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1.
Pestic Biochem Physiol ; 203: 105965, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-39084763

RESUMO

Herein, we focused on the larvicidal effects and potential mechanisms of 5-ethenyl-2,2'-bithiophene (5 EB), a compound isolated from Echinops ritro L. on Aedes aegypti larvae. Our results show that 5 EB exhibits pronounced larvicidal activity against A. aegypti larvae, with an LC50 = 0.24 mg/L, considerably lesser than that of the traditional insecticide, rotenone. Observations using fluorescence microscopy, electron microscopy, and imaging flow cytometry demonstrated that 5 EB targets the hemocytes of larvae, leading to the disruption of their intracellular membrane systems. This disruption leads to considerable damage to the cellular structure and function, leading to the death of test subjects. Note that additional investigation into the molecular mechanism of 5 EB's action was conducted using transcriptomic analysis. Both GO and KEGG enrichment analyses reported that the differentially expressed genes were predominantly associated with membranes, lysosomes, and catalytic activities. To summarize, this study provides new options for developing new, environmentally friendly, plant-based larvicides for mosquito control.


Assuntos
Aedes , Inseticidas , Larva , Animais , Aedes/efeitos dos fármacos , Larva/efeitos dos fármacos , Inseticidas/farmacologia , Echinops (Planta)/química , Tiofenos/farmacologia , Controle de Mosquitos/métodos , Extratos Vegetais/farmacologia , Extratos Vegetais/química
2.
Molecules ; 29(10)2024 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-38792128

RESUMO

The main varieties of Echinopsis Radix recorded in the Chinese Pharmacopoeia are the roots of Echinops latifolius Tausch or Echinops grijsii Hance. However, the chemical constituents and biological activities of this herb have not been reviewed. In order to clarify the chemical constituents of the main varieties of this herb and improve the quality of Chinese medicinal material resources, this paper systematically reviewed their chemical constituents and related biological activities. Phytochemical investigations reveal eighty-five compounds including fort y-nine thiophenes (1-49), eight flavonoids (50-57), seven caffeic acids and its derivatives (58-64), eight sesquiterpenoids (65-72), and thirteen triterpenoids and other compounds (73-85) were reported from Echinopsis Radix. The review of biological activities suggests that thiophenes are the main secondary metabolites of the medicinal material which exert antitumor, insecticidal and antifungal activities. In addition, caffeic acid and its derivatives and sesquiterpenes are potential active ingredients worthy of further study. This review provides an important scientific basis for the development of active ingredients and resource quality evaluation of Echinopsis Radix.


Assuntos
Compostos Fitoquímicos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Echinops (Planta)/química , Humanos , Raízes de Plantas/química , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Animais , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia
3.
Biochem Cell Biol ; 97(2): 176-186, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30933551

RESUMO

This study was designed to evaluate the possible mechanisms through which Echinops spinosus (ES) extract demonstrates nephroprotective effect on the paracetamol acetominophen (N-acetyl-p-aminophenol (APAP)) induced nephrotoxicity in rats. Twenty-four Swiss albino rats were divided into four groups (six rats each). The placebo group was orally administered sterile saline, the APAP group received APAP (200 mg·kg-1·day-1 i.p.) daily, the ES group was given ES extract orally (250 mg/kg), and the APAP + ES group received APAP as for the APAP group and administrated the ES extract as for the ES group. Pretreatment of methyl alcohol extract of ES reduced the protein expression of inflammatory parameters including cyclooxygenase-2 and nuclear factor κB in the kidney. It also reduced the mRNA gene expression of tumor necrosis factor-α and interleukin-1ß. The ES extract compensated for deficits in the total antioxidant activity, suppressed lipid peroxidation, and amended the APAP-induced histopathological kidney alterations. Moreover, ES treatment restored the elevated levels of urea nitrogen in the blood and creatinine in the serum by APAP. The ES extract attenuated the APAP-induced elevations in renal nitric oxide levels. We clarified that the ES extract has the potential to defend the kidney from APAP-induced inflammation, and the protection mechanism might be through decreasing oxidative stress and regulating the inflammatory signaling pathway through modulating key signaling inflammatory biomarkers.


Assuntos
Acetaminofen/efeitos adversos , Echinops (Planta)/química , Nefropatias/induzido quimicamente , Nefropatias/tratamento farmacológico , Rim/metabolismo , Extratos Vegetais/farmacologia , Acetaminofen/farmacologia , Animais , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Rim/patologia , Nefropatias/metabolismo , Nefropatias/patologia , Masculino , Extratos Vegetais/química , Ratos
4.
Molecules ; 24(4)2019 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-30813374

RESUMO

Three new substituted bithiophenes (1⁻3), and one new sulf-polyacetylene ester, ritroyne A (16) were isolated from the whole plant of Echinops ritro together with twelve known substituted thiophenes. The structures were elucidated on the basis of extensive spectroscopic analysis including 1D and 2D NMR as well as MS. Furthermore, the absolute configuration of ritroyne A (16) was established by computational methods. In bioscreening experiments, four compounds (2, 4, 12, 14) showed similar antibacterial activity against Staphylococcus aureus ATCC 2592 with levofloxacin (8 µg/mL). Five compounds (2, 4, 9, 12, 14) exhibited antibacterial activities against Escherichia coli ATCC 25922, with minimum inhibitory concentration (MIC) values of 32⁻64 µg/mL. Three compounds (2, 4, 12) exhibited antifungal activities against Candida albicans ATCC 2002 with MIC values of 32⁻64 µg/mL. However, compound 16 did not exhibit antimicrobial activities against three microorganisms.


Assuntos
Echinops (Planta)/química , Polímero Poliacetilênico/química , Polímero Poliacetilênico/farmacologia , Tiofenos/química , Tiofenos/farmacologia , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Extratos Vegetais/química , Staphylococcus aureus/efeitos dos fármacos
5.
Pak J Pharm Sci ; 32(2): 505-514, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31081759

RESUMO

Echinops echinatus is traditionally an important plant that finds its extensive use as a diuretic, anti-inflammatory, anti-pyretic, nerve tonic, abortifacient, aphrodisiac, antiasthmatic, and antidiabetic agent. The current study investigates protection against the hyperglycemia and dyslipidemia in alloxan-induced (type I diabetes) and fructose-fed insulin resistance (type II diabetes) models of diabetes treated with aqueous methanolic root extract of E. echinatus (Ee.Cr). Albino rats were treated orally with Ee.Cr at doses 100, 300 and 500mg/kg. The fasting blood glucose was measured by glucometer, while standard kits were used to determine the levels of serum total cholesterol, triglycerides and HDL. The administration of Ee.Cr significantly (P<0.001) reduced the FBG concentration in a dose-dependent pattern in alloxan-induced and fructose-fed diabetic rats. The Ee.Cr also corrected the dyslipidemia associated with fructose and alloxan-induced diabetes by significantly (P<0.001) decreasing the concentration of serum total cholesterol, triglycerides, and LDL and by increasing HDL concentration. Ee.Cr also significantly (P<0.001) improved the glucose tolerance in fructose-fed rats. We conclude that Ee.Cr has antidiabetic and antidyslipidemic effects in both insulin-dependent alloxan-induced diabetes and fructose-induced insulin resistance diabetes rat models.


Assuntos
Diabetes Mellitus Tipo 1/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Echinops (Planta)/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Aloxano/toxicidade , Animais , Peso Corporal/efeitos dos fármacos , Colesterol/sangue , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 1/metabolismo , Diabetes Mellitus Tipo 2/metabolismo , Dislipidemias/tratamento farmacológico , Dislipidemias/metabolismo , Feminino , Frutose/efeitos adversos , Hipoglicemiantes/química , Hipoglicemiantes/toxicidade , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Ratos Sprague-Dawley , Testes de Toxicidade Aguda , Triglicerídeos/sangue
6.
Planta ; 248(2): 323-346, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29725817

RESUMO

MAIN CONCLUSION: The exceptionally complex exine of Echinops, representing a significant investment of energy, develops from an elaborate glycocalyx which establishes, by self-assembly, a multi-layered system of micelles upon which sporopollenin polymerizes. We report on pollen development in two species of Echinops (Asteraceae, Cynareae) studied using transmission and scanning electron microscopy with an emphasis on the organisation and development of the massive sporoderm (maximum thickness 18 µm). The major events of exine deposition during the tetrad stage follow the now familiar sequence of self-assembling micellar mesophases and the subsequent incorporation of sporopollenin, observed here as: (1) spherical units with light cores; (2) columns of spherical units with dark cores; (3) large branched macromolecules arranged in a dendritic, three-dimensional network of long alveoli; and (4) alveoli with electron-transparent cores and dense walls. Later, (5) the primexine exhibits an elongated-alveolate pattern in which the alveoli have electron-dense cores and lighter exteriors. When (6) the thick inner columellae make contact with the outer primexine, sporopollenin accumulation in the cores of the primexine alveolae establishes continuity between the inner and outer columellae. In the free microspore stage, (7) the foot layer and first lamellae of the endexine appear (8). The endexine lamellae then increase in number and massive accumulation of sporopollenin occurs on all exine elements, making individual elements such as tectal spines, more pronounced. These and earlier findings, as well as experimental simulations of exine development, show that pollen wall morphogenesis involves a subtle interplay of gene-driven biological processes and physico-chemical factors offering abundant opportunities for the generation of complex, taxon-specific patterns.


Assuntos
Biopolímeros/metabolismo , Carotenoides/metabolismo , Echinops (Planta)/crescimento & desenvolvimento , Pólen/crescimento & desenvolvimento , Ontologias Biológicas , Parede Celular/ultraestrutura , Echinops (Planta)/ultraestrutura , Micelas , Microscopia Eletrônica de Varredura , Pólen/ultraestrutura
7.
Molecules ; 22(2)2017 Jan 27.
Artigo em Inglês | MEDLINE | ID: mdl-28134799

RESUMO

The screening of Chinese medicinal herbs for insecticidal principles showed that the essential oil of Echinops grijsii Hance roots possessed significant larvicidal activity against mosquitoes. The essential oil was extracted via hydrodistillation and its constituents were determined by gas chromatography-mass spectrometry (GC-MS) analysis. GC-MS analyses revealed the presence of 31 components, with 5-(3-buten-1-yn-1-yl)-2,2'-bithiophene (5-BBT, 27.63%), αterthienyl (α-T, 14.95%),1,8-cineole (5.56%) and cis-ß-ocimene (5.01%) being the four major constituents. Based bioactivity-directed chromatographic separation of the essential oil led to the isolation of 5-BBT, 5-(4-isovaleroyloxybut-1-ynyl)-2,2'-bithiophene (5-IBT) and αT as active compounds. The essential oil of E. grijsii exhibited larvicidal activity against the fourth instar larvae of Aedes albopictus, Anopheles sinensis and Culex pipiens pallens with LC50 values of 2.65 µg/mL, 3.43 µg/mL and 1.47 µg/mL, respectively. The isolated thiophenes, 5-BBT and 5-IBT, possessed strong larvicidal activity against the fourth instar larvae of Ae. albopictus(LC50 = 0.34 µg/mL and 0.45 µg/mL, respectively) and An. sinensis(LC50 = 1.36 µg/mL and 5.36 µg/mL, respectively). The two isolated thiophenes also had LC50 values against the fourth instar larvae of C. pipiens pallens of 0.12 µg/mL and 0.33 µg/mL, respectively. The findings indicated that the essential oil of E. grijsii roots and the isolated thiophenes have an excellent potential for use in the control of Ae.albopictus, An. sinensis and C. pipiens pallens larvae and could be used in the search for new, safer and more effective natural compounds as larvicides.


Assuntos
Culicidae/efeitos dos fármacos , Echinops (Planta)/química , Inseticidas/química , Inseticidas/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Raízes de Plantas/química , Animais , Cromatografia Gasosa-Espectrometria de Massas , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Parasitária , Compostos Fitoquímicos/química
8.
Molecules ; 22(11)2017 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-29160791

RESUMO

Malaria is one of the world's most severe endemic diseases and due to the emergence of resistance to the currently available medicines, the need for new targets and relevant antimalarial drugs remains acute. The crude extract, four solvent fractions and two isolated compounds from the roots of Echinops hoehnelii were tested for their antimalarial activity using the standard four-day suppressive method in Plasmodium berghei-infected mice. The 80% methanol extract exhibited suppression of 4.6%, 27.8%, 68.5% and 78.7% at dose of 50, 100, 200 and 400 mg/kg respectively. The dichloromethane fraction displayed chemosuppression of 24.9, 33.5 and 43.0% dose of 100, 200 and 400 mg/kg of body weight. Five acetylenicthiophenes were isolated from the dichloromethane fraction of which 5-(penta-1,3-diynyl)-2-(3,4-dihydroxybut-1-ynyl)-thiophene decreased the level of parasitaemia by 43.2% and 50.2% while 5-(penta-1,3-diynyl)-2-(3-chloro-4-acetoxy-but-1-yn)-thiophene suppressed by 18.8% and 32.7% at 50 and 100 mg/kg, respectively. The study confirmed the traditional claim of the plant to treat malaria and could be used as a new lead for the development of antimalarial drugs.


Assuntos
Antimaláricos/química , Antimaláricos/farmacologia , Echinops (Planta)/química , Tiofenos/química , Tiofenos/farmacologia , Animais , Antimaláricos/isolamento & purificação , Modelos Animais de Doenças , Feminino , Malária/tratamento farmacológico , Malária/parasitologia , Masculino , Camundongos , Testes de Sensibilidade Parasitária , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Plasmodium berghei/efeitos dos fármacos , Tiofenos/isolamento & purificação
9.
Bioorg Med Chem Lett ; 26(24): 5995-5998, 2016 12 15.
Artigo em Inglês | MEDLINE | ID: mdl-27865705

RESUMO

Phytochemical investigation of the roots of Echinops latifolius led to the isolation of a new carbon skeleton dimeric sesquiterpene (1) and a new thiophene (2), along with six known compounds (3-8). Their structures and relative stereochemistry were elucidated by spectroscopic and spectrometric methods (1H and 13C NMR, COSY, HSQC, HMBC, ROESY, and MS). All isolates were evaluated for their inhibition of LPS-induced NO production in RAW 264.7 cells. Compounds 4 and 5 exhibited the most potent inhibitory effects on NO production.


Assuntos
Echinops (Planta)/química , Raízes de Plantas/química , Sesquiterpenos/farmacologia , Tiofenos/farmacologia , Animais , Dimerização , Relação Dose-Resposta a Droga , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Camundongos , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Células RAW 264.7 , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade , Tiofenos/química , Tiofenos/isolamento & purificação
10.
Zhejiang Da Xue Xue Bao Yi Xue Ban ; 44(1): 43-8, 2015 01.
Artigo em Zh | MEDLINE | ID: mdl-25851974

RESUMO

OBJECTIVE: To investigate the effect of Flavonoids extracted from Echinps latifolius Tausch(FELT) on rheumatoid arthritis (RA) in rat model. METHOD: Fifty SD rats were randomly divided into model group, control group, and low, medium, and high-dose FELT groups (n=10 in each group). Complete Freund's adjuvant (0.1 mL) was used to induce RA in rats. FELT in doses of 50 mg/kg, 100 mg/kg, 150 mg/kg was given to rats in low, medium and high-dose FELT groups by gavage, and same volume of PBS was given to rats in control group. The arthritis score and the paw swelling score were measured to evaluate the therapeutic effect of FELT. Real time qPCR was used to detect the mRNA expression of fibronectin and MMP3 in synovial tissue and the mRNA expression of caspase 3, Bcl-2 and Bcl-2 associated X protein (Bax) in fibroblast-like synoviocytes (FLS). RESULTS: The arthritis score and the paw swelling score were significantly decreased in three FELT groups compared to RA model rats (P <0.05). The relative expression levels of FN and MMP3 mRNA in synovium of three FELT-treatment groups were significantly lower than those in model group (1.80, 1.76 and 1.67 vs 2.53; 1.69, 1.46 and 1.45 vs 2.67, respectively, all P <0.05). The relative expression levels of Bax and caspase 3 mRNA in FLSs of three FELT groups were higher than those in model group (0.56, 0.58 and 0.60 vs 0.30; 0.54, 0.56 and 0.59 vs 0.29, respectively, all P <0.05); while the relative expression levels of Bcl-2 mRNA in FELT groups were lower than that in model group (2.20, 2.08 and 2.08 vs 4.04, respectively, P <0.05). CONCLUSION: FELT may inhibit the synovium proliferation in RA model rats through promoting the FLS apoptosis.


Assuntos
Artrite Reumatoide/tratamento farmacológico , Echinops (Planta)/química , Flavonoides/farmacologia , Animais , Apoptose , Caspase 3/metabolismo , Modelos Animais de Doenças , Fibroblastos/metabolismo , Ratos , Ratos Sprague-Dawley , Membrana Sinovial/citologia , Proteína X Associada a bcl-2/metabolismo
11.
Chem Biodivers ; 11(7): 1001-9, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25044586

RESUMO

Structureactivity relationships of nine thiophenes, 2,2': 5',2″-terthiophene (1), 2-chloro-4-[5-(penta-1,3-diyn-1-yl)thiophen-2-yl]but-3-yn-1-yl acetate (2), 4-(2,2'-bithiophen-5-yl)but-3-yne-1,2-diyl diacetate (3), 4-[5-(penta-1,3-diyn-1-yl)thiophen-2-yl]but-3-yne-1,2-diyl diacetate (4), 4-(2,2'-bithiophen-5-yl)-2-hydroxybut-3-yn-1-yl acetate (5), 2-hydroxy-4-[5-(penta-1,3-diyn-1-yl)thiophen-2-yl]but-3-yn-1-yl acetate (6), 1-hydroxy-4-[5-(penta-1,3-diyn-1-yl)thiophen-2-yl]but-3-yn-2-yl acetate (7), 4-(2,2'-bithiophen-5-yl)but-3-yne-1,2-diol (8), and 4-[5-(penta-1,3-diyn-1-yl)thiophen-2-yl]but-3-yne-1,2-diol (9), isolated from the roots of Echinops transiliensis, were studied as larvicides against Aedes aegypti. Structural differences among compounds 3, 5, and 8 consisted in differing AcO and OH groups attached to C(3″) and C(4″), and resulted in variations in efficacy. Terthiophene 1 showed the highest activity (LC50 , 0.16 µg/ml) among compounds 1-9, followed by bithiophene compounds 3 (LC50 , 4.22 µg/ml), 5 (LC50 , 7.45 µg/ml), and 8 (LC50 , 9.89 µg/ml), and monothiophene compounds 9 (LC50 , 12.45 µg/ml), 2 (LC50 , 14.71 µg/ml), 4 (LC50 , 17.95 µg/ml), 6 (LC50 , 18.55 µg/ml), and 7 (LC50 , 19.97 µg/ml). These data indicated that A. aegypti larvicidal activities of thiophenes increase with increasing number of thiophene rings, and the most important active site in the structure of thiophenes could be the tetrahydro-thiophene moiety. In bithiophenes, 3, 5, and 8, A. aegypti larvicidal activity increased with increasing number of AcO groups attached to C(3″) or C(4″), indicating that AcO groups may play an important role in the larvicidal activity.


Assuntos
Aedes/efeitos dos fármacos , Echinops (Planta)/química , Inseticidas/química , Inseticidas/toxicidade , Tiofenos/química , Tiofenos/toxicidade , Aedes/crescimento & desenvolvimento , Aedes/fisiologia , Animais , Dípteros , Inseticidas/isolamento & purificação , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Larva/fisiologia , Extratos Vegetais/química , Raízes de Plantas/química , Tiofenos/isolamento & purificação
12.
Chem Biodivers ; 10(4): 658-76, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23576352

RESUMO

Herein, we report, for the first time, the results of detailed chemical and statistical analyses of the essential oils from the roots of two Echinops species (Asteraceae), E. bannaticus Rochel ex Schrad., and E. sphaerocephalus L., from the weed flora of Serbia. Among 106 and 81 constituents, respectively, S-containing polyacetylene compounds and triquinane sesquiterpenoids made up ca. 80% of the oils. Several of these compounds are reported here as new metabolites for the two species or even for the genus Echinops. A multivariate statistical comparison of the essential-oil composition data for these two and additional six taxa of this genus available from the literature permitted an examination of the mutual relationships of the taxa within this morphologically highly uniform genus. Principal component analysis (PCA) and agglomerative hierarchical clustering revealed a grouping of E. bannaticus and E. sphaerocephalus (both belonging to the section Echinops), and their close relationship with E. grijsii, suggesting a circumscription of this Chinese taxon to the section Echinops. PCA Correlation matrix offered valuable insight into the biosynthetic links between essential-oil constituents, and these agreed excellently with the currently proposed ones for the polyacetylene S-containing compounds, triquinanes, and monoterpenes.


Assuntos
Echinops (Planta)/química , Óleos Voláteis/química , Análise por Conglomerados , Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis/isolamento & purificação , Raízes de Plantas/química , Análise de Componente Principal
13.
Chem Biodivers ; 8(4): 614-23, 2011 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-21480507

RESUMO

Potential toxicity, costs, and drug-resistant pathogens necessitate the development of new antileishmanial agents. Medicinal and aromatic plants constitute a major source of natural organic compounds. In this study, essential oils of Artemisia absinthium L. and Echinops kebericho Mesfin were investigated by GC and GC/MS analyses. Isolated oils were screened for antileishmanial activity against two Leishmania strains (L. aethiopica and L. donovani), and toxicity on the human monocytic leukemia (THP-1) cell line and red blood cells in vitro. GC/MS Analysis revealed 65 compounds (93.74%) for Artemisia absinthium and 43 compounds (92.85%) for Echinops kebericho oil. The oils contained the oxygenated monoterpene camphor (27.40%) and the sesquiterpene lactone dehydrocostus lactone (41.83%) as major constituents, respectively. Both oils showed activity against promastigote (MIC 0.0097-0.1565 µl/ml) and axenic amastigote forms (EC(50) 0.24-42.00 nl/ml) of both leishmania species. Weak hemolytic effect was observed for both oils, showing a slightly decreased selectivity index (SI 0.8-19.2) against the THP-1 cell line. Among the two oils tested, E. kebericho exerted strong antileishmanial activity that was even higher than that of amphotericin B with significant cytotoxicity. This study, therefore, demonstrated the potential use of both oils as source of novel agents for the treatment of leishmaniasis.


Assuntos
Antiprotozoários/farmacologia , Artemisia absinthium/química , Echinops (Planta)/química , Leishmania/efeitos dos fármacos , Leishmaniose/tratamento farmacológico , Óleos Voláteis/farmacologia , Antiprotozoários/efeitos adversos , Antiprotozoários/química , Antiprotozoários/isolamento & purificação , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Hemólise/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Óleos Voláteis/efeitos adversos , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação
14.
Biomed Pharmacother ; 143: 112203, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34563954

RESUMO

Hepatic insulin resistance is a crucial pathological process in type 2 diabetes mellitus (T2DM) associated with visceral adiposity and metabolic disorders. Echinops latifolius polysaccharide B (ETPB), a polysaccharide extracted from Echinops latifolius Tausch, increases insulin sensitivity in the high-fat diet-fed and STZ induced SD rat model and even prevented hepatic metabolic disorders. However, the mechanism by which ETPB improves carbohydrate and lipid metabolisms in the liver with insulin resistance remains largely unknown. In the present work, an lnsulin resistance cell model (IR-HepG2) was established. Glucose consumption, glycogen content, triglycerides (TG), and free fatty acids (FFAs) levels were detected. The result revealed that the intervention of ETPB significantly increased glucose consumption and glycogen synthesis and reduced FFAs and TG production in IR-HepG2 cells. Further, we also employed RNA-seq to identify differentially expressed miRNAs (DEMs) and mRNAs (DEGs) with a fold change of ≥ 1.5 and p-value of <0.05. Finally, we identified 1028, 682, 382, 1614, 519 and 825 DEGs, and 71, 113, 94, 68, 52 and 38 DEMs in different comparisons, respectively. Based on a short time-series expression miner (STEM) analysis, six profiles were chosen for further analysis. Seventeen insulin resistance-associated dynamic DEGs were identified during ETPB stimulation. Based on these dynamic DEGs, the related miRNAs were acquired from DEMs, and an integrated miRNA-mRNA regulatory network was subsequently constructed. Besides, some DEGs and DEMs were validated using qPCR. This study provides transcriptomic evidence of the molecular mechanism involved in HepG2 insulin resistance, leading to the discovery of miRNA-based target therapies for ETPB.


Assuntos
Echinops (Planta) , Perfilação da Expressão Gênica , Hepatócitos/efeitos dos fármacos , Hipoglicemiantes/farmacologia , Resistência à Insulina , Palmitatos/toxicidade , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Transcriptoma , Echinops (Planta)/química , Metabolismo Energético/efeitos dos fármacos , Células Hep G2 , Hepatócitos/metabolismo , Humanos , Hipoglicemiantes/isolamento & purificação , Resistência à Insulina/genética , MicroRNAs/genética , MicroRNAs/metabolismo , Extratos Vegetais/isolamento & purificação , Polissacarídeos/isolamento & purificação , RNA-Seq
15.
Biomed Res Int ; 2021: 6670984, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33816625

RESUMO

BACKGROUND: Toxicity and untoward effects are very ostensible in most standard drugs including antipyretic agents. Searching for conceivable antipyretic drugs with minimal toxicities and side effects from traditional plants is a growing concern to date. Echinops kebericho M. (Asteraceae) is one of the most prominent traditional medicinal plants, which is frequently testified for its traditionally claimed uses of treating fever and different infectious and noninfectious disorders by traditional healers in Ethiopian folk medicine. However, this plant has not been scientifically assessed for its traditionally claimed uses. This study therefore is aimed at investigating the antipyretic and antioxidant activities of 80% methanol root extract and the derived solvent fraction of Echinops kebericho M. in mouse models. METHODS: Successive solvent maceration with increased polarity was used as the method of extractions, and chloroform, ethyl acetate, methanol, and water were used as solvents. After extraction, the crude extract and its derived solvent fractions were assessed for their antipyretic activities using yeast-induced pyrexia while, the antioxidant activities were measured in vitro using the diphenyl-2-picrylhydrazyl (DPPH) assay method. Both the extract and solvent fractions were evaluated at the doses of 100, 200, and 400 mg/kg for its antipyretic activities, and the antioxidant activity was evaluated at the doses of 50, 100, 200, 400, 600, 800, and 1000 mg/kg. The positive control group was treated with standard drug (ASA 100 mg/kg), while normal saline-receiving groups were assigned as negative control. RESULT: E. kebericho crude extract along with its derived solvent fractions showed statistically significant (p < 0.05, 0.01, and 0.001) temperature reduction activities. The maximum percentage of temperature reduction was observed by the highest dose (400 mg/kg) of the crude extract. The aqueous fraction also showed significantly (p < 0.05 and 0.01) higher temperature reduction than those of ethyl acetate and chloroform fractions. The free radical scavenging activities of the crude extract were also significantly high at the maximum dose, and the aqueous fraction showed the significantly highest antioxidant activity. CONCLUSION: In general, the data obtained from the present study clarified that the extract possessed significant antipyretic and antioxidant activities, upholding the traditionally claimed use of the plant.


Assuntos
Antioxidantes , Antipiréticos , Echinops (Planta)/química , Metanol/química , Extratos Vegetais , Raízes de Plantas/química , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Antipiréticos/química , Antipiréticos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/farmacologia
16.
Anal Bioanal Chem ; 397(5): 1975-84, 2010 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-20437033

RESUMO

Michael addition acceptors are considered as biologically active molecules, which regulate many signal pathways in cells. In the present study, it was demonstrated that the dichloromethane extract of Echinops grijisii had phase II detoxifying enzyme-inducing and nuclear factor-kappaB (NF-kappaB)-inhibiting activities, which might be attributed to the modification of key cysteine residues in Keap1 and NF-kappaB by Michael addition acceptors in it. To screen these Michael addition acceptors, glutathione (GSH) was employed, and a simple liquid chromatography-tandem mass spectrometry screening method was established to investigate the formation of GSH conjugates. Three thiophenes, 5-(penta-1,3-diynyl)-2-(3,4-diacetoxybut-1-ynyl)-thiophene (6), 2-(penta-1,3-diynyl)-5-(4-hydroxybut-1-ynyl)-thiophene (7), and 2-(penta-1,3-diynyl)-5-(3,4-dihydroxybut-1-ynyl)-thiophene (8) were demonstrated to react with GSH. Then NAD(P)H/quinone oxidoreductase1(NQO1) induction assay and an ultrafiltration mass spectrometric screening method were performed to investigate whether the above three compounds had NQO1-inducing and NF-kappaB (p65) alkylating activities. The result indicated that compounds 6-8, which had a common structural moiety, a penta-1,3-diynyl group, had strong NQO1-inducing activities, and compounds 7 and 8 could effectively alkylate the cysteine residues in NF-kappaB (p65).


Assuntos
Echinops (Planta)/química , Extratos Vegetais/química , Tiofenos/química , Alquilação/efeitos dos fármacos , Animais , Linhagem Celular , Ativação Enzimática/efeitos dos fármacos , Espectrometria de Massas , Cloreto de Metileno/química , Camundongos , Estrutura Molecular , NAD(P)H Desidrogenase (Quinona)/metabolismo , NF-kappa B/antagonistas & inibidores , NF-kappa B/química , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , Tiofenos/farmacologia
17.
Molecules ; 15(8): 5273-81, 2010 Aug 03.
Artigo em Inglês | MEDLINE | ID: mdl-20714298

RESUMO

A natural alkynol group-substituted thiophene, 2-(penta-1,3-diynyl)-5-(3,4-dihydroxybut-1-ynyl)-thiophene (PDDYT), was isolated from the roots of Echinops grijsii Hance. It possessed potent NAD(P)H: quinone oxidoreductase1 (NQO1) inducing activity and could activate Keap1-Nrf2 pathway effectively in murine hepatoma Hepa 1c1c7 cells. Further investigations indicated that the activation of Keap1-Nrf2 pathway by PDDYT might be attributed to the activation of Akt and depleting the cellular glutathione (GSH).


Assuntos
Echinops (Planta)/química , NAD(P)H Desidrogenase (Quinona)/biossíntese , Tiofenos/farmacologia , Proteínas Adaptadoras de Transdução de Sinal/metabolismo , Animais , Linhagem Celular Tumoral , Cromatografia Líquida , Proteínas do Citoesqueleto/metabolismo , Ativação Enzimática/efeitos dos fármacos , Indução Enzimática/efeitos dos fármacos , Glutationa/química , Glutationa/metabolismo , Quinase 3 da Glicogênio Sintase/metabolismo , Glicogênio Sintase Quinase 3 beta , Proteína 1 Associada a ECH Semelhante a Kelch , Espectrometria de Massas , Camundongos , Fator 2 Relacionado a NF-E2/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Tiofenos/química
18.
Nurs Outlook ; 58(2): 87-96, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-20362777

RESUMO

Despite an increasing number of feminist studies in nursing, few reviews on current trends in feminist nursing research have been published. This article aims to explore the current trends in feminist nursing research and provide recommendations for future feminist studies in nursing. In multiple database searches, 207 articles were retrieved. These were reviewed based on 5 criteria: (1) epistemological background, (2) research questions, (3) research participants, (4) research methods, and (5) implications for changes. The review indicated that feminist nurse researchers with diverse epistemological backgrounds adopted new research methods to ask new questions; expanded their focus to include differences in ethnicity, class, sexual preference, and disability; and incorporated these diversities among women in a global context in their research. Based on these findings, recommendations for future feminist research in nursing are outlined.


Assuntos
Feminismo , Pesquisa em Enfermagem/tendências , Filosofia em Enfermagem , Diversidade Cultural , Echinops (Planta) , Previsões , Necessidades e Demandas de Serviços de Saúde , Humanos , Conhecimento , Pesquisa em Enfermagem/métodos , Pós-Modernismo , Preconceito , Pesquisa Qualitativa , Projetos de Pesquisa/tendências , Saúde da Mulher
19.
Sci Rep ; 10(1): 20287, 2020 11 20.
Artigo em Inglês | MEDLINE | ID: mdl-33219310

RESUMO

In a globalized world, plant invasions are common challenges for native ecosystems. Although a considerable number of invasive plants form arbuscular mycorrhizae, interactions between arbuscular mycorrhizal (AM) fungi and invasive and native plants are not well understood. In this study, we conducted a greenhouse experiment examining how AM fungi affect interactions of co-occurring plant species in the family Asteracea, invasive Echinops sphaerocephalus and native forb of central Europe Inula conyzae. The effects of initial soil disturbance, including the effect of intact or disturbed arbuscular mycorrhizal networks (CMNs), were examined. AM fungi supported the success of invasive E. sphaerocephalus in competition with native I. conyzae, regardless of the initial disturbance of CMNs. The presence of invasive E. sphaerocephalus decreased mycorrhizal colonization in I. conyzae, with a concomitant loss in mycorrhizal benefits. Our results confirm AM fungi represent one important mechanism of plant invasion for E. sphaerocephalus in semi-natural European grasslands.


Assuntos
Echinops (Planta)/microbiologia , Glomeromycota/fisiologia , Espécies Introduzidas , Inula/microbiologia , Micorrizas/fisiologia , Echinops (Planta)/fisiologia , Europa (Continente) , Pradaria , Inula/fisiologia , Microbiologia do Solo
20.
BMC Complement Med Ther ; 20(1): 2, 2020 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-32020865

RESUMO

BACKGROUND: Echinops kebericho is widely used for treatment of a variety of diseases including infectious, non-infectious disease and fumigation during child birth. Antibacterial, antimalarial, anti-leshimania, anti-diarrheal and insect repellent activities have been elucidated. Its toxicity profile is not yet investigated and thus this study was to investigate acute and sub-acute toxicity of E. kebericho decoctions. METHODS: Acute toxicity study was performed in female Wistar albino rats with single oral dose and followed up to 14 days. The sub-acute oral dose toxicity studies were conducted in rats of both sexes in accordance with the repeated dose 28-day oral toxicity study in rodent OECD guidelines. Physical observations were made regularly during the study period while body weight was measured weekly. Organ weight, histopathology, clinical chemistry and hematology data were collected on the 29th day. Results were presented as mean ± standard deviation. One-way analysis of variance (ANOVA) was performed if assumptions were met; otherwise Kruskal-Wallis analysis was performed. RESULT: Oral administration of E. kebericho decoction showed no treatment-related mortality in female rats up to the dose of 5000 mg/kg. In sub-acute toxicity studies, no significant treatment-related abnormalities were observed compared to negative controls. Food consumption, body weight, organ weight, hematology, clinical chemistry, and histopathology did not show significant variation between controls and treatment groups. However, creatinine, relative lung weight, triglycerides, and monocytes were lower in treated compared to control groups. Significant variations between male and female groups in food consumption, relative organ weight, hematology, clinical chemistry were observed. Histolo-pathology of high-dose treated groups showed fatty liver. CONCLUSION: Echinops kebericho showed LD50 of greater than 5000 mg/kg in acute toxicity study and is well tolerated up to the dose of 600 mg/kg body weight in sub-acute toxicity study.


Assuntos
Echinops (Planta)/toxicidade , Extratos Vegetais/toxicidade , Animais , Feminino , Ratos , Ratos Wistar , Testes de Toxicidade Aguda , Testes de Toxicidade Subcrônica
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