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1.
Nat Prod Res ; 34(2): 300-304, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30375259

RESUMO

A phytochemical study was carried out on Ajuga multiflora, and obtained a novel ursane-type triterpene saponin, i.e., 3-epi-ursolic acid 3-O-palmitoyl 28-O-α-L-arabinofuranosyl ester (1), named ajugoside. Its structure and relative configuration were identified mainly by spectroscopic methods including 1D- and 2D-NMR techniques as well as HR-MS analysis. This paper described the isolation and structural elucidation of ajugoside (1) for the first time.


Assuntos
Ajuga/química , Glucosídeos/química , Piranos/química , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Glucosídeos/isolamento & purificação , Conformação Molecular , Estrutura Molecular , Extratos Vegetais/análise , Extratos Vegetais/química , Piranos/isolamento & purificação , Saponinas/química , Triterpenos/química
2.
Am J Chin Med ; 47(5): 959-1003, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31416340

RESUMO

The present review is aimed at providing a comprehensive summary of the botanical characteristics, ethnomedicinal uses, phytochemical, pharmacological, and toxicological studies of the genus Ajuga L. The extensive literature survey revealed Ajuga L. species to be a group of important medicinal plants used for the ethnomedical treatment of rheumatism, fever, gout, sclerosis, analgesia, inflammation, hypertension, hyperglycemia, joint pain, palsy, amenorrhea, etc., although only a few reports address the clinical use and toxicity of these plants. Currently, more than 280 chemical constituents have been isolated and characterized from these plants. Among these constituents, neo-clerodane diterpenes and diterpenoids, phytoecdysteroids, flavonoids, and iridoids are the major bioactive compounds, possessing wide-reaching biological activities both in vivo and in vitro, including anti-inflammatory, antinociceptive, antitumor, anti-oxidant, antidiabetic, antimicrobial, antifeedant, antidiarrhoeal, hypolipidemic, diuretic, hypoglycaemic, immunomodulatory, vasorelaxant, larvicidal, antimutagenic, and neuroprotective activity. This review is aimed at summarizing the current knowledge of the ethnomedicinal uses, phytochemistry, biological activities, and toxicities of the genus Ajuga L. to reveal its therapeutic potentials, offering opportunities for future researches. Therefore, more focus should be paid to gathering information about their toxicology data, quality-control measures, and the clinical application of the bioactive ingredients from Ajuga L. species.


Assuntos
Ajuga/química , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Compostos Fitoquímicos/farmacologia , Animais , Antidiarreicos/efeitos adversos , Antidiarreicos/química , Antidiarreicos/farmacologia , Antineoplásicos/efeitos adversos , Antineoplásicos/química , Antineoplásicos/farmacologia , Antioxidantes/efeitos adversos , Antioxidantes/química , Antioxidantes/farmacologia , Medicamentos de Ervas Chinesas/efeitos adversos , Humanos , Medicina Tradicional , Compostos Fitoquímicos/efeitos adversos , Compostos Fitoquímicos/química
3.
Molecules ; 24(8)2019 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-31018502

RESUMO

Several Ajuga species are used in Romanian folk medicine for their antioxidant, antimicrobial and anti-inflammatory properties, to treat pain, fever or arthritis. Still, the active compounds responsible for these effects and their mechanism of action are scarcely known. This research was designed to investigate the phytochemical profile (e.g. iridoids, polyphenolic compounds, phytosterols), as well as the biological potential (antioxidant, antibacterial, antifungal, anti-inflammatory properties) of two selected Ajuga species collected from different regions of Romanian spontaneous flora. The main compounds identified in A. reptans aerial parts extracts were 8-O-acetylharpagide, isoquercitrin and ß-sitosterol, whilst in A. genevensis were 8-O-acetylharpagide, luteolin and campesterol. The extracts were screened for their antioxidant potential using different methods (DPPH, TEAC, EPR) and the results showed a good activity, in accordance with the polyphenol content (18-26 mg GAE/g dw). The antifungal activity on the tested strains was good. The determination of few parameters linked with the inflammatory mechanism allowed the assessment of in vivo anti-inflammatory potential. Ajuga reptans and A. genevensis ethanol extracts had anti-inflammatory activity through lowering the oxidative stress, phagocytosis, PMN and total leukocytes. The best anti-oxidative and anti-inflammatory activity was observed for the Ajuga reptans 100 mg dw/mL extract when compared with diclofenac, thus the dose could be correlated with the pharmacological effect. These findings provide substantial evidence that both selected Ajuga species have the potential to be valued as sources of phytochemicals in effective anti-inflammatory herbal preparations.


Assuntos
Ajuga/química , Iridoides/farmacologia , Fitosteróis/farmacologia , Fitoterapia/métodos , Polifenóis/farmacologia , Animais , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Compostos de Bifenilo/antagonistas & inibidores , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Humanos , Inflamação/tratamento farmacológico , Iridoides/química , Iridoides/isolamento & purificação , Testes de Sensibilidade Microbiana , Neutrófilos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Fagocitose/efeitos dos fármacos , Fitosteróis/química , Fitosteróis/isolamento & purificação , Picratos/antagonistas & inibidores , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Plantas Medicinais , Polifenóis/química , Polifenóis/isolamento & purificação , Ratos , Ratos Wistar , Romênia
4.
J Photochem Photobiol B ; 193: 109-117, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30836321

RESUMO

Ajuga bracteosa an important medicinal herb, is getting endangered worldwide due to destructive harvesting by pharmaceutical industries in its different habitats. It is in dire need for protection and demands conservation and sustainable utilization. In the present study, effects of α-naphthalene acetic acid (NAA) under different spectral lights were estimated on the growth, secondary metabolism and biosynthesis of phenolic acids in adventitious roots (AR) cultures of A. bracteosa. Among the different spectral lights, highest AR induction frequency (88%) and formation of biomass (72 g/L FW and 22 g/L DW) were recorded in explants incubated in the presence of 1.5 mg/L NAA under yellow light. Maximum production of poly phenols (TPC;44.2 mg) and flavonoids (TFC;2.51 mg) were recorded in the AR cultures grown in the presence of blue light. Further, highest total protein content of (401.6 µg) was detected in the AR in response to normal white light. Blue spectral light induced maximum superoxide dismutase (SOD; 2.5 nM) and peroxidase activity (POD;0.85 nM) respectively, in AR cultures. Compared with other monochromatic lights, red light significantly enhanced the antioxidant potential of the AR cultures. Analysis through High performance liquid chromatography (HPLC-DAD) revealed significant variations in the levels of important phenolic acids such as gallic acid, catechin, rutin, caffeic acid, myricetin and apigenin in the AR samples treated with the lights of different spectra.


Assuntos
Ajuga/metabolismo , Biomassa , Luz , Ajuga/crescimento & desenvolvimento , Ajuga/efeitos da radiação , Antioxidantes/química , Catequina/análise , Catequina/metabolismo , Cromatografia Líquida de Alta Pressão , Flavonoides/química , Flavonoides/metabolismo , Ácido Gálico/análise , Ácido Gálico/metabolismo , Proteínas de Plantas/metabolismo , Raízes de Plantas/metabolismo , Raízes de Plantas/efeitos da radiação , Polifenóis/química , Polifenóis/metabolismo , Rutina/análise , Rutina/metabolismo
5.
J Photochem Photobiol B ; 190: 59-65, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30500677

RESUMO

Ajuga bracteosa (A. bracteosa) is one of the critically endangered and high-valued medicinal plants worldwide. Light is one of the major factor or stimulus involved in the morphogenic responses and bioactive compounds production in various medicinal plants. In this study, unique properties of colored lights have been observed on induction of somatic embryos from non-embryonic calli cultures of A. bracteosa. The maximum callogenic response (92.32%) from leaf explants was observed on Murashige and Skoog (MS) medium augmented with benzyl adenine (BA; 2.0 l-1) and 2, 4-Dichlorophenoxy acetic acid (2.4-D; 1.0 mg l-1). Calli cultures with same hormonal concentrations were placed under different spectral lights for somatic embryogenesis and photochemical variations. Red lights were found effective for maximum somatic embryos induction (92.75%) with optimum biomass accumulation (152.64 g l-1) on day 40. Similarly, among all the spectral lights, red light exhibited the highest DPPH-radical scavenging activity (DRSA; 92.86%). In contrast, blue lights induced maximum biosynthesis of chemically important total phenolics content and total flavonoids content (TPC; 0.264 and TFC; 0.06 mg/g-DW), respectively. Furthermore, blue, green and red lights also enhanced phenolics and production, polyphenolics content and total polyphenolics production in somatic embryos. It is concluded that exposure of calli cultures to colored lights provides an effective and promising in vitro technique for conservation of endangered A. bracteosa species and enhancement of its bioactive compounds. Steps should be taken to adopt these strategies/ techniques at a larger scale in order to yield maximum benefits from this highly valued medicinal plant species.


Assuntos
Ajuga/fisiologia , Desenvolvimento Embrionário/efeitos da radiação , Plantas Medicinais/fisiologia , Biomassa , Cor , Flavonoides/análise , Luz , Fenóis/análise
6.
Nat Prod Res ; 33(19): 2856-2859, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30422013

RESUMO

A new abietane diterpenoid glycoside, ajugaside B (1), along with three known compounds (2-4), were isolated from the whole plants of Ajuga ovalifolia var. calantha. The structure of the new compound (1) was elucidated by means of spectroscopic analyses (HRESIMS, IR, NMR and ECD). All of the isolated compounds were evaluated for their antitumor activities against MGC803, MCF-7, A549, HT29 and HepG2 cell lines. Compounds 3-4 showed moderate cytotoxicity against all tested cell lines with IC50 values of 1.8-7.3 µM.


Assuntos
Abietanos/farmacologia , Ajuga/química , Antineoplásicos Fitogênicos/farmacologia , Abietanos/química , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Glicosídeos/química , Glicosídeos/farmacologia , Humanos , Estrutura Molecular , Extratos Vegetais/química
7.
Molecules ; 23(9)2018 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-30150579

RESUMO

This study describes an innovative in-line near-infrared (NIR) process monitoring method for the quantification of the total polyphenolic content (TPC) of Ajuga genevensis dry extracts. The dry extract was obtained in a fluidized bed processor, by spraying and adsorbing a liquid extract onto an inert powder support. NIR spectra were recorded continuously during the extract's spraying process. For the calibration of the in-line TPC quantification method, samples were collected during the entire process. The TPC of each sample was assessed spectroscopically, by applying a UV-Vis reference method. The obtained values were further used in order to develop a quality OPLS prediction model by correlating them with the corresponding NIR spectra. The final dry extract registered good flowability and compressibility properties, a concentration in active principles three times higher than the one of the liquid extract and an overall process yield of 85%. The average TPC's recovery of the NIR in-line prediction method, compared with the reference UV-Vis one, was 98.7%, indicating a reliable monitoring method which provided accurate predictions of the TPC during the process, permitting a good process overview and enabling us to establish the process's end point at the exact moment when the product reaches the desired TPC concentration.


Assuntos
Polifenóis/análise , Polifenóis/química , Espectroscopia de Luz Próxima ao Infravermelho , Ajuga/química , Extração Líquido-Líquido , Extratos Vegetais/química
8.
Fitoterapia ; 129: 7-12, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29894737

RESUMO

Five novel compounds, including four neoclerodane diterpenoids, named ajugacumbins KN (1-4) along with a phytoecdysterone, named ajugacetalsterone E (5), were isolated from the whole herbs of Ajuga decumbens (Labiatae). Their structures were elucidated on the basis of detailed spectroscopic analysis including IR, HRESIMS, CD, 1D and 2D NMR spectroscopic experiments. Compounds 1-5 were evaluated for their cytotoxic activities and the effects on superoxide anion generation and elastase release in FMLP/CB-induced human neutrophils.


Assuntos
Ajuga/química , Diterpenos/química , Neutrófilos/efeitos dos fármacos , Elastase Pancreática/metabolismo , Superóxidos/metabolismo , Linhagem Celular Tumoral , Diterpenos/farmacologia , Diterpenos Clerodânicos , Humanos , Estrutura Molecular
9.
Microb Pathog ; 121: 173-178, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29775724

RESUMO

The use of synthetic food additive and the appearance of antibiotic resistance are at the basis of important human health problems. The substitution of synthetic compounds with new natural substances extracted from plants or microorganisms is therefore the ideal solution to this scourge. The objective of this work was to evaluate the phyto-constituents (polyphenols, flavonoids and condensed tannins), and to test the biological activities (antioxidant, antibacterial and antiviral) of the Ajuga iva (L) aerial part extracts. The antioxidant activity assayed by DPPH method showed an IC50 of 0.43 ±â€¯0.03 mg/mL. Antibacterial activity of aqueous and hydro methalonic extracts was tested against seven pathogenic bacteria (Staphylococcus aureus, Methicillin Resistant Staphylococcus aureus (MRS), Listeria monocytogenes, Pseudomonas aeruginosa, Bacillus cereus, Escherichia coli and Salmonella enteritidis) using the diffusion method. A Thin Layer Chromatography-bioautotography-guided was performed, and the isolated antibacterial fraction was identified by CG-MS analysis. Antiviral effect of methanolic extract performed on 4 viruses: Coxsackie Virus type B-3 (CVB-3), Adenovirus type 5 (ADV-5), Respiratory Syncytial Virus type B (RSV-B) and Herpes Simplex Virus type 2 (HSV-2) showed an activity against Coxsackie Virus. As a result of this study, the aerial parts of Ajuga iva (L) extract could be used in the food, cosmetic, medical and health sectors.


Assuntos
Ajuga/química , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Antivirais/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Argélia , Bactérias/efeitos dos fármacos , Cromatografia em Camada Delgada , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Extratos Vegetais/análise , Vírus/efeitos dos fármacos
10.
J Photochem Photobiol B ; 183: 242-250, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29730585

RESUMO

Light is an important physical factor necessary for the growth, morphogenesis and production of bioactive compounds in plants. In this study, effects of different photoperiod regimes and hormonal elicitors were investigated on the accumulation of biomass, antioxidant potential and biosynthesis of secondary volatiles in the cell cultures of Ajuga bracteosa. Maximum accumulation of biomass (13.2 g/L) was recorded in cell cultures established at 1.0 mg/L benzylaminopurine (BA) in exposure to continuous dark. Biochemical assays showed that in the presence of 0.5 methyl jasmonate (Me-J), cell cultures grown under continuous dark had the higher activities of superoxide dismutase (SOD: 4.5 U/mg), peroxidase (POD: 3.1 U/mg), total phenolic content (TPC: 8.1 mg GAE/g of DW) and total flavonoid content (TFC: 5.2 mg QE/g of DW) respectively. Nonetheless, the free radical scavenging activity (FRSA) was found correlated with the phenyl ammonia lyase (PAL) activity in the dark grown cell cultures. Analysis through gas chromatography-mass spectrometry (GC-MS) showed, biosynthesis of 29 compounds in the in vitro raised cell cultures. The major identified compounds consisted of monoterpene hydrocarbons such as ß-pinene (2.1-9.5%), ß-ocimene (1.4-8.3%), 1-terpinene-4-ol (5.8-9.6%), caryophyllene (1.3-6.2%), ß-farnesene (0.82-7.8), oxygenated monoterpenes including myrtenal (2.2-8.4%), citronellyl acetate (2.1-7.3%) and sesquiterpenes such as caryophyllene oxide (1.5-5.5) and ß-elemene (2.2-8.8%). This protocol has the potential for commercial production of important secondary volatiles.


Assuntos
Ajuga/metabolismo , Flavonoides/análise , Fenóis/análise , Acetatos/química , Ajuga/citologia , Ajuga/efeitos dos fármacos , Compostos de Benzil/química , Compostos de Benzil/farmacologia , Biomassa , Ciclopentanos/química , Flavonoides/química , Cromatografia Gasosa-Espectrometria de Massas , Oxilipinas/química , Peroxidase/metabolismo , Fenóis/química , Fenilalanina Amônia-Liase/metabolismo , Fotoperíodo , Células Vegetais/química , Células Vegetais/efeitos dos fármacos , Células Vegetais/metabolismo , Purinas/química , Purinas/farmacologia , Superóxido Dismutase/metabolismo
11.
Inflamm Res ; 67(7): 617-626, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29679313

RESUMO

OBJECTIVE AND DESIGN: To characterize the impact of inflammatory process and oxidative stress in the degree of benign prostatic hyperplasia (BPH), a common condition in which chronic inflammation plays a crucial role, we investigated the effect of different plant extract preparations in an in vivo model of BPH as new therapeutic target. MATERIAL: BPH was made in rats with daily administration of testosterone propionate (3 mg/kg) for 14 days. TREATMENT: Rats were randomized into different groups to receive oral administration of plant extract preparations: Serenoa repens with selenium (SeR 28.5 mg/kg associated with Se 0.005 mg/kg), Teoside (2 mg/kg), and Puryprost (14 mg/kg containing Teoside 50% 2 mg/kg and Epilobium 12 mg/kg). METHODS: After 14 days, rats were killed and histological changes, prostate weight and apoptotic pathways were assayed. RESULTS: The results obtained demonstrated that the association of treatments reduced prostate weight and hyperplasia, while treatment with Puryprost demonstrated a greater trend of protection compared to the other treatments. CONCLUSION: Thus, our results indicate that plant extract could be considered as new useful therapy in the treatment of BPH with particular attention on Puryprost that represents a rational approach to reduce BPH through modulation of inflammatory process and anti-oxidant process.


Assuntos
Ajuga , Epilobium , Extratos Vegetais/uso terapêutico , Hiperplasia Prostática/tratamento farmacológico , Selênio/uso terapêutico , Serenoa , Animais , Apoptose/efeitos dos fármacos , Colestenona 5 alfa-Redutase/metabolismo , Ciclo-Oxigenase 2/metabolismo , Di-Hidrotestosterona/sangue , Dinoprostona/metabolismo , Modelos Animais de Doenças , Masculino , Malondialdeído/metabolismo , Inibidor de NF-kappaB alfa/metabolismo , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Fitoterapia , Extratos Vegetais/farmacologia , Próstata/efeitos dos fármacos , Próstata/metabolismo , Próstata/patologia , Hiperplasia Prostática/induzido quimicamente , Hiperplasia Prostática/patologia , Ratos Sprague-Dawley , Selênio/farmacologia , Propionato de Testosterona
12.
Microb Pathog ; 118: 154-158, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29571723

RESUMO

Hepatitis C is a serious health issue and cause liver disorders in millions of people. Available therapeutic agents require long term administration with numerous side effects. Therefore, there is a dire need to find alternative treatment options for this disease. Since ancient times, medicinal plants are widely used to cure various diseases with no or less harmful effects. Therefore, this study was designed to find out phytochemicals and investigate antiviral activity of methanol extract of Ajuga bracteosa, Ajuga parviflora, Berberis lycium and Citrus lemon against Hepatitis C Virus (HCV infection). Phytochemical analysis of the plant extract was performed using various chemical tests. Toxicity of the plant extract was determined against using trypan blue exclusion method. Antiviral activity of the selected plant extract was find out against HCV infected HepG2 cells. For this purpose, HepG2 cells were seeded with HCV positive and negative serum and nontoxic doses of plant extract for 24 and 48 h. After this RNA was extracted and viral load was determined using Real-time PCR. Phytochemical analysis showed the presence of flavonoids and phenols in all plant extracts while amino acids, alkaloids and tannins were present in B. lycium and saponins were detected in C. lemon. Toxicity assay showed that all plant extracts were nontoxic at maximum concentration of 200 µg/ml except B. lycium, which showed mild toxicity at 40 µg/ml and were extremely toxic at 60 µg/ml and above doses. Real-time PCR quantitation result revealed that after 24 h treatments A. parviflora showed highest antiviral activity, followed by A. bracteosa, while B. lycium extract had low (35%) and C. lemon has no antiviral effects. The 48 h treatments showed an increase antiviral activity by A. bracteosa followed by A. parviflora and B. lycium while C. lemon showed negative effect. Our results depicted that mentioned plants might be used as an alternative therapeutic regime or in combination with existing treatments against HCV.


Assuntos
Ajuga/química , Antivirais/farmacologia , Berberis/química , Citrus/química , Hepacivirus/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Adulto , Idoso , Alcaloides/análise , Aminoácidos/análise , Proliferação de Células/efeitos dos fármacos , Feminino , Flavonoides/análise , Células Hep G2/efeitos dos fármacos , Células Hep G2/virologia , Hepatite C/tratamento farmacológico , Hepatócitos/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Fenóis/análise , Extratos Vegetais/química , Plantas Medicinais/química , Taninos/análise , Carga Viral , Adulto Jovem
13.
Pharm Biol ; 56(1): 649-657, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31070535

RESUMO

CONTEXT: Ajuga ovalifolia Bur. et Franch. var. calantha (Diels) C. Y. Wu et C. Chen (Labiatae), a traditional Chinese medicine, has been used to treat several inflammatory diseases. OBJECTIVE: To assess the anti-inflammatory activity of ajudecumin A isolated from Ajuga ovalifolia var. calantha, and its possible mechanisms. MATERIALS AND METHODS: Lipopolysaccharide (LPS, 0.5 µg/mL)-stimulated RAW264.7 macrophages were used to assess the anti-inflammatory activity of ajudecumin A (1-40 µM) in vitro. Nitric oxide levels were evaluated by Griess reagent. The mRNA levels of iNOS, COX-2, TNF-α, IL-1ß and IL-6 were determined using qRT-PCR. Phosphorylation of ERK, JNK, p38 MAPK and IκBα were detected by western Blot. To further assess the anti-inflammatory of ajudecumin A in vivo, mice were oral treated with ajudecumin A (10 mg/kg) or dexamethasone (0.25 mg/kg, positive control) for 5 days before administration of carrageenan or xylene. Paw and ear edema were then measured, respectively. RESULTS: Ajudecumin A (10-40 µM) decreased LPS-induced nitric oxide production with an IC50 value of 16.19 µM. Ajudecumin A (20 and 40 µM) also attenuated cell spreading and formation of pseudopodia-like structures, and decreased the mRNA levels of iNOS (55.23-67.04%, p < 0.001), COX-2 (57.58-70.25%, p < 0.001), TNF-α (53.75-58.94%, p < 0.01-0.001), IL-1ß (79.41-87.85%, p < 0.001) and IL-6 (54.26-80.52%, p < 0.01-0.001) in LPS-activated RAW264.7 cells. Furthermore, ajudecumin A suppressed LPS-induced phosphorylation of ERK, p38 MAPK, and IκBα, as well as IκBα degradation (p < 0.05-0.001). Finally, ajudecumin A (10 mg/kg) attenuated carrageenan- and xylene-induced inflammation in mice by about 28 and 24%, respectively. DISCUSSION AND CONCLUSIONS: Ajudecumin A exhibited a potent anti-inflammatory activity in vitro and in vivo through inhibition on NF-κB and ERK/p38 MAPK pathways, suggesting that ajudecumin A may be potentially developed as a lead compound in anti-inflammatory drug discovery.


Assuntos
Ajuga , Anti-Inflamatórios/uso terapêutico , Modelos Animais de Doenças , Lipopolissacarídeos/toxicidade , Macrófagos/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Relação Dose-Resposta a Droga , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Macrófagos/metabolismo , Macrófagos/patologia , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Células RAW 264.7
14.
Nat Prod Res ; 32(8): 977-981, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28874070

RESUMO

A phytochemical investigation of Ajuga forrestii Diels led to the isolation of 14 compounds, including eight neo-clerodane diterpenes (1-8), two phytoecdysteroids (9, 11), one stigmastane sterol (10) and three iridoid glycosides (12-14). The structures of these compounds were identified by spectroscopic methods and a comparison of their data with those reported in the literature. This is the first report of compounds 1-14 from A. forrestii. The cytotoxic activities of the aqueous extract of A. forrestii and several compounds have been studied and the chemotaxonomic significance of isolated compounds has also been summarised.


Assuntos
Ajuga/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ajuga/classificação , Linhagem Celular Tumoral , Diterpenos Clerodânicos/análise , Diterpenos Clerodânicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Glicosídeos Iridoides/análise , Glicosídeos Iridoides/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espectrometria de Massas por Ionização por Electrospray
15.
Catheter Cardiovasc Interv ; 90(7): 1105-1106, 2017 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-29226579

RESUMO

Radial access for catheterization is associated with reduced bleeding and mortality across a spectrum of clinical conditions compared to femoral. Transradial technique is associated with a higher rate of access site failure but this is in those most likely to have a femoral-based complication. Improved outcomes will come with further radial technique refinement and not with a retreat to legacy femoral approaches.


Assuntos
Ajuga , Artéria Radial , Angiografia Coronária , Artéria Femoral , Resultado do Tratamento
16.
Biomed Pharmacother ; 96: 480-488, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29031208

RESUMO

The present study investigated the protective effect of phytoecdysteroids extracted from the Ajuga iva plant on body weight changes, blood glucose, insulin total protein, blood urea nitrogen (BUN), creatinine, triglycerides (TG), cholesterol, lipid peroxidation, antioxidant enzymes, pancreatic histopathology and hexokinase-I expression in the alloxan-induced diabetic rats. Experimental diabetes was induced following 15day intraperitoneal administration of alloxan. The rats were divided into four groups. Group I served as a sham group, and group II served as the diabetic control. Group III served as a treatment for phytoecdysteroids (10mg/kg), and group IV served as a treatment for phytoecdysteroids (20mg/kg). Phytoecdysteroids restored body weight loss to its antihyperglycemic effect. Blood glucose was reduced 19.2 and 52.9% in group III and IV respectively. Blood insulin (54.9 and 105.88%) and total protein (25 and 72.2%) was increased in group III and IV respectively. BUN, creatinine, TG, cholesterol and lipid peroxidation was significantly reduced following treatment. Catalase, superoxide dismutase (SOD), and glutathione peroxidase activity were significantly increased following treatment. Islet ß-cells are lost in alloxan-induced diabetic rats. Regeneration of islets and reduced atrophy of acinar cells were noted. The number of insulin-secreting cells was tremendously reduced in alloxan-induced diabetic rats. Insulin-secreting cells were increased 48 and 61% in group III and IV respectively. Hexokinase-I mRNA (28.3 & 93.5%) and protein (27.9 and 55.3%) expression were significantly increased following treatment. Taking all these data together, it is suggested that the phytoecdysteroid could be a potential therapeutic agent against experimental diabetes.


Assuntos
Ajuga , Diabetes Mellitus Experimental/tratamento farmacológico , Ecdisteroides/uso terapêutico , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Aloxano , Animais , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Ecdisteroides/isolamento & purificação , Ecdisteroides/farmacologia , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Masculino , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar
17.
BMC Complement Altern Med ; 17(1): 443, 2017 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-28870197

RESUMO

BACKGROUND: The concept of botanical therapeutics has revitalized due to wide importance of plant derived pharmaceuticals. Therefore, the ameliorative characteristics of Ajuga bracteosa were studied. METHODS: Total phenolic content, flavonoid content, antioxidant capacity, reducing power and free-radical scavenging activity were determined colorimetrically. Specific polyphenols were quantified by RP-HPLC analysis. Preliminary cytotoxicity was tested using brine shrimp lethality assay while antiproliferative activity against THP-1 and Hep-G2 cell lines was determined by MTT and SRB protocols respectively. Antileishmanial potential was assessed via MTT colorimetric method. To investigate antidiabetic prospect, α-amylase inhibition assay was adopted whereas disc diffusion method was used to detect likely protein kinase inhibitory, antibacterial and antifungal activities. RESULTS: Among fifteen different extracts, maximum total phenolic content (10.75 ± 0.70 µg GAE/mg DW), total reducing power (23.90 ± 0.70 µg AAE/mg DW) and total antioxidant capacity (11.30 ± 0.80 µg AAE/mg DW) were exhibited by methanol extract with superlative percent extract recovery (17.50 ± 0.80% w/w). Chloroform-methanol extract demonstrated maximum flavonoid content (4.10 ± 0.40 µg QE/mg DW) and ethanol extract exhibited greatest radical scavenging activity (IC50 14.40 ± 0.20 µg/ml). RP-HPLC based quantification confirmed polyphenols such as pyrocatechol, gallic acid, resorcinol, catechin, chlorogenic acid, caffeic acid, syringic acid, p-coumaric acid, ferulic acid, vanillic acid, coumarin, sinapinic acid, trans-cinnamic acid, rutin, quercetin and kaempferol. The brine shrimp lethality assay ranked 78.60% extracts as cytotoxic (LC50 ≤ 250 µg/ml) whereas significant THP-1 inhibition was shown by methanol-acetone extract (IC50 4.70 ± 0.43 µg/ml). The antiproliferative activity against Hep-G2 hepatoma cancer cell line was demonstrated by n-hexane, ethylacetate and methanol-distilled water (IC50 8.65-8.95 µg/ml) extracts. Methanol extract displayed prominent protein kinase inhibitory activity (MIC 12.5 µg/disc) while n-hexane extract revealed remarkable antileishmanial activity (IC50 4.69 ± 0.01 µg/ml). The antidiabetic potential was confirmed by n-hexane extract (44.70 ± 0.30% α-amylase inhibition at 200 µg/ml concentration) while a moderate antibacterial and antifungal activities were unveiled. CONCLUSION: The variation in biological spectrum resulted due to use of multiple solvent systems for extraction. We also deduce that the valuable information gathered can be utilized for discovery of anticancer, antileishmanial, antioxidant and antidiabetic bioactive lead candidates.


Assuntos
Ajuga/química , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Animais , Antioxidantes/análise , Antioxidantes/farmacologia , Artemia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/farmacologia , Flavonoides/análise , Flavonoides/farmacologia , Humanos , Fenóis/análise , Fenóis/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química
18.
Mol Med Rep ; 16(4): 4895-4902, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28791415

RESUMO

The aim of the current study was to investigate the impacts and possible mechanisms of total flavonoids of Ajuga (TFA) on glomerular mesangial cells (GMC) through in vitro observations of the impacts of TFA­containing serum on GMC proliferation and extracellular matrix (ECM) secretion in lipopolysaccharides (LPS)­induced rats. Rat GMC was cultured in vitro, using LPS to stimulate the proliferation of GMC and the secretion of ECM; meanwhile, TFA­containing serum (TFA­S) was used for the intervention. Methyl thiazolyl tetrazolium (MTT) assay was performed to test the proliferation of GMC; enzyme­linked immunosorbent assay (ELISA) was used to detect the expressions of fibronectin (FN) and collagen IV (Col­IV) in cell supernatant, flow cytometry was performed to detect the cell cycle, and reverse transcription-polymerase chain reaction was performed to detect the expression levels of matrix metalloproteinase 9 (MMP­9) mRNA and transforming growth factor ß1 (TGF­ß1) mRNA. The GMC proliferation and the expressions of FN and Col­IV in cell supernatant were significantly reduced after 24 and 48 h TFA­S intervention (P<0.05 or 0.01). A total of 48 h subsequent to the intervention, the proportion of GMC in the G1 phase and the relative expression of MMP­9 mRNA were significantly increased (P<0.05 or 0.01), however the proportion of GMC in S phase and the relative expression of TGF­ß1 mRNA were significantly reduced (P<0.05 or 0.01). TFA­S can inhibit LPS­induced GMC proliferation and ECM accumulation, and its roles are associated with regulating the cell cycle and the expression levels of TGF­ß1 and MMP­9.


Assuntos
Ajuga/química , Flavonoides/farmacologia , Células Mesangiais/efeitos dos fármacos , Células Mesangiais/metabolismo , Animais , Ciclo Celular/efeitos dos fármacos , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Colágeno Tipo IV/metabolismo , Fibronectinas/metabolismo , Flavonoides/farmacocinética , Regulação da Expressão Gênica/efeitos dos fármacos , Masculino , Metaloproteinase 9 da Matriz/genética , Metaloproteinase 9 da Matriz/metabolismo , Ratos , Fator de Crescimento Transformador beta1/genética , Fator de Crescimento Transformador beta1/metabolismo
19.
Biotechnol Lett ; 39(9): 1291-1298, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28597370

RESUMO

The genus Ajuga L., belonging to Lamiaceae family, is widespread. The demand for Ajuga species has risen sharply because of their medicinal, ornamental, and pharmacological properties. These wide-ranging plants are being rapidly depleted due to over-collection for ornamental and medicinal purposes, as well as by habitat destruction and deforestation. Ajuga boninsimae, A. bracteosa, A. ciliate, A. genevensis, A. incisa, A. makinoi, A. multiflora, A. pyramidalis, A. shikotanensis, A. reptans, and A. vestita are categorized and protected as endangered plants. In vitro plant culture has therefore emerged for the conservation and mass clonal propagation of rare plants. This mini-review covers the current in vitro scenario in the propagation of Ajuga species. Adventitious or axillary shoots are initiated on the leaf, petiole and internodes, as well as roots, nodes, and shoot tip explants. Shoot induction is predominantly dependent on plant growth regulators added to the culture medium. Full- or half-strength Murashige and Skoog medium with or without auxin is used for in vitro rooting. Rooted shoots need to be acclimatized in the greenhouse with an estimated 82-100% survival rate.


Assuntos
Ajuga/crescimento & desenvolvimento , Técnicas de Cultura de Células/métodos , Reguladores de Crescimento de Planta/metabolismo , Meios de Cultura/química
20.
BMC Complement Altern Med ; 17(1): 243, 2017 May 02.
Artigo em Inglês | MEDLINE | ID: mdl-28464813

RESUMO

BACKGROUND: Ajuga remota Benth is traditionally used in Ethiopia for the management of diabetes mellitus. Since this claim has not been investigated scientifically, the aim of this study was to evaluate the antidiabetic effect and phytochemical screening of the aqueous and 70% ethanol extracts on alloxan-induced diabetic mice. METHODS: After acute toxicity test, the Swiss albino mice were induced with alloxan to get experimental diabetes animals. The fasting mean blood glucose level before and after treatment for two weeks in normal, diabetic untreated and diabetic mice treated with aqueous and 70% ethanol extracts were performed. Data were statistically evaluated by using Statistical Package for the Social Sciences software version 20. P-value <0.05 was considered statistically significant. RESULTS: The medium lethal doses (LD50) of both extracts were higher than 5000 mg/kg, indicating the extracts are not toxic under the observable condition. Aqueous extracts of A.remota (300 mg/kg and 500 mg/kg body weight) reduced elevated blood glucose levels by 27.83 ± 2.96% and 38.98 ± 0.67% (P < 0.0001), respectively while the 70% ethanol extract caused a reduction of 27.94 ± 1.92% (300 mg/kg) & 28.26 ± 1.82% (500 mg/kg). Treatment with the antidiabetic drug, Glibenclamide (10 mg/kg body weight) lowered blood glucose level by 51.06% (p < 0.05). Phytochemical screening of both extracts indicated the presence of phenolic compounds, flavonoids, saponins, tannins, and steroids, which might contribute to the antidiabetic activity. The extracts, however, did not contain alkaloids and anthraquinones. CONCLUSION: The aqueous extract (500 mg/kg) showed the highest percentage reduction in blood glucose levels and the ability of A. remota extracts in reducing blood glucose levels presumably due to the presence of antioxidant constituents such as flavonoids. The effect of the extract supported the traditional claim of the plant.


Assuntos
Ajuga/química , Glicemia/metabolismo , Diabetes Mellitus Experimental/metabolismo , Hipoglicemiantes/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Etiópia , Flavonoides/análise , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Hipoglicemiantes/uso terapêutico , Masculino , Medicina Tradicional Africana , Camundongos , Fenóis/análise , Fenóis/farmacologia , Fenóis/uso terapêutico , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/uso terapêutico , Fitosteróis/análise , Fitosteróis/farmacologia , Fitosteróis/uso terapêutico , Fitoterapia , Extratos Vegetais/uso terapêutico , Folhas de Planta , Polifenóis/análise , Polifenóis/uso terapêutico , Saponinas/análise , Saponinas/farmacologia , Saponinas/uso terapêutico , Taninos/análise , Taninos/farmacologia , Taninos/uso terapêutico
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