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1.
Molecules ; 28(9)2023 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-37175357

RESUMO

Anthyllis henoniana stems were harvested in two seasons: winter and spring (February and May 2021). In this study, we investigated the antioxidant (DPPH, ABTS, FRAP and TAC) and antimicrobial activities, total phenolic contents and total flavonoid contents of the obtained extracts (hexane, ethyl acetate and methanol). The results showed that ethyl acetate extract from stems harvested in winter exhibited the highest antioxidant activity, while ethyl acetate extract from the stems harvested in spring showed the most potent antibacterial and antifungal activities. To explain these differences, we investigated the phytochemical composition of these two extracts using liquid chromatography coupled with mass spectrometry. Therefore, 45 compounds were detected, from which we identified 20 compounds (flavonoids, triterpenoids, chalcones and phenolic acids); some were specific to the harvest month while others were common for both periods. Some of the major compounds detected in ethyl acetate (spring) were dihydrochalcone (Kanzonol Y, 8.2%) and flavanone (sophoraflavanone G, 5.9%), previously recognized for their antimicrobial effects. We therefore concluded that the difference in activities observed for the two harvest periods depends on the chemical composition of the extracts and the relative abundance of each compound.


Assuntos
Anti-Infecciosos , Antioxidantes , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Estações do Ano , Anti-Infecciosos/farmacologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Flavonoides/análise
2.
Molecules ; 27(14)2022 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-35889269

RESUMO

The phytochemical analysis of antioxidant and antibacterial activities of Erodium arborescens aerial part extracts constitute the focus of this research. The chemical composition of an acetone extract was investigated using LC-HESI-MS2, which revealed the presence of 70 compounds. The major identified components were tannin derivatives. Total polyphenol and total flavonoid contents were assessed in plant extracts (hexane, ethyl acetate, acetone and methanol). The results showed that the acetone extract exhibited the highest contents of polyphenols and flavonoids, 895.54 and 36.39 mg QE/g DE, respectively. Furthermore, when compared to other extracts, Erodium arborescens acetone extract was endowed with the highest antioxidant activity with 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC) tests. In addition, the four extracts of Erodium arborescens showed variable degrees of antimicrobial activity against the tested strains, and the interesting activity was obtained with acetone and methanol extracts.


Assuntos
Acetona , Antioxidantes , Antibacterianos/farmacologia , Antioxidantes/química , Flavonoides/química , Metanol , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/análise
3.
Molecules ; 27(7)2022 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-35408713

RESUMO

Considering medicinal plants as an inexhaustible source of active ingredients that may be easily isolated using simple and inexpensive techniques, phytotherapy is becoming increasingly popular. Various experimental approaches and analytical methods have been used to demonstrate that the genus Calendula (Asteraceae) has a particular richness in active ingredients, especially phenolic compounds, which justifies the growing interest in scientific studies on this genus' species. From a chemical and biological viewpoint, Calendula aegyptiaca is a little-studied plant. For the first time, high-performance liquid chromatography combined with negative electrospray ionization mass spectrometry (HPLC-HESI-MS) was used to analyze methanolic extracts of Calendula aegyptiaca (C. aegyptiaca) fruits. Thirty-five molecules were identified. Flavonoids (47.87%), phenolic acids (5.18%), and saponins (6.47%) formed the majority of these chemicals. Rutin, caffeic acid hexoside, and Soyasaponin ßg' were the most abundant molecules in the fruit methanolic extract, accounting for 17.49% of total flavonoids, 2.32 % of total phenolic acids, and 0.95% of total saponins, respectively. The antioxidant activity of the fruit extracts of C. aegyptiaca was investigated using FRAP, TAC, and DPPH as well as flavonoids and total phenols content. Because the phenolic components were more extractable using polar solvents, the antioxidant activity of the methanolic extract was found to be higher than that of the dichloromethane and hexane extracts. The IC50 value for DPPH of methanolic extract was found to be 0.041 mg·mL-1. Our findings showed that C. aegyptiaca is an important source of physiologically active compounds.


Assuntos
Calendula , Saponinas , Antioxidantes/química , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/química , Frutas/química , Fenóis/química , Extratos Vegetais/química , Espectrometria de Massas em Tandem/métodos
4.
Molecules ; 26(14)2021 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-34299613

RESUMO

Aeonium is a genus of succulents belonging to the Crassulaceae family. Their importance in traditional medicine has stimulated both pharmacological and chemical research. In this study, we optimized extraction, separation, and analytical conditions using a high performance liquid chromatographic method coupled with electrospray ionization mass spectrometry by the negative mode (HPLC-ESI-MS) in order to, for the first time, determine thirty-four compounds from Aeonium arboreum leaves. Twenty-one of them are assigned among which are sixteen flavonoids and five phenolic acids. FRAP, TAC, DPPH, and ABTS•+ radical scavenging were used to evaluate antioxidant activity. The obtained IC50 values ranged from 0.031 to 0.043 mg.mL-1 for DPPH and between 0.048 and 0.09 mg·mL-1 for ABTS•+. Antimicrobial activity was also assessed. The obtained minimum inhibitory concentrations (MIC) of these extracts ranged from 12.5 to 50 µg·mL-1 against Micrococcus luteus, Listeria ivanovii, Staphylococcus aureus, Salmonella enterica, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger, and Fusarium oxysporum, and from 25 to 50 µg·mL-1 against Candida albicans. Therefore, these extracts can be considered as a potential source of biological active compounds.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Crassulaceae/química , Fenóis/química , Extratos Vegetais/química , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem
5.
Pharm Biol ; 55(1): 124-131, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27925497

RESUMO

CONTEXT AND OBJECTIVE: Diplotaxis harra (Forssk.) Boiss. (Brassicaceae) is traditionally used as an antidiabetic, anti-inflammatory or anticancer agent. In these pathologies, the glycogen synthase kinase 3 ß (GSK3ß) is overactivated and represents an interesting therapeutic target. Several flavonoids can inhibit GSK3ß and the purpose of this study was to search for the compounds in Diplotaxis harra which are able to modulate GSK3ß. MATERIALS AND METHODS: Methanol extracts from D. harra flowers were prepared and the bio-guided fractionation of their active compounds was performed using inflammatory [protease-activated receptor 2 (PAR2)-stimulated IEC6 cells] and cancer (human Caco-2 cell line) intestinal cells. 50-100 µg/mL of fractions or compounds purified by HPLC were incubated with cells whose inhibited form of GSK3ß (Pser9 GSK3ß) and survival were analyzed by Western blot at 1 h and colorimetric assay at 24 h, respectively. LC-UV-MS profiles and MS-MS spectra were used for the characterization of extracts and flavonoids-enriched fractions, and the identification of pure flavonoids was achieved by MS and NMR analysis. RESULTS: The methanol extract from D. harra flowers and its flavonoid-enriched fraction inhibit GSK3ß in PAR2-stimulated IEC6 cells. GSK3ß inhibition by the flavonoid-enriched D. harra fraction was dependent on PKC activation. The flavonoid-enriched D. harra fraction and its purified compound isorhamnetin-3,7-di-O-glucoside induced a 20% decrease of PAR2-stimulated IEC6 and Caco-2 cell survival. Importantly, normal cells (non-stimulated IEC6 cells) were spared by these treatments. CONCLUSION: This work indicates that flavonoids from D. harra display cytotoxic activity against inflammatory and cancer intestinal cells which could depend on GSK3ß inhibition.


Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Brassicaceae/química , Neoplasias do Colo/tratamento farmacológico , Flavonóis/farmacologia , Glicogênio Sintase Quinase 3 beta/antagonistas & inibidores , Glicosídeos/farmacologia , Doenças Inflamatórias Intestinais/tratamento farmacológico , Extratos Vegetais/farmacologia , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Células CACO-2 , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Neoplasias do Colo/enzimologia , Neoplasias do Colo/patologia , Flavonóis/isolamento & purificação , Flores , Glicogênio Sintase Quinase 3 beta/metabolismo , Glicosídeos/isolamento & purificação , Humanos , Doenças Inflamatórias Intestinais/enzimologia , Doenças Inflamatórias Intestinais/patologia , Espectroscopia de Ressonância Magnética , Metanol/química , Fitoterapia , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Inibidores de Proteínas Quinases/farmacologia , Transdução de Sinais/efeitos dos fármacos , Solventes/química , Espectrometria de Massas em Tandem
6.
Am J Physiol Gastrointest Liver Physiol ; 311(2): G221-36, 2016 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-27313176

RESUMO

Protease-activated receptors PAR1 and PAR2 play an important role in the control of epithelial cell proliferation and migration. However, the survival of normal and tumor intestinal stem/progenitor cells promoted by proinflammatory mediators may be critical in oncogenesis. The glycogen synthase kinase-3ß (GSK3ß) pathway is overactivated in colon cancer cells and promotes their survival and drug resistance. We thus aimed to determine PAR1 and PAR2 effects on normal and tumor intestinal stem/progenitor cells and whether they involved GSK3ß. First, PAR1 and PAR2 were identified in colon stem/progenitor cells by immunofluorescence. In three-dimensional cultures of murine crypt units or single tumor Caco-2 cells, PAR2 activation decreased numbers and size of normal or cancerous spheroids, and PAR2-deficient spheroids showed increased proliferation, indicating that PAR2 represses proliferation. PAR2-stimulated normal cells were more resistant to stress (serum starvation or spheroid passaging), suggesting prosurvival effects of PAR2 Accordingly, active caspase-3 was strongly increased in PAR2-deficient normal spheroids. PAR2 but not PAR1 triggered GSK3ß activation through serine-9 dephosphorylation in normal and tumor cells. The PAR2-triggered GSK3ß activation implicates an arrestin/PP2A/GSK3ß complex that is dependent on the Rho kinase activity. Loss of PAR2 was associated with high levels of GSK3ß nonactive form, strengthening the role of PAR2 in GSK3ß activation. GSK3 pharmacological inhibition impaired the survival of PAR2-stimulated spheroids and serum-starved cells. Altogether our data identify PAR2/GSK3ß as a novel pathway that plays a critical role in the regulation of stem/progenitor cell survival and proliferation in normal colon crypts and colon cancer.


Assuntos
Colo/enzimologia , Células Epiteliais/enzimologia , Glicogênio Sintase Quinase 3 beta/metabolismo , Células-Tronco Neoplásicas/enzimologia , Receptor PAR-2/metabolismo , Células-Tronco/enzimologia , Animais , Arrestina/metabolismo , Células CACO-2 , Proliferação de Células , Sobrevivência Celular , Colo/patologia , Ativação Enzimática , Células Epiteliais/patologia , Humanos , Masculino , Camundongos Endogâmicos C57BL , Células-Tronco Neoplásicas/patologia , Fosforilação , Proteína Fosfatase 2/metabolismo , Interferência de RNA , Receptor PAR-2/genética , Transdução de Sinais , Esferoides Celulares , Nicho de Células-Tronco , Células-Tronco/patologia , Transfecção , Microambiente Tumoral , Quinases Associadas a rho/metabolismo
7.
Chem Biodivers ; 13(12): 1674-1684, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27476999

RESUMO

The hexane extract of Echinops spinosissimus Turra subsp. spinosus flower heads was analyzed for its fatty acid and sterol composition. Its physicochemical characteristics were also studied. The saponification, iodine and peroxide values were determined as 255 mg KOH/g, 42.57 g I2 /100 g and 110 m equiv. O2 /kg of oil, respectively. The oleic (C18:1; 61.14%), palmitic (C16:0; 21.36%) and linoleic (C18:2; 10.45%) acids were the dominant fatty acids. This extract was also found to contain high levels of ß-sitosterol and stigmasterol (44.97% and 34.95% of total sterols, respectively). On the other hand, the identification of terpenoid compounds was investigated by using GC/MS, which revealed fourteen major terpenoids mainly taraxasterol, lupeol, pseudotaraxasterol, lup-22(29)-en-3-yl acetate, taraxasteryl acetate, α-amyrin, ß-amyrin, pseudotaraxasteryl acetate, hop-20(29)-en3-ß-ol, α-amirenone, along with ß-sitosterol and stigmasterol. Moreover, we have evaluated the in vitro antibacterial and antifungal activities of the unsaponifiable matter and a fraction isolated from this extract. These activities were conducted using the diffusion disc methods and broth microdilution assay. The resulted fraction from this extract showed the highest antibacterial activity with significant minimum inhibitory concentrations (MIC) values 125.0 µg/ml against Staphylococcus aureus, Micrococcus luteus and Bacillus cereus. However, it did exhibit no substantial antifungal activity.


Assuntos
Antibacterianos/farmacologia , Asteraceae/química , Hexanos/farmacologia , Extratos Vegetais/farmacologia , Esteróis/química , Acetilação , Antibacterianos/análise , Bacillus cereus/efeitos dos fármacos , Relação Dose-Resposta a Droga , Flores/química , Hexanos/análise , Testes de Sensibilidade Microbiana , Micrococcus luteus/efeitos dos fármacos , Extratos Vegetais/análise , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade , Tunísia
8.
Pharm Biol ; 54(4): 726-31, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26429590

RESUMO

CONTEXT: The persistence of fascioliasis in many developing countries urges the search for simple, cheap, and effective substances. In this view, plants provide interesting molluscicidal activities thanks to the secondary metabolites they produce. The genus Solanum is known for its potent effect on vector snails. OBJECTIVE: The molluscicidal activity of Solanum elaeagnifolium Cav. (Solanaceae) seeds against Galba truncatula Müll. (Lymnaeidae), intermediate host of Fasciola hepatica L. (Fasciolidae), was evaluated. MATERIALS AND METHODS: Solanum elaeagnifolium seeds were powdered and successively extracted using n-hexane, methylene chloride, acetone, and methanol, for 20 h each. After filtration, solvents were evaporated. An acid-base treatment was conducted on seed methanolic extract to isolate total alkaloids and ß-solamarine. Total saponins fraction was obtained after successive macerations and evaporations. The molluscicidal activity was evaluated by subjecting snails, in groups of 10, for 48 h to 500 mL of extracts, fractions, and pure product aqueous solutions, each containing amounts, ranging from 1 to 50 mg of plant material in 5 mg increments. RESULTS: The methanolic extract of seeds, ß-solamarine isolated for the first time from this plant and total saponins fraction showed very potent activities on snails, giving respective median lethal concentrations (LC50) of 1.18, 0.49, and 0.94 mg/L. Total alkaloids fraction obtained from the methanolic extract was less active giving an LC50 value of 14.67 mg/L. DISCUSSION AND CONCLUSION: This study emphasizes that glycoalkaloids and saponins of Solanum elaeagnifolium are potent molluscicidal agents. Seed methanolic extract, ß-solamarine, and total saponins fraction may be used as molluscicides.


Assuntos
Fasciola hepatica/efeitos dos fármacos , Lymnaea/efeitos dos fármacos , Moluscocidas/farmacologia , Extratos Vegetais/farmacologia , Sementes , Alcaloides de Solanáceas/farmacologia , Solanum , Animais , Fasciola hepatica/metabolismo , Lymnaea/metabolismo , Moluscocidas/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Caramujos , Alcaloides de Solanáceas/isolamento & purificação
9.
Molecules ; 20(10): 18001-15, 2015 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-26437392

RESUMO

Two new tetracyclic cucurbitane-type triterpene glycosides were isolated from an ethyl acetate extract of Citrullus colocynthis leaves together with four known cucurbitacins. Their structures were established on the basis of their spectroscopic data (mainly NMR and mass spectrometry). Evaluation of the in vitro cytotoxic activity of the isolated compounds against two human colon cancer cell lines (HT29 and Caco-2) and one normal rat intestine epithelial cell line (IEC6), revealed that one of the isolated compounds presented interesting specific cytotoxic activity towards colorectal cell lines.


Assuntos
Citrullus colocynthis/química , Cucurbitacinas/química , Extratos Vegetais/química , Folhas de Planta/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Cucurbitacinas/farmacologia , Relação Dose-Resposta a Droga , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Extratos Vegetais/farmacologia
10.
Molecules ; 20(8): 14902-14, 2015 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-26287146

RESUMO

A broad biological screening of the natural alkaloid N-methylisosalsoline (2) extracted from Hammada scoparia leaves against a panel of human and parasitic proteases revealed an interesting activity profile of 2 towards human 20S proteasome. This outcome suggests that the 1,2,3,4-tetrahydroisoquinoline skeleton may be exploited as a template for the development of novel anticancer agents. In this article, we report the synthesis and chemical characterization of a new series of isosalsoline-type alkaloids (10-11) with variations at N2 and C3 positions with respect to the natural Compound 2, obtained by a synthetic strategy that involves the Bischler-Napieralski cyclization. The substrate for the condensation to the tetrahydroisoquinoline system, i.e., a functionalized ß-arylethyl amine, was obtained through an original double reduction of nitroalkene. The synthetic strategy can be directed to the construction of highly substituted and functionalized 1,2,3,4-tetrahydroisoquinolines.


Assuntos
Tetra-Hidroisoquinolinas/síntese química , Animais , Bovinos , Proliferação de Células/efeitos dos fármacos , Humanos , Parasitos/efeitos dos fármacos , Parasitos/enzimologia , Peptídeo Hidrolases/metabolismo , Tetra-Hidroisoquinolinas/química , Tetra-Hidroisoquinolinas/farmacologia
11.
Pharm Biol ; 53(12): 1810-7, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25885934

RESUMO

CONTEXT: Hepatic ischemia/reperfusion injury (IRI) is a major cause of liver damage during liver surgery and transplantation. Plants have historically been used in treating liver damage, and Hammada scoparia (Pomel) (Chenopodiaceae) has been reported to possess a broad spectrum of pharmacological and therapeutic activities. OBJECTIVE: In this study, a flavonoid-enriched fraction was used before the warm ischemia (WI) process as pharmacological preconditioning and in combination with technical postconditioning to evaluate their protective effects. MATERIALS AND METHODS: The rats were divided into five groups: a sham group; a control group (Control-IR) that was submitted to 60 min WI; a Pharmacological Preconditioning group (PreC-IR) that received flavonoid-enriched fraction (200 mg/kg body weight); a Postconditioning group (PostC) and a PreC + PostC group. RESULTS: The use of the flavonoid-enriched fraction was noted to significantly (p < 0.05) reduce liver injury, as evidenced by the decrease in liver transaminase activities (AST and ALT) and lactic dehydrogenase (LDH), alkaline phosphatase (ALP), and lipid peroxidation (TBARS), levels as well as the enhancement of antioxidant enzymes (catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx)) responses. The results also indicated that, compared with the separate application of pharmacological preconditioning and postconditioning, the combination of both treatments was more effective in reducing tissue oxidative stress levels through modulating SOD, GSH-PX, and CAT activities. Furthermore, the combined protocol further decreased the liver morphological score compared with solo treatment. DISCUSSION AND CONCLUSION: Overall, the results indicate that the H. scoparia flavonoid-enriched fraction could be a promising candidate for future application as a pharmacological preconditioning agent against hepatic IRI.


Assuntos
Flavonoides/uso terapêutico , Fígado/irrigação sanguínea , Fígado/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Traumatismo por Reperfusão/prevenção & controle , Scoparia , Isquemia Quente/efeitos adversos , Animais , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Fígado/metabolismo , Masculino , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Traumatismo por Reperfusão/metabolismo , Resultado do Tratamento
12.
Toxicol Ind Health ; 30(2): 113-22, 2014 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22778112

RESUMO

Aqueous extract (AE) of Hammada scoparia leaves was chemically characterized and its hepatoprotective activities were investigated in vivo in rat model. Wistar rats were treated daily with 35% ethanol solution (3 g/kg/day) during 4 weeks and fed with basal diet or basal diet containing AE (200 mg/kg/day). Control rats were treated with saline solution and fed with basal diet. The bioactivity of AE against ethanol-induced oxidative stress in rat liver was studied in order to explore its hepatoprotective effects. H. scoparia extract used at 200 mg/kg body weight significantly prevented the effects of ethanol, which induced a hepatic pathological damage and increased the levels of the serum markers of the enzymes such as alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP). Concomitantly, with these changes, this extract also prevented ethanol-induced oxidative stress in the rat liver as evidenced by the decreased lipid peroxidation level, a considerable decrease in the activities of AST, ALT and ALP and restoring the activities of antioxidant enzymes: superoxide dismutase, catalase and glutathione peroxidase. These biochemical changes were consistent with histopathological observations suggesting marked hepatoprotective effect of the AE of H. scoparia.


Assuntos
Amaranthaceae/química , Etanol/efeitos adversos , Fígado/citologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Alanina Transaminase/sangue , Fosfatase Alcalina/sangue , Animais , Aspartato Aminotransferases/sangue , Peso Corporal/efeitos dos fármacos , Catalase/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/patologia , Glutationa Peroxidase/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Tamanho do Órgão/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismo
13.
Antioxidants (Basel) ; 13(7)2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-39061863

RESUMO

Plant extracts are considered as a large source of active biomolecules, especially in phytosanitary and pharmacological fields. Anthyllis henoniana is a woody Saharan plant located in the big desert of North Africa. Our previous research paper proved the richness of the methanol extract obtained from the stems in flavonoids and phenolic compounds as well as its remarkable antioxidant activity. In this research, we started by investigating the phytochemical composition of the methanol extract using high performance liquid chromatography coupled with electrospray ionization mass spectrometry (LC-MS/MS). Among the 41 compounds identified, we isolated and characterized (structurally and functionally) the most abundant product, a flavonoid triglycoside (AA770) not previously described in this species. This compound, which presents no cytotoxic activity, exhibits an interesting cellular antioxidant effect by reducing reactive oxygen species (ROS) generation, and an antiproliferative action on breast cancer cells. This study provides a preliminary investigation into the pharmacological potential of the natural compound AA770, isolated and identified from Anthyllis henoniana for the first time.

14.
Int J Biol Macromol ; 125: 730-742, 2019 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-30521922

RESUMO

Periploca angustifolia has numerous biological properties and also used against various diseases. In our study, this plant has been used for biotechnological production of polysaccharides. The prevention action of polysaccharides isolated from P. angustifolia (PAPS) against Cd-caused oxidative stress in HEK293 cells and kidneys of rats was tested. PAPS were characterized by HPLC, FT-IT, DRX, 1D-and 2D-MNR. PAPS present strong capacity to slow the rate of lipid peroxidation and protein glycation in vitro. In addition, the results indicated that the Cd treatment caused a significant decrease in HEK293 cells viability which wasattenuated by PAPS pre-treatment. Furthermore, our findings revealed that Cd injection increased the levels of urea and creatinine in the serum. The increased levels of protein oxidation and lipid peroxidation along with decreased activities of SOD, CAT and GPx were significantly (p < 0.01) ameliorated by PAPS pre-treatment. Finally, histopathological studies also supported the prevention action of PAPS.


Assuntos
Antioxidantes/farmacologia , Cádmio/farmacologia , Rim/efeitos dos fármacos , Periploca/química , Polissacarídeos/farmacologia , Substâncias Protetoras/farmacologia , Animais , Antioxidantes/química , Linhagem Celular , Creatinina/metabolismo , Células HEK293 , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Polissacarídeos/química , Ratos , Ratos Wistar , Ureia/metabolismo
15.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 9): o1714, 2008 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-21201700

RESUMO

THE TITLE COMPOUND (SYSTEMATIC NAME: 1,2-dimethyl-6-meth-oxy-1,2,3,4-tetra-hydro-isoquinolin-7-ol), C(12)H(17)NO(2), is a major alkaloid isolated from Hammada scoparia leaves. It belongs to the isoquinoline family and it was characterized by NMR spectroscopy and X-ray crystallographic techniques. The absolute configuration could not be reliably determined. An intermolecular O-H⋯N hydrogen bond is present in the crystal structure.

16.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 9): o1739, 2008 Aug 09.
Artigo em Inglês | MEDLINE | ID: mdl-21201722

RESUMO

THE TITLE COMPOUND (SYSTEMATIC NAME: 16-hydroxy-methyl-12-methoxy-ibogamine), C(21)H(28)N(2)O(2), was prepared by reaction of ibogaine with a formaldehyde-acetic acid solution (pH = 4). The crystal structure of this new product, belonging to the iboga indole family, is stabilized by an inter-molecular O-H⋯N hydrogen bond. The identity of the compound was confirmed by one- and two-dimensional NMR spectroscopic techniques.

17.
Artigo em Inglês | MEDLINE | ID: mdl-30034500

RESUMO

BACKGROUND: This study investigates the biological activities of Anthyllis henoniana flowers extracts. MATERIALS AND METHODS: Antioxidant activity and the in vitro inhibitory effect of key digesting enzymes related to postprandial hyperglycemia were determined. Diabetic rats were orally and daily given the best extract from flowers of Anthyllis henoniana at a dose of acarbose for one month. RESULTS: Among the extracts, the ethyl acetate one displayed remarkable antioxidant activity including DPPH (IC50 = 2.34 mg/mL) and was more effective in inhibiting α-glucosidase (IC50 = 17 µg/mL) than α-amylase (IC50 = 920 µg /mL) activities. In vivo, the results proved that ethyl acetate extract at doses of 400 mg/kg bw decreased significantly the blood glucose level and lipid profile levels and increased the activities of antioxidant enzymes. These protective impacts of Anthyllis henoniana ethyl acetate flowers extract were confirmed by histological results. CONCLUSION: This study demonstrates, for the first time, that Anthyllis henoniana flowers ethyl acetate extract is effective in inhibiting hyperglycemia and oxidative stress caused by diabetes.

18.
J Oleo Sci ; 67(11): 1483-1499, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30404969

RESUMO

The aerial part of Clematis flammula (Ranunculaceae) has been traditionally used in the treatment of skin diseases including mycotic infection in the Tunisian traditional medicine. The study was undertaken to extract and determine the essential oil chemical composition of Clematis flammula aerial parts and to assess the potential of anemonin in wound healing on mechanically wounded wistar rats. The essential oil was obtained by hydrodistillation and analyzed by GC-MS. Anemonin was isolated and then incorporated as active in a cream for which the cytotoxicity was evaluated by methyl thiazolyl tetrazolium (MTT)-based colorimetric assay. Then, its potential in wound healing on mechanically wounded wistar rats was assessed. The GC-MS analysis showed that the major compound was protoanemonin (86.74%) which spontaneously dimerised in part to form the anemonin. The wound healing activity of anemonin cream exhibited a non toxic potential of anemonin at a concentration of 25 µg/mL with a cell migration efficiency that reaches more than 80% after 48 hours of treatment. Wound healing efficiency was evaluated by monitoring morphological and skin histological analyses. Comparable wound surface reduction of the group treated by anemonin cream (p ≥ 0.05) when compared to the reference treated group. The skin histological analysis showed the completely wound closure. Antioxidant activity was assessed by the malondialdehyde (MDA) rates and antioxidant enzymes (glutathione peroxidase (GPx) and catalase) determination. The results provided strong support for the effective wound healing activity of anemonin cream, making it a promising candidate as a therapeutic agent in tissue repairing processes.


Assuntos
Clematis/química , Furanos/isolamento & purificação , Furanos/farmacologia , Óleos Voláteis/isolamento & purificação , Óleos Voláteis/farmacologia , Cicatrização/efeitos dos fármacos , Administração Tópica , Animais , Antioxidantes/metabolismo , Catalase/metabolismo , Feminino , Furanos/administração & dosagem , Cromatografia Gasosa-Espectrometria de Massas , Glutationa Peroxidase/metabolismo , Malondialdeído/metabolismo , Óleos Voláteis/administração & dosagem , Ratos Wistar , Pele/metabolismo , Pele/patologia , Creme para a Pele , Estimulação Química , Tunísia
19.
Biomed Res Int ; 2018: 7295848, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29744362

RESUMO

Over the last few decades, Rumex species have been recognized as a promising source of new compounds with numerous pharmacological activities. Therefore, the antioxidant activity of Rumex tingitanus (R. tingitanus) leaves extracts was evaluated in vitro and then confirmed in vivo as well as the antidepressant-like and toxicological effects of the extracts. The ethyl acetate fraction (Rt EtOAcF) followed by hydroalcoholic extract (Rt EtOH-H2O) showed a remarkable in vitro antioxidant activity. The hydroalcoholic extract (Rt EtOH-H2O) showed significant hepatoprotective activity against carbon tetrachloride- (CCl4-) induced liver toxicity which is seen from inhibition of the malondialdehyde (MDA) accumulation and enhancement of the liver antioxidant enzymes activities. The Rt EtOH-H2O and Rt EtOAcF extracts were able to reduce the immobility time in mice and then elicited a significant antidepressant-like effect. The ethyl acetate fraction (Rt EtOAcF) was purified and resulted in the identification of a new antioxidant component called 4'-p-acetylcoumaroyl luteolin. The Rt EtOAcF and the 4'-p-acetylcoumaroyl luteolin revealed a strong antioxidant activity using DPPH test with IC50 of 11.7 ± 0.2 and 20.74 ± 0.6 µg/ml, respectively, and AAI of 3.39 and 1.92 better than that of BHT, used as control.


Assuntos
Antioxidantes/administração & dosagem , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Rumex/química , Animais , Antidepressivos/administração & dosagem , Antidepressivos/química , Antioxidantes/química , Tetracloreto de Carbono/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/patologia , Humanos , Camundongos , Fitoterapia , Extratos Vegetais/química , Folhas de Planta/química
20.
Meat Sci ; 125: 22-29, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27883958

RESUMO

This study was undertaken to investigate the antibacterial and antifungal activities of Rumex tingitanus leaves extracts as well as the identification of bioactive components and their performance in meat preservation. Total phenolics and flavonoids showed the highest content of phenolics and flavonoids in the ethyl acetate fraction (Rt EtOAcF). For antimicrobial efficacy, leaves extract and derived fraction were tested for their capacity to inhibit bacterial and fungal proliferation in vitro and in vivo. The ethyl acetate fraction showed the most potent antibacterial and antifungal activities compared to the others extracts. Thus, the efficacy of this extract to inhibit the proliferation of Listeria monocytogenes in minced beef meat model was examined. This fraction eradicates the L. monocytogenes population in meat in a concentration- and time-dependent manner. A bio-guided purification of the Rt EtOAc fraction resulted in the isolation of the compound responsible for the observed antimicrobial activity. This compound was identified as luteolin by analysis of spectroscopic data. CHEMICAL COMPOUNDS ISOLATED IN THIS ARTICLE: Luteolin (PubChem CID: 5280445); p-iodonitrotetrazolium chloride (PubChem CID: 64957); Amphotericin B (PubChem CID: 5280965); Gentamicin and (PubChem CID: 6419933); Hexane (PubChem CID: 8058); Methanol (PubChem CID: 887); Ethanol (PubChem CID: 702); Dimethylsulfoxide (PubChem CID: 679); Quercetin (PubChem CID: 5280343); Gallic acid (PubChem CID: 370).


Assuntos
Anti-Infecciosos/farmacologia , Conservantes de Alimentos/farmacologia , Carne/microbiologia , Extratos Vegetais/farmacologia , Rumex/química , Alternaria/efeitos dos fármacos , Aspergillus niger/efeitos dos fármacos , Fracionamento Químico , Flavonoides/farmacologia , Contaminação de Alimentos , Microbiologia de Alimentos , Conservação de Alimentos , Fusarium/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Listeria monocytogenes/efeitos dos fármacos , Luteolina/farmacologia , Carne/análise , Testes de Sensibilidade Microbiana , Fenóis/farmacologia , Folhas de Planta/química , Taninos/farmacologia
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