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1.
Pharmaceuticals (Basel) ; 16(10)2023 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-37895850

RESUMO

Onion peels are often discarded, representing an unlimited amount of food by-products; however, they are a valuable source of bioactive phenolics. Thus, we utilized UPLC-MS/MS to analyze the metabolomic profiles of red (RO) and yellow (YO) onion peel extracts. The cytotoxic (SRB assay), anti-inflammatory (Griess assay), and antimicrobial (sensitivity test, MIC, antibiofilm, and SP-SDS tests) properties were assessed in vitro. Additionally, histological analysis, immunohistochemistry, and ELISA tests were conducted to investigate the healing potential in excisional skin wound injury and Candida albicans infection in vivo. RO extract demonstrated antibacterial activity, limited skin infection with C. albicans, and improved the skin's appearance due to the abundance of quercetin and anthocyanin derivatives. Both extracts reduced lipopolysaccharide-induced nitric oxide release in vitro and showed a negligible cytotoxic effect on MCF-7 and HT29 cells. When extracts were tested in vivo for their ability to promote tissue regeneration, it was found that YO peel extract had the greatest impact. Further biochemical analysis revealed that YO extract suppressed NLRP3/caspase-1 signaling and decreased inflammatory cytokines. Furthermore, YO extract decreased Notch-1 levels and boosted VEGF-mediated angiogenesis. Our findings imply that onion peel extract can effectively treat wounds by reducing microbial infection, reducing inflammation, and promoting tissue regeneration.

2.
Food Chem Toxicol ; 175: 113721, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36907500

RESUMO

Berberine (Berb) is a major alkaloid with potential protective effects against multiple neurological disorders. Nevertheless, its positive effect against 3-nitropropionic acid (3NP) induced Huntington's disease (HD) modulation has not been fully elucidated. Accordingly, this study aimed to assess the possible action mechanisms of Berb against such neurotoxicity using an in vivo rats model pretreated with Berb (100 mg/kg, p.o.) alongisde 3NP (10 mg/kg, i.p.) at the latter 2 weeks to induce HD symptoms. Berb revealed its capacity to partially protect the striatum as mediated via the activation of BDNF-TrkB-PI3K/Akt signaling and amelioration of neuroinflammation status by blocking NF-κB p65 with a concomitant reduction in its downstream cytokines TNF-α and IL-1ß. Moreover, its antioxidant potential was evidenced from induction of Nrf2 and GSH levels concurrent with a reduction in MDA level. Furthermore, Berb anti-apoptotic effect was manifested through the induction of pro-survival protein (Bcl-2) and down-regulation of the apoptosis biomarker (caspase-3). Finally, Berb intake ascertained its striatum protective action by improving the motor and histopathological abnormalities with concomitant dopamine restoration. In conclusion, Berb appears to modulate 3NP-induced neurotoxicity by moderating BDNF-TrkB-PI3K/Akt signaling besides its anti-inflammatory, antioxidant, as well as anti-apoptotic effect.


Assuntos
Berberina , Fármacos Neuroprotetores , Ratos , Animais , NF-kappa B/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Berberina/farmacologia , Fosfatidilinositol 3-Quinases/metabolismo , Antioxidantes , Fármacos Neuroprotetores/farmacologia
3.
Molecules ; 27(9)2022 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-35566153

RESUMO

Saussurea costus is a plant traditionally used for the treatment of several ailments. Our study accomplished the UPLC/T-TOF-MS/MS analysis of a methanol extract of Saussurea costus roots (MESC), in addition to lipoidal matter determination and assessment of its in vivo hepatoprotective activity. In this study, we were able to identify the major metabolites in MESC rather than the previously known isolated compounds, improving our knowledge of its chemical constituents. The flavones apigenin, acacetin, baicalein, luteolin, and diosmetin, and the flavonol aglycones quercetin, kaempferol, isorhamnetin, gossypetin, and myricetin and/or their glycosides and glucuronic derivatives were the major identified compounds. The hepatoprotective activity of MESC was evaluated by measuring catalase activity using UV spectrophotometry, inflammatory cytokines and apoptotic markers using ELISA techniques, and genetic markers using PCR. Paracetamol toxicity caused a significant increase in plasma caspase 2, cytokeratin 18 (CK18), liver tumor necrosis factor-α (TNF-α), interleukin 6 (IL-6), miRNA-34a, and miRNA-223, as well as a significant decrease in liver catalase (CAT) activity and in the levels of liver nuclear factor 1α (HNF-1α), sirtuin-1, and C/ebpα. Oral pretreatment with MESC (200 mg/kg) showed a significant decrease in caspase 2, CK18, TNF-α, IL-6 and a significant increase in liver CAT activity. MESC decreased the levels of liver miRNA-34a and miRNA-223 and induced HNF-1α, sirtuin-1, and C/ebpα gene expression. The histological examination showed a significant normalization in rats pretreated with MESC. Our findings showed that Saussurea costus may exert a potent hepatoprotective activity through the modulation of the expression of cellular cytokines, miRNA-34a, and miRNA-223.


Assuntos
MicroRNAs , Saussurea , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Proteína alfa Estimuladora de Ligação a CCAAT/metabolismo , Caspase 2/metabolismo , Catalase/metabolismo , Fator 1-alfa Nuclear de Hepatócito/metabolismo , Interleucina-6/metabolismo , MicroRNAs/genética , MicroRNAs/metabolismo , Extratos Vegetais/química , Raízes de Plantas , Ratos , Saussurea/química , Sirtuína 1/genética , Sirtuína 1/metabolismo , Espectrometria de Massas em Tandem , Fator de Necrose Tumoral alfa/metabolismo
4.
Molecules ; 27(8)2022 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-35458677

RESUMO

Reusing food waste is becoming popular in pharmaceutical industries. Watermelon (Citrullus lanatus) rind is commonly discarded as a major solid waste. Here, the in vitro cytotoxic potential of watermelon rind extracts was screened against a panel of human cancer cell lines. Cell cycle analysis was used to determine the induction of cell death, whereas annexin V-FITC binding, caspase-3, BAX, and BCL-2 mRNA expression levels were used to determine the degree of apoptosis. VEGF-promoting angiogenesis and cell migration were also evaluated. Moreover, the identification of phytoconstituents in the rind extract was achieved using UPLC/T-TOF-MS/MS, and a total of 45 bioactive compounds were detected, including phenolic acids, flavonoids aglycones, and their glycoside derivatives. The tested watermelon rind extracts suppressed cell proliferation in seven cancer cell lines in a concentration-dependent manner. The cytotoxicity of the rind aqueous extract (RAE) was higher compared with that of the other extracts. In addition to a substantial inhibitory effect on cell migration, the RAE triggered apoptosis in HCT116 and Hep2 cells by driving the accumulation of cells in the S phase and elevating the activity of caspase-3 and the BAX/BCL-2 ratio. Thus, a complete phytochemical and cytotoxic investigation of the Citrullus lanatus rind extract may identify its potential potency as an anticancer agent.


Assuntos
Antineoplásicos , Citrullus , Antineoplásicos/metabolismo , Caspase 3/metabolismo , Citrullus/química , Humanos , Compostos Fitoquímicos/metabolismo , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espectrometria de Massas em Tandem , Proteína X Associada a bcl-2/metabolismo
5.
Food Chem ; 326: 126993, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-32408002

RESUMO

Food industries are yielding annually plentiful by-products worldwide, these concomitants could be an excellent source of natural functional ingredients. Hence, the antimicrobial and cytotoxic effects of pomegranate husk were examined and chromatographic analyzes were applied for isolation of the bioactive compounds. Lignans; isohydroxymatairesinol, punicatannin C, flavonoids; phloretin, quercetin glycoside, indolamine; punigratane, and phenolic acid; coutaric acid were identified for the first time from pomegranate pericarp, and their structures were elucidated by spectroscopic analysis. Compared to isolated compounds, which showed a weak cytotoxic effects, punicatannin C induced a moderate cytotoxic activity against HepG2 and MCF-7 cell lines. Phloretin and coutaric acid exhibited potent antimicrobial activity againstStaphylococcus epidermidis,while punigratane possesses the most substantial antimicrobial effect onMicrococcus kristinae. In conclusion, pomegranate agrifood by-product; phloretin, punigratane, and coutaric acid display remarkablemicrobicideeffects and could be used in medical, cosmetic, and food industries purposes as a safe, and economical alternative to synthetic agents.


Assuntos
Bioensaio , Punica granatum/química , Antibacterianos/farmacologia , Linhagem Celular Tumoral , Flavonoides/análise , Frutas/química , Humanos , Taninos Hidrolisáveis/análise , Lignanas/análise , Fenóis/análise
6.
AAPS PharmSciTech ; 19(5): 2346-2357, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29869310

RESUMO

The present study demonstrates a preparative medium-pressure liquid chromatography (MPLC) method for isolation of Morin besides evaluating its efficacy in comparison with its self-nanoemulsifying drug delivery (SNEDD) and nanoemulsion (NE) systems against in-vivo HgCl2-induced lung toxicity in rats. Morin was isolated from hydroalcoholic (70%) extract of Psidium guajava leaves by MPLC. The purity (> 90%) was done using HPLC. Screening of Morin solubility was studied to identify the components of each system. The prepared formulae were assessed for their thermodynamic stability, rheological properties, emulsification time, size, zeta potential beside its dissolution. The selected formulae according to the smallest size, highest zeta potential, and release at Q10 min were assessed for their morphology by transmission electron microscopy (TEM) and protective potential against in-vivo HgCl2-induced lung toxicity in rats. All formulae were stable with Newtonian flow, emulsification time was (< 134 ± 10 s), size (< 40 nm) with zeta potential (> - 10.36 ± 0.99 mV). The extent of free Morin dissolved from capsule showed significantly the lowest percent released (22.21 ± 1.45%) while in case of SNEDDs and NEs (> 55% dissolved). The morphology of the selected Morin formulae showed spherical shape within the nano-range. Supplementation of Morin and its formulae to rats caused significant decrease in C-reactive protein, hepatoglobin, hydroproxide, lung nitric oxide, tumor necrosis factor-α, immunoglobulin (E and G), histamine, malondialdehyde, and interleukin-6 gene expression while significant increase in immunoglobulin A, caspase-3, catalase, and glutathione peroxidase compared to HgCl2. SNEDD and NE formulae could ameliorate lung toxicity in a mechanism related to their antioxidant and anti-inflammatory potential.


Assuntos
Antioxidantes/química , Portadores de Fármacos/química , Emulsões/química , Flavonoides/química , Pulmão/efeitos dos fármacos , Cloreto de Mercúrio/toxicidade , Animais , Antioxidantes/administração & dosagem , Antioxidantes/metabolismo , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/metabolismo , Composição de Medicamentos , Sistemas de Liberação de Medicamentos/métodos , Emulsões/administração & dosagem , Emulsões/metabolismo , Flavonoides/administração & dosagem , Flavonoides/metabolismo , Pulmão/metabolismo , Masculino , Microscopia Eletrônica de Transmissão , Nanopartículas/química , Tamanho da Partícula , Ratos , Ratos Wistar , Solubilidade
7.
Molecules ; 24(1)2018 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-30602714

RESUMO

A hitherto unknown polyoxygenated flavonol robinobioside (gossypetin-3-O-ß-d-robinobioside) was isolated from the leaves of Caesalpinia gilliesii along with thirteen known phenolic secondary metabolites. The isolated compounds were characterized using spectroscopic analysis, including 1D and 2D NMR and mass spectrometry (MS) analyses. The extract reduced the level of liver damage in CCl4-induced liver injury in rats. A decrease of the liver biomarkers-aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and an increase of total antioxidant capacity (TAC) levels-were observed similar to the liver protecting drug silymarin. In addition, the extract showed promising activity against carrageenan-induced paw edema in rats and protected their stomachs against ethanol-induced gastric ulcers in a concentration dependent fashion. The observed activities could be attributed to the high content of antioxidant polyphenols. Our results suggest that the C. gilliesii has the capacity to scavenge free radicals and can protect against oxidative stress, and liver and stomach injury.


Assuntos
Caesalpinia/química , Edema/prevenção & controle , Flavonóis/administração & dosagem , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/administração & dosagem , Úlcera/prevenção & controle , Alanina Transaminase/genética , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Aspartato Aminotransferases/genética , Tetracloreto de Carbono/toxicidade , Carragenina/toxicidade , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/metabolismo , Flavonóis/química , Flavonóis/farmacologia , Fígado/efeitos dos fármacos , Fígado/enzimologia , Masculino , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Silimarina/administração & dosagem , Silimarina/química , Silimarina/farmacologia , Úlcera/induzido quimicamente
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