dosages prevented weight loss of rats from the 2nd week till the end of the experiment, compared to diabetic control rats. The extract further exhibited marked improvement in diabetic complications including liver, kidney and testis performance, oxidative stress, and relative weight of vital organs, with respect to diabetic control. Histopathological examinations confirmed the previous biochemical analysis, where the extract showed a protective effect on the pancreas, liver, kidney, and testis that degenerated in diabetic control rats. To characterize extract composition, UPLC-ESI-qTOF-MS identified 85 chromatographic peaks belonging to flavonoids, phenolics, acyl glycerols, nitrogenous compounds, and fatty acids, with four novel phenolics reported. The potential anti-diabetic effect warrants its inclusion in further studies and or isolation of the main bioactive agent(s).


Assuntos
Asteraceae/química , Diabetes Mellitus Experimental/tratamento farmacológico , Etanol/química , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Animais , Antioxidantes/metabolismo , Biomarcadores/sangue , Glicemia/metabolismo , Peso Corporal/efeitos dos fármacos , Diabetes Mellitus Experimental/sangue , Hipoglicemiantes/farmacologia , Insulina/sangue , Rim/efeitos dos fármacos , Rim/fisiopatologia , Lipídeos/sangue , Fígado/efeitos dos fármacos , Fígado/fisiopatologia , Masculino , Malondialdeído/sangue , Metabolômica , Tamanho do Órgão/efeitos dos fármacos , Especificidade de Órgãos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Ratos Wistar , Estreptozocina , Testes de Toxicidade Aguda
15.
ACS Omega ; 6(5): 3587-3601, 2021 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-33585742

RESUMO

High consumption of industrialized food with high fat content is generally associated with insulin resistance, which in turn causes memory impairment and cognitive decline. Nicotinamide and ascorbic acid are among the promising neuroprotective molecules; however, an appreciable therapeutic activity necessitates the administration of a large dose of either. Therefore, the study aimed to assess if loading them in chitosan nanoparticles in doses 5-10 times lower than the unencapsulated forms would achieve comparable therapeutic results. Animals were fed a high-fat-high-fructose (HFHF) diet for 75 days. The vitamins in their conventional form (100 mg/kg) and the nanoparticles under investigation (10 and 20 mg/kg) were given orally concomitantly with the diet in the last 15 days. The intake of HFHF diet for 75 days led to an insulin-resistant state, with memory impairment, which was verified behaviorally through the object recognition test. This was accompanied by significant reduction in brain insulin-like growth factor 1 (IGF-1), increased acetylcholine esterase activity, increase in the serotonin and dopamine turnover ratio, and increase in oxidative stress and 8-OHdG, indicating cellular DNA fragmentation. Cellular energy was also decreased, and immunohistochemical examination verified the high immunoreactivity in both the cortex and hippocampus of the brain. The administration of nanoparticulated nicotinamide or ascorbic acid with a 10 times lesser dose than the unencapsulated forms managed to reverse all aforementioned harmful effects, with an even lesser immunoreactivity score than the unencapsulated form. Therefore, it can be concluded that nicotinamide or ascorbic acid chitosan nanoparticles can be recommended as daily supplements for neuroprotection in patients suffering from insulin resistance after conduction of clinical investigations.

16.
Hum Exp Toxicol ; 40(3): 526-537, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32909844

RESUMO

Acute paracetamol over dose-induced hepatotoxicity is considered an important medical hazard especially among women. Omega-3 long-chain polyunsaturated fatty acids (Omega-3 PUFAs) daily doses are nowadays recommended for their antioxidant and anti-inflammatory potentials. Fourier transform infrared (FTIR) spectroscopy is considered a reliable method in analyzing cellular alterations and is now efficiently used to diagnose several diseases and the efficacy of drugs even in the early stages. The aim of our study was to evaluate the hepatoprotective effect of Omega-3 PUFAs against paracetamol-induced hepatotoxicity in rats confirmed through measuring protein alterations in hepatocytes by FTIR. Rats were pretreated with Omega-3 PUFAs (50 and 100 mg/kg) for 21 days prior to oral ingestion of paracetamol. FTIR results revealed that Omega-3 PUFAs (50 mg/kg) limited the toxic effects of paracetamol by restoring the hepatic amide I to amide II ratio. In addition; biochemical analyses demonstrated that serum ALT, AST, Cholesterol, LDL-cholesterol and Il-6 levels as well as hepatic TNF-α, MDA, NOx levels were decreased. Besides; serum HDL-cholesterol level and hepatic GSH level were increased. Histopathological examinations of hepatic sections validated the hepatoprotective potential. The overall effect of this dose was comparable to those of the usual recommended hepatoprotective supplement; silymarin. In conclusion; it would be recommended to use Omega-3 PUFAs in low doses on daily bases as a hepatoprotective agent.


Assuntos
Acetaminofen/toxicidade , Analgésicos não Narcóticos/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Ácidos Graxos Ômega-3/uso terapêutico , Substâncias Protetoras/uso terapêutico , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Doença Hepática Induzida por Substâncias e Drogas/sangue , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Colesterol/sangue , Ácidos Graxos Ômega-3/farmacologia , Feminino , Glutationa/metabolismo , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Hepatócitos/patologia , Interleucina-6/sangue , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Malondialdeído/metabolismo , Óxido Nítrico/metabolismo , Substâncias Protetoras/farmacologia , Ratos Wistar , Espectroscopia de Infravermelho com Transformada de Fourier , Fator de Necrose Tumoral alfa/metabolismo
17.
Life Sci ; 263: 118540, 2020 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-33035588

RESUMO

AIMS: Non-alcoholic fatty liver disease (NAFLD) caused by consumption of high levels of fat and sugars (HFHS) in diet is considered one of the most dangerous medical complications among children and adolescents. Nicotinamide is among the promising candidates in ameliorating HFHS diet-induced NAFLD, but its use is limited by the possibility of prompting hepatotoxicity in high doses. Ascorbic acid is another promising candidate, however its use as a hepatoprotective agent is limited by its chemical instability. Therefore, the aim of the study was to overcome their delivery limitations and enhance their hepatoprotective activity by loading into nanoparticles. KEY FINDINGS: In the present study, upon incorporating nicotinamide or ascorbic acid in chitosan nanoparticles, they ameliorated the insulin-resistant status induced in rats by a high-fat-high-fructose (HFHF) diet. Both formulae decreased serum level of ALT and AST, as well as liver tissue total cholesterol, triglycerides and 8-hydroxy-2-deoxyguanosine (8-OHdG) levels. They also decreased oxidative and nitrosative stresses along with a significant increase in the hepatocellular energy. The biochemical findings were further confirmed by histopathological examination. Finally from the obtained data it could be concluded that chitosan nicotinamide nanoparticles at a dose level (10 mg/kg, p.o.) demonstrated beneficial pharmacological effect with safer toxicity profile than chitosan ascorbic acid nanoparticles. SIGNIFICANCE: Nicotinamide chitosan nanoparticles could be recommended as daily supplement in the recovery from NAFLD.


Assuntos
Ácido Ascórbico/farmacologia , Dieta Hiperlipídica/efeitos adversos , Frutose/toxicidade , Nanopartículas/administração & dosagem , Niacinamida/farmacologia , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Substâncias Protetoras/farmacologia , Animais , Antioxidantes/farmacologia , Biomarcadores/análise , Suplementos Nutricionais , Masculino , Nanopartículas/química , Hepatopatia Gordurosa não Alcoólica/etiologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Hepatopatia Gordurosa não Alcoólica/patologia , Ratos , Edulcorantes/toxicidade , Complexo Vitamínico B/farmacologia
18.
Pharm Dev Technol ; 25(9): 1139-1149, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32729753

RESUMO

The objective of the study was to explore the potential of a novel nicotinamide extrudate as an anti-aging platform compared to the conventional gel. Nicotinamide extrudates were prepared by hot melt extrusion and characterized pharmaceutically for their thermal behavior, mositure uptake, skin adhesion, and deposition in different skin layers. The pharmacological potential of the extrudates was explored in terms of induction of skin amino acids, cellular energy estimation, 8-hydroxy-2-deoxyguanosine content, Nitrate + nitrite content and histological chacaterization of collagen area percent. Results revealed that the extrusion technique managed to amorphize nicotinamide and enhance its skin deposition (46%) compared to the gel form which only showed about 10% deposition, owing to the mucoadhesive nature of the former. Extrudates were also found superior to the gel form as demonstrated by the increased amino acids level (glycine, proline, hydroxyproline), increased cellular energy, decreased oxidative stress and increased collagen formation. Nictotinamide extrudates were proven to be a scalable promising anti-aging platform which are worthy of entering the cosmeceutical market as products.


Assuntos
Envelhecimento/efeitos dos fármacos , Colágeno/farmacologia , Cosmecêuticos/farmacologia , Géis/farmacologia , Niacinamida/farmacologia , Envelhecimento/metabolismo , Aminoácidos/metabolismo , Animais , Colágeno/química , Cosmecêuticos/química , Portadores de Fármacos/química , Composição de Medicamentos/métodos , Feminino , Géis/química , Masculino , Niacinamida/química , Estresse Oxidativo/efeitos dos fármacos , Polímeros/química , Ratos , Ratos Wistar , Pele/efeitos dos fármacos , Pele/metabolismo , Solubilidade/efeitos dos fármacos
19.
Sci Rep ; 7(1): 9910, 2017 08 30.
Artigo em Inglês | MEDLINE | ID: mdl-28855590

RESUMO

The aim of the current manuscript was to test the applicability of a nanocomposite system of penetration enhancer vesicles (PEVs) within polymeric in situ forming gel network composed of poloxamer and hyaluronic acid for the intranasal delivery of the antiemetic dimenhydrinate (DMH). PEVs were prepared using phospholipids and labrasol/transcutol/PEG 400 as penetration enhancers, and characterized for entrapment efficiency (EE%), particle size, zeta potential and morphology. The nanocomposite in situ forming gel system was characterized for its sol-gel temperature, viscosity and mucoadhesiveness, and was pharmacodynamically tested on a cisplatin induced emesis model in rats in terms of food, water, kaolin intake and stomach weight content. The selected PEVs formula displayed EE% of 83% for DMH, particle size of 121 nm and a surface charge of 0.83 mV. The selected nanocomposite in situ gelling formula showed a viscosity of 2.13 Pa.S, mucoadhesive force of 0.62 N and DMH controlled release over 6 hours. The pharmacodynamic study showed the superiority of the nanocomposite in situ gelling formula; being administered at a lower dose than the oral marketed formula. The described nanocomposite system proved to be successful for the intranasal delivery of DMH, thus presenting a promising delivery modality for similar antiemetics.


Assuntos
Dimenidrinato/administração & dosagem , Géis/administração & dosagem , Nanocompostos/administração & dosagem , Vômito/prevenção & controle , Administração Intranasal , Animais , Antieméticos/administração & dosagem , Antieméticos/química , Antieméticos/farmacocinética , Cisplatino , Dimenidrinato/química , Dimenidrinato/farmacocinética , Ingestão de Líquidos/efeitos dos fármacos , Composição de Medicamentos , Ingestão de Alimentos/efeitos dos fármacos , Géis/química , Masculino , Microscopia Eletrônica de Transmissão , Estrutura Molecular , Nanocompostos/química , Nanocompostos/ultraestrutura , Ratos Wistar , Viscosidade , Vômito/induzido quimicamente , Vômito/fisiopatologia
20.
J Biomed Sci ; 24(1): 66, 2017 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-28865467

RESUMO

BACKGROUND: Malnutrition resulting from protein and calorie deficiency continues to be a major concern worldwide especially in developing countries. Specific deficiencies in the protein intake can adversely influence reproductive performance. The present study aimed to evaluate the effects of curcumin and curcumin nano-emulsion on protein deficient diet (PDD)-induced testicular atrophy, troubled spermatogenesis and decreased reproductive performance in male rats. METHODS: Juvenile rats were fed the protein deficient diet (PDD) for 75 days. Starting from day 60 the rats were divided into 4 groups and given the corresponding treatments for the last 15 days orally and daily as follows: 1st group; curcumin group (C) received 50 mg/kg curcumin p.o. 2ndgroup; curcumin nano-form low dose group (NCL) received 2.5 mg/kg nano-curcumin. 3rd group; curcumin nano-form high dose group (NCH) received 5 mg/kg nano-curcumin. 4th group served as malnutrition group (PDD group) receiving the protein deficient diet daily for 75 days and received distilled water ingestions (5 ml/kg p.o) daily for the last 15 days of the experiment. A normal control group was kept under the same conditions for the whole experiment and received normal diet according to nutrition requirement center daily for 75 days and received distilled water ingestions (5 ml/kg p.o) daily for the last 15 days of the experiment. RESULTS: PDD induced significant (P < 0.05) reduction in serum testosterone level, sperm motility, testicular GSH, CAT, SOD, testicular cell energy (ATP, ADP and AMP), essential and non-essential amino acids in seminal plasma, an increase in testicular MDA, NOx, GSSG and 8-OHDG. Data was confirmed by histological examination and revealed pathological alteration in the PDD group. Ingestion of curcumin (50 mg/kg) and curcumin nano-emulsion (2.5 and 5 mg/kg) showed significant (P< 0.05) amelioration effects against PDD-induced disrupted reproductive performance as well as biochemical and pathological alterations and the overall results of the nano-emulsion (5 mg/kg) were comparable to curcumin (50 mg/kg). CONCLUSIONS: The present study suggests that administration of curcumin nano-emulsion as a daily supplement would be beneficial in malnutrition- induced troubled male reproductive performance and spermatogenesis cases.


Assuntos
Curcumina/farmacologia , Substâncias Protetoras/metabolismo , Reprodução/efeitos dos fármacos , Espermatogênese/efeitos dos fármacos , Testículo/patologia , Ração Animal/análise , Animais , Atrofia/tratamento farmacológico , Atrofia/patologia , Curcumina/administração & dosagem , Dieta , Proteínas Alimentares/administração & dosagem , Suplementos Nutricionais/análise , Sistemas de Liberação de Medicamentos , Emulsões , Masculino , Substâncias Protetoras/administração & dosagem , Ratos , Ratos Wistar
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