RESUMO
Erigeron bonariensis is widely distributed throughout the world's tropics and subtropics. In folk medicine, E. bonariensis has historically been used to treat head and brain diseases. Alzheimer's disease (AD) is the most widespread form of dementia initiated via disturbances in brain function. Herein, the neuroprotective effect of the chemically characterized E. bonariensis ethanolic extract is reported for the first time in an AD animal model. Chemical profiling was conducted using UPLC-ESI-MS analysis. Female rats underwent ovariectomy (OVX) followed by 42 days of D-galactose (D-Gal) administration (150 mg/kg/day, i.p) to induce AD. The OVX/D-Gal-subjected rats received either donepezil (5 mg/kg/day) or E. bonariensis at 50, 100, and 200 mg/kg/day, given 1 h prior to D-Gal. UPLC-ESI-MS analysis identified 42 chemicals, including flavonoids, phenolic acids, terpenes, and nitrogenous constituents. Several metabolites, such as isoschaftoside, casticin, velutin, pantothenic acid, xanthurenic acid, C18-sphingosine, linoleamide, and erucamide, were reported herein for the first time in Erigeron genus. Treatment with E. bonariensis extract mitigated the cognitive decline in the Morris Water Maze test and the histopathological alterations in cortical and hippocampal tissues of OVX/D-Gal-subjected rats. Moreover, E. bonariensis extract mitigated OVX/D-Gal-induced Aß aggregation, Tau hyperphosphorylation, AChE activity, neuroinflammation (NF-κBp65, TNF-α, IL-1ß), and apoptosis (Cytc, BAX). Additionally, E. bonariensis extract ameliorated AD by increasing α7-nAChRs expression, down-regulating GSK-3ß and FOXO3a expression, and modulating Jak2/STAT3/NF-ĸB p65 and PI3K/AKT signaling cascades. These findings demonstrate the neuroprotective and memory-enhancing effects of E. bonariensis extract in the OVX/D-Gal rat model, highlighting its potential as a promising candidate for AD management.
Assuntos
Doença de Alzheimer , Erigeron , Fármacos Neuroprotetores , Ratos , Feminino , Animais , Ratos Wistar , Galactose/efeitos adversos , Cromatografia Líquida de Alta Pressão , Fosfatidilinositol 3-Quinases , Glicogênio Sintase Quinase 3 beta , Doença de Alzheimer/induzido quimicamente , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/metabolismo , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêuticoRESUMO
CONTEXT: Stomach ulcer is one of the most common gastrointestinal problems in the world. OBJECTIVE: This study aimed to isolate flavonoid compounds from methanol extract of the aerial parts of Stachytarpheta jamaicensis (L.) Vahl. and evaluate its protective and therapeutic effects against gastric ulcer. MATERIALS AND METHODS: Chromatographic techniques were used for the identification of the isolated compounds. To explore the effects of the plant extract, it was administrated by oral gavage for one week either before or post-ethanol ulcer induction. Ranitidine was also evaluated as a reference drug. Stomach pH, gastric juice volume, lesions number, glutathione, superoxide dismutase, malondialdehyde, succinate dehydrogenase, lactate dehydrogenase, acid phosphatase, Interleukin-10, intracellular adhesion molecule-1, prostaglandin E2, and total protein levels were estimated in gastric tissue. Stomach histopathological features were also monitored. RESULTS: Six flavonoid compounds were isolated, where five of them were isolated for the first time (vitexin, isovitexin, apigenin 7,4'-dimethyl ether, 5,7,2'-trimethoxyflavone, and scutellarein), while apigenin was previously reported. Treatment with plant extract recorded amelioration in all the biochemical parameters. CONCLUSION: The methanol extract of plant aerial parts had prophylactic and treatment effects against gastric ulcer in rats, where its treatment effect exceeded its protective role. The extract recorded anti-inflammatory, and antioxidant effects due to the presence of flavonoid compounds.
Assuntos
Antiulcerosos/farmacologia , Flavonoides/farmacologia , Úlcera Gástrica/prevenção & controle , Verbenaceae/química , Animais , Antiulcerosos/uso terapêutico , Biomarcadores/metabolismo , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13/métodos , Flavonoides/química , Flavonoides/isolamento & purificação , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/enzimologia , Mucosa Gástrica/patologia , Mediadores da Inflamação/metabolismo , Masculino , Estrutura Molecular , Estresse Oxidativo , Componentes Aéreos da Planta/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Espectroscopia de Prótons por Ressonância Magnética/métodos , Ratos , Ratos Wistar , Espectrofotometria Ultravioleta/métodosRESUMO
Plants belonging to the Asteraceae family are widely used as traditional medicinal herbs around the world for the treatment of numerous diseases. In this work, the chemical profiles of essential oils (EOs) of the above-ground parts of Pluchea dioscoridis (L.) DC. and Erigeron bonariensis (L.) were studied in addition to their cytotoxic and anti-aging activities. The extracted EOs from the two plants via hydrodistillation were analyzed by gas chromatography-mass spectroscopy (GC-MS). GC-MS of EO of P. dioscoridis revealed the identification of 29 compounds representing 96.91% of the total oil. While 35 compounds were characterized from EO of E. bonariensis representing 98.21%. The terpenoids were found the main constituents of both plants with a relative concentration of 93.59% and 97.66%, respectively, including mainly sesquiterpenes (93.40% and 81.06%). α-Maaliene (18.84%), berkheyaradulen (13.99%), dehydro-cyclolongifolene oxide (10.35%), aromadendrene oxide-2 (8.81%), ß-muurolene (8.09%), and α-eudesmol (6.79%), represented the preponderance compounds of EO of P. dioscoridis. While, trans-α-farnesene (25.03%), O-ocimene (12.58%), isolongifolene-5-ol (5.53%), α-maaliene (6.64%), berkheyaradulen (4.82%), and α-muurolene (3.99%), represented the major compounds EO of E. bonariensis. A comparative study of our results with the previously described data was constructed based upon principal component analysis (PCA) and agglomerative hierarchical clustering (AHC), where the results revealed a substantial variation of the present studied species than other reported ecospecies. EO of P. dioscoridis exhibited significant cytotoxicity against the two cancer cells, MCF-7 and A-549 with IC50 of 37.3 and 22.3 µM, respectively. While the EO of the E. bonariensis showed strong cytotoxicity against HepG2 with IC50 of 25.6 µM. The EOs of P. dioscoridis, E. bonariensis, and their mixture (1:1) exhibited significant inhibitory activity of the collagenase, elastase, hyaluronidase, and tyrosinase comparing with epigallocatechin gallate (EGCG) as a reference. The results of anti-aging showed that the activity of mixture (1:1) > P. dioscoridis > E. bonariensis against the four enzymes.
RESUMO
Ficus spragueana Mildbr. & Burret (family Moraceae) was reported to have various biological activities. However, its activity in treatment of renal injury has not been investigated yet. The current study aimed to evaluate the effects of F. spragueana leaf extract on nephrotoxicity caused by gentamicin. Gentamicin is an important broad-spectrum antibiotic; nevertheless, it exhibits serious nephrotoxic adverse effects. HPLC-ESI/MS spectrometric analysis of the extract revealed the presence of 37 phenolic compounds. Moreover, five compounds were isolated from the leaf extract, and identified on the basis of spectroscopic analysis. The isolated compounds were syringic acid (1), p-coumaric acid (2), 3',5' O-dicaffeoylquinic acid (3), luteolin-8-C-ß-D glucopyranoside (orientin) (4) and 8-methoxy kaempferol-3-O-[α-L-rhamnopyranosyl (1â2) ß-D-glucopyranoside] (5). The gentamicin-induced nephrotoxicity model was used to evaluate the protective effect of F. spragueana on renal toxicity biomarkers throughout the development of acute kidney injury. Administration of extract led to improvement in kidney function through inhibition of kidney injury molecule-1, creatinine, blood urea nitrogen and total bilirubin, as well as decreasing the inflammatory markers interlukin1-beta and myeloperoxidase. Furthermore, it reduced the oxidative stress by increasing reduced glutathione and total antioxidant capacity levels while decreasing malondialdehyde and nitric oxide content, and improved renal histopathological injuries.
Assuntos
Antioxidantes/farmacologia , Ficus/química , Gentamicinas/toxicidade , Rim , Estresse Oxidativo/efeitos dos fármacos , Injúria Renal Aguda/induzido quimicamente , Injúria Renal Aguda/metabolismo , Animais , Cromatografia Líquida de Alta Pressão/métodos , Modelos Animais de Doenças , Inflamação/metabolismo , Rim/efeitos dos fármacos , Rim/metabolismo , Rim/patologia , Masculino , Ressonância Magnética Nuclear Biomolecular , Extratos Vegetais/farmacologia , Ratos , Espectrometria de Massas por Ionização por Electrospray/métodosRESUMO
In the present study, a new ceramide, namely 2S, 3R-4E, 8E-2-(heptadecanoylamino)-heptadeca-4, 8-diene-1, 3-diol (1), along with four known steroids, including 24-methylcholesta-5, 24(28)-diene-3ß-ol (2), 24-methylcholesta-5, 24(28)-diene-3ß-acetate (3), 4-methyl-24-methylcholesta-22-ene-3-ol (4), and cholesterol, was isolated and characterized from CH2Cl2/MeOH extract of Cespitularia stolonifera. A new acetate derivative of compound 1, termed 2S, 3R-4E, 8E-2-(heptadecanoylamino)-heptadeca-4, 8-diene-1, 3-diacetate (1a), was also prepared in the present study. All the structures were established on the basis of modern spectroscopic techniques, including FT-IR, 1D, 2D-NMR, HRESI-MS, and GC-MS, in addition of chemical methods. (-)-Alloaromadendren, ledane, (1)-alloaromadendren oxide, isoaromadendrene epoxide and (-)-caryophellen oxide were identified from the n-hexane fraction using GC-MS. The extract and the two ceramides (1) and (1a) exhibited significant cytotoxic activity against lung cancer A549 cells, while the extract and the two steroids (2) and (3) exhibited significant cytotoxic activity against breast cancer MCF-7 cells. The CH2Cl2/MeOH extract exhibited significant antiulcer activity in both ethanol and acetic acid induced ulcer models in rats, as evidenced by histopathological, histochemical, and biochemical examinations.
Assuntos
Antozoários/química , Antiulcerosos/farmacologia , Antineoplásicos/farmacologia , Produtos Biológicos/farmacologia , Ceramidas/farmacologia , Esteroides/farmacologia , Células A549 , Ácido Acético , Animais , Antiulcerosos/química , Antiulcerosos/isolamento & purificação , Antiulcerosos/uso terapêutico , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/uso terapêutico , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/uso terapêutico , Neoplasias da Mama/tratamento farmacológico , Ceramidas/química , Ceramidas/isolamento & purificação , Ceramidas/uso terapêutico , Modelos Animais de Doenças , Etanol , Feminino , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Células MCF-7 , Espectroscopia de Ressonância Magnética/métodos , Ratos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Esteroides/química , Esteroides/isolamento & purificação , Esteroides/uso terapêutico , Úlcera/induzido quimicamente , Úlcera/tratamento farmacológicoRESUMO
BACKGROUND: Albizia species are rich in phenolics and terpenes in the different plant organs. They are widely used in traditional Chinese medicine. So this study investigated the phytochemical and biological activities of Albizia Anthelmintica. MATERIALS AND METHODS: Column chromatography has been performed for the isolation of compounds. Bioactivity studies of A. anthelmintica leaves were carried out on aqueous ethanol extract and some pure compounds were tested for their antioxidant activities. RESULTS: Eight compounds have been isolated for the first time from A. anthelmintica. The aqueous ethanol extract of A. anthelmintica showed moderate anti-inflammatory activity and significant for both analgesic and antioxidant activities. Quercetin-3-O-ß-D-glucopyranoside, kaempferol-3-O-ß-D-glucopyranoside, kaempferol-3-O-(6ß-O-galloyl-ß-D-glucopyranoside and quercetin-3-O-(6ß-O-galloyl-ß-D-glucopyranoside) exhibited potent antioxidant scavenging activity towards diphenyl-picrylhydrazine.
RESUMO
BACKGROUND: Cynara scolymus L. (Asteraseae) (artichoke) is commonly eaten as a vegetable; its leaves are frequently used in folk medicine in the treatment of hepatitis, hyperlipidaemia, obesity and dyspeptic disorders. The purpose of this study is to determine the chemical composition of the volatile oil and alcoholic extract of artichoke head scales. In addition, the role of the methanol extract as an anti-ulcer agent against ethanol-induced gastric ulcer in rats was evaluated. RESULTS: Six flavonoids and one phenolic acid were obtained from the methanol extract. Also, 37 compounds were identified in the volatile oil, the majority including mono- and sesquiterpenes. The artichoke extracts (200 and 400 mg kg(-1)) significantly (P < 0.05) reduced the ulcer index (55.33% and 72.14% inhibition). Histopathological examination of rat stomachs demonstrated that artichoke induced an increase in gastric mucus production, and a reduction of the depth and severity of mucosal lesions. Artichoke dose-dependently reduced the elevated ethanol gastric malonylaldehyde, and reduced glutathione levels and catalase activity. These results suggest that the head scales of artichoke possess potential anti-ulcer activity. CONCLUSIONS: The present paper describes the identification of volatile oil for the first time along with the isolation and identification of the constituents of the methanol extract. Moreover, the high anti-ulcerogenic potential of scales of C. scolymus heads was established here for the first time.
Assuntos
Antiulcerosos/uso terapêutico , Cynara/química , Flavonoides/uso terapêutico , Óleos Voláteis/uso terapêutico , Fenóis/uso terapêutico , Fitoterapia , Úlcera Gástrica/tratamento farmacológico , Animais , Antiulcerosos/isolamento & purificação , Antiulcerosos/farmacologia , Catalase/metabolismo , Relação Dose-Resposta a Droga , Etanol , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Glutationa/metabolismo , Inflorescência/química , Malondialdeído/metabolismo , Monoterpenos/análise , Monoterpenos/farmacologia , Monoterpenos/uso terapêutico , Muco/metabolismo , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Fenóis/isolamento & purificação , Fenóis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Sprague-Dawley , Sesquiterpenos/análise , Sesquiterpenos/farmacologia , Sesquiterpenos/uso terapêutico , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patologiaRESUMO
Investigation of the aqueous alcoholic extract of Pyruscalleryana Decne. leaves led to the isolation of two new phenolic acids glycosides, namely protocatechuoylcalleryanin-3-O-ß-glucopyranoside (1) and 3'-hydroxybenzyl-4-hydroxybenzoate-4'-O-ß-glucopyranoside (2), together with nine known compounds among them lanceoloside A and methylgallate, which have been isolated for the first time from the genus Pyrus. Structures of the isolated compounds were established by spectroscopic analysis, including UV, IR, HRESI-MS, and 1D/2D NMR. The total extract and some isolated compounds were determined against DPPH (2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydrazinyl radical, for their free radical scavenging activity, the total alcoholic extract showed strong antioxidant activity while the two new compounds showed weak antioxidant activity.
Assuntos
Sequestradores de Radicais Livres/química , Fenóis/química , Extratos Vegetais/química , Pyrus/química , Sequestradores de Radicais Livres/isolamento & purificação , Estrutura Molecular , Fenóis/isolamento & purificação , Extratos Vegetais/isolamento & purificaçãoRESUMO
In addition to apigenin, apigenin 7-O-glucoside, kaempferol 3-O-glucoside, kaempferol 3,7-di-O-rhamnoside, quercetin, and quercetin 3-O-glucoside, the methanolic extract of Fagonia taeckholmiana afforded a new compound identified as kaempferol 3-O-beta-l-arabinopyranosyl-(1-->4)-alpha-l-rhamnopyranoside-7-O-alpha-l-rhamnopyranoside. Identification of the isolated compounds was based on chemical and spectroscopic analyses including UV, FABMS, (1)H, (13)C and 2D NMR, and DEPT. The cytotoxic activities of the compounds against several cancer cell lines were determined.
Assuntos
Antineoplásicos/isolamento & purificação , Glicosídeos/isolamento & purificação , Plantas Medicinais/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Glicosídeos/química , Glicosídeos/farmacologia , Humanos , Quempferóis , Metanol , Extratos Vegetais , TrissacarídeosRESUMO
In addition to luteolin and its 7-methyl ether, the CH2Cl2-MeOH (1:1) extract of Cyperus conglomeratus afforded two new prenylflavans identified as 7,3'-dihydroxy-5,5'-dimethoxy-8-prenylflavan and 5,7,3'-trihydroxy-5'-methoxy-8-prenylflavan. The structures were established by CIMS, 1H-NMR, 13C-NMR, H-H COSY, HMQC, HMBC and DEPT analysis.
Assuntos
Cyperus/química , Flavonoides/isolamento & purificação , Flavonoides/química , Luteolina/isolamento & purificaçãoRESUMO
A benzoquinone, named alopecuquinone, was isolated from the ethanol extract of the inflorescences of Cyperus alopecuroides. Its structure was primarily elucidated by spectroscopic analysis including 1H, 13C NMR, APT, HMQC, 1H-1H COSY and CIMS. The known flavonoids, vicenin 2, orientin, diosmetin, quercetin 3,3'-dimethyl ether and its 3,4'-dimethyl ether, were also isolated and characterized. The ethanol extract of the plant material showed moderate estrogenic activity using a strain of Saccharomyces cerevisiae.