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1.
Food Funct ; 15(9): 4983-4999, 2024 May 07.
Artículo en Inglés | MEDLINE | ID: mdl-38606532

RESUMEN

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.


Asunto(s)
Antiinflamatorios , Antioxidantes , Populus , Própolis , Própolis/química , Própolis/farmacología , Populus/química , Antioxidantes/farmacología , Antioxidantes/química , Antiinflamatorios/farmacología , Antiinflamatorios/química , Animales , Antimutagênicos/farmacología , Antimutagênicos/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Ratones , Humanos , Fenoles/química , Fenoles/farmacología , Fenoles/análisis , Supervivencia Celular/efectos de los fármacos
2.
Chem Biodivers ; 20(9): e202300896, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37605961

RESUMEN

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.


Asunto(s)
Antimutagênicos , Antimutagênicos/farmacología , Antimutagênicos/química , Mutágenos/toxicidad , Salmonella typhimurium , Aminacrina , Daño del ADN
3.
Molecules ; 26(17)2021 Sep 04.
Artículo en Inglés | MEDLINE | ID: mdl-34500813

RESUMEN

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.


Asunto(s)
Suplementos Dietéticos , Magnoliopsida/química , Extractos Vegetales/química , Plantas Comestibles/química , Antibacterianos/química , Antibacterianos/farmacología , Antimutagênicos/química , Antimutagênicos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Plantas Tolerantes a la Sal/química , Staphylococcus aureus/efectos de los fármacos
4.
Molecules ; 26(11)2021 May 29.
Artículo en Inglés | MEDLINE | ID: mdl-34072474

RESUMEN

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.


Asunto(s)
Antimutagênicos/química , Antioxidantes/química , Ficus/metabolismo , Extractos Vegetales/química , Animales , Aniones , Línea Celular , Cricetulus , Diabetes Mellitus , Fibroblastos/efectos de los fármacos , Fibroblastos/metabolismo , Glutatión , Ratones , Mutagénesis/efectos de los fármacos , Pruebas de Mutagenicidad , Mutágenos , Estrés Oxidativo , Salmonella typhimurium/efectos de los fármacos , Sales de Tetrazolio/química , Tiazoles/química , Vitamina K 3/química , Agua
5.
Molecules ; 26(5)2021 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-33652778

RESUMEN

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.


Asunto(s)
Antioxidantes/farmacología , Morus/química , Extractos Vegetales/farmacología , Motilidad Espermática/efectos de los fármacos , Animales , Antimutagênicos/química , Antimutagênicos/farmacología , Antioxidantes/química , Ciclofosfamida/toxicidad , Etanol/química , Humanos , Masculino , Mutágenos/toxicidad , Extractos Vegetales/química , Ratas
6.
J Biomater Appl ; 36(4): 592-604, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-33593129

RESUMEN

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.


Asunto(s)
Antimutagênicos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos/farmacología , Aromatizantes/farmacología , Fluorouracilo/farmacología , Nanopartículas/química , Acroleína/análogos & derivados , Animales , Antimutagênicos/química , Antineoplásicos/química , Antineoplásicos Fitogénicos/química , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Portadores de Fármacos/farmacología , Liberación de Fármacos , Sinergismo Farmacológico , Aromatizantes/química , Fluorouracilo/química , Células Hep G2 , Humanos , Masculino , Ratones , Ratones Endogámicos ICR
7.
Int J Mol Sci ; 22(2)2021 Jan 09.
Artículo en Inglés | MEDLINE | ID: mdl-33435390

RESUMEN

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.


Asunto(s)
Antimutagênicos/farmacología , Antioxidantes/farmacología , Daño del ADN/efectos de los fármacos , Quinazolinonas/farmacología , Antimutagênicos/química , Antimutagênicos/toxicidad , Antioxidantes/química , Antioxidantes/toxicidad , Línea Celular , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , ADN/genética , Humanos , Peróxido de Hidrógeno/toxicidad , Mutágenos/toxicidad , Oxidantes/toxicidad , Quinazolinonas/química , Quinazolinonas/toxicidad , Relación Estructura-Actividad
8.
Anticancer Agents Med Chem ; 21(16): 2250-2257, 2021 10 28.
Artículo en Inglés | MEDLINE | ID: mdl-33397268

RESUMEN

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.


Asunto(s)
Antimutagênicos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Polygonaceae/química , Antimutagênicos/química , Antimutagênicos/aislamiento & purificación , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Radicales Libres/antagonistas & inhibidores , Humanos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Salmonella typhimurium/efectos de los fármacos , Azida Sódica/antagonistas & inhibidores , Células Tumorales Cultivadas
9.
Molecules ; 26(1)2021 Jan 02.
Artículo en Inglés | MEDLINE | ID: mdl-33401767

RESUMEN

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.


Asunto(s)
Extractos Vegetales/química , Zea mays/química , Zea mays/metabolismo , Animales , Antocianinas/aislamiento & purificación , Antibacterianos/química , Antibacterianos/farmacología , Antiinflamatorios no Esteroideos/farmacología , Antimutagênicos/química , Antimutagênicos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Fraccionamiento Químico/métodos , Colorantes/aislamiento & purificación , Productos Agrícolas , Humanos , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Pigmentación , Extractos Vegetales/farmacología , Metabolismo Secundario , Residuos , Zea mays/genética
10.
Artículo en Inglés | MEDLINE | ID: mdl-33198932

RESUMEN

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.


Asunto(s)
Antimutagênicos/farmacología , Gentiana/química , Glucósidos Iridoides/farmacología , Extractos Vegetales/farmacología , Xantonas/farmacología , Antimutagênicos/química , Supervivencia Celular/efectos de los fármacos , Alimentos , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Glutatión/metabolismo , Disulfuro de Glutatión/metabolismo , Células Hep G2 , Humanos , Glucósidos Iridoides/química , Peroxidación de Lípido/efectos de los fármacos , Estructura Molecular , Mutágenos/metabolismo , Factor 2 Relacionado con NF-E2/genética , Extractos Vegetales/química , Xantonas/química
11.
Food Chem ; 322: 126725, 2020 Aug 30.
Artículo en Inglés | MEDLINE | ID: mdl-32283373

RESUMEN

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.


Asunto(s)
Aminas/farmacología , Antimutagênicos/farmacología , Asclepias/química , Carcinógenos/farmacología , Compuestos Heterocíclicos/farmacología , Carne/análisis , Extractos Vegetales/química , Extractos Vegetales/farmacología , Aminas/análisis , Aminas/química , Animales , Antimutagênicos/química , Carcinógenos/química , Proliferación Celular/efectos de los fármacos , Culinaria , Compuestos Heterocíclicos/análisis , Calor , Humanos , Imidazoles
12.
Molecules ; 24(23)2019 Nov 29.
Artículo en Inglés | MEDLINE | ID: mdl-31795320

RESUMEN

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.


Asunto(s)
Antimutagênicos , Antioxidantes , Citoprotección/efectos de los fármacos , Nueces/química , Pistacia/química , Células A549 , Antimutagênicos/química , Antimutagênicos/aislamiento & purificación , Antimutagênicos/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Humanos , Peróxido de Hidrógeno/farmacología
13.
Molecules ; 24(21)2019 Oct 23.
Artículo en Inglés | MEDLINE | ID: mdl-31652733

RESUMEN

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.


Asunto(s)
Antocianinas , Antimutagênicos , Antineoplásicos Fitogénicos , Antioxidantes , Ipomoea batatas/química , Animales , Antocianinas/química , Antocianinas/aislamiento & purificación , Antocianinas/uso terapéutico , Antimutagênicos/química , Antimutagênicos/aislamiento & purificación , Antimutagênicos/uso terapéutico , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/uso terapéutico , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/uso terapéutico , Biotransformación , Humanos , Hígado/metabolismo
14.
Molecules ; 24(13)2019 Jul 09.
Artículo en Inglés | MEDLINE | ID: mdl-31323993

RESUMEN

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.


Asunto(s)
Anticonvulsivantes/química , Anticonvulsivantes/farmacología , Ciclohexanoles/química , Ciclohexanoles/farmacología , Miembro 1 de la Subfamilia B de Casetes de Unión a ATP/metabolismo , Activación Metabólica/efectos de los fármacos , Anticonvulsivantes/toxicidad , Antimutagênicos/química , Antimutagênicos/farmacología , Biotransformación/efectos de los fármacos , Ciclohexanoles/toxicidad , Relación Dosis-Respuesta a Droga , Humanos , Hígado/efectos de los fármacos , Estructura Molecular , Mutágenos/química , Mutágenos/farmacología
15.
Mini Rev Med Chem ; 19(20): 1666-1680, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31161986

RESUMEN

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.


Asunto(s)
Antimutagênicos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Neoplasias/tratamiento farmacológico , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Spinacia oleracea/química , Animales , Antimutagênicos/química , Antimutagênicos/aislamiento & purificación , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Alimentos Funcionales/análisis , Humanos , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación
16.
Molecules ; 24(6)2019 Mar 26.
Artículo en Inglés | MEDLINE | ID: mdl-30917556

RESUMEN

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.


Asunto(s)
Polifenoles/farmacología , Tracheophyta/química , Antibacterianos/química , Antibacterianos/farmacología , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antimutagênicos/química , Antimutagênicos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Estructura Molecular , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Polifenoles/química
17.
Vopr Pitan ; 87(1): 92-97, 2018.
Artículo en Ruso | MEDLINE | ID: mdl-30592847

RESUMEN

The aim of the work was to determine the possibility of using the powder from the leaves of Hippophae rhamnoides L. for enriching flour confectionery and to evaluate the antimutagenic and antioxidant activity of the product. The experiment was carried out on 24 white Wistar rats with initial body weight (b.w.) 180-200 g. The animals of the experimental group (n=8) received confection containing sea buckthorn powder at a rate of 20 mg per 100 g b.w. for 14 days on the background of a standard vivarium diet. The animals of the control and intact groups received confection containing no bioactive supplement at the same dose. Antimutagenic and antioxidant effects were estimated in a day after a single injection of cyclophosphamide at a dose of 20 mg/kg b.w. The number of chromosomal aberrations in bone marrow cells of white rats was counted and the activity of catalase, superoxide dismutase (SOD), the level of reduced glutathione and the concentration of TBA-active products in blood were evaluated. The intake of the confectionery containing the powdered H. rhamnoides leaves resulted in the 45% decrease of the number of damaged cells, 50% decrease of the proportion of cells with multiple chromosome breaks and 52% decrease of the number of achromatic gaps as compared to animals of the control group (n=8). The cake intake increased the activity of catalase (by 52%) and SOD (by 33%) and glutathione content (by 26%) in blood.


Asunto(s)
Antimutagênicos , Dulces/análisis , Análisis de los Alimentos , Hippophae/química , Valor Nutritivo , Hojas de la Planta/química , Animales , Antimutagênicos/química , Antimutagênicos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Catalasa/sangre , Ratas , Ratas Wistar , Superóxido Dismutasa/sangre
18.
BMC Complement Altern Med ; 18(1): 93, 2018 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-29544492

RESUMEN

BACKGROUND: Sutherlandia frutescens (L.) R. Br is endemic to Southern Africa where it has been traditionally used for cancer and diabetes. In recent times it has been marketed for its reputed (but not proven) anticancer, antidiabetic and anti-HIV properties. Little is known about the mutagenic and antimutagenic potential of extracts and common marker compounds of Sutherlandia frutescens. Therefore this study aimed to investigate the putative efficacy and possible long-term adverse effects of using this herb. METHODS: Ethylacetate (EA) and 50% Methanol (MeOH) extracts were screened for mutagenic and antimutagenic activity using the Ames assay utilising TA97a, TA98, TA100 and TA102 in the presence and absence of metabolic activation. Four compounds, L-arginine, L-canavanine, GABA and D-pinitol known to occur in sutherlandia were also included. The total polyphenolic content of the both extracts was determined using the Folin-Ciocalteau method and FRAP and ABTS were used to determine the anti-oxidant potential of the extracts. RESULTS: The extracts and the standards did not show any cytotoxicity except in TA97a. The EA extract exhibited antimutagenicity against all the bacterial strains at all concentrations tested. The MeOH extract showed both pro-mutagenic and antimutagenic activities with 2-acetamidofluorene and aflatoxin B1 in the presence of metabolic activation of TA98 and TA100, respectively. All compounds, except L-canavanine exhibited antimutagenic activity against all strains. L-canavanine, on the other hand showed co-mutagenicity with 9-aminoacridine on TA97a, at all test concentrations. The extracts and pure compounds exhibited their antimutagenic activity in a dose response manner. L-arginine and GABA showed an some antimutagenic response. EA extract had three times the total phenolic content (12.56 µg GE / mg) observed in the MeOH extract. There was correlation between total phenolic content, antioxidant potential and antimutagenicity. CONCLUSION: Both extracts exhibited a protective effect, with the EA extract exhibiting greater potency. L-canavanine acted as a co-mutagen in a dose response manner without metabolic activation. It is suggested that the EA extract be priotized for future development work as it showed a better risk profile and activity.


Asunto(s)
Antimutagênicos/farmacología , Fabaceae/química , Mutágenos/farmacología , Extractos Vegetales/farmacología , África Austral , Antimutagênicos/química , Antimutagênicos/aislamiento & purificación , Mutagénesis/efectos de los fármacos , Pruebas de Mutagenicidad , Mutágenos/química , Mutágenos/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Salmonella typhimurium/efectos de los fármacos , Salmonella typhimurium/genética
19.
Chem Biodivers ; 15(4): e1800023, 2018 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-29537689

RESUMEN

European Pharmacopoeia accepts two equivalent species Solidago canadensis L. and S. gigantea Aiton as goldenrod (Solidaginis herba). We compared phytochemical profile of both species from invasive populations in Poland. Further, we compared in vitro antimutagenic and antioxidant activities of solvent extracts from aerial (AP) and underground parts (UP). In S. gigantea, flavonoid profile was dominated by quercetin glycosides, with quercitrin as the major compound. In S. canadensis, quercetin and kaempferol rutinosides were two major constituents. Caffeoylquinic acids (CQAs) were less diverse with 5-CQA as a main compound. In UP, over 20 putative diterpenoids were detected, mostly unidentified. Several CQAs were present in higher amounts than in AP. Antioxidant and antimutagenic activities were different between species and organs, with the strongest inhibition of lipid peroxidation by Et2 O and AcOEt fractions from AP of both species (IC50 13.33 - 16.89 µg/mL) and BuOH fraction from S. gigantea UP (IC50  = 13.32 µg/mL). Chemical mutagenesis was completely inhibited by non-polar fractions, but oxidative mutagenesis was inhibited up to 35% only by S. canadensis. No clear relationship was found between chemical profiles and antimutagenic activity. In conclusion, both species have diverse activity and their phytochemical profiles should be considered in quality evaluation. UP of these weeds can also provide potential chemopreventive substances for further studies.


Asunto(s)
Antimutagênicos/farmacología , Antioxidantes/farmacología , Mutagénesis/efectos de los fármacos , Extractos Vegetales/farmacología , Solidago/química , Antimutagênicos/química , Antimutagênicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Compuestos de Bifenilo/antagonistas & inhibidores , Relación Dosis-Respuesta a Droga , Quempferoles/química , Quempferoles/aislamiento & purificación , Quempferoles/farmacología , Peroxidación de Lípido/efectos de los fármacos , Picratos/antagonistas & inhibidores , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Quercetina/química , Quercetina/aislamiento & purificación , Quercetina/farmacología , Ácido Quínico/análogos & derivados , Ácido Quínico/química , Ácido Quínico/aislamiento & purificación , Ácido Quínico/farmacología , Especificidad de la Especie , Relación Estructura-Actividad
20.
Environ Sci Pollut Res Int ; 25(11): 10829-10836, 2018 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-29397502

RESUMEN

Todays, bioactive compounds extracted from Spirulina platensis have been intensively studied for their therapeutical values. Therefore, in the present study, we aimed to evaluate the effects of S. platensis extract on DNA damage and chromosomal aberrations induced by cadmium in rats. Four groups of male albino rats (n = 7 rats) were used. The first group served as a control group and received distilled water. The second group was exposed intraperitoneally to cadmium chloride (CdCl2) (3.5 mg/kg body weight dissolved in 2 ml distilled water). The third group included the rats that were orally treated with S. platensis extract (1 g/kg dissolved in 5 ml distilled water, every other day for 30 days). The fourth group included the rats that were intraperitoneally and orally exposed to cadmium chloride and S. platensis, respectively. The experiment in all groups was extended for 60 days. The results of cadmium-mediated toxicity revealed significant genetic effects (DNA fragmentation, deletion or disappearance of some base pairs of DNA, and appearance of few base pairs according to ISSR-PCR analysis). Moreover, chromosomes showed structural aberrations such as reduction of chromosomal number, chromosomal ring, chromatid deletions, chromosomal fragmentations, and dicentric chromosomes. Surprisingly, S. platensis extract plus CdCl2-treated group showed less genetic effects compared with CdCl2 alone. Further, S. platensis extract upon CdCl2 toxicity was associated with less chromosomal aberration number and nearly normal appearance of DNA fragments as indicated by the bone marrow and ISSR-PCR analysis, respectively. In conclusion, the present novel study showed that co-treatment with S. platensis extract could reduce the genotoxic effects of CdCl2 in rats.


Asunto(s)
Antimutagênicos/farmacología , Cloruro de Cadmio/toxicidad , Aberraciones Cromosómicas/efectos de los fármacos , Daño del ADN/efectos de los fármacos , Mutágenos/toxicidad , Spirulina/química , Animales , Antimutagênicos/química , Masculino , Ratas
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