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1.
Anticancer Res ; 39(8): 4043-4053, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31366486

RESUMO

BACKGROUND/AIM: Triple-negative breast cancer (TNBC) is the most aggressive subtype, predominant in African American women. In this study, the antioxidant/anticancer activity of muscadine grape extracts and the role of their phenolic and flavonoid contents in exerting these properties were investigated in TNBC cells. MATERIALS AND METHODS: Berry extracts from muscadine genotypes were investigated for total phenolic content (TPC), total flavonoid content (TFC), antioxidant capacity, and anticancer effects using breast cancer cell lines, representing Caucasians and African Americans. RESULTS: The antioxidant activity was associated with high TPC content. Extracts showed cytotoxicity up to 78.6% in Caucasians and 90.7% in African American cells, with an association with high antioxidant capacity. There was a strong correlation between TPC and anticancer/antioxidant activities. CONCLUSION: The anticancer and antioxidant effects of muscadine grapes are attributed to the TPC of extracts, which showed a stronger positive correlation with growth inhibition of African American breast cancer cells compared to Caucasians.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Extratos Vegetais/farmacologia , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Vitis/química , Afro-Americanos/genética , Antineoplásicos Fitogênicos/química , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão , Feminino , Flavonoides/química , Flavonoides/farmacologia , Frutas/química , Humanos , Células MCF-7 , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Neoplasias de Mama Triplo Negativas/genética , Neoplasias de Mama Triplo Negativas/patologia
2.
Sheng Li Xue Bao ; 71(4): 575-580, 2019 Aug 25.
Artigo em Chinês | MEDLINE | ID: mdl-31440754

RESUMO

The aim of the present study was to investigate the effect of salidroside (Sal) on inflammatory activation induced by lipopolysaccharide (LPS) in the co-culture of rat alveolar macrophages (AM) NR 8383 and type II alveolar epithelial cells (AEC II) RLE-6TN. CCK-8 colorimetric method was used to detect cell proliferation percentage. The enzyme-linked immunosorbent assay (ELISA) was used to determine the content of tumor necrosis factor alpha (TNF-α), macrophage inflammatory protein-2 (MIP-2) and interleukin-10 (IL-10) in the supernatant. Western blot was used to examine the expression levels of phosphorylated AKT (p-AKT) and total AKT protein. The results showed that pretreatment of RLE-6TN cells or co-culture of RLE-6TN and NR 8383 cells with 32 and 128 µg/mL Sal for 1 h, followed by continuous culture for 24 h, significantly increased the cell proliferation (P < 0.05). Compared with control group, 32 and 128 µg/mL Sal pretreatment significantly increased the ratio of p-AKT/AKT in RLE-6TN cells (P < 0.05). Pretreatment of 32 µg/mL Sal not only inhibited the secretion of TNF-α and MIP-2 by NR 8383 cells induced by LPS (P < 0.05), but also enhanced the inhibitory effect of RLE-6TN and NR 8383 cells co-culture on the secretion of TNF-α and MIP-2 by NR 8383 cells induced by LPS (P < 0.05). In addition, 32 µg/mL Sal pretreatment promoted LPS-induced IL-10 secretion by NR 8383 cells (P < 0.05), and enhanced the promoting effect of co-culture of RLE-6TN and NR 8383 cells on the IL-10 secretion by LPS-induced NR 8383 cells (P < 0.05). In conclusion, Sal may directly inhibit LPS-induced inflammatory activation of AM (NR 8383), promote the proliferation of AEC II (RLE-6TN) through PI3K/AKT signaling pathway, and enhance the regulatory effect of AEC II on LPS-induced inflammatory activation of AM.


Assuntos
Células Epiteliais Alveolares/efeitos dos fármacos , Glucosídeos/farmacologia , Macrófagos Alveolares/efeitos dos fármacos , Fenóis/farmacologia , Transdução de Sinais , Células Epiteliais Alveolares/metabolismo , Animais , Linhagem Celular , Quimiocina CXCL2/metabolismo , Técnicas de Cocultura , Interleucina-10/metabolismo , Lipopolissacarídeos , Macrófagos Alveolares/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos , Fator de Necrose Tumoral alfa/metabolismo
3.
Bol. latinoam. Caribe plantas med. aromát ; 18(4): 347-358, jul. 2019. ilus
Artigo em Inglês | LILACS | ID: biblio-1008172

RESUMO

Manilkara zapota (Sapotaceae), commonly known as Sapodilla, is widely known for its delicious fruit. Various parts of this plant are also used in folk medicine to treat a number of conditions including fever, pain, diarrhoea, dysentery, haemorrhage and ulcers. Scientific studies have demonstrated analgesic, anti-inflammatory, antioxidant, cytotoxic, antimicrobial, antidiarrheal, anti-hypercholesteremic, antihyperglycemic and hepatoprotective activities in several parts of the plant. Phytochemical studies have revealed the presence of phenolic compounds including protocatechuic acid quercitrin, myricitrin, catechin, gallic acid, vanillic acid, caffeic acid, syringic acid, coumaric acid, ferulic acid, etc. as main constituents of the plant. Several fatty acids, carotenoids, triterpenes, sterols, hydrocarbons and phenylethanoid compounds have also been isolated from M. zapota. The present review is a comprehensive description focused on pharmacological activities and phytochemical constituents of M. zapota.


Manilkara zapota (Sapotaceae), comúnmente conocida como Sapodilla, es ampliamente conocida por su delicioso fruto. Variadas partes de esta planta se usan en medicina popular para tratar una serie de afecciones, como fiebre, dolor, diarrea, disentería, hemorragia y úlceras. Estudios científicos han demostrado actividad analgésica, antiinflamatoria, antioxidante, citotóxica, antimicrobiana, antidiarreica, antihipercolesterolémica, antihiperglucémica y hepatoprotectora en diferentes partes de la planta. Los estudios fitoquímicos han revelado la presencia de compuestos fenólicos que incluyen ácido protocatechúico, quercitrina, miricitrina, catequina, ácido galico, ácido vanílico, ácido cafeico, ácido sirínico, ácido cumárico, ácido fúnico y ácido ferúlico como componentes principales de la planta. Varios ácidos grasos, carotenoides, triterpenos, esteroles, hidrocarburos y compuestos feniletanoides también han sido aislados de M. zapota. La presente revisión es una descripción exhaustiva centrada en las actividades farmacológicas y los constituyentes fitoquímicos de M. zapota.


Assuntos
Extratos Vegetais/farmacologia , Manilkara/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Saponinas/isolamento & purificação , Saponinas/farmacologia , Esteróis/isolamento & purificação , Esteróis/farmacologia , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Carotenoides/isolamento & purificação , Carotenoides/farmacologia , Sapotaceae/química , Compostos Fenólicos/análise , Medicina Tradicional
4.
Plant Foods Hum Nutr ; 74(3): 430-435, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31302831

RESUMO

The beneficial health effects of apple consumption are well known, however, little is known about the potential of its phenolic fractions to inhibit α-glucosidases and thereafter to treat diseases related to the carbohydrate metabolism, such as postprandial hyperglycemia and diabetes. In the present study, the α-glucosidase inhibition and antioxidant activity of different phenolic fractions of apple were evaluated using the 2,2-diphenyl-1-picrylhydrazyl and hydroxyl radical scavenging activity. Moreover, the phenolic fractions were chemically characterized by LC-MS in order to identify the compounds responsible for the biological properties. The purified extract (not fractionated) had the highest α-glucosidase and hydroxyl radical inhibitions. The purified extract and fractions III and IV were more active against the enzyme activity than the positive control acarbose, the drug used by diabetic patients to treat postprandial hyperglycaemia. Our results show that apple phenolic extracts strongly inhibit α-glucosidase acitivity, validating their potential to be used in the management of type 2 diabetes.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases/farmacologia , Hiperglicemia/tratamento farmacológico , Malus/química , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Metabolismo dos Carboidratos , Fenóis/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/isolamento & purificação , alfa-Glucosidases/metabolismo
5.
Ceska Slov Farm ; 68(2): 48-68, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31331175

RESUMO

This review deals with cytotoxic and antiproliferative activity of fifty seven prenylated phenols isolated from Morus alba. Prenyl side chain, which can be variously modified, increases lipophilicity of the substances, thereby improving their penetration through biological membranes and thus results in an increased bioavailability. The objective was to describe the relationship between structure of the prenylated phenols and their cytotoxic effect and to clarify various mechanisms by which cytotoxic prenylated phenols induce apoptosis. The conclusions showed that the cytotoxicity of the substances increases with increasing number of the prenyl side chains and ketal groups. Conversely, modification of the prenyl side chain, such as hydroxylation, reduces cytotoxicity. The cytotoxic activity is also influenced by the presence of prenyl and hydroxyl groups at specific positions.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Citotoxinas/farmacologia , Morus/química , Fenóis/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Citotoxinas/isolamento & purificação , Estrutura Molecular , Fenóis/isolamento & purificação , Prenilação
6.
J Agric Food Chem ; 67(31): 8573-8580, 2019 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-31293156

RESUMO

Glycosylation endows both natural and synthetic small molecules with modulated physicochemical and biological properties. Plant and bacterial glycosyltransferases capable of decorating various privileged scaffolds have been extensively studied, but those from kingdom Fungi still remain underexploited. Here, we use a combination of genome mining and heterologous expression techniques to identify four novel glycosyltransferase-methyltransferase (GT-MT) functional modules from Hypocreales fungi. These GT-MT modules display decent substrate promiscuity and regiospecificity, methylglucosylating a panel of natural products such as flavonoids, stilbenoids, anthraquinones, and benzenediol lactones. Native GT-MT modules can be split up and regrouped into hybrid modules with similar or even improved efficacy as compared with native pairs. Methylglucosylation of kaempferol considerably improves its insecticidal activity against the larvae of oriental armyworm Mythimna separata (Walker). Our work provides a set of efficient biocatalysts for the combinatorial biosynthesis of small molecule glycosides that may have significant importance to the pharmaceutical, agricultural, and food industries.


Assuntos
Proteínas Fúngicas/química , Glicosiltransferases/química , Hypocreales/enzimologia , Metiltransferases/química , Fenóis/química , Animais , Biocatálise , Cristalografia por Raios X , Proteínas Fúngicas/genética , Proteínas Fúngicas/metabolismo , Glicosilação , Glicosiltransferases/genética , Glicosiltransferases/metabolismo , Hypocreales/genética , Inseticidas/química , Inseticidas/farmacologia , Metilação , Metiltransferases/genética , Metiltransferases/metabolismo , Mariposas/efeitos dos fármacos , Fenóis/farmacologia , Especificidade por Substrato
7.
J Sci Food Agric ; 99(13): 6049-6059, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31342530

RESUMO

BACKGROUND: The scarcity of irrigation water is severely affecting global crop production. In this context, biostimulants are increasingly used as alternatives means against abiotic stress conditions. In this study, phenolic compounds composition and bioactive properties of common bean (Phaseolus vulgaris L.) plants grown under water stress conditions and biostimulants application were investigated. RESULTS: Sixteen individual phenolic compounds were detected in both pods and seeds with a notable difference in their compositional profile. A significant effect on phenolic compounds content and composition was also observed for the biostimulants tested. Regarding the antibacterial activity, pods of the second harvest and seed extracts showed significant efficacy against Bacillus cereus, especially in water-stressed plants, where all biostimulant treatments were more effective than positive controls. Moreover, all biostimulant treatments for seed extracts of water-stressed plants were more effective against Staphylococcus aureus compared with ampicillin, whereas streptomycin showed the best results. Extracts from pods of the second harvest from normally irrigated plants showed the best results against the fungi tested, except for Penicillium verrucosum var. cyclopium. Finally, no significant cytotoxic effects were detected. CONCLUSION: In conclusion, the biostimulants tested increased total phenolic compounds content compared with control treatment, especially in pods of the first harvest and seeds of water-stressed plants. Moreover, bioactive properties showed a varied response in regard to irrigation and biostimulant treatment. Therefore, biostimulants can be considered as a useful means towards increasing phenolic compounds content, and they may also affect the antimicrobial properties of pods and seeds extracts. © 2019 Society of Chemical Industry.


Assuntos
Desidratação , Phaseolus/química , Phaseolus/fisiologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Água/metabolismo , Bacillus cereus/efeitos dos fármacos , Bacillus cereus/crescimento & desenvolvimento , Phaseolus/crescimento & desenvolvimento , Phaseolus/microbiologia , Fenóis/química , Fenóis/metabolismo , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Sementes/química , Sementes/crescimento & desenvolvimento , Sementes/metabolismo , Sementes/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento , Estresse Fisiológico , Água/análise
8.
Fitoterapia ; 137: 104252, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31271787

RESUMO

The stems of Fissistigma polyanthoides (A.DC.) Merr. are traditionally used for the treatment of rheumatism and for recuperating women after childbirth. In our continuous phytochemical investigation of this plant, four new (1, 2, 5, and 19) and fifteen known (3, 4, and 6-18) phenolic compounds were isolated. The structures of all compounds were elucidated based on extensive spectroscopic analyses (1D-, 2D-NMR, and MS), and in comparison with reported literature data. The new natural products showed to be two poly-methoxylated chalcones (1 and 2) and two flavonoid glycosides, with 19 containing an uncommon sugar moiety (quinovose). Compounds with sufficient amount were tested for their anti-oxidant activity in a cell-based assay using the human bronchial epithelial cell line BEAS-2B. The compounds' capacity to inhibit the peroxyl radical triggered formation of dichlorofluorescein (DCF) was investigated in a dose-dependent manner. Both, anti-oxidant (3, 4, 6, 8-12, and 14) and pro-oxidative (5 and 16) properties were found for the investigated substances. The half maximal concentrations (IC50) for the inhibition of ROS formation ranged between 18.8 µM and 63.5 µM. Compounds, which acted protectively in the cellular antioxidant activity (CAA) assay and did not negatively affect cell viability, could be interesting targets for further investigations.


Assuntos
Annonaceae/química , Antioxidantes/farmacologia , Células Epiteliais/efeitos dos fármacos , Fenóis/farmacologia , Antioxidantes/isolamento & purificação , Linhagem Celular , Chalconas/isolamento & purificação , Chalconas/farmacologia , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Humanos , Estrutura Molecular , Fenóis/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Caules de Planta/química , Espécies Reativas de Oxigênio/metabolismo , Vietnã
9.
Ceska Gynekol ; 84(2): 161-165, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31238688

RESUMO

OBJECTIVE: Bisphenols are one of the most widespread endocrine disruptors that the population of west world countries is exposed to. Objective of this study is to summarize information about influence of bisphenols on reproduction health. DESIGN: Review article, Setting: Department of Obstetrics and Gynecology, Faculty of Medicine, Masaryk University and University Hospital Brno. METHODS: PubMed was searched for articles in English indexed bisphenol and reproduction up to October 2018. RESULTS: Increased levels of bisphenol A and S have been proven in body fluids and tissues. Bisphenol molecules have effect similar to estrogens therefore they influence hormonal regulation and activity of estrogen receptors. Their negative influence on oocyte maturation, spermatogenesis and development of reproductive system has been shown. Bisphenol S, which has replaced bisphenol A, has comparable negative effects on reproduction. CONCLUSION: Bisphenols are widespread endocrine disruptors that could cause severe fertility disorders of men and women.


Assuntos
Compostos Benzidrílicos/farmacologia , Disruptores Endócrinos/farmacologia , Estrogênios não Esteroides/farmacologia , Oócitos/efeitos dos fármacos , Fenóis/farmacologia , Reprodução/efeitos dos fármacos , Espermatogênese/efeitos dos fármacos , Feminino , Humanos , Masculino , Gravidez
10.
Phytochemistry ; 165: 112049, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31229788

RESUMO

Five undescribed phenolic compounds, inclusing a depsidone derivative, hyperwightin A, a flavone derivative, hyperwightin B, and three benzophenone glycosides, hyperwightins C-E, along with four known ones were isolated from the 95% EtOH extract of the whole plants of Hypericum wightianum. Structures of the obtained compounds were elucidated by spectroscopic analyses. The protective effects of the isolates against corticosterone-induced PC12 cell injury were assessed. Hyperwightin E, petiolin G and hyperxanthone exhibited noticeable neuroprotection at 10 µM.


Assuntos
Hypericum/química , Neuroproteção/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Fenóis/farmacologia , Compostos Fitoquímicos/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Corticosterona/antagonistas & inibidores , Corticosterona/farmacologia , Estrutura Molecular , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Células PC12 , Fenóis/química , Fenóis/isolamento & purificação , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Ratos
11.
BMC Complement Altern Med ; 19(1): 111, 2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31146723

RESUMO

BACKGROUND: Atherosclerosis is a condition with the vascular accumulation of lipid plaques, and its main major contributing factor is endothelial injury induced by oxidized low-density lipoprotein (ox-LDL). Salidroside (SAL) is the primary active ingredient of Rhodiola rosea, and exhibits antioxidant properties on endothelial cells and alleviates atherosclerosis. However, the effect of SAL on autophagy in ox-LDL-induced vascular endothelial injury remains unclear. Here, we investigated the effect and underlying mechanisms of SAL on autophagy in human umbilical vein endothelial cells (HUVECs). METHODS: HUVECs were incubated with ox-LDL to induce in vitro atherosclerosis model. The cell viability and injury were evaluated by cell counting kit-8 (CCK-8) assay and lactate dehydrogenase (LDH) release assay. The oxidative stress was evaluated by NADPH oxidase, malondialdehyde (MDA) and superoxide dismutase (SOD) activities. Immunofluorescence was performed to detect autophagy using LC3ß antibody. Quantitative real-time PCR (qRT-PCR) and western blot were performed to measure the mRNA expressions of SIRT1 and Forkhead box O1 (FOXO1). Nicotinamide (NAM) and AS1842856 were used to inhibit activities of SIRT1 and FOXO1, respectively. RESULTS: Exposure of HUVECs to ox-LDL (100 µg/mL) reduced cell viability, increased cellular MDA, and reduced SOD in a concentration-dependent manner. The pretreatment with SAL (20, 50 and 100 µM) significantly enhanced the cell viability and decreased LDH release in HUVECs exposed to ox-LDL (100 µg/mL). ox-LDL induced autophagy in HUVECs, which was further enhanced by pretreatment with SAL. However, SAL attenuated increase in oxidative stress in HUVECs induced by ox-LDL. ox-LDL reduced mRNA and protein expressions of SIRT1 and FOXO1, which could be reversed by SAL. The protective, anti-oxidative and pro-autophagic effects of SAL could be obviously abolished by cotreatment with SIRT1 inhibitor or FOXO1 inhibitor. CONCLUSION: Salidroside shows protective effect on endothelial cell induced by ox-LDL, and the mechanisms might be related to autophagy induction via increasing SIRT1 and FoxO1 expressions.


Assuntos
Autofagia/efeitos dos fármacos , Células Endoteliais/efeitos dos fármacos , Glucosídeos/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Rhodiola , Aterosclerose/prevenção & controle , Avaliação Pré-Clínica de Medicamentos , Células Endoteliais/metabolismo , Proteína Forkhead Box O1/metabolismo , Glucosídeos/uso terapêutico , Células Endoteliais da Veia Umbilical Humana , Humanos , Lipoproteínas LDL , Estresse Oxidativo/efeitos dos fármacos , Fenóis/uso terapêutico , Fitoterapia , Extratos Vegetais/uso terapêutico , Sirtuína 1/metabolismo
12.
BMC Complement Altern Med ; 19(1): 149, 2019 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-31238921

RESUMO

BACKGROUND: The kidney is an essential organ required by the body to perform several important functions. Nephrotoxicity is one of the most prevailing kidney complications that result from exposure to an extrinsic or intrinsic toxicant, which increase the need for the acquisition of proper remedies. Recently, natural remedies are gaining great attention owed to the fact that they have fewer side effects than most conventional drugs. METHODS: The current study recorded a new therapeutic role of the well-known medicinal plants for kidney stones [Ammi visnaga (AVE), Petroselinum crispum (PCE), Hordeum vulgare (HVE), and Cymbopogon schoenanthus (CSE)]. Hence, the aqueous extracts of these plants examined against CCl4-induced toxicity in mammalian kidney (Vero) cells. RESULTS: These extracts showed the presence of varying amounts of phenolic and triterpenoid compounds, as well as vitamin C. Owing to the antioxidant potential of these constituents, the extracts suppressed the CCl4-induced oxidative stress significantly (p < 0.05) by scavenging the reactive oxygen species and enhancing the cellular antioxidant indices. In addition, these extracts significantly (p < 0.05) reduced the CCl4-induced inflammation by inhibiting the gene expression of NF-кB, iNOS, and in turn the level of nitric oxide. Consequently, the morphological appearance of Vero cells, cellular necrosis, and the gene expression of kidney injury molecule-1 (a marker of renal injury) after these treatments were improved. The AVE improved CCl4-induced oxidative and inflammatory stress in Vero cells and showed a more potent effect than the commonly used alpha-Ketoanalogue drug (ketosteril) in most of the studied assays. CONCLUSION: Thus, the studied plant extracts, especially AVE can be considered as promising extracts in the management of nephrotoxicity and other chronic diseases associated with oxidative stress and inflammation.


Assuntos
Ammi/química , Cymbopogon/química , Hordeum/química , Rim/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Petroselinum/química , Extratos Vegetais/farmacologia , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Cercopithecus aethiops , Rim/imunologia , NF-kappa B/genética , NF-kappa B/imunologia , Óxido Nítrico/imunologia , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Sementes/química , Células Vero
13.
BMC Complement Altern Med ; 19(1): 148, 2019 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-31238930

RESUMO

BACKGROUND: Sea buckthorn (Elaeagnus rhamnoides (L.) A. Nelson, SBT) is a valuable plant because of its medical and therapeutic potential. Different bioactive compounds in SBT berries are of special interest to various researchers. However, not only sea buckthorn berries, but also leaves of this plant (both fresh and dried) contain a lot of nutrients and bioactive compounds, including phenolic compounds. The present study was carried out in order to investigate antioxidant and anticoagulant properties of sea buckthorn twig and leaf extracts (0.5-50 µg/mL) by using various in vitro models. Moreover, the aim of present experiments was to compare the biological activity of SBT leaf extract and SBT twig extract with selected berry extracts (a rich source of phenolic compounds): SBT berry extract (flavonoids being the dominant components), a commercial extract from the berries of Aronia melanocarpa (Aronox®), and a grape seed extract. METHODS: We determined the effect of plant extracts on the oxidative stress using selected markers of this process, i.e. the level of carbonyl groups in proteins. Additionally, we analysed the potential mechanism of modulation of hemostatic properties of human plasma (using selected coagulation times). RESULTS: SBT twig and leaf extracts were observed to exhibit an antioxidant activity against two strong biological oxidants: hydrogen peroxide (H2O2) and H2O2/Fe (the donor of hydroxyl radicals), which induced human plasma lipid peroxidation and protein carbonylation. Both extracts also showed anticoagulant properties. CONCLUSIONS: Our present results have demonstrated that extracts from different parts of SBT, especially berries and twigs, in comparison to well-known berries (aronia and grape), may also be viewed as a good source of active substances - antioxidants for pharmacological or cosmetic applications. Moreover, it is very important from an economic point of view to know that there is a possibility of obtaining phenolic compounds not only from the berries or leaves, but also from twigs, which constitute a production waste.


Assuntos
Elaeagnaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Caules de Planta/química , Anticoagulantes/química , Anticoagulantes/isolamento & purificação , Anticoagulantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Frutas/química , Humanos , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Photinia/química , Extratos Vegetais/isolamento & purificação , Tempo de Protrombina
14.
Fitoterapia ; 137: 104244, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31220578

RESUMO

Five new caffeoyl cyclobutantetraol esters (1-5) and one hydroxycinnamoyl cyclobutantetraol ester (6), were isolated from Scindapsus officinalis (Roxb.) Schott, which were the first reported phenolic metabolites incorporating a cyclobutantetraol in nature. Structures of the isolated compounds, including absolute configurations, were elucidated by spectroscopic analysis, especially 2D NMR techniques and exciton chirality CD (ECCD) method. All isolates were evaluated for cytotoxic activity toward MCF-7 human breast cancer cell, anti-inflammatory activity against nitric oxide (NO) production, and their antioxidative activity in the 1,1-diphenyl-2-picrylhydrazyl assay in vitro. Compound 1 showed strong antioxidative activity with IC50 value of 59.2 µM, and compounds 1-6 exhibited weak inhibitory effects on NO production, while hardly showing any cytotoxic effects against MCF-7 cell.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Araceae/química , Ésteres/farmacologia , Fenóis/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Ésteres/isolamento & purificação , Humanos , Células MCF-7 , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Fenóis/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Células RAW 264.7
15.
J Food Sci ; 84(7): 1764-1775, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31218702

RESUMO

Orostachys japonicus has traditionally been used as a food product and a fork medicine in Asia to treat various diseases. Angiogenesis is a critical process that contributes to various chronic diseases via excessive delivery of oxygen and nutrients. Common anti-angiogenic drugs have serious problems related to high costs and side effects; thus, natural products with low costs and no cytotoxicity have garnered increasing interest. In this study, we evaluated and compared the anti-angiogenic effects and phenolic compound contents between wild (WOEs) and cultivated O. japonicus extracts (COEs) prepared under various extract conditions. WOEs and COEs suppressed cell proliferation of human umbilical vein endothelial cells (HUVECs) and inhibited vascular endothelial growth factor-induced chemotactic migration, invasion, and capillary-like tube formation in HUVECs. Among COEs, that prepared by 70% EtOH (70% CE) showed the most effective anti-angiogenic activity in HUVECs. When compared to WOEs, total polyphenol and total flavonoid contents were 1.28 to 4.38 times higher in COEs, and 70% CE contained the greatest flavonoid contents (28.28 ± 0.93 mg%), as well as the highest levels of major phenolic compounds including gallic acid (21.84 µg/mL), epicatechin-gallate (6.58 µg/mL), kaempferol (6.32 µg/mL), and quercetin (8.55 µg/mL). Although further studies are required to identify the molecular mechanisms behind these anti-angiogenic effects, 70% CE could be used as an herbal medicine, functional food ingredient, and potent angiogenesis inhibitor. PRACTICAL APPLICATION: Environmental factors such as altitude, nutrients, exposure to sunlight, and temperature can influence the type and quantity of bioactive components in plants. The advantage of cultivated plants is that the above-mentioned factors can be artificially adjusted compared to wild plants. Based on economic efficiency, productivity, and consistent quality, anti-angiogenesis activity of cultivated O. japonicus is of greater commercial value as a functional food than wild O. japonicus.


Assuntos
Inibidores da Angiogênese/farmacologia , Crassulaceae/química , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Inibidores da Angiogênese/química , Animais , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Crassulaceae/crescimento & desenvolvimento , Flavonoides/química , Flavonoides/farmacologia , Ácido Gálico/química , Ácido Gálico/farmacologia , Células Endoteliais da Veia Umbilical Humana/citologia , Células Endoteliais da Veia Umbilical Humana/metabolismo , Humanos , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Plantas Medicinais/crescimento & desenvolvimento , Fator A de Crescimento do Endotélio Vascular/metabolismo
16.
J Enzyme Inhib Med Chem ; 34(1): 1100-1109, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31124384

RESUMO

Inhibition of Leishmania arginase leads to a decrease in parasite growth and infectivity and thus represents an attractive therapeutic strategy. We evaluated the inhibitory potential of selected naturally occurring phenolic substances on Leishmania infantum arginase (ARGLi) and investigated their antileishmanial activity in vivo. ARGLi exhibited a Vmax of 0.28 ± 0.016 mM/min and a Km of 5.1 ± 1.1 mM for L-arginine. The phenylpropanoids rosmarinic acid and caffeic acid (100 µM) showed percentages of inhibition of 71.48 ± 0.85% and 56.98 ± 5.51%, respectively. Moreover, rosmarinic acid and caffeic acid displayed the greatest effects against L. infantum with IC50 values of 57.3 ± 2.65 and 60.8 ± 11 µM for promastigotes, and 7.9 ± 1.7 and 21.9 ± 5.0 µM for intracellular amastigotes, respectively. Only caffeic acid significantly increased nitric oxide production by infected macrophages. Altogether, our results broaden the current spectrum of known arginase inhibitors and revealed promising drug candidates for the therapy of visceral leishmaniasis.


Assuntos
Antiprotozoários/farmacologia , Arginase/antagonistas & inibidores , Inibidores Enzimáticos/farmacologia , Leishmania infantum/efeitos dos fármacos , Fenóis/farmacologia , Animais , Antiprotozoários/química , Arginase/metabolismo , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Leishmania infantum/enzimologia , Leishmania infantum/crescimento & desenvolvimento , Macrófagos/efeitos dos fármacos , Macrófagos/parasitologia , Camundongos , Camundongos Endogâmicos BALB C , Modelos Moleculares , Estrutura Molecular , Testes de Sensibilidade Parasitária , Fenóis/química , Células RAW 264.7 , Relação Estrutura-Atividade
17.
Food Chem ; 292: 304-313, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31054679

RESUMO

Rice and legumes have great potential in the development of novel gluten-free snacks that are healthier than traditional snacks. Novel gluten-free extruded foods (composed of rice: 50-80%, beans: 20-40% and carob: 5-10%) were analysed and the extrusion effects regarding organic acids, tocopherols, phenolic compounds and bioactive properties were evaluated. The total concentration of organic acids was not significantly affected by extrusion, while tocopherols showed a significant reduction. Extrusion did not produce an increase of the total phenolic content. For the bioactivity assays, commercial extruded rice, carob and most of the extruded samples showed anti-proliferative activity, which was higher than in the non-extruded samples, while for the anti-inflammatory activity, the extrusion process did not show a significant effect. Regarding the antimicrobial activity, low potential was observed with extruded and non-extruded samples showing high values of MIC and MBC as the microorganisms tested were multi-resistant isolated clinical strains.


Assuntos
Fabaceae/química , Oryza/química , Fenóis/análise , Tocoferóis/análise , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Dieta Livre de Glúten , Fabaceae/metabolismo , Farinha/análise , Frutas/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Óxido Nítrico/metabolismo , Oryza/metabolismo , Fenóis/farmacologia , Células RAW 264.7 , Espectrometria de Massas por Ionização por Electrospray , Tocoferóis/farmacologia
18.
J Agric Food Chem ; 67(22): 6241-6247, 2019 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-31117508

RESUMO

A question in cell culture and dietary studies on protection by flavonoids against conditions such as hepatocyte steatosis is whether effects might be due to phenolic breakdown/digestion products. In HepG2 hepatocytes, treatment with quercetin, cyanidin, or their phenolic breakdown/digestion products (protocatechuic acid, 2,4,6-trihydroxybenzaldehyde, and caffeic acid), starting 2 h prior to oleic acid for 24 h, protected similarly against increases in intracellular lipid and reactive oxygen species and decreased mitochondrial membrane potential. Cyanidin or the phenolic products also protected against decreased mitochondrial content. After preincubation for only 1 h (to limit spontaneous degradation) and removal prior to oleic acid, only the phenolic products protected against decreased mitochondrial content, and without adding oleic acid, only protocatechuic acid and caffeic acid, and less so cyanidin, induced mitochondrial content. The results suggest that phenolic breakdown/digestion products of cyanidin and quercetin contribute to the protective effects in vitro, and perhaps in vivo.


Assuntos
Antocianinas/farmacologia , Fígado Gorduroso/tratamento farmacológico , Mitocôndrias/efeitos dos fármacos , Fenóis/metabolismo , Quercetina/farmacologia , Antocianinas/química , Antocianinas/metabolismo , Fígado Gorduroso/metabolismo , Flavonoides/química , Flavonoides/metabolismo , Flavonoides/farmacologia , Células Hep G2 , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Humanos , Mitocôndrias/metabolismo , Modelos Biológicos , Estresse Oxidativo/efeitos dos fármacos , Fenóis/química , Fenóis/farmacologia , Quercetina/química , Quercetina/metabolismo , Espécies Reativas de Oxigênio/metabolismo
19.
J Agric Food Chem ; 67(19): 5552-5559, 2019 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-31042377

RESUMO

The present study was designed to investigate the role of the canonical and noncanonical inflammasome, MAPKs and NRF-2/HO-1, signaling pathways involved in the antioxidant and anti-inflammatory activities of oleocanthal in lipopolysaccharide (LPS)-stimulated murine peritoneal macrophages. Isolated cells were treated with oleocanthal in the presence or absence of LPS (5 µg mL-1) for 18 h. Oleocanthal showed a potent reduction of reactive oxygen species (ROS) (25 µM, 50. 612 ± 0.02; 50 µM, 53. 665 ± 0.09; 100 µM, 52. 839 ± 0.02), nitrites (25 µM, 0.631 ± 0.07; 50 µM, 0.652 ± 0.07; 100 µM, 0.711 ± 0.08), and pro-inflammatory cytokines levels when compared with LPS-DMSO-treated control cells. In terms of enzymes protein expression, oleocanthal was able to downregulate iNOS (25 µM, 0.173 ± 0.02; 50 µM, 0.149 ± 0.01; 100 µM, 0.150 ± 0.01; p < 0.001), COX-2 (25 µM, 0.482 ± 0.08; 50 µM, 0.469 ± 0.05; 100 µM, 0.418 ± 0.06; p < 0.001), and mPGES-1 (25 µM, 0.185 ± 0.11; 50 µM, 0.218 ± 0.13; 100 µM, 0.161 ± 0.15; p < 0.001) as well as p38 (25 µM, 0.366 ± 0.11; 50 µM, 0.403 ± 0.13; 100 µM, 0.362 ± 0.15; p < 0.001), JNK (25 µM, 0.443 ± 0.11; 50 µM, 0.514 ± 0.13; 100 µM, 0.372 ± 0.15; p < 0.001), and ERK (25 µM, 0.294 ± 0.01; 50 µM, 0.323 ± 0.01; 100 µM, 0.274 ± 0.01; p < 0.001) protein phosphorylation, which was accompanied by an upregulation of Nrf-2 (25 µM, 1.57 ± 0.01; 50 µM, 1.54 ± 0.01; 100 µM, 1.63 ± 0.05; p < 0.05) and HO-1(25 µM, 2.12 ± 0,03; 50 µM, 2.24 ± 0.01; 100 µM, 1.92 ± 0.05; p < 0.01) expression in comparison with LPS-DMSO cells. Moreover, oleocanthal inhibited canonical and noncanonical inflammasome signaling pathways. Thus, oleocanthal might be a promising natural agent for future treatment of immune-inflammatory diseases.


Assuntos
Aldeídos/farmacologia , Heme Oxigenase-1/imunologia , Inflamassomos/imunologia , Lipopolissacarídeos/farmacologia , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/imunologia , Fator 2 Relacionado a NF-E2/imunologia , Fenóis/farmacologia , Animais , Células Cultivadas , Feminino , Heme Oxigenase-1/genética , Inflamassomos/efeitos dos fármacos , Inflamassomos/genética , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Ativação de Macrófagos/efeitos dos fármacos , Camundongos , Fator 2 Relacionado a NF-E2/genética , Fosforilação , Espécies Reativas de Oxigênio/imunologia
20.
Oxid Med Cell Longev ; 2019: 1346878, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31049124

RESUMO

2-Allylphenol (2-AP) is a synthetic phenylpropanoid, structurally related to cardanol, thymol, and ortho-eugenol. Phenylpropanoids are described in the literature as being capable of promoting biological activity. Due to the similarity between 2-AP and other bioactive phenylpropanoids, the present research aims at evaluating the antioxidant, antinociceptive, and anti-inflammatory potential of 2-AP in silico, in vitro, and in vivo. At 30 min prior to the start of in vivo pharmacological testing, administration of 2-AP (25, 50, 75, and 100 mg/kg i.p.), morphine (6 mg/kg i.p.), dexamethasone (2 mg/kg s.c.), or vehicle alone was performed. In the acetic acid-induced abdominal writhing tests, pretreatment with 2-AP significantly reduced the number of abdominal writhes, as well as decreased licking times in the glutamate and formalin tests. Investigation of the mechanism of action using the formalin model led to the conclusion that the opioid system does not participate in its activity. However, the adenosinergic system is involved. In the peritonitis tests, 2-AP inhibited leukocyte migration and reduced releases of proinflammatory mediators TNF-α and IL-1ß. In vitro antioxidant assays demonstrated that 2-AP presents significant ability to sequester superoxide radicals. In silico docking studies confirmed interaction between 2-AP and the adenosine A2a receptor through hydrogen bonds with the critical asparagine 253 residues present in the active site. Investigation of 2-AP demonstrated its nociception inhibition and ability to reduce reactive oxygen species. Its interaction with A2a receptors may well be related to proinflammatory cytokines TNF-α and IL-1ß reduction activity, corroborating its antinociceptive effect.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Interleucina-1beta/metabolismo , Fenóis/farmacologia , Fator de Necrose Tumoral alfa/metabolismo , Animais , Masculino , Camundongos , Simulação de Acoplamento Molecular , Peritonite/tratamento farmacológico , Peritonite/metabolismo , Peritonite/patologia , Fenóis/química , Receptor A2A de Adenosina/química , Receptor A2A de Adenosina/metabolismo
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