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1.
Molecules ; 26(12)2021 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-34204643

RESUMO

Plant-derived protein hydrolysates have potential applications in nutrition. Rice protein hydrolysates (RPHs), an excellent source of proteins, have attracted attention for the development of cosmeceuticals. However, few studies have reported the potential application of RPH in analysis, and this study examined their antioxidant activities and the inhibitory activities of skin aging enzymes. The results indicated that the total phenolic and flavonoid concentrations were 2.06 ± 0.13 mg gallic acid equivalent/g RPHs and 25.96 ± 0.52 µg quercetin equivalent/g RPHs, respectively. RPHs demonstrated dose-dependent activity for scavenging free radicals from 1,1-diphenyl-2-picrylhydrazyl [half-maximal inhibitory concentration (IC50) = 42.58 ± 2.1 mg/g RPHs] and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (IC50 = 2.11 ± 0.88 mg/g RPHs), dose-dependent reduction capacity (6.95 ± 1.40 mg vitamin C equivalent/g RPHs) and oxygen radical absorbance capacity (473 µmol Trolox equivalent/g RPHs). The concentrations of the RPH solution required to achieve 50% inhibition of hyaluronidase and tyrosinase activities were determined to be 8.91 and 107.6 mg/mL, respectively. This study demonstrated that RPHs have antioxidant, antihyaluronidase, and antityrosinase activities for future cosmetic applications.


Assuntos
Hidrolisados de Proteína/química , Hidrolisados de Proteína/farmacologia , Envelhecimento/efeitos dos fármacos , Animais , Antioxidantes/farmacologia , Compostos de Bifenilo/química , Compostos de Bifenilo/farmacologia , Clareadores/química , Clareadores/metabolismo , Flavonoides/farmacologia , Sequestradores de Radicais Livres/química , Ácido Gálico/farmacologia , Camundongos , Oryza/química , Oryza/enzimologia , Oryza/metabolismo , Oxirredução , Fenóis/farmacologia , Picratos/química , Picratos/farmacologia , Extratos Vegetais/química , Quercetina/farmacologia , Células RAW 264.7 , Ácidos Sulfônicos/química , Ácidos Sulfônicos/farmacologia , Tiazóis/química , Tiazóis/farmacologia
2.
Molecules ; 26(12)2021 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-34205312

RESUMO

In the current study, in vitro antimicrobial and antioxidant activities and in vivo anti-inflammatory and analgesic activities of Scutellaria edelbergii Rech. f. (crude extract and subfractions, i.e., n-hexane, ethyl acetate (EtOAc), chloroform, n-butanol (n-BuOH) and aqueous) were explored. Initially, extraction and fractionation of the selected medicinal plant were carried out, followed by phytochemical qualitative tests, which were mostly positive for all the extracts. EtOAc fraction possessed a significant amount of phenolic (79.2 ± 0.30 mg GAE/g) and flavonoid (84.0 ± 0.39 mg QE/g) content. The EtOAc fraction of S. edelbergii exhibited appreciable antibacterial activity against Gram-negative (Escherichia coli and Klebsiella pneumoniae) strains and significant zones of inhibition were observed against Gram-positive bacterial strains (Bacillus subtilis and Staphylococcus aureus). However, it was found inactive against Candida Albicans and Fusarium oxysporum fungal strains. The chloroform fraction was the most effective with an IC50 value of 172 and 74 µg/mL against DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays, in comparison with standard ascorbic acid 59 and 63 µg/mL, respectively. Moreover, the EtOAc fraction displayed significant in vivo anti-inflammatory activity (54%) using carrageenan-induced assay and significant (55%) in vivo analgesic activity using acetic acid-induced writing assay. In addition, nine known compounds, ursolic acid (UA), ovaul (OV), oleanolic acid (OA), ß-sitosterol (BS), micromeric acid (MA), taraxasterol acetate (TA), 5,3',4'-trihydroxy-7-methoxy flavone (FL-1), 5,7,4'-trihydroxy-6,3'-dimiethoxyflavone (FL-2) and 7-methoxy catechin (FL-3), were isolated from methanolic extract of S. edelbergii. These constituents have never been obtained from this source. The structures of all the isolated constituents were elucidated by spectroscopic means. In conclusion, the EtOAc fraction and all other fractions of S. edelbergii, in general, displayed a significant role as antibacterial, free radical scavenger, anti-inflammatory and analgesic agents which may be due to the presence of these constituents and other flavonoids.


Assuntos
Extratos Vegetais/farmacologia , Scutellaria/química , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Pesquisa Biomédica/métodos , Flavonoides/farmacologia , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Fenóis/farmacologia , Compostos Fitoquímicos/farmacologia , Plantas Medicinais/química
3.
Molecules ; 26(12)2021 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-34205329

RESUMO

The content of plant secondary metabolites is not stable, and factors such as the region/location effect and seasonal variations have an impact on their chemical composition, especially in parasitic plants. Research in this area is an important step in the development of quality parameter standards of medicinal plants and their finished products. The effects of the time and place of harvest and the host tree species on the chemical composition and antioxidant activity of mistletoe extracts were investigated. Statistical tools were used to evaluate the results of the spectrophotometric and LC-ESI-MS/MS studies of the phenolic composition and antioxidant activity. The investigations indicate that the qualitative and quantitative composition, influencing the biological activity of mistletoe extracts, largely depends on the origin of the plant. The mistletoe extracts exhibited a rich phenol profile and high antioxidant activity. The chemometric analysis indicated that mistletoe collected from conifers (Viscum abietis and Viscum austriacum) had the most advantageous chemical composition and antioxidant activity. Moreover, the chemical profile and biological activity of the plant material were closely related to the climatic conditions and location of the harvested plant. Higher levels of phenolic compounds and high antioxidant activity were found in extracts obtained from plant material collected in cold weather with the presence of snow and less sunshine (autumn-winter period).


Assuntos
Antioxidantes/química , Antioxidantes/fisiologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Árvores/química , Viscum album/química , Cromatografia Líquida/métodos , Erva-de-Passarinho/química , Fenóis/química , Fenóis/farmacologia , Plantas Medicinais/química , Espectrometria de Massas em Tandem/métodos
4.
Molecules ; 26(12)2021 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-34205369

RESUMO

The benefits of natural honeybee products (e.g., honey, royal jelly, beeswax, propolis, beevenom and pollen) to the immune system are remarkable, and many of them are involved in the induction of antibody production, maturation of immune cells and stimulation of the immune system. The type of plants in the geographical area, climatic conditions and production method have a significantly influence on the nutritional quality of honey. However, this variability can influence consumer liking by the sensory attributes of the product. The aim of this work was to compare the most popular honeys from Poland in terms of nutritional value, organoleptic properties and antioxidant activity. In the study, five varieties of honey (honeydew, forest, buckwheat, linden and dandelion) from conventional and organic production methods were tested. The nutritional characteristics of honey samples included acidity, content of water, sugars, vitamin C, HMF and phenolics (total and flavonoids), while honey color, taste, aroma and consistency were investigated in the organoleptic characteristics. The antioxidant activity was determined in water- and ethanol-soluble honey extracts using DPPH and ORAC tests. The results showed that organoleptic and nutritional characteristics of popular Polish honeys differ significantly in relation to plant source and production method. The significant effect of honey variety on the content of HMF, saccharose and phenolics, as well as acidity and antioxidant capacity were noted. The impact of variety and variety × production method interaction was significant in the case of the content of vitamin C, glucose and fructose. A visible difference of buckwheat and forest honeys from other samples was observed. The highest content of total phenolics with antioxidant activity based on the SET mechanism was found in buckwheat honeys, while forest honeys were richer in flavonoids.


Assuntos
Antioxidantes/farmacologia , Abelhas/metabolismo , Mel/análise , Nutrientes/farmacologia , Animais , Ácido Ascórbico/farmacologia , Etanol/química , Fagopyrum , Feminino , Flavonoides/farmacologia , Frutose/farmacologia , Glucose/farmacologia , Sistema Imunitário/efeitos dos fármacos , Masculino , Fenóis/farmacologia , Polônia , Água/química
5.
Viruses ; 13(7)2021 06 29.
Artigo em Inglês | MEDLINE | ID: mdl-34209556

RESUMO

Vitis vinifera represents an important and renowned source of compounds with significant biological activity. Wines and winery bioproducts, such as grape pomace, skins, and seeds, are rich in bioactive compounds against a wide range of human pathogens, including bacteria, fungi, and viruses. However, little is known about the biological properties of vine leaves. The aim of this study was the evaluation of phenolic composition and antiviral activity of Vitis vinifera leaf extract against two human viruses: the Herpes simplex virus type 1 (HSV-1) and the pandemic and currently widespread severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). About 40 phenolic compounds were identified in the extract by HPLC-MS/MS analysis: most of them were quercetin derivatives, others included derivatives of luteolin, kaempferol, apigenin, isorhamnetin, myricetin, chrysoeriol, biochanin, isookanin, and scutellarein. Leaf extract was able to inhibit both HSV-1 and SARS-CoV-2 replication in the early stages of infection by directly blocking the proteins enriched on the viral surface, at a very low concentration of 10 µg/mL. These results are very promising and highlight how natural extracts could be used in the design of antiviral drugs and the development of future vaccines.


Assuntos
Antivirais/farmacologia , Herpesvirus Humano 1/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , SARS-CoV-2/efeitos dos fármacos , Vitis/química , Células A549 , Animais , Produtos Biológicos/análise , Produtos Biológicos/farmacologia , Linhagem Celular , Chlorocebus aethiops , Cromatografia Líquida de Alta Pressão , Humanos , Células MCF-7 , Fenóis/farmacologia , Extratos Vegetais/análise , Espectrometria de Massas em Tandem , Células Vero
6.
Molecules ; 26(12)2021 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-34200718

RESUMO

Euterpe oleracea Mart. (açai) is a native palm from the Amazon region. There are various chemical constituents of açai with bioactive properties. This study aimed to evaluate the chemical composition and cytotoxic effects of açai seed extract on breast cancer cell line (MCF-7). Global Natural Products Social Molecular Networking (GNPS) was applied to identify chemical compounds present in açai seed extract. LC-MS/MS and molecular networking were employed to detect the phenolic compounds of açai. The antioxidant activity of açai seed extract was measured by DPPH assay. MCF-7 breast cancer cell line viability was evaluated by MTT assay. Cell death was evaluated by flow cytometry and time-lapse microscopy. Autophagy was evaluated by orange acridin immunofluorescence assay. Reactive oxygen species (ROS) production was evaluated by DAF assay. From the molecular networking, fifteen compounds were identified, mainly phenolic compounds. The açai seed extract showed cytotoxic effects against MCF-7, induced morphologic changes in the cell line by autophagy and increased the ROS production pathway. The present study suggests that açai seed extract has a high cytotoxic capacity and may induce autophagy by increasing ROS production in breast cancer. Apart from its antioxidant activity, flavonoids with high radical scavenging activity present in açai also generated NO (nitric oxide), contributing to its cytotoxic effect and autophagy induction.


Assuntos
Neoplasias da Mama/tratamento farmacológico , Morte Celular/efeitos dos fármacos , Euterpe/química , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Sementes/química , Antioxidantes/química , Antioxidantes/farmacologia , Autofagia/efeitos dos fármacos , Linhagem Celular Tumoral , Cromatografia Líquida/métodos , Feminino , Flavonoides/química , Flavonoides/farmacologia , Frutas/química , Humanos , Células MCF-7 , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Polifenóis/química , Polifenóis/farmacologia , Espectrometria de Massas em Tandem/métodos
7.
Int J Mol Sci ; 22(11)2021 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-34073604

RESUMO

Dietary phenolic compounds possess potent bioactivity against inflammatory pathways of chronic inflammatory conditions, such as type 2 diabetes. Here, the phenolic profile and bioactivity of Italian red wines Gaglioppo, Magliocco, and Nerello Mascalese were characterized. NMR, HPLC/UV-Vis and spectrophotometric characterization showed that Magliocco was the richest wine in monomeric anthocyanins (two-fold), catechins, and low molecular weight phenolics (LMWP). A positive correlation was observed between the polyphenolic content and antioxidant capacity (p < 0.05), with Magliocco displaying the highest antioxidant capacity (p < 0.01). In vitro evidence on the endothelial cell models of insulin resistance and hyperglycemia showed the ability of Magliocco to reduce reactive oxygen species (ROS) (p < 0.01) and cytokine release (p < 0.01) and to upregulate SIRT1 and SIRT6 (p < 0.01). On the whole, the results indicated that the quantitative and qualitative phenolic profiles of red wines influence their in vitro beneficial effects on oxidative and proinflammatory milieu in endothelial cells, showing a positive modulation of SIRT1 and SIRT6, both implied in vascular aging.


Assuntos
Antioxidantes/farmacologia , Células Endoteliais/enzimologia , Fenóis/farmacologia , Sirtuína 1/metabolismo , Sirtuínas/metabolismo , Vinho , Antioxidantes/química , Linhagem Celular , Humanos , Fenóis/química
8.
Int J Mol Sci ; 22(11)2021 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-34073890

RESUMO

The breast cancer resistance protein (BCRP) is an important efflux transporter in the blood-brain barrier (BBB), protecting the brain from a wide range of substances. In this study, we investigated if BCRP function is affected by bisphenol A (BPA), a high production volume chemical used in common consumer products, as well as by bisphenol F (BPF) and bisphenol S (BPS), which are used to substitute BPA. We employed a transwell-based in vitro cell model of iPSC-derived brain microvascular endothelial cells, where BCRP function was assessed by measuring the intracellular accumulation of its substrate Hoechst 33342. Additionally, we used in silico modelling to predict if the bisphenols could directly interact with BCRP. Our results showed that BPA significantly inhibits the transport function of BCRP. Additionally, BPA was predicted to bind to the cavity that is targeted by known BCRP inhibitors. Taken together, our findings demonstrate that BPA inhibits BCRP function in vitro, probably by direct interaction with the transporter. This effect might contribute to BPA's known impact on neurodevelopment.


Assuntos
Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo , Compostos Benzidrílicos/farmacologia , Barreira Hematoencefálica/metabolismo , Células Endoteliais/efeitos dos fármacos , Proteínas de Neoplasias/metabolismo , Fenóis/farmacologia , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/antagonistas & inibidores , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/química , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/genética , Compostos Benzidrílicos/química , Compostos Benzidrílicos/toxicidade , Benzimidazóis/metabolismo , Técnicas de Cultura de Células , Células Cultivadas , Dicetopiperazinas/química , Dicetopiperazinas/farmacologia , Expressão Gênica , Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Humanos , Técnicas In Vitro , Células-Tronco Pluripotentes Induzidas/metabolismo , Simulação de Acoplamento Molecular , Proteínas de Neoplasias/antagonistas & inibidores , Proteínas de Neoplasias/química , Proteínas de Neoplasias/genética , Fenóis/química , Fenóis/toxicidade , Ligação Proteica , Sulfonas/química , Sulfonas/farmacologia , Sulfonas/toxicidade
9.
Gene ; 794: 145746, 2021 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-34062258

RESUMO

The expression of HOXB2, a homeobox transcription factor, is altered in a variety of solid tumors. Using an in vivo screen to identify regulators of breast tumor growth in murine mammary fat pads, Boimel and co-workers recently identified HOXB2 as a tumor suppressor. However, the mechanistic underpinnings of its role in breast cancer is not understood. Given the emerging interaction of estrogen-regulated gene expression and altered HOX gene expression network in the pathophysiology of breast cancer, this study addressed the relationship between estrogen signaling and HOXB2 expression. Using a mouse model and human breast cancer cell lines, we show that estrogen suppresses HOXB2 expression. Suppression of HOXB2 by PPT, a known ERα agonist, in MCF-7 and T47D cells indicated the involvement of ERα, which was confirmed by siRNA-mediated ERα knockdown experiments. In-silico analysis of the upstream promoter region revealed the presence of three putative EREs. Chromatin immunoprecipitation experiments showed that upon estrogen binding, ERα engaged with EREs in the 5' upstream region of HOXB2 in MCF-7 and T47D cells. Future investigations should address the implications of estrogen-mediated suppression on the proposed tumor suppressor function of HOXB2.


Assuntos
Neoplasias da Mama/genética , Regulação para Baixo , Receptor alfa de Estrogênio/genética , Proteínas de Homeodomínio/genética , Fenóis/administração & dosagem , Pirazóis/administração & dosagem , Fatores de Transcrição/genética , Animais , Linhagem Celular Tumoral , Feminino , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Células MCF-7 , Camundongos , Transplante de Neoplasias , Fenóis/farmacologia , Regiões Promotoras Genéticas , Pirazóis/farmacologia
10.
Molecules ; 26(11)2021 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-34070837

RESUMO

Bioassay-guided separation of young leaves extracts of Syzygium antisepticum (Blume) Merr. & L.M. Perry led to the isolation of four triterpenoids (betulinic acid, ursolic acid, jacoumaric acid, corosolic acid) and one sterol glucoside (daucosterol) from the ethyl acetate extract, and three polyphenols (gallic acid, myricitrin, and quercitrin) from the methanol (MeOH) extract. The MeOH extract of S. antisepticum and some isolated compounds, ursolic acid and gallic acid potentially exhibited acetylcholinesterase activity evaluated by Ellman's method. The MeOH extract and its isolated compounds, gallic acid, myricitrin, and quercitrin, also strongly elicited DPPH radical scavenging activity. In HEK-293 cells, the MeOH extract possessed cellular antioxidant effects by attenuating hydrogen peroxide (H2O2)-induced ROS production and increasing catalase, glutathione peroxidase-1 (GPx-1), and glutathione reductase (GRe). Furthermore, myricitrin and quercitrin also suppressed ROS production induced by H2O2 and induced GPx-1 and catalase production in HEK-293 cells. These results indicated that the young leaves of S. antisepticum are the potential sources of antioxidant and anticholinesterase agents. Consequently, S. antisepticum leaves are one of indigenous vegetables which advantage to promote the health and prevent diseases related to oxidative stress.


Assuntos
Extratos Vegetais/química , Syzygium/química , Acetatos/química , Antioxidantes/química , Antioxidantes/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Sequestradores de Radicais Livres/farmacologia , Células HEK293 , Humanos , Metanol/química , Estresse Oxidativo/efeitos dos fármacos , Fenóis/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polifenóis/farmacologia , Syzygium/metabolismo
11.
Molecules ; 26(9)2021 May 08.
Artigo em Inglês | MEDLINE | ID: mdl-34066799

RESUMO

Honey has good antimicrobial properties and can be used for medical treatment. The antimicrobial properties of unifloral honey varieties are different. In this study, we evaluated the antimicrobial and antioxidant activities of nine kinds of Chinese monofloral honeys. In addition, headspace gas chromatography-ion mobility spectrometry (HS-GC-IMS) technology was used to detect their volatile components. The relevant results are as follows: 1. The agar diffusion test showed that the diameter of inhibition zone against Staphylococcus aureus of Fennel honey (21.50 ± 0.41 mm), Agastache honey (20.74 ± 0.37 mm), and Pomegranate honey (18.16 ± 0.11 mm) was larger than that of Manuka 12+ honey (14.27 ± 0.10 mm) and Manuka 20+ honey (16.52 ± 0.12 mm). The antimicrobial activity of Chinese honey depends on hydrogen peroxide. 2. The total antioxidant capacity of Fennel honey, Agastache honey, and Pomegranate honey was higher than that of other Chinese honeys. There was a significant positive correlation between the total antioxidant capacity and the total phenol content of Chinese honey (r = 0.958). The correlation coefficient between the chroma value of Chinese honey and the total antioxidant and the diameter of inhibition zone was 0.940 and 0.746, respectively. The analyzed dark honeys had better antimicrobial and antioxidant activities. 3. There were significant differences in volatile components among Fennel honey, Agastache honey, Pomegranate honey, and Manuka honey. Hexanal-D and Heptanol were the characteristic components of Fennel honey and Pomegranate honey, respectively. Ethyl 2-methylbutyrate and 3-methylpentanoic acids were the unique compounds of Agastache honey. The flavor fingerprints of the honey samples from different plants can be successfully built using HS-GC-IMS and principal component analysis (PCA) based on their volatile compounds. Fennel honey, Agastache honey, and Pomegranate honey are Chinese honey varieties with excellent antimicrobial properties, and have the potential to be developed into medical grade honey.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Mel/análise , Mel/classificação , Staphylococcus aureus/efeitos dos fármacos , Agastache/química , Antibacterianos/química , Antioxidantes/química , China , Cromatografia Gasosa , Foeniculum/química , Peróxido de Hidrogênio/farmacologia , Espectrometria de Mobilidade Iônica , Leptospermum/química , Testes de Sensibilidade Microbiana , Fenóis/farmacologia , Romã (Fruta)/química
12.
Molecules ; 26(11)2021 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-34070495

RESUMO

In recent years, the use of Sideritis species as bioactive agents is increasing exponentially. The present study aimed to investigate the chemical constituents, as well as the anti-ageing potential of the cultivated Sideritis euboea Heldr. The chemical fingerprinting of the ethyl acetate residue of this plant was studied using 1D and 2D-NMR spectra. Isomeric compounds belonging to acylated flavone derivatives and phenylethanoid glycosides were detected in the early stage of the experimental process through 2D-NMR techniques. Overall, thirty-three known compounds were isolated and identified. Some of them are reported for the first time not only in S. euboea, but also in genus Sideritis L. The anti-ageing effect of the ethyl acetate residue and the isolated specialized products was assessed as anti-hyaluronidase activity. In silico docking simulation revealed the interactions of the isolated compounds with hyaluronidase. Furthermore, the in vitro study on the inhibition of hyaluronidase unveiled the potent inhibitory properties of ethyl acetate residue and apigenin 7-O-ß-d-glucopyranoside. Though, the isomers of apigenin 7-O-p-coumaroyl-glucosides and also the 4'-methyl-hypolaetin 7-O-[6'''-O-acetyl-ß-d-allopyranosyl]-(1→2)-ß-d-glucopyranoside exerted moderate hyaluronidase inhibition. This research represents the first study to report on the anti-hyaluronidase activity of Sideritis species, confirming its anti-inflammatory, cytotoxic and anti-ageing effects and its importance as an agent for cosmetic formulations as also anticancer potential.


Assuntos
Envelhecimento/efeitos dos fármacos , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Sideritis/química , Acetatos/química , Simulação por Computador , Hialuronoglucosaminidase/antagonistas & inibidores , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Espectroscopia de Prótons por Ressonância Magnética/métodos , Termodinâmica
13.
Int J Mol Sci ; 22(10)2021 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-34067838

RESUMO

Resveratrol can affect the physiology or biochemistry of offspring in the maternal-fetal animal model. However, it exhibits low bioavailability in humans and animals. Fifteen-week SD pregnant female rats were orally administered bisphenol A (BPA) and/or resveratrol butyrate ester (RBE), and the male offspring rats (n = 4-8 per group) were evaluated. The results show that RBE treatment (BPA + R30) compared with the BPA group can reduce the damage caused by BPA (p < 0.05). RBE enhanced the expression of selected genes and induced extramedullary hematopoiesis and mononuclear cell infiltration. RBE increased the abundance of S24-7 and Adlercreutzia in the intestines of the male offspring rats, as well as the concentrations of short-chain fatty acids (SCFAs) in the feces. RBE also increased the antioxidant capacity of the liver by inducing Nrf2, promoting the expression of HO-1, SOD, and CAT. It also increased the concentration of intestinal SCFAs, enhancing the barrier formed by intestinal cells, thereby preventing BPA-induced metabolic disruption in the male offspring rats, and reduced liver inflammation. This study identified a potential mechanism underlying the protective effects of RBE against the liver damage caused by BPA exposure during the peri-pregnancy period, and the influence of the gut microbiota on the gut-liver axis in the offspring.


Assuntos
Compostos Benzidrílicos/efeitos adversos , Hepatopatias/prevenção & controle , Fenóis/efeitos adversos , Resveratrol/farmacologia , Animais , Antioxidantes/metabolismo , Compostos Benzidrílicos/farmacologia , Butiratos/metabolismo , Ésteres/metabolismo , Ácidos Graxos Voláteis/metabolismo , Feminino , Microbioma Gastrointestinal , Fígado/metabolismo , Fígado/patologia , Hepatopatias/metabolismo , Masculino , Fenóis/farmacologia , Gravidez , Efeitos Tardios da Exposição Pré-Natal/induzido quimicamente , Ratos , Ratos Sprague-Dawley , Resveratrol/análogos & derivados
14.
Food Chem ; 361: 129866, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34091399

RESUMO

This study investigated the in vitro bioactivities of extracts obtained from viscera, spines, shells, and gonads of Stomopneustes variolaris using subcritical water extraction (SWE) at 110 °C, 150 °C, 190 °C, and 230 °C and Soxhlet extraction. The highest amounts of phenolics (22.68 ± 0.05 mg GAE/g), flavonoids (27.11 ± 0.10 mg RE/g), and proteins (40.25 ± 0.84 mg BSA/g) were recorded from gonads at 230 °C, whereas maximum sugar content (23.38 ± 1.30 mg glucose/g) was in viscera at 150 °C. Gonads at 230 °C exhibited the highest DPPH activity (78.68 ± 0.18%), whereas viscera at 150 °C exhibited the highest ABTS+ (98.92 ± 1.27%) and protein denaturation inhibition activity (37.13 ± 9.94%). Viscera at 110 °C claimed the highest amylase inhibition (42.46 ± 0.83%), and spines at 150 °C had the highest anticancer activity (IC50 = 767.47 µg/mL). SWE achieved superior results in bioactive compound recovery and detected higher levels of bioactivities (p < 0.05). Results suggest processing sea urchin extracts via SWE has potential application to the food and pharmaceutical industries.


Assuntos
Produtos Biológicos/farmacologia , Fracionamento Químico/métodos , Ouriços-do-Mar/química , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Produtos Biológicos/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos , Flavonoides/análise , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Química Verde , Células HeLa , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Fenóis/análise , Fenóis/isolamento & purificação , Fenóis/farmacologia , Água/química
15.
Life Sci ; 278: 119583, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-33957170

RESUMO

Despite unprecedented advances in modern medicine, no safe and effective drug is available to date for oral administration to combat drug-induced liver injury, which is a vital concern nowadays. The present study deals with the hepatoprotective effect of pure glabridin, a key phytoconstituent from Glycyrrhiza glabra with mechanistic investigations using an in-vivo methotrexate-induced liver injury model as there is no such precedent. The study was performed in the Swiss mice model where a single dose of methotrexate (40 mg/kg) was given on the 7th day through an intraperitoneal route to induce hepatotoxicity, and glabridin as a test compound was administered orally for eleven consecutive days at 10 to 40 mg/kg. Glabridin markedly improved serum biochemical parameters (SGPT, SGOT), proinflammatory cytokine (TNF-α) level, oxidative stress markers (MDA, GSH, SOD, CAT) as compared to methotrexate alone. Alterations in methotrexate-induced liver architecture were considerably prevented by glabridin treatment as suggested by liver histopathological examination and SEM investigation. Glabridin substantially prevented methotrexate-induced down-regulation of Nrf2, & activation of NF-κB, and caused up-regulation of BAX at different dose levels. Overall, glabridin is found to protect methotrexate-induced hepatotoxicity by improving important factors for oxidative stress, inflammation, and apoptosis.


Assuntos
Apoptose , Doença Hepática Crônica Induzida por Substâncias e Drogas/tratamento farmacológico , Inflamação/terapia , Isoflavonas/farmacologia , Fígado/efeitos dos fármacos , Estresse Oxidativo , Fenóis/farmacologia , Animais , Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/patologia , Doença Hepática Crônica Induzida por Substâncias e Drogas/metabolismo , Regulação para Baixo , Glycyrrhiza , Humanos , Fígado/lesões , Fígado/metabolismo , Metotrexato , Camundongos , NF-kappa B/metabolismo , Substâncias Protetoras/farmacologia , Fator de Necrose Tumoral alfa/metabolismo
16.
Food Chem ; 361: 130102, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34029891

RESUMO

Protein glycation and formation of advanced glycation end-products (AGEs) impose threats to the human health. This study firstly investigated the inhibition of Chinese bayberry (Myrica rubra) phenolics on AGEs formation through mechanistic analysis. Four common Chinese bayberry cultivars were selected to prepare phenolic-rich extracts (CBEs) and characterized for phenolic composition, and their anti-AGE properties were evaluated in multiple in vitro systems. Total sixteen phenolics were quantified in CBEs by UPLC-ESI-MS/MS. CBEs reduced total and specific fluorescent AGEs formation in various simulating models, and protected the protein from structural modification, oxidation, and cross-linking. Mechanistic analysis unveiled that scavenging of free radicals, inactivation of transition metals, interaction with protein to form complexes, and trapping of reactive α-dicarbonyls to form adducts underlain the mechanisms of the anti-glycative actions of CBEs. Chinese bayberry fruits, especially the cultivars Biqi and Wuzi, may be a promising dietary strategy to mitigate AGEs load in the human body.


Assuntos
Produtos Finais de Glicação Avançada/metabolismo , Myrica/química , Fenóis/farmacologia , DNA Glicosilases/efeitos dos fármacos , Frutas/química , Oxirredução/efeitos dos fármacos , Fenóis/análise
17.
Free Radic Biol Med ; 171: 284-301, 2021 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-34019932

RESUMO

Polar phenols found in plant foods have been suggested to act protectively against pathogenic processes underlying Alzheimer's disease (AD), such as oxidative stress. The major risk factor for AD is apolipoprotein E4 (apoE4) and apoE4 forms can affect AD-related processes. It was shown previously that the hereditary apoE4 mutant apoE4[L28P], as well as the apoE4 fragment apoE4-165, induce neuronal oxidative stress. The effect of polar phenols on AD-related pathogenic functions of apoE4 forms is largely unexplored. The aim was to examine the effect of Corinthian currant polar phenolic extract and specific polar phenols resveratrol, quercetin, kaempferol and epigallocatechin gallate on AD-related functions of apoE4 forms. The polar phenolic extract and the individual compounds restored the viability of human neuroblastoma SK-N-SH cells in the presence of lipoprotein-associated apoE4[L28P] and prevented changes in cellular redox status. Furthermore, resveratrol, quercetin, kaempferol and epigallocatechin gallate prevented redox status changes induced by Aß42 uptake in SK-N-SH cells treated with lipid-free apoE4[L28P] or apoE4-165. Investigation of the molecular mechanism of action of these polar phenols showed that resveratrol prevented cellular Aß42 uptake via changes in cell membrane fluidity. Interestingly, kaempferol prevented cellular Aß42 uptake by apoE4[L28P], but not by apoE4-165, due to a modulating effect on apoE4[L28P] secondary structure and stability. The action of quercetin and epigallocatechin gallate could be attributed to free radical-scavenging or other protective activity. Overall, it is shown for the first time that natural compounds could modify the structure of apoE4 forms and ameliorate AD-related pathogenic effects of apoE4 forms.


Assuntos
Doença de Alzheimer , Apolipoproteína E4 , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/genética , Peptídeos beta-Amiloides , Apolipoproteína E4/genética , Humanos , Neurônios , Fenóis/farmacologia
18.
Food Chem ; 361: 130078, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34023692

RESUMO

Ora-pro-nobis (Pereskia aculeata Miller) is a non-conventional food plant common in Brazil. The objective of this study was to optimize the extraction of bioactive phenolic compounds from ora-pro-nobis leaves by employing solvent mixtures. Ten extracts were obtained with water, ethanol, acetone, and their binary and ternary mixtures, evaluating the chemical composition, antioxidant activity and bioactivities in vitro. The response surface methodology was applied to model the results and calculate the optimal solvent composition, which is 60% water, 40% ethanol and 0% acetone. The optimized extract is rich in phenolic compounds (64 mg GAE/g) and proteins (823 mg/g) and presents antioxidant activity (in intracellular media as well) and inhibits lipid peroxidation (32%) along with hypotonic hemolysis (H50 = 0.339%), it does not present toxicity in vitro against cancer and normal cells. This is the first report of chicoric, caffeoyl-hexaric and coumaroyl-hexaric acids and some glycosylate derivatives of flavonols in ora-pro-nobis leaves.


Assuntos
Antioxidantes/química , Cactaceae/química , Extratos Vegetais/química , Antioxidantes/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química
19.
Bioorg Med Chem Lett ; 43: 128079, 2021 07 01.
Artigo em Inglês | MEDLINE | ID: covidwho-1269240

RESUMO

In the current study, the interaction of SARS-CoV-2 protein (A and B chains of nsp13) with different recently synthesized phenolic compounds (Sreenivasulu et al., Synthetic Communications, 2020, 112-122) has been studied. The interactions have been investigated by using molecular docking, quantum chemical and molecular dynamics simulations methods. The molecular structures of all the ligands are studied quantum chemically in terms of their optimized structures, 3-D orbital distributions, global chemical descriptors, molecular electrostatic potential plots and HOMO-LUMO orbital energies. All the ligands show reasonably good binding affinities with nsp-13 protein. The ligand L2 shows to have better binding affinities to Chain A and Chain B of nsp13 protein, which are -6.7 and -6.4 kcal/mol. The study of intermolecular interactions indicates that L2 shows different hydrophobic and hydrogen bond interactions with both chains. Furthermore, molecular dynamic simulations of the nsp13-L2 complex are obtained over a time scale of 60 ns, which indicates its stability and flexibility behavior as assessed in terms of its RMSD and RMSF graphs. The ADMET analysis also shows no violation of Lipinski rule (RO5) by studied phenolic compounds. We believe that the current findings will be further confirmed by in vitro and in vivo studies of these recent phenolic compounds for their potential as inhibitors for SARS-Co-V-2 virus.


Assuntos
Antivirais/farmacologia , COVID-19/tratamento farmacológico , COVID-19/virologia , Fenóis/farmacologia , SARS-CoV-2/efeitos dos fármacos , Antivirais/química , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Fenóis/química , Teoria Quântica , SARS-CoV-2/isolamento & purificação , SARS-CoV-2/metabolismo
20.
J Food Sci ; 86(7): 2886-2897, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34057206

RESUMO

This study aimed to produce soluble potato starch ultrafine fibers for the encapsulation of pinhão coat extract (PCE), evaluating their relative crystallinity (RC), thermal stability, antioxidant activity, antimicrobial activity against Escherichia coli and Staphylococcus aureus, as well as in vitro biological digestion. In the simulation of in vitro biological digestion, the phenolic compounds release profile was also evaluated. The ultrafine fibers were produced by electrospinning, based on a polymeric solution composed of soluble potato starch (50% w/v) and formic acid. Then, PCE was incorporated at various concentrations (0.5%, 1.0%, and 1.5%, w/w, dry basis). The endothermic event of free PCE was not observed in the ultrafine fibers, which suggests its encapsulation. The RC decreased according to the increase in PCE concentration in the ultrafine fibers. The PCE resisted thermal treatments when encapsulated into the ultrafine fibers (100 and 180°C), and the ultrafine fibers with 1% PCE presented the highest amount of preserved phenolic compounds. Regarding antioxidant activity, the free PCE presented 85% of DPPH inhibition and the ultrafine fibers had 18% inhibition, not differing among the PCE concentrations (p < 0.05). The free PCE and the ultrafine fibers with 0.5% PCE showed inhibitory effect against S. aureus and the ones with 1.5% PCE showed controlled release of phenolic compounds during the simulation of in vitro digestion. Starch ultrafine fibers showed potential to be applied in food industries due to their capacity of protecting phenolic compounds when submitted to high temperatures or gastrointestinal conditions. Nevertheless, their application depends on the end use of the product. PRACTICAL APPLICATION: The encapsulation of pinhão coat extract (PCE) in ultrafine starch fibers promotes greater preservation of phenolic compounds. Thus, it can be incorporated into different foods that are produced using the ultra-high temperature (UHT) process-at 135-145°C for 5 to 10 s, or some other equivalent time/temperature combination. Another possibility is the incorporation of ultrafine fibers in active packaging: compounds can migrate to food, improving sensory characteristics, increasing shelf life, preventing chemical and microbiological deterioration, and ensuring food safety.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Araucaria/química , Bactérias/efeitos dos fármacos , Digestão , Material Particulado/farmacologia , Extratos Vegetais/farmacologia , Antibacterianos/química , Antioxidantes/química , Bactérias/crescimento & desenvolvimento , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Técnicas In Vitro , Material Particulado/química , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Polímeros/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento , Amido/química , Temperatura
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