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1.
Food Funct ; 15(9): 4983-4999, 2024 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-38606532

RESUMO

Propolis is a resinous mixture produced by honeybees which has been used since ancient times for its useful properties. However, its chemical composition and bioactivity may vary, depending on the geographical area of origin and the type of tree bees use for collecting pollen. In this context, this research aimed to investigate the total phenolic content (using the Folin-Ciocalteu assay) and the total antioxidant capacity (using the FRAP, DPPH, and ABTS assays) of three black poplar (Populus nigra L.) propolis (BPP) solutions (S1, S2, and S3), as well as the chemical composition (HPLC-ESI-MSn) and biological activities (effect on cell viability, genotoxic/antigenotoxic properties, and anti-inflammatory activity, and effect on ROS production) of the one which showed the highest antioxidant activity (S1). The hydroalcoholic BPP solution S1 was a prototype of an innovative, research-type product by an Italian nutraceutical manufacturer. In contrast, hydroalcoholic BPP solutions S2 and S3 were conventional products purchased from local pharmacy stores. For the three extracts, 50 phenolic compounds, encompassing phenolic acids and flavonoids, were identified. In summary, the results showed an interesting chemical profile and the remarkable antioxidant, antigenotoxic, anti-inflammatory and ROS-modulating activities of the innovative BPP extract S1, paving the way for future research. In vivo investigations will be a possible line to take, which may help corroborate the hypothesis of the potential health benefits of this product, and even stimulate further ameliorations of the new prototype.


Assuntos
Anti-Inflamatórios , Antioxidantes , Populus , Própole , Própole/química , Própole/farmacologia , Populus/química , Antioxidantes/farmacologia , Antioxidantes/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Animais , Antimutagênicos/farmacologia , Antimutagênicos/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Camundongos , Humanos , Fenóis/química , Fenóis/farmacologia , Fenóis/análise , Sobrevivência Celular/efeitos dos fármacos
2.
Chem Biodivers ; 20(9): e202300896, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37605961

RESUMO

Heterocyclic compounds are found in a variety of drug molecules, and bioactive natural products. 4-Thiazolidinones (4-TZDs), which represent an important class of heterocyclic compounds, are of great interest today with their diverse bioactivities. In this study, ten novel 4-TZD derivatives (C1-C10) were synthesized, characterized by spectroscopic techniques, and their genotoxic, and antigenotoxic properties were investigated in vitro using the Ames Salmonella/microsome mutagenicity assay in the concentration range of 0.2-1.0 mM/plate. The results revealed that none of the compounds were mutagenic on the three different Salmonella typhimurium strains up to the highest concentration tested. Furthermore, in our study, C1, C4, C6, and C9 showed significant, ranging from moderate to strong, antigenotoxic effects against mutagen-induced DNA damage at relatively higher doses. Among these, C4 had the best potential to inhibit the number of revertant colonies induced by 9-aminoacridine (9-AA), with a maximum inhibition rate of 47.9 % for 1.0 mM/plate. As a result, preliminary knowledge about the safety of the use of ten novel synthesized 4-TZD compounds likely to exhibit many bioactivities was obtained in this study. In addition, the significant in vitro antimutagenic activity of some derivatives increases the importance of studies for the development of new pharmacological agents for cancer prevention.


Assuntos
Antimutagênicos , Antimutagênicos/farmacologia , Antimutagênicos/química , Mutagênicos/toxicidade , Salmonella typhimurium , Aminacrina , Dano ao DNA
3.
Molecules ; 26(17)2021 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-34500813

RESUMO

Aromatic halophytes represent an exceptional source of natural bioactive compounds for the food industry. Crithmum maritimum L., also known as sea fennel, is a halophyte plant colonizing cliffs and coastal dunes along Mediterranean and Atlantic coasts. It is well known to produce essential oils and polyphenols endowed with antioxidant and biological effects. The present work reports the phytochemical profile, as well as antioxidant, antimicrobial and antimutagenic properties of C. maritimum leaf hydro-alcoholic extract. From LC-ESI-MS analysis, eighteen phenolic compounds were depicted in sea fennel extract and the amount of total phenolic content exceeds 3% DW. Accordingly, C. maritimum extract showed strong antioxidant activities, as evidenced by in vitro (DPPH, ORAC, FRAP) and ex vivo (CAA-RBC and hemolysis) assays. An important antimicrobial activity against pathogenic strains was found as well as a strong capacity to inhibit Staphylococcus aureus (ATCC 35556) biofilm formation. Sea fennel extracts showed a significant decrease of mutagenesis induced by hydrogen peroxide (H2O2) and menadione (ME) in Saccharomyces cerevisiae D7 strain. In conclusion, our results show that C. maritimum is an exceptional source of bioactive components and exert beneficial effects against oxidative or mutagenic mechanisms, and pathogenic bacteria, making it a potential functional food.


Assuntos
Suplementos Nutricionais , Magnoliopsida/química , Extratos Vegetais/química , Plantas Comestíveis/química , Antibacterianos/química , Antibacterianos/farmacologia , Antimutagênicos/química , Antimutagênicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Tolerantes a Sal/química , Staphylococcus aureus/efeitos dos fármacos
4.
Chem Biodivers ; 18(10): e2000936, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34432933

RESUMO

The antioxidant and mutagenic/antimutagenic activities of the fixed oils from Nigella sativa (NSO) and Nigella damascena (NDO) seeds, obtained by cold press-extraction from the cultivar samples, were comparatively investigated for the first time. The antimutagenicity test was carried out using classical and modified Ames tests. The fatty acid composition of the fixed oils was characterized by gas chromatography-mass spectrometry (GC-MS) while the quantification of thymoquinone in the fixed oils was determined by UPC2 . The main components of the NSO and NDO were found to be linoleic acid, oleic acid, and palmitic acid. The results of the Ames test confirmed the safety of NSO and NDO from the viewpoint of mutagenicity. The results of the three antioxidant test methods were correlated with each other, indicating NDO as having a superior antioxidant activity, when compared to the NSO. Both NSO and NDO exhibited a significant protective effect against the mutagenicity induced by aflatoxin B1 in Salmonella typhimurium TA98 and TA100 strains. When microsomal metabolism was terminated after metabolic activation of the mycotoxin, a significant increase in antimutagenic activity was observed, suggesting that the degradation of aflatoxin B1 epoxides by these oils may be a possible antimutagenic mechanism. It is worthy to note that this is the first study to assess the mutagenicity of NSO and NDO according to the OECD 471 guideline and to investigate antimutagenicity of NDO in comparison to NSO against aflatoxin.


Assuntos
Antimutagênicos/farmacologia , Antioxidantes/farmacologia , Nigella damascena/química , Nigella sativa/química , Óleos de Plantas/farmacologia , Substâncias Protetoras/farmacologia , Aflatoxina B1/antagonistas & inibidores , Antimutagênicos/química , Antimutagênicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/antagonistas & inibidores , Picratos/antagonistas & inibidores , Óleos de Plantas/química , Óleos de Plantas/isolamento & purificação , Substâncias Protetoras/química , Substâncias Protetoras/isolamento & purificação , Salmonella typhimurium/química
5.
Molecules ; 26(11)2021 May 29.
Artigo em Inglês | MEDLINE | ID: mdl-34072474

RESUMO

Ficus deltoidea var. deltoidea is used as traditional medicine for diabetes, inflammation, and nociception. However, the antimutagenic potential and cytoprotective effects of this plant remain unknown. In this study, the mutagenic and antimutagenic activities of F. deltoidea aqueous extract (FDD) on both Salmonella typhimurium TA 98 and TA 100 strains were assessed using Salmonella mutagenicity assay (Ames test). Then, the cytoprotective potential of FDD on menadione-induced oxidative stress was determined in a V79 mouse lung fibroblast cell line. The ferric-reducing antioxidant power (FRAP) assay was conducted to evaluate FDD antioxidant capacity. Results showed that FDD (up to 50 mg/mL) did not exhibit a mutagenic effect on either TA 98 or TA 100 strains. Notably, FDD decreased the revertant colony count induced by 2-aminoanthracene in both strains in the presence of metabolic activation (p < 0.05). Additionally, pretreatment of FDD (50 and 100 µg/mL) demonstrated remarkable protection against menadione-induced oxidative stress in V79 cells significantly by decreasing superoxide anion level (p < 0.05). FDD at all concentrations tested (12.5-100 µg/mL) exhibited antioxidant power, suggesting the cytoprotective effect of FDD could be partly attributed to its antioxidant properties. This report highlights that F. deltoidea may provide a chemopreventive effect on mutagenic and oxidative stress inducers.


Assuntos
Antimutagênicos/química , Antioxidantes/química , Ficus/metabolismo , Extratos Vegetais/química , Animais , Ânions , Linhagem Celular , Cricetulus , Diabetes Mellitus , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Glutationa , Camundongos , Mutagênese/efeitos dos fármacos , Testes de Mutagenicidade , Mutagênicos , Estresse Oxidativo , Salmonella typhimurium/efeitos dos fármacos , Sais de Tetrazólio/química , Tiazóis/química , Vitamina K 3/química , Água
6.
Molecules ; 26(5)2021 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-33652778

RESUMO

Cytogenetic analysis is essential to determine the effect of mutagens and antimutagens on genetic material. This study was done to evaluate the protective effect of root bark extract of Morus alba (M. alba) against cyclophosphamide induced somatic and germinal cell damage in male rats. The ethanolic extract of M. alba (0.25, 0.5 and 1 g/kg, 2 weeks) was evaluated against cyclophosphamide (75 mg/kg, single dose) induced nuclear damage. The sampling was done after 48 h of the clastogen treatment. The somatic and germinal nuclear damage was studied by bone marrow micronucleus and sperm analysis, respectively. Serum superoxide and catalase levels were estimated to determine the antioxidant status in each group. The results were analyzed statistically to find the significant variation. The administration of M. alba for 2 weeks suppressed dose-dependently the changes induced by cyclophosphamide. M. alba (0.5 g/kg) decreased the frequency of micronucleated erythrocyte, sperm shape abnormality and enhanced the sperm count, sperm motility and polychromatic-normochromatic erythrocytes ratio significantly (p < 0.05) in comparison with the cyclophosphamide treated group. The highest tested dose of M. alba (1 g/kg) produced more prominent suppression (p < 0.01) in the cyclophosphamide-induced somatic and germinal cell defects. The results also showed significant (p < 0.05) improvement in the serum antioxidant enzymes levels with M. alba when compared with the challenge group. The lower dose of M. alba extract (0.25 g/kg) prevented the CP-induced changes but was found to be statistically insignificant. Therefore, antimutagenic potential of the high dose of the extract of M. alba is possibly due to its antioxidant nature. The ability of the M. alba extract to prevent the nuclear damage could play an important role in overcoming several mutational defects that are associated with anticancer chemotherapy.


Assuntos
Antioxidantes/farmacologia , Morus/química , Extratos Vegetais/farmacologia , Motilidade dos Espermatozoides/efeitos dos fármacos , Animais , Antimutagênicos/química , Antimutagênicos/farmacologia , Antioxidantes/química , Ciclofosfamida/toxicidade , Etanol/química , Humanos , Masculino , Mutagênicos/toxicidade , Extratos Vegetais/química , Ratos
7.
J Biomater Appl ; 36(4): 592-604, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-33593129

RESUMO

The preferred cancer treatment is to achieve a high therapeutic effect as well as reduce side effects. In this study, we developed carrier-free nano drugs based on 5-fluorouracil (5FU) and cinnamaldehyde (CA) to meet the above goals. Two model drugs were spliced by acetal linkage and ester bond, which could self-assemble into nano drug particles (5FU-CA NPs) with a size of ∼170 nm. In vitro cell experiments showed 5FU-CA NPs were efficiently internalized by HepG2 cells. They then quickly exerted dual drug activities by the cleavage of acetal and ester bond, resulting in enhanced cell-killing efficacy and apoptosis. Synergistic mechanisms were achieved via the anti-metabolic effects mediated by 5FU-COOH and the oxidative damage induced by CA. In vivo anti-tumor evaluation further indicated that 5FU-CA NPs had higher tumor growth inhibition than 5FU-COOH/CA mixture (5FU-COOH + CA) and exhibited lower systemic toxicity under the same reducing dose of each drug. Overall, this is a successful synergistic anti-tumor attempt through rational self-assembly of drugs with different mechanisms and it can be extrapolated to other agents.


Assuntos
Antimutagênicos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos/farmacologia , Aromatizantes/farmacologia , Fluoruracila/farmacologia , Nanopartículas/química , Acroleína/análogos & derivados , Animais , Antimutagênicos/química , Antineoplásicos/química , Antineoplásicos Fitogênicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Portadores de Fármacos/farmacologia , Liberação Controlada de Fármacos , Sinergismo Farmacológico , Aromatizantes/química , Fluoruracila/química , Células Hep G2 , Humanos , Masculino , Camundongos , Camundongos Endogâmicos ICR
8.
Int J Mol Sci ; 22(2)2021 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-33435390

RESUMO

The evaluation of antioxidant compounds that counteract the mutagenic effects caused by the direct action of reactive oxygen species on DNA molecule is of considerable interest. Therefore, a series of 2,3-substituted quinazolinone derivatives (Q1-Q8) were investigated by different assays, and the relationship between their biological properties and chemical structure was examined. Genotoxicity and the potential DNA-protective effects of Q1-Q8 were evaluated by comet assay and DNA topology assay. Antioxidant activity was examined by DPPH-radical-scavenging, reducing-power, and total antioxidant status (TAS) assays. The cytotoxic effect of compounds was assessed in human renal epithelial cells (TH-1) and renal carcinoma cells (Caki-1) by MTT assay. Analysis of the structure-activity relationship disclosed significant differences in the activity depending on the substitution pattern. Derivatives Q5-Q8, bearing electron-donating moieties, were the most potent members of this series. Compounds were not genotoxic and considerably decreased the levels of DNA lesions induced by oxidants (H2O2, Fe2+ ions). Furthermore, compounds exhibited higher cytotoxicity in Caki-1 compared to that in TH-1 cells. Substantial antioxidant effect and DNA-protectivity along with the absence of genotoxicity suggested that the studied quinazolinones might represent potential model structures for the development of pharmacologically active agents.


Assuntos
Antimutagênicos/farmacologia , Antioxidantes/farmacologia , Dano ao DNA/efeitos dos fármacos , Quinazolinonas/farmacologia , Antimutagênicos/química , Antimutagênicos/toxicidade , Antioxidantes/química , Antioxidantes/toxicidade , Linhagem Celular , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , DNA/genética , Humanos , Peróxido de Hidrogênio/toxicidade , Mutagênicos/toxicidade , Oxidantes/toxicidade , Quinazolinonas/química , Quinazolinonas/toxicidade , Relação Estrutura-Atividade
9.
Anticancer Agents Med Chem ; 21(16): 2250-2257, 2021 10 28.
Artigo em Inglês | MEDLINE | ID: mdl-33397268

RESUMO

BACKGROUND: Cancer is a disease characterized by the invasion and uncontrolled growth of cells. One of the best ways to minimize the harmful effects of mutagens is through the use of natural antimutagens. In this regard, the search for new antimutagens that act in the chemoprevention could represent a promising field in this area. OBJECTIVE: In this study biological potential of 11 fractions from Coccoloba uvifera L. leaf hexane extract was evaluated by several in vitro tests. METHODS: Leaves were lyophilized and hexane extraction was performed. The extract was fractionated by column chromatography with hexane, ethyl acetate, and methanol. The antimutagenic (Ames test), antiproliferative (MTT test), and antioxidant capacity (DPPH, ABTS, and ferrous ion chelation) of the fractions were evaluated. RESULTS: Fractions 4, 6, 8, and 9 have antimutagenic activity (against sodium azide in strain TA100), fraction 11 showed antiproliferative capacity (IC50 of 24 ± 9 µg/mL in cells of HCT 116). The fractions with the highest activity were analyzed by HPLC-MS and lupeol, acacetin, and ß-sitosterol were identified. CONCLUSION: This study demonstrates, for the first time, the bioactivity of C. uvifera leaf as a new source of High Biological Value Compounds (HBVC), which can be of interest to the food and pharmaceutical industries.


Assuntos
Antimutagênicos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polygonaceae/química , Antimutagênicos/química , Antimutagênicos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Radicais Livres/antagonistas & inibidores , Humanos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Salmonella typhimurium/efeitos dos fármacos , Azida Sódica/antagonistas & inibidores , Células Tumorais Cultivadas
10.
Molecules ; 26(1)2021 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-33401767

RESUMO

Colored (orange, pink, red, purple, and blue) corn strongly attracted attention on its healthy properties mainly due to its anthocyanin and carotenoid composition which is also responsible for its pigmentation. The present review summarized the recent updates on the extraction and chemical characterization of the main plant secondary metabolites present in colored seeds, kernel, cob, husk, and silk. The main approaches used to stabilize the extracts have been discussed as well as their food and non-food uses. Both in vitro and in vivo (animal models) studies on the different effects (antibacterial, antimutagenic, antioxidant, and anti-inflammatory activities, effects on metabolic syndrome, diabetes, glucose and lipidic metabolism, and neuroprotection) of pigmented extracts on animal and human health have been summarized.


Assuntos
Extratos Vegetais/química , Zea mays/química , Zea mays/metabolismo , Animais , Antocianinas/isolamento & purificação , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Antimutagênicos/química , Antimutagênicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Fracionamento Químico/métodos , Corantes/isolamento & purificação , Produtos Agrícolas , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Pigmentação , Extratos Vegetais/farmacologia , Metabolismo Secundário , Resíduos , Zea mays/genética
11.
Artigo em Inglês | MEDLINE | ID: mdl-33198932

RESUMO

Food mutagens formed from amino acids during heating of meat have the potential to induce serious consequences on human health. As a result, the identification of naturally occurring, genoprotective agents, is of great importance. The aim of this study was to chemically characterize a root and leaf extracts of Gentiana lutea and to investigate the antigenotoxic effects of extracts and pure constituents (gentiopicroside and mangiferin). Antigenotoxic effects were shown for combinations with the food borne mutagens IQ and PhIP using hepatoma HepG2 cells. Furthermore, their antioxidant activity and their capacity to modulate Nrf2 expression and affect the glutathione redox status were tested. Chemical analyses showed that the most abundant constituents found in root extract are gentiopicroside and sweroside. On the other hand, homoorientin and isovitexin were the dominant ones in leaf extract. Strong genoprotective activities of all tested compounds against both mutagens were observed in alkaline comet assays (up to 77% of tail intensity inhibition, p < 0.001). The protection against glutathione depletion was partially due to the radical scavenging activity and up-regulation of Nrf2 expression by the substances. The results of this study strongly encourage further investigations of the antimutagenic properties of G. lutea.


Assuntos
Antimutagênicos/farmacologia , Gentiana/química , Glucosídeos Iridoides/farmacologia , Extratos Vegetais/farmacologia , Xantonas/farmacologia , Antimutagênicos/química , Sobrevivência Celular/efeitos dos fármacos , Alimentos , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Glutationa/metabolismo , Dissulfeto de Glutationa/metabolismo , Células Hep G2 , Humanos , Glucosídeos Iridoides/química , Peroxidação de Lipídeos/efeitos dos fármacos , Estrutura Molecular , Mutagênicos/metabolismo , Fator 2 Relacionado a NF-E2/genética , Extratos Vegetais/química , Xantonas/química
12.
Food Chem ; 322: 126725, 2020 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-32283373

RESUMO

The antimutagenicity of an extract from the medicinal plant Asclepias subulata (ASE) against heterocyclic aromatic amines (HAAs) commonly found in cooked meat, as well as its stability to heat treatment (HT), was evaluated. HT (180 °C/3 min) had no effect on the content in ASE of the bioactive compound corotoxigenin-3-O-glucopyranoside; conversely, calotropin significantly decreased by 72%. ASE exerted antimutagenicity against PhIP, MelQ, and MelQx in TA98 and TA100 Salmonella strains, and this activity was not affected by heat, with the exception of MelQ (p < 0.05). Since HAAs can induce colorectal cancer, the thermal stability of ASE's antiproliferative effect against colorectal cancer cells was also evaluated. HT decreased (p < 0.05) the antiproliferative activity of ASE; however, the remaining activity was still strong with an IC50 of 16.8 ± 2.03 µg/mL. Therefore, ASE can be used as a food ingredient to reduce the carcinogenic potential of thermally induced HAAs.


Assuntos
Aminas/farmacologia , Antimutagênicos/farmacologia , Asclepias/química , Carcinógenos/farmacologia , Compostos Heterocíclicos/farmacologia , Carne/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Aminas/análise , Aminas/química , Animais , Antimutagênicos/química , Carcinógenos/química , Proliferação de Células/efeitos dos fármacos , Culinária , Compostos Heterocíclicos/análise , Temperatura Alta , Humanos , Imidazóis
13.
Molecules ; 25(5)2020 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-32121158

RESUMO

Traditional medicinal plants are an important source of active compounds with potential antimutagenic activity. Polyscias filicifolia Bailey (Araliaceae) is a South Asian traditional herb used as an adaptogenic and cardiac drug. Extracts of P. filicifolia contain a wide range of biologically active compounds like phenolic acids and triterpenoid saponins. In the present study. antigenotoxic potential of three naturally occurring phenolic acids and extracts of P. filicifolia growing in vitro with the addition of elicitors was evaluated against direct (4-nitroquinoline-N-oxide (4NQO) and mitomycin C (MMC)) and indirect mutagens (2-aminoanthracene (2AA)). The evaluation was made using a bacterial umu-test. Moreover, the ability to prevent photogenotoxicity induced by chlorpromazine (CPZ) under UVA irradiation was measured. The phytochemical profiling of examined extracts revealed the presence of numerous compounds with the prevelance of chlorogenic, caffeic, and ferulic acid derivatives; however, saponin fractions were also determined. The antioxidant potential of extracts strictly correlated with their composition. The tested extracts exhibited high antigenotoxic activity if the assay was performed with 2AA and metabolic activation. Moreover, the extracts slightly decreased the MMC-induced genotoxicity. However, an increase of the genotoxic effect was observed in the assay performed with 4NQO. In addition, photo-antigenotoxic activity was observed. In our study, phenolic acids exhibited lower activity than the extracts.


Assuntos
Antimutagênicos/farmacologia , Antioxidantes/farmacologia , Araliaceae/química , Dano ao DNA , Extratos Vegetais/farmacologia , Brotos de Planta/química , Animais , Antimutagênicos/química , Antioxidantes/química , Clorpromazina/efeitos adversos , Clorpromazina/farmacologia , Masculino , Mitomicina/efeitos adversos , Mitomicina/farmacologia , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
14.
Molecules ; 24(23)2019 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-31795320

RESUMO

Pistachio nuts are included among the foods with the highest antioxidant capacity. Stressed cultivating conditions, such as the use of regulated deficit irrigation (RDI), are expected to create a plant response that might increase the production of secondary metabolites. Fruits that are obtained under RDI treatments are commonly called hydroSOS products. The aim of this work was to study the influence of using different rootstocks (P. atlantica, P. integerrima, and P. terebinthus) and two RDI treatments on the antioxidant (ABTS, ferric reducing antioxidant power (FRAP), and DPPH), antimutagenic (Ames test), and cytotoxicity (MTT assay in five human cell lines) activities of pistachios. P. terebinthus showed the best antioxidant activity, and the RDI treatments maintained and improved the antioxidant properties of pistachios. Neither the rootstock nor the RDI had significant impact on the antimutagenic potential of pistachios. The nut extracts had no toxic effect on non-cancerous cells and the application of RDI did not reduce their cytoprotective capacity. Furthermore, neither rootstock nor RDI treatments affected the ability of the pistachio extracts of preventing the oxidative damage by H2O2. The application of RDI strategies, in addition to allowing irrigation water saving, led to obtaining pistachios with the same or even better biofunctional characteristics as compared to fully irrigated pistachios.


Assuntos
Antimutagênicos , Antioxidantes , Citoproteção/efeitos dos fármacos , Nozes/química , Pistacia/química , Células A549 , Antimutagênicos/química , Antimutagênicos/isolamento & purificação , Antimutagênicos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Humanos , Peróxido de Hidrogênio/farmacologia
15.
J Toxicol Environ Health A ; 82(17): 956-968, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31570063

RESUMO

Myrciaria dubia is a native plant from the Amazon region which produces red-purplish fruit rich in antioxidant compounds such as ascorbic acid, carotenoids, and phenolic. M. dubia fruit is used to prepare juices considered to possess high nutritional content providing health benefits. The aim of this study was to examine the ability of M. dubia juice to protect DNA against genomic instability induced by sub-acute ethanol consumption attributed to oxidative stress. Mice were treated for 28 days with juice at 25% and 50% diluted in distilled water or with the diluted combination juice plus ethanol (5 g/kg). The genotoxic/antigenotoxic and mutagenic/antimutagenic effects were assessed using comet assay in blood, liver, and kidney and micronucleus (MN) test with bone marrow. In addition, the mutagenicity was also evaluated using Salmonella/microsome assay. Phytochemical compounds were determined using HPLC/PDA/MS/MS. The juice did not induce genotoxic effects in blood, kidney, and liver cells at both doses. In combination with ethanol, the juice reduced the alcohol-mediated DNA damage in all tissues analyzed. Further, the juice did not produce mutagenic effects and decreased mutagenicity induced by ethanol in the bone marrow. The anthocyanins were major compounds detected by HPLC/PDA/MS/MS, which modulated genotoxic and mutagenic effects initiated by ethanol and at least in part appeared responsible for the observed antigenotoxic and antimutagenic effects of M. dubia juice.


Assuntos
Antimutagênicos/química , Dano ao DNA/efeitos dos fármacos , Frutas/química , Mutagênicos/efeitos adversos , Myrtaceae/química , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Animais , Brasil , Masculino , Camundongos
16.
Molecules ; 24(21)2019 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-31652733

RESUMO

Purple sweet potato anthocyanins are kinds of natural anthocyanin red pigments extracted from the root or stem of purple sweet potato. They are stable and have the functions of anti-oxidation, anti-mutation, anti-tumor, liver protection, hypoglycemia, and anti-inflammation, which confer them a good application prospect. Nevertheless, there is not a comprehensive review of purple sweet potato anthocyanins so far. The extraction, structural characterization, stability, functional activity, application in the food, cosmetics, medicine, and other industries of anthocyanins from purple sweet potato, together with their biotransformation in vitro or by gut microorganism are reviewed in this paper, which provides a reference for further development and utilization of anthocyanins.


Assuntos
Antocianinas , Antimutagênicos , Antineoplásicos Fitogênicos , Antioxidantes , Ipomoea batatas/química , Animais , Antocianinas/química , Antocianinas/isolamento & purificação , Antocianinas/uso terapêutico , Antimutagênicos/química , Antimutagênicos/isolamento & purificação , Antimutagênicos/uso terapêutico , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/uso terapêutico , Biotransformação , Humanos , Fígado/metabolismo
17.
Molecules ; 24(13)2019 Jul 09.
Artigo em Inglês | MEDLINE | ID: mdl-31323993

RESUMO

Epilepsy is one of the most common neurological disorder in the world. Many antiepileptic drugs cause multiple adverse effects. Moreover, multidrug resistance is a serious problem in epilepsy treatment. In the present study we evaluated the safety profile of three (1-3) new chiral N-aminoalkyl derivatives of trans-2-aminocyclohexan-1-ol demonstrating anticonvulsant activity. Our aim was also to determine differences between the enantiomeric compounds with respect to their safety profile. The results of the study indicated that compounds 1-3 are non-cytotoxic for astrocytes, although they exhibit cytotoxic activity against human glioblastoma cells. Moreover, 1-3 did not affect the viability of HepG2 cells and did not produce adducts with glutathione. Compounds 1-3 demonstrated no mutagenic activity either in the Salmonella typhimurium or in Vibrio harveyi tests. Additionally, the compounds displayed a strong or moderate antimutagenic effect. Finally, the P-glycoprotein (P-gp) ATPase assay demonstrated that both enantiomers are potent P-gp inhibitors. To sum up, our results indicate that the newly synthesized derivatives may be considered promising candidates for further research on anticonvulsant drug discovery and development. Our study indicated the similar safety profile of the enantiomeric N-aminoalkyl derivatives of trans-2-aminocyclohexan-1-ol, although in the previous studies both enantiomers differ in their biotransformation pathways and pharmacological activity.


Assuntos
Anticonvulsivantes/química , Anticonvulsivantes/farmacologia , Cicloexanóis/química , Cicloexanóis/farmacologia , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Ativação Metabólica/efeitos dos fármacos , Anticonvulsivantes/toxicidade , Antimutagênicos/química , Antimutagênicos/farmacologia , Biotransformação/efeitos dos fármacos , Cicloexanóis/toxicidade , Relação Dose-Resposta a Droga , Humanos , Fígado/efeitos dos fármacos , Estrutura Molecular , Mutagênicos/química , Mutagênicos/farmacologia
18.
Mini Rev Med Chem ; 19(20): 1666-1680, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31161986

RESUMO

BACKGROUND: Leaves of Spinacia oleracea have been widely used as vegetarian foods. Some studies on the chemical composition of spinach have shown that it contains a high content of micronutrients (vitamins and minerals), and has an important economic value with some agronomic advantages. S. oleracea in traditional medicine is reported to cure more than one health problem. OBJECTIVE: This review focuses on the ethnopharmacological uses and pharmacological and phytochemical studies of Spinacia oleracea. METHODS: Information on S. oleracea was obtained via electronic search of scientific databases such as Scopus, PubMed, Google Scholar, Scirus, Science Direct, Scielo, Web of Science, Medline, Springerlink, BioMed Central (BMC), and SciFinder for publications on this plant. In addition, books on medicinal herbs were also consulted. RESULTS: Approximately 100 chemical compounds were isolated and characterized from S. oleracea. The major active components of the plant are flavones, flavanols, methylenedioxyflavonol glucuronides, glucuronides, and carotenoids, which were extensively investigated. This review revealed potential pharmacological properties of these isolated compounds such as anti-obesity, anti-α-amylase, bileacid binding capacity, anti-mutagenic, anti-oxidant, anticancer, anti-inflammatory, cognitive and mood effect, hypoglycemic, and anti-hypertriglyceridemia. CONCLUSION: S. oleracea is an important edible plant also used for ethnomedical therapy of obesity, inflammation of lungs, lumbago, flatulence, and treatment of urinary calculi. Pharmacological and phytochemical studies of this plant including bioactives, which have been adequately studied, support its uses in traditional medicine. Additionally, prospects and future trends of this plant are proposed.


Assuntos
Antimutagênicos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Neoplasias/tratamento farmacológico , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Spinacia oleracea/química , Animais , Antimutagênicos/química , Antimutagênicos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Alimento Funcional/análise , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
19.
Molecules ; 24(6)2019 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-30917556

RESUMO

Polyphenols are one of the largest and most widespread groups of secondary metabolites in the plants world. These compounds are of particular interest due to their occurrence and the properties they possess. The main sources of phenolic compounds are fruits and vegetables, but lately, more and more studies refer to woody vascular plants, especially to bark, as an important source of phenolic compounds with a potential biological effect. This study aims to bring together information on the phenolic compounds present in the bark of woody vascular plants by discussing extraction methods, the chemical composition of the extracts and potential biological effects. The literature data used in this paper were collected via PubMed (2004⁻2019). Search terms were: bark, rhytidome, woody vascular plant, polyphenols, phenolic compounds, biologic activity, antioxidant, immunostimulatory, antimutagenic, antibacterial, anti-inflammatory, and antitumoral. This paper intends to highlight the fact that the polyphenolic extracts obtained from the bark of woody vascular plants represent sources of bioactive compounds with antioxidant, immunostimulatory, antimutagenic, antibacterial properties, etc. Future research directions should be directed towards identification and isolation of bioactive compounds. Consequently, biologically active compounds obtained from the bark of woody plants could be exploited on an industrial scale.


Assuntos
Polifenóis/farmacologia , Traqueófitas/química , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antimutagênicos/química , Antimutagênicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Estrutura Molecular , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/química
20.
Pak J Pharm Sci ; 32(6): 2679-2686, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31969302

RESUMO

The aim of this study is to investigate for the first time in vitro antimicrobial and antimutagenic activities of Schiff bases included the azomethine group. Antimutagenic activity was evaluated by micronucleus (MN) assay. These group have been examined for antibacterial activity against pathogenic strains, Staphylococcus aureus, Escherichia coli, Salmonella typhi H, Brucella abortus, Micrococcus luteus, Bacillus cereus, Pseudomonas aeroginosa and antifungal activity against Candida albicans and Saccharomyces cerevisiae. The results of MN showed that Schiff bases ((E)-N-(4-chlorophenyl)-1-(5-nitrothiophen-2-yl)methanimine ; (E)-N-(2,4-dichlorophenyl)-1-(5-nitrothiophen-2-yl) methanimine) different concentrations decreased the toxic effects of Aflatoxin B1. Especially, high concentration (20µM) of (E)-N-(4-chlorophenyl)-1-(5-nitrothiophen-2-yl)methanimine (compound 1) has strong antimutagenic activity. In our in vitro test systems, it was observed that Schiff bases had antimutagenic effects on human lymphocytes. On the other hand these compounds were also found to possess antimicrobial activity against some test bacteria and yeast. The antimicrobial test results of these Schiff bases included the azomethine group exhibited better activity than some known antibiotics. In particular, Compound 1 were more potent bactericides than all of the substances synthesized. In conclusion, this Schiff bases included the azomethine group can be use pharmacy industries as recognized with their noncytotoxic, antimicrobial and antimutagenic features.


Assuntos
Anti-Infecciosos/síntese química , Antimutagênicos/síntese química , Bases de Schiff/síntese química , Tiofenos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antimutagênicos/química , Antimutagênicos/farmacologia , Bacillus cereus/efeitos dos fármacos , Brucella abortus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Escherichia coli/efeitos dos fármacos , Humanos , Linfócitos/efeitos dos fármacos , Micrococcus luteus/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Saccharomyces cerevisiae/efeitos dos fármacos , Salmonella typhi/efeitos dos fármacos , Bases de Schiff/química , Bases de Schiff/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Tiofenos/química , Tiofenos/farmacologia
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