RESUMO
Cuphea ignea A. DC. is an ornamental tropical plant belonging to the family Lythraceae. The aim of this study is to verify the in vivo antihypertensive potential of C. ignea A. DC. and to explore its metabolic profile using a UHPLC-Orbitrap-HRMS technique. The results revealed that the ethanolic extract of the leaves in two doses (250 and 500 mg/kg b.wt.) significantly normalized the elevated systolic blood pressure in N(G)-nitro-l-arginine-methyl ester-induced hypertension in rats. An angiotensin-converting enzyme (ACE) concentration was significantly decreased by the high dose extract compared to lisinopril. Nitric oxide (NO) level was significantly restored by both doses. Concerning the oxidative stress parameters, both doses displayed significant reduction in malondialdehyde (MDA) level while the high dose restored elevated glutathione level. These biochemical results were clearly supported by the histopathological examination of the isolated heart and aorta. A UHPLC-Orbitrap-HRMS study was represented by a detailed metabolic profile of leaves and flowers of C. ignea A. DC., where 53 compounds were identified among which flavonoids, fatty acids, and hydrolysable tannins were the major identified classes. This study established scientific evidence for the use of C. ignea A. DC., a member of genus Cuphea as a complementary treatment in the management of hypertension.
RESUMO
BACKGROUND: The current work planned to evaluate Cordia africana Lam. stem bark, a traditionally used herb in curing of different ailments in Africa such as gastritis and wound infections, based on phytochemical and antibacterial studies of two pathogenic microorganisms: methicillin-resistant Staphylococcus aureus (MRSA) and Helicobacter pylori. METHODS: High performance liquid chromatography (HPLC) profiling was used for qualitative and quantitative investigation of the ethanol extract. The minimum inhibitory concentration (MIC) of the ethanolic extract and isolated compounds was estimated using the broth microdilution method and evidenced by molecular dynamics simulations. RESULTS: Four compounds were isolated and identified for the first time: α-amyrin, ß-sitosterol, rosmarinic acid (RA) and methyl rosmarinate (MR). HPLC analysis illustrated that MR was the dominant phenolic acid. MR showed the best bacterial inhibitory activity against MRSA and H. pylori with MIC 7.81 ± 1.7 µg/mL and 31.25 ± 0.6, respectively, when compared to clarithromycin and vancomycin, respectively. CONCLUSION: The antibacterial activity of the stem bark of Cordia africana Lam. was evidenced against MRSA and H. pylori. Computational modeling of the studied enzyme-ligands systems reveals that RA and MR can potentially inhibit both MRSA peptidoglycan transpeptidases and H. pylori urease, thereby creating a pathway via the use of a double target approach in antibacterial treatment.
Assuntos
Cordia , Helicobacter pylori , Staphylococcus aureus Resistente à Meticilina , Antibacterianos/química , Simulação por Computador , Cordia/química , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Casca de Planta/química , Extratos Vegetais/químicaRESUMO
Many researches have been undergone to hasten the natural wound healing process. In this study, several Hibiscus species (leaves) were extracted with petroleum ether, methanol, and their mucilage was separated. All the tested species extracts were assessed for their viability percentage using the water-soluble tetrazolium. H.syriacus was the plant of choice to be incorporated in a new drug delivery system and evaluated for its wound healing activity. H.syriacus petroleum ether extract (PEE) showed a high percentage of palmitic and oleic acids while its mucilage demonstrated high glucosamine and galacturonic acid. It was selected to be formulated and pharmaceutically evaluated into three different composite sponges using chitosan in various ratios. Fourier-transformed infrared spectroscopy investigated the chemical interaction between the utilized sponges' ingredients. Morphological characteristics were evaluated using scanning electron microscopy. H.syriacus composite sponge of mucilage: chitosan (1:5) was loaded with three different concentrations of PEE. Medicated formulations were assessed in rat model of excision wound model. The wound healing ability was clearly proved by the clinical acceleration, histopathological examination, and modulation of correlated inflammatory parameters as tumor necrosis factor in addition to vascular endothelial growth factor suggesting a promising valuable candidate that supports the management of excision wounds using single-dose preparation.
Assuntos
Hibiscus , Lipídeos/administração & dosagem , Extratos Vegetais/administração & dosagem , Pele/efeitos dos fármacos , Tampões de Gaze Cirúrgicos , Cicatrização/efeitos dos fármacos , Ferimentos Penetrantes/tratamento farmacológico , Administração Cutânea , Animais , Linhagem Celular , Quitosana/administração & dosagem , Modelos Animais de Doenças , Hibiscus/química , Humanos , Mediadores da Inflamação/metabolismo , Lipídeos/isolamento & purificação , Masculino , Extratos Vegetais/isolamento & purificação , Ratos Wistar , Reepitelização/efeitos dos fármacos , Pele/lesões , Pele/metabolismo , Pele/patologia , Fator de Crescimento Transformador beta/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismo , Ferimentos Penetrantes/metabolismo , Ferimentos Penetrantes/patologiaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Combretum aculeatum Vent was traditionally used in Sudan, Eretria and Ethiopia as anti-inflammatory in case of skin inflammation, catarrh, wounds, scorpion stings and snake bites. Nevertheless, there is no scientific information regarding this activity. AIM OF STUDY: The present study aimed to evaluate the phytochemical constituents and the scientific basis for the traditional use of Combretum aculeatum Vent through studying its anti-inflammatory properties for the first time to illustrate the putative mechanisms behind this bioactivity. MATERIALS AND METHODS: the ethanolic extract was partitioned by petroleum ether, methylene chloride, ethyl acetate, and n-butanol saturated with water. The petroleum ether fraction was saponified and the saponifiable and unsaponifiable fractions were analyzed on GC/MS. The different fractions were subjected to phytochemical investigation to isolate pure compounds. In-vivo anti-inflammatory activity of the ethanolic extract was evaluated using carrageenan induced rat paws edema method at doses of 200, 400 and 600â¯mg/kg and proved based on histopathological and biochemical parameters. RESULTS: Five known compounds were isolated for the first time from the aerial parts of Combretum aculeatum Vent: quercetin, vitexin, isorhamnetin 3-O-ß-glucoside, isovitexin and rutin, in addition to two previously isolated ones: ß-sitosterol and its glucoside. The ethanolic extract evidenced in-vivo anti-inflammatory activity by oral intake of 400â¯mg/kg of the ethanolic extract significantly (Pâ¯≥â¯0.05) decreased the paw edema (only 32±1.9% increase in paw weight after 4â¯h) compared to indomethacin (28.6±2.5%). Moreover, it significantly suppressed the serum malondialdehyde (MDA) and nitric oxide (NO) and increased the GSH to be 11.76±0.85, 5.13±0.62 µmol/mL and 5.66±0.28 µM/mL, respectively. It diminished the serum cytokines TNF-α, IL-6 and IL-1ß levels to be 39.1±1.2, 32.6±1.1 and 37.5±1.2â¯pg/mL, respectively. Results are accompanied by histopathological examination. CONCLUSION: Overall, the results herein presented significant anti-inflammatory properties traditionally ascribed to Combretum aculeatum Vent. Moreover, the biochemical mechanisms associated to this action were highlighted, introducing new prospects for the development of effective anti-inflammatory herbal medicinal products.
Assuntos
Anti-Inflamatórios , Combretum , Edema/tratamento farmacológico , Compostos Fitoquímicos , Extratos Vegetais , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios/toxicidade , Carragenina , Citocinas/imunologia , Edema/induzido quimicamente , Edema/imunologia , Edema/patologia , Dose Letal Mediana , Masculino , Camundongos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Extratos Vegetais/toxicidade , Ratos , SudãoRESUMO
BACKGROUND: Natural antioxidants and anti-inflammatory agents have the ability to restore normal balance to destructed liver cells. The genus Erythrina has attracted attention for its broad spectrum of physiological activities and its rich polyphenolic and alkaloid contents. HYPOTHESIS/PURPOSE: The major phytoconstituents of Erythrinaâ¯×â¯neillii, an ornamental coral tree and a hybrid between E. herbacea and E. humeana that was not previously studied, were investigated. The hepatoprotective effect and underlying mechanisms were also assessed. STUDY DESIGN AND METHODS: The main phytoconstituents in the different fractions of the alcoholic leaf extract (dichloromethane and ethyl acetate) were identified using high resolution high-performance liquid chromatography coupled with mass spectrometry (HR-HPLC-MS-MS) based on the fragmentation pattern and molecular formula of the identified compounds and on previous literature. In addition, the hepatoprotective, anti-inflammatory and antioxidant activities of three doses of E.â¯×â¯neillii alcoholic leaf extract (100, 250, 500â¯mg/kg) were investigated in methotrexate (MTX)-intoxicated rats and were compared with those of silymarin-treated rats. Liver function parameters were obtained, and a histopathological study was performed. In addition, the anti-inflammatory mediators and the antioxidant system in the liver tissues were assessed. RESULTS: The dichloromethane extract revealed an abundance of alkaloids (25), in addition to tentatively identifying flavone (1), flavanone (1) and three fatty acids. Additionally, thirty-six compounds belonging to different classes of phytoconstituents with a predominance of flavonoids (21), O/C-flavone and flavonol glycosides, followed by alkaloids (9), fatty acids (4) and (2), and phenolic glycoside were identified in the ethyl acetate extract. Compared with MTX, alcoholic leaf extract (500â¯mg/kg) ameliorated the MTX-induced alterations by improving several biochemical marker levels, fighting oxidative stress in serum and liver tissues, and decreasing inflammatory mediators; this finding was further confirmed by the histopathological study. CONCLUSION: This study reveals E.â¯×â¯neillii, a rich source of flavonoids and alkaloids, which could be further exploited to provide a promising and safe antihepatotoxic agent source.
Assuntos
Erythrina/química , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Flavonoides/química , Glicosídeos/análise , Glicosídeos/química , Fígado/metabolismo , Fígado/patologia , Masculino , Metotrexato/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Folhas de Planta/química , Substâncias Protetoras/química , Ratos Wistar , Espectrometria de Massas em TandemRESUMO
Investigation of the ethanol extract of the corms of Liatris spicata (L.) willd led to the isolation of two sterols: stigmasterol and its 3-O-glucoside, a triterpene: obtusifoliyl acetate, two benzofurans: euparin and 6-hydroxy-3-methoxytremetone, three phenolic acids: protocatechuic, vanillic and ferulic acid and a sesquiterpene lactone igalan. The structures of the isolated compounds were established on the basis of physicochemical properties and spectral analysis (IR, EI/MS, 1H NMR and 13C NMR). The ethanol extract and its isolated compounds evidenced cytotoxic activities against human liver cancer cell line (HepG2), where igalan showed the highest potency (3.83 ± 0.043) µg/mL, its effect was comparable to that of the standard drug doxorubicin® (3.73 ± 0.036) µg/mL.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Asteraceae/química , Ácidos Cumáricos/isolamento & purificação , Etanol , Glucosídeos/isolamento & purificação , Células Hep G2 , Humanos , Hidroxibenzoatos/isolamento & purificação , Estrutura Molecular , Extratos Vegetais/química , Análise EspectralRESUMO
Phytochemical investigation of the flowering aerial parts of Asteriscus maritimus (L.) Less (Asteraceae) led to the isolation of a new compound: patuletin 7-O-ß-D-[(2â³'S) 6â³(3â³'-hydroxy-2â³'-methyl-propanoyl)] glucopyranoside, together with five known metabolites; ß-sitosterol 2, chlorogenic acid 3, P-hydroxy -methylbenzoate 4, luteolin 5 and protocatechuic acid 6. The structures of the isolated compounds were determined by comprehensive analyses of its 1D and 2D NMR, HRMS and compared with previously known analogues. The ethanolic extract of the flowering aerial parts of A. maritimus was found to be safe (LD50 = 4.6 mg/kg) and possess significant antioxidant and anti-inflammatory activities and this was in accordance with its high phenolic content (107.36 ± 0.051 mg GAE/g extract).