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1.
Fitoterapia ; 140: 104444, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31790768

RESUMO

Alpinia zerumbet (Pers.) B.L.Burtt & R.M.Sm. (Zingiberaceae) is a perennial plant native to the East Indies and is widely distributed in South America, Oceania, and Asia. The mature fruits of the plant have been used in traditional medicine in China. In this study, we compared the chemical constituents in the methanol extracts of the leaves, the placenta, the pericarps, and the seeds obtained from the same plant using LC-MS, and we examined the NO inhibitory activities of the respective extracts and the isolated compounds. As a result of LC-MS analyses, kavalactone derivatives (1-6) were detected in the methanol extracts of the leaves, placenta, and pericarps. Of these, compound 6 was identified as a new asymmetrical cyclobutane dimer of 5,6-dehydrokawain. Quantitative analysis showed that the total amounts of kavalactone derivatives were highest in the methanol extract of the pericarps. Moreover, the results of measurements of the anti-inflammatory activity revealed that the pericarps extract showed the strongest activity. The compounds responsible for the anti-inflammatory activity of the extracts from A. zerumbet were identified. Of these, five were known kavalactone derivatives and one was a new kavalactone derivative (aniba dimer C). The results showed that the pericarps of A. zerumbet are a rich source of kavalactone derivatives, and that the pericarps of A. zerumbet can be utilized as an important medicinal resource.


Assuntos
Alpinia/química , Anti-Inflamatórios/farmacologia , Lactonas/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Células Cultivadas , Hepatócitos/efeitos dos fármacos , Japão , Lactonas/isolamento & purificação , Estrutura Molecular , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Folhas de Planta/química , Ratos
2.
Prep Biochem Biotechnol ; 50(1): 82-90, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31545661

RESUMO

To optimize the extraction of total flavonoids (TFL) from the leaves of Alpinia oxyphylla Miq. using microwave-assisted method, a orthogonal test was used. The optimal extraction conditions for TFL were determined as follows: ethanol concentration of 50%, solid-liquid ratio of 1:20, temperature of 70 °C, and cycle index of 3. Under these conditions, the extraction yield of TFL was 28.24%. The scavenging rate of TFL against a,a-diphenyl-b-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzoth- iazoline-6-sulphonica cid) (ABTS), and superoxide anion radical (O2-·) was screened. The results showed that the bioactivity of extracts appeared to be TFL dose-dependent, while it also presented stronger ferric reducing antioxidant power (FRAP). The contents of chrysin and tectochrysin in TFL were quantitatively analyzed by HPLC.


Assuntos
Alpinia/química , Antioxidantes/isolamento & purificação , Flavonoides/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Antioxidantes/farmacologia , Fracionamento Químico , Flavonoides/farmacologia , Micro-Ondas , Extratos Vegetais/farmacologia
3.
J Pharm Biomed Anal ; 177: 112874, 2020 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-31542420

RESUMO

Alzheimer's disease (AD) is a neurodegenerative disease that seriously affects daily life. Schisandra chinensis (Turcz.) Baill. Fructus (SCF) and Alpinia oxyphylla Miq. Fructus (AOF) have been regarded as classical herbs for dementia since ancient times. Alpinia oxyphylla Miq.-Schisandra chinensis (Turcz.) Baill. herb pair (ASHP) is the compatible form of the two herbs. Ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was established for the simultaneous determination of protocatechuic acid, chrysin, schisandrin, gomisin A, gomisin B, nootkatone, deoxyschizandrin, schisandrin B and schisandrin C in rat plasma. The pharmacokinetic differences of the above nine active components in normal rats and AD model rats after oral administration of SCF, AOF, and ASHP ethanol extracts were investigated. Chloramphenicol and bifendate were used as the internal standards. Extraction of plasma sample was by liquid-liquid extraction with ethyl acetate. A SBC18 column (2.1 mm × 100 mm, 1.8 µm) was used in this experiment at a flow rate of 0.3 mL/min at 30 °C with linear gradient elution using acetonitrile and water containing 0.1% formic acid. This study showed ASHP can improve the absorption of protocatechuic acid, chrysin, schisandrin, gomisin B, nootkatone, deoxyschizandrin, schisandrin B and schisandrin C in vivo and slow down part of these components' elimination. In addition, compared with normal rats, the pharmacokinetic parameters changed significantly in AD model rats' plasma after oral administration of ASHP. Hence, these may be the pharmacokinetic mechanism of ASHP, in addition to serving as a potential agent in the treatment of AD.


Assuntos
Alpinia/química , Doença de Alzheimer/tratamento farmacológico , Monitoramento de Medicamentos/métodos , Medicamentos de Ervas Chinesas/farmacocinética , Schisandra/química , Administração Oral , Doença de Alzheimer/sangue , Doença de Alzheimer/etiologia , Peptídeos beta-Amiloides/administração & dosagem , Peptídeos beta-Amiloides/toxicidade , Animais , Cromatografia Líquida de Alta Pressão/métodos , Modelos Animais de Doenças , Combinação de Medicamentos , Avaliação Pré-Clínica de Medicamentos , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/química , Humanos , Injeções Intraventriculares , Masculino , Fragmentos de Peptídeos/administração & dosagem , Fragmentos de Peptídeos/toxicidade , Ratos , Espectrometria de Massas em Tandem/métodos
4.
J Photochem Photobiol B ; 201: 111649, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31710925

RESUMO

In the present systematic study, silver nanoparticles have been synthesized using the fruits of Alpinia nigra. Apart from the presence of saponins, glycosides, alkaloids, steroids, the extract of A. nigra fruits are rich in polyphenols. The Total Flavonoid and Phenol Content of A. nigra fruits extract is 718 mgRE/g extract and 74.9 mgGAE/g extract respectively. The formation of the nanoparticles was validated through characterization techniques like UV-Vis spectroscopy, X- ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS) and Energy dispersive X-ray spectroscopy (EDX). The spherical shape of silver nanoparticles is observed in Transmission Electron Microscopy (TEM) images. The average particle size of the silver nanoparticles is 6 nm. The biomolecules of the fruit extract played the dual role of reducing and capping agents which is evident from Fourier Transform Infrared (FTIR) spectrometer and Scanning Electron Microscopy (SEM) image analysis. The A. nigra capped silver nanoparticles exhibited promising antimicrobial activity against gram negative bacteria Klebsiella pneumoniae, gram positive bacteria Staphylococcus aureus and the pathogenic fungus, Candida albicans. Amongst the three pathogens, Klebsiella pneumoniae is the most susceptible to silver nanoparticles. Furthermore, the nanoparticles efficiently catalysed the degradation of the anthropogenic dyes Methyl orange, Rhodamine B and Orange G in the presence of sunlight. The photocatalytic degradation process follows the pseudo-first order kinetics. These results confirm that the silver nanoparticles can be efficiently synthesized via a green route using A. nigra fruits with applications as antimicrobial and catalytic agents.


Assuntos
Alpinia/química , Anti-Infecciosos/síntese química , Nanopartículas Metálicas/química , Prata/química , Alpinia/metabolismo , Anti-Infecciosos/farmacologia , Compostos Azo/química , Catálise , Corantes/química , Frutas/química , Frutas/metabolismo , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Química Verde , Nanopartículas Metálicas/toxicidade , Tamanho da Partícula , Extratos Vegetais/química , Luz Solar
5.
Integr Cancer Ther ; 18: 1534735419866924, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31409145

RESUMO

Recent advances in mammography screening, chemotherapy, and adjuvant treatment modalities have improved the survival rate of women with breast cancer. Nevertheless, the breast tumor with metastatic progression is still life-threatening. Indeed, combination therapy with Ras-ERK and PI3K inhibitors is clinically effective in malignant breast cancer treatment. Constituents from genus Alpinia plants have been implicated as potent anticancer agents in terms of their efficacy of inhibiting tumor cell metastasis. In this study, we tested the effects of ethanol extracts of Alpinia nantoensis (rhizome, stem, and leaf extracts) in cultured human breast cancer cells and particularly focused on the Ras-ERK and PI3K/AKT pathways. We found that the rhizome and leaf extracts from A nantoensis inhibited cell migration, invasion, and sphere formation in MCF-7 and MDA-MB-231 cells. The potency was extended with the inhibition of serum-induced PI3K/AKT and Ras-ERK activation and epidermal growth factor (EGF)-mediated EGFR activation in MDA-MB-231 cells. These results indicate that extracts of A nantoensis could inhibit signal transduction at least involved in EGFR as well as the PI3K/AKT and Ras-ERK pathways, which are crucial players of tumor cell migration and invasion. Our study strongly supports that the extracts of A nantoensis could be a novel botanical drug lead for the development of an antimetastatic agent for the treatment of human malignant breast cancer.


Assuntos
Alpinia/química , Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Extratos Vegetais/farmacologia , Neoplasias da Mama/metabolismo , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Fator de Crescimento Epidérmico/metabolismo , Receptores ErbB/metabolismo , Etanol/química , Feminino , Humanos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Células MCF-7 , Fosfatidilinositol 3-Quinases/metabolismo , Fosforilação/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos
6.
Molecules ; 24(13)2019 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-31288458

RESUMO

BACKGROUND/AIM: Plants play an important role in anti-cancer drug discovery, therefore, the current study aimed to evaluate the biological activity of Alpinia zerumbet (A. zerumbet) flowers. METHODS: The phytochemical and biological criteria of A. zerumbet were in vitro investigated as well as in mouse xenograft model. RESULTS: A. zerumbet extracts, specially CH2Cl2 and MeOH extracts, exhibited the highest potent anti-tumor activity against Ehrlich ascites carcinoma (EAC) cells. The most active CH2Cl2 extract was subjected to bioassay-guided fractionation leading to isolatation of the naturally occurring 5,6-dehydrokawain (DK) which was characterized by IR, MS, 1H-NMR and 13C-NMR. A. zerumbet extracts, specially MeOH and CH2Cl2 extracts, exhibited significant inhibitory activity towards tumor volume (TV). Furthermore, A. zerumbet extracts declined the high level of malonaldehyde (MDA) as well as elevated the levels of superoxide dismutase (SOD) and catalase (CAT) in liver tissue homogenate. Moreover, DK showed anti-proliferative action on different human cancer cell lines. The recorded IC50 values against breast carcinoma (MCF-7), liver carcinoma (Hep-G2) and larynx carcinoma cells (HEP-2) were 3.08, 6.8, and 8.7 µg/mL, respectively. CONCLUSION: Taken together, these findings open the door for further investigations in order to explore the potential medicinal properties of A. zerumbet.


Assuntos
Alpinia/química , Antineoplásicos Fitogênicos/química , Extratos Vegetais/química , Pironas/química , Animais , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Catalase/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Clorofórmio/química , Flores/química , Xenoenxertos , Humanos , Malondialdeído/metabolismo , Metanol/química , Camundongos , Transplante de Neoplasias , Extratos Vegetais/farmacologia , Plantas Medicinais , Pironas/farmacologia , Solventes , Superóxido Dismutase/metabolismo
7.
Zhongguo Zhong Yao Za Zhi ; 44(9): 1960-1964, 2019 May.
Artigo em Chinês | MEDLINE | ID: mdl-31342727

RESUMO

Alpinia oxyphylla is mainly produced in Hainan,and also one of the four famous traditional Chinese medicines in South China with increasing importance in traditional Chinese medicine industry. Field surveys and literatures show that A. oxyphylla has widely used as a medicinal and edible plant,it is an important raw material for many Chinese patent medicines,health products and food,with a long history of artificial cultivation and application. The future development is prospected on health market. But A. oxyphylla industry has faced a lot of problems,including unreasonable planting layout,lack of good varieties,imperfect seed breeding system,low level of standardization,inconsistent quality of medicinal materials,low level of industry,and so on. The suggestions for sustainable development are listed below.First,it is essential to strengthen the research on the basis and application technology of A. oxyphylla,speed up the selection and breeding of improved varieties,and popularize standardized cultivation techniques. Secondly,it is important to strengthen the research on quality standards,improve the quality evaluation system of medicinal materials. Thirdly,it is necessary to take full advantage of the functional components to develop functional products with Hainan characteristics,find out the unique product characteristics of A. oxyphylla,build a famous brand and improve the product competitiveness in the market. It is also important to strengthen policy support and industrial supervision,promote the healthy and rapid development of A. oxyphylla industry.


Assuntos
Alpinia/química , Medicamentos de Ervas Chinesas/farmacologia , China , Medicina Tradicional Chinesa/tendências , Melhoramento Vegetal , Plantas Medicinais/química , Sementes
8.
Chem Biodivers ; 16(6): e1900032, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30957403

RESUMO

The inhibition of carbohydrate-hydrolyzing enzymes in human digestive organs is crucial in controlling blood sugar levels, which is important in treating type 2 diabetes. In the current study, pahangensin A (1), a bis-labdanic diterpene characterized previously in the rhizomes of Alpinia pahangensis Ridl., was identified as an active dual inhibitor for α-amylase (IC50 =114.80 µm) and α-glucosidase (IC50 =153.87 µm). This is the first report on the dual α-amylase and α-glucosidase inhibitory activities of a bis-labdanic diterpene. The Lineweaver-Burk plots of compound 1 indicate that it is a mixed-type inhibitor with regard to both enzymes. Based on molecular docking studies, compound 1 docked in a non-active site of both enzymes. The dual inhibitory activity of compound 1 makes it a suitable natural alternative in the treatment of type 2 diabetes.


Assuntos
Alpinia/química , Diterpenos/química , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , Alpinia/metabolismo , Sítios de Ligação , Domínio Catalítico , Diterpenos/isolamento & purificação , Diterpenos/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Cinética , Simulação de Acoplamento Molecular , Extratos Vegetais/química , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/química
9.
Sensors (Basel) ; 19(3)2019 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-30704021

RESUMO

Background: Alpinia officinarum Hance is both an herbal medicine and a condiment, and generally has different cultivars such as Zhutou galangal and Fengwo galangal. The appearance of these A. officinarum cultivars is similar, but their chemical composition and quality are different. It is therefore important to discriminate between different A. officinarum plants to ensure the consistency of the efficacy of the medicine. Therefore, we used an electronic nose (E-nose) to explore the differences in odor information between the two cultivars for fast and robust discrimination. Methods: Odor and volatile components of all A. officinarum samples were detected by the E-nose and gas chromatography-mass spectrometry (GC-MS), respectively. The E-nose sensors and GC-MS data were analyzed respectively by principal component analysis (PCA), the correlation between E-nose sensors and GC-MS data were analyzed by partial least squares (PLS). Results: It was found that Zhutou galangal and Fengwo galangal can be discriminated by combining the E-nose with PCA, and the E-nose sensors S2, S6, S7, S9 were important sensors for distinguishing different cultivars of A. officinarum. A total of 56 volatile components of A. officinarum were identified by the GC-MS analysis, and the composition and content of the volatile components from the two different A. officinarum cultivars were different, in particular the relative contents of 1,8-cineole and α-farnesene. The classification result by PCA analysis based on GC-MS data was consistent with the E-nose results. The PLS analysis demonstrated that the volatile terpene, alcohol and ester components primarily interacted with the sensors S2 and S7, indicating that particular E-nose sensors were highly correlated with some aroma constituents. Conclusions: Combined with advanced chemometrics, the E-nose detection technology can discriminate two cultivars of A. officinarum, with GC-MS providing support to determine the material basis of the E-nose sensors' response.


Assuntos
Alpinia/química , Técnicas Biossensoriais/métodos , Cromatografia Gasosa-Espectrometria de Massas/métodos , Compostos Orgânicos Voláteis/análise , Nariz Eletrônico , Medicina Herbária , Odorantes/análise
10.
Int J Biol Macromol ; 128: 804-813, 2019 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-30708017

RESUMO

The purpose of this paper was to investigate the effects and mechanism of polysaccharide (PAOF) from Alpiniae oxyphyllae fructus on urinary incontinence (UI) in old-age hydruric model rats (OHMR). Results suggested that PAOF can significantly reduce the urination volume, Na+, Cl- emission and increase K+ excretion of OHMR. In addition, PAOF can increase the content of aldosterone (ALD) and antidiuretic hormone (ADH) in blood of OHMR. The coefficients of spleen, thymus and adrenal of OHMR were improved by PAOF. Furthermore, PAOF can not only elevate significantly the expression of ß3-adrenoceptor mRNA in bladder detrusor of OHMR, but also increase the content of adenylate cyclase (AC), cyclic adenosine monophosphate (cAMP) and protein kinase A (PKA) in bladder detrusor of OHMR. Meanwhile, PAOF can elevate significantly the expression of PKA protein in bladder detrusor of rats with polyuria. The data implied that PAOF may offer therapeutic potential against UI.


Assuntos
Alpinia/química , Frutas/química , Polissacarídeos/farmacologia , Incontinência Urinária/tratamento farmacológico , Adenilil Ciclases/metabolismo , Aldosterona/sangue , Aminoácidos Cíclicos/metabolismo , Animais , AMP Cíclico/metabolismo , Proteínas Quinases Dependentes de AMP Cíclico/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Polissacarídeos/uso terapêutico , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Receptores Adrenérgicos beta 3/genética , Incontinência Urinária/sangue , Incontinência Urinária/genética , Incontinência Urinária/urina , Vasopressinas/sangue
11.
J AOAC Int ; 102(3): 726-733, 2019 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-30388970

RESUMO

Background: Alpinia officinarum Hance (ginger family) is an important Chinese medicine, especially in Southern China. Objective: A simple and effective high-performance thin-layer chromatography coupled with 2, 2-diphenyl-1-picrylhydrazyl bioautography (HPTLC-DPPH) and electrospray ionization quadrupole time-of-flight tandem mass spectrometry (ESI-Q-TOF-MS/MS) method was developed for the bioactivity-based quality control of A. officinarum. Methods: The HPTLC-DPPH and ESI-Q-TOF-MS/MS were applied for the analysis of different parts of A. officinarum after using methanol extraction for 23 batches of taproot, four batches of aerial, and three batches of fibril parts. Results: The systematic evaluation showed that similar components in taproot and aerial parts make the major antioxidant activity. However, based on our evaluation, the antioxidant ability of the aerial parts is lower than the taproot parts. There is also a significant difference (P < 0.05) between taproot and fibril parts of the root. The chemical structures of compounds with the antioxidant capacity were tentatively identified as 5R-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenyl-3-heptanone (band 1), kaempferide (band 2), and galangin (band 3) based on ESI-Q-TOF-MS/MS analytical results and further confirmed by standards. Conclusions: This identification indicated that two flavonoid compounds and one diarylheptanoid compound possessed high potentials to be used as the antioxidant biomarkers for the quality control of A. officinarum. Highlights: The comparison of different parts could be considered as guidelines for the usage of A. officinarum.


Assuntos
Alpinia/química , Antioxidantes/isolamento & purificação , Flavonoides/isolamento & purificação , Guaiacol/análogos & derivados , Quempferóis/isolamento & purificação , Biomarcadores , Compostos de Bifenilo/química , Cromatografia em Camada Delgada/métodos , Guaiacol/isolamento & purificação , Picratos/química , Componentes Aéreos da Planta/química , Raízes de Plantas/química , Extração em Fase Sólida/métodos
12.
Ecotoxicol Environ Saf ; 168: 324-329, 2019 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-30390531

RESUMO

Secondary plant metabolites play an important role in providing protection to plants against herbivore insect pests. Keeping in view the increasing importance of biopesticides, the crude extracts from different plants are being investigated for insecticidal activities. Alpinia galanga, a medicinal plant belonging to family Zingiberaceae exhibits a wide range of biological activities. In the present study, crude extracts of A. galanga and its purified compounds i.e. 1'-acetoxychavicol acetate and galangin were evaluated for their effect on various nutritional parameters of Spodoptera litura (Fab.). All the extracts exhibited a significant influence on relative growth and consumption rates as well as efficiency of conversion of ingested and digested food. Ethyl acetate extract was found to be the most effective causing significant reduction in values of RGR, RCR, ECI and ECD of S. litura larvae in comparison to control larvae. The highest concentration of the ethyl acetate extract (2500 ppm) resulted in 44.95%, 10.99%, 38.08% and 37.04% decrease respectively in RGR, RCR, ECI and ECD in comparison to control. The purified compounds also showed inhibitory effects on various nutritional parameters. 1'-Acetoxychavicol acetate was found to be more effective in comparison to galangin.


Assuntos
Alpinia/química , Fenômenos Fisiológicos da Nutrição/efeitos dos fármacos , Extratos Vegetais/farmacologia , Spodoptera/efeitos dos fármacos , Animais , Álcoois Benzílicos/farmacologia , Agentes de Controle Biológico/farmacologia , Flavonoides/farmacologia , Larva/efeitos dos fármacos , Plantas Medicinais/química , Spodoptera/metabolismo
13.
Eur J Pharmacol ; 842: 365-372, 2019 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-30412728

RESUMO

Alzheimer's disease (AD), a neurodegenerative disease, is diagnosed by impaired learning and memory in elderly individuals. Tectochrysin (TEC) is a flavonoid compound isolated from Alpinia Oxyphylla Miq., which has been traditionally used for the treatment of diarrhea, salivation, diuresis and dementia. In our study, model mice with AD induced by intracerebroventricular injection of Aß1-42 were used to determine the role of TEC on memory retrieval. The results revealed that AD mice received intracerebroventricular injection of TEC (140 µg/kg) showed improved spatial memory performance and down-regulated expressions of ß-secretase and accumulation of Aß1-42 in brain tissues. TEC also decreased the concentration of malondialdehyde and total cholinesterase, and increased activities of both antioxidant superoxide dismutase and glutathione peroxidase in hippocampal and cortex. In addition, Aß1-42 induced injury of neurons in hippocampal CA1 layer was rehabilitated in TEC treated mice. These findings highlight the beneficial role of TEC in amnestic mice induced by Aß1-42 through the down-regulation of Aß1-42 accumulation, oxidative stress, and total cholinesterase. Our study indicated a therapeutic potential of TEC in the treatment of AD.


Assuntos
Alpinia/química , Peptídeos beta-Amiloides/toxicidade , Flavonoides/farmacologia , Memória/efeitos dos fármacos , Fragmentos de Peptídeos/toxicidade , Secretases da Proteína Precursora do Amiloide/metabolismo , Peptídeos beta-Amiloides/metabolismo , Animais , Aprendizagem da Esquiva/efeitos dos fármacos , Região CA1 Hipocampal/citologia , Região CA1 Hipocampal/efeitos dos fármacos , Região CA1 Hipocampal/metabolismo , Região CA1 Hipocampal/fisiologia , Córtex Cerebral/citologia , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/metabolismo , Córtex Cerebral/fisiologia , Colinesterases/metabolismo , Relação Dose-Resposta a Droga , Locomoção/efeitos dos fármacos , Locomoção/fisiologia , Aprendizagem em Labirinto/efeitos dos fármacos , Camundongos , Neurônios/efeitos dos fármacos , Fragmentos de Peptídeos/metabolismo , Memória Espacial/efeitos dos fármacos
14.
Microb Pathog ; 126: 239-244, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30414839

RESUMO

Alpinetin, a type of novel plant flavonoid derived from Alpinia katsumadai Hayata, has been reported to have anti-inflammatory effects. The aim of this investigation was designed to reveal the protective effects of alpinetin on Lipopolysaccharide (LPS)/d-galactosamine (D-Gal)-induced liver injury in mice. Alpinetin (12.5, 25, 50 mg/kg) were given 1 h before LPS and D-Gal treatment. 12 h after LPS and D-Gal treatment, the liver tissues and serum were collected. Our results showed that alpinetin treatment improved liver histology, indicating a marked decrease of inflammatory cell infiltration and restore hepatic lobular architecture. Alpinetin also inhibited liver myeloperoxidase (MPO) activity and malondialdehyde (MDA) level. Furthermore, LPS/D-Gal-induced tumor necrosis factor-α (TNF-α) and Interleukin-1ß (IL-1ß) production were dose-dependently inhibited by alpinetin. Alpinetin also attenuated LPS/D-Gal-induced expression of phospho-NF-κB p65 and phospho-IκBα. In addition, alpinetin was found to increase the expression of nuclear factor E2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1). In conclusion, these findings suggested that alpinetin inhibited liver injury through inhibiting NF-κB and activating the Nrf2 signaling pathway.


Assuntos
Flavanonas/farmacologia , Galactosamina/efeitos adversos , Lipopolissacarídeos/efeitos adversos , Fígado/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Alpinia/química , Animais , Anti-Inflamatórios/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Flavanonas/administração & dosagem , Heme Oxigenase-1/metabolismo , Proteínas I-kappa B/metabolismo , Interleucina-1beta/metabolismo , Fígado/lesões , Fígado/patologia , Malondialdeído/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Fator 2 Relacionado a NF-E2/metabolismo , Peroxidase/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição RelA/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
15.
Environ Toxicol ; 34(2): 172-178, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30367734

RESUMO

Cardiac fibrosis is a common pathophysiological process observed during chronic and stress-induced acceleration of cardiac aging. Fibrosis is a necessary process during wound healing and tissue repair. However, its deposition in organs would proceed to scarring and organ damage. Here Alpinate Oxyphyllae Fructus (AOF), a Chinese medicine extract was used to protect aging heart from collagen accumulation. About 8 weeks old, male SD rats were randomly divided into (i) Control, (ii) D-galactose induced aging (IA), (iii) IA + AOF 50 (AOF low, AL), (iv) IA + AOF 100 (AOF medium, AM), (v) IA + AOF 150 (AOF high, AH) mg/kg/day, AOF was administered orally. After 8 weeks rats were sacrificed and hearts were collected. Results showed collagen deposition and up-regulation of matrix metalloproteinases-MMP-2 and -9 in D-galactose-induced aging rats. Furthermore, western blotting and immunostaining were also confirmed the upregulation of TGF-ß1 mediated fibrosis in aging induced rats. However, collagen deposition and fibrosis were significantly decreased by AOF treatments (AM and AH). AOF treatments salvaged the cardiac fibrosis. Hence, AOF might be a potential therapeutic agent in the prevention of cardiac fibrosis associated with aging. The protective effects of AOF might have promising results in anti-aging treatments.


Assuntos
Envelhecimento/efeitos dos fármacos , Alpinia/química , Medicamentos de Ervas Chinesas/farmacologia , Coração/efeitos dos fármacos , Miocárdio/patologia , Substâncias Protetoras/farmacologia , Envelhecimento/metabolismo , Envelhecimento/patologia , Animais , Colágeno/metabolismo , Medicamentos de Ervas Chinesas/isolamento & purificação , Fibrose , Frutas/química , Galactose , Masculino , Metaloproteinase 2 da Matriz/genética , Miocárdio/metabolismo , Substâncias Protetoras/isolamento & purificação , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Fator de Crescimento Transformador beta1/genética
16.
Nat Prod Res ; 33(6): 862-865, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29183163

RESUMO

Pinocembrin (1) and cardamonin (2) from Sozuku showed a suppressive effect on umu gene expression of SOS response in Salmonella typhimurium TA1535/pSK1002 against the mutagen furylfuramide. Compounds 1 and 2 suppressed 52% and 36% of SOS-inducing activity at a concentration of 0.20 µmol/mL. The ID50 value of 1 was 0.18 µmol/mL. These compounds showed the suppression of 2-amino-3,4-dimethylimidazo-[4,5-f]quinolone (MeIQ) and UV irradiation-induced SOS response. Pinostrobin (3) and 5,7-dimethoxyflavanone (4), methyl ethers of 1, showed similar activity to 1 against MeIQ-induced SOS response, but that of furylfuramide and UV irradiation were decreased. On the other hand, compounds 1-4 did not show the suppression of activated MeIQ-induced SOS response. Furthermore, compounds 1-4 showed potent antimutagenic activity against MeIQ mutagenesis in Ames test using the S. typhimurium TA100 and TA98 strains.


Assuntos
Alpinia/química , Antimutagênicos/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Flavonoides/farmacologia , Salmonella typhimurium/efeitos dos fármacos , Antimutagênicos/isolamento & purificação , Chalconas/isolamento & purificação , Chalconas/farmacologia , Flavanonas/isolamento & purificação , Flavanonas/farmacologia , Flavonoides/isolamento & purificação , Furilfuramida , Testes de Mutagenicidade , Mutagênicos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Quinolinas , Sementes/química
17.
Phytomedicine ; 50: 223-230, 2018 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-30466982

RESUMO

BACKGROUND: Alpinia nantoensis (Zingiberaceae) is an aromatic plant endemic to Taiwan, which is used as food flavoring and traditional herbal medicine. The biological activities of compounds isolated from this plant are rarely investigated. PURPOSE: The present study was aimed to investigate the anti-metastatic potential of trans-3­methoxy­5-hydroxystilbene (MHS) a major stilbene isolated from the rhizomes of A. nantonensis. METHODS: We investigated the anti-metastatic potential of MHS on human non-small cell lung carcinoma (A549) cell line using wound healing, trans-well, western blot, zymography and immunofluorescence assays. RESULTS: Initial cytotoxicity assay showed that treatment with MHS did not exhibit cytotoxicity to A549 cells up to the concentration of 40 µM. Further in vitro wound healing and transwell chamber assays revealed that MHS significantly inhibited tumor cell migration in a dose-dependent manner, which is associated with inhibition of matrix mettalloprotinase-2 (MMP-2) and matrix mettalloprotinase-9 (MMP-9) at both enzyme and protein levels. The inhibition of MMPs activity by MHS was reasoned by suppression of their corresponding transcription factor, ß-catenin as indicated by reduced levels of ß-catenin in the nucleus. MHS also regulates epithelial-to-mesenchymal transition (EMT) by increasing E-cadherin and occludin as well as decreasing N-cadherin levels in A549 cells. Furthermore, pre-treatment with MHS significantly inhibited A549 cells migration and EMT in TGF-ß induced A549 cells. CONCLUSION: To the best of our knowledge, this is the first report demonstrating that MHS, a plant-derived stilbene has a promising ability to inhibit lung cancer cell metastasis in vitro.


Assuntos
Alpinia/química , Antineoplásicos Fitogênicos/farmacologia , Movimento Celular/efeitos dos fármacos , Transição Epitelial-Mesenquimal , Estilbenos/farmacologia , Células A549 , Antígenos CD/metabolismo , Caderinas/metabolismo , Carcinoma Pulmonar de Células não Pequenas/patologia , Linhagem Celular Tumoral , Humanos , Neoplasias Pulmonares/patologia , Metaloproteinase 9 da Matriz/metabolismo , Metástase Neoplásica , Rizoma/química , Taiwan , Fator de Crescimento Transformador beta , beta Catenina/metabolismo
18.
Int J Biol Macromol ; 120(Pt B): 2442-2447, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30193916

RESUMO

Six diarylheptanoids (1-6) and two flavonoids (7 and 8) derived from Alpinia officinarum were evaluated for their ability to inhibit acetylcholinesterase. Compound 1 showed the highest degree of inhibition, with an IC50 of approximately 2 µM, followed by moderate degrees of inhibition by 2, 4 and 7, with IC50 values ranging from 20 to 40 µM. The remaining isolated compounds 3, 5, 6 and 8 had IC50 values greater than 50 µM. Enzyme kinetic studies showed that the compounds with high or moderate activity were competitive inhibitors, anchored to the active site of acetylcholinesterase. In particular, compounds 1 and 2 were docked at slightly different positions from those occupied by 4 and 7. Furthermore, molecular dynamics studies showed that compound 1 maintained its interactions with residues Thr74 and Phe295 throughout the simulation trajectory. Our findings suggest that compound 1 is a potential therapeutically relevant inhibitor of acetylcholinesterase.


Assuntos
Alpinia/química , Inibidores da Colinesterase/farmacologia , Colinesterases/metabolismo , Simulação por Computador , Simulação de Dinâmica Molecular , Extratos Vegetais/farmacologia , Rizoma/química , Domínio Catalítico , Inibidores da Colinesterase/química , Inibidores da Colinesterase/metabolismo , Concentração Inibidora 50 , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/metabolismo
19.
Food Funct ; 9(9): 4998-5006, 2018 Sep 19.
Artigo em Inglês | MEDLINE | ID: mdl-30187896

RESUMO

The anti-lung cancer activity of volatile oil from Alpinia officinarum (VOAO) and the underlying mechanism has not been studied. Herein, VOAO was extracted by steam distillation and its components were identified by GC-MS analysis. Cells viability was measured by an MTT assay and the cell survival capacity was tested via a colony formation assay. Apoptosis cells were detected using the Annexin V-FITC/PI method. Hoechst 33342 cell unclear staining was employed to evaluate the nuclear morphology change. The mitochondrial membrane potential was detected by a JC-1 staining assay. Bcl-2, Mcl-1 and cleaved caspase-3 proteins were quantified by immune blotting. Furthermore, VOAO anti-cancer activity was evaluated on an A549 cell xenograft nude mice model. Our results have revealed that VOAO could inhibit the cell viability of lung carcinoma cells and the colony formation capacity. VOAO downregulates Bcl-2 and Mcl-1 and triggers dysfunction of the mitochondrial membrane potential. VOAO further activates caspase-3 cleavage and induces lung cancer cells apoptosis. In addition, VOAO administration significantly suppresses lung cancer growth in xenograft mice without obvious hepatotoxicity. We conclude that VOAO could be an effective, low cytotoxicity natural component for treatment of lung carcinoma.


Assuntos
Alpinia/química , Antineoplásicos Fitogênicos/uso terapêutico , Apoptose/efeitos dos fármacos , Carcinoma/tratamento farmacológico , Neoplasias Pulmonares/tratamento farmacológico , Pulmão/efeitos dos fármacos , Óleos Voláteis/uso terapêutico , Animais , Anticarcinógenos/administração & dosagem , Anticarcinógenos/efeitos adversos , Anticarcinógenos/farmacologia , Anticarcinógenos/uso terapêutico , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/efeitos adversos , Antineoplásicos Fitogênicos/farmacologia , Carcinoma/metabolismo , Carcinoma/patologia , Carcinoma/prevenção & controle , Linhagem Celular Tumoral , Forma do Núcleo Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Pulmão/metabolismo , Pulmão/patologia , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/patologia , Neoplasias Pulmonares/prevenção & controle , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos Nus , Proteínas de Neoplasias/metabolismo , Óleos Voláteis/administração & dosagem , Óleos Voláteis/efeitos adversos , Óleos Voláteis/farmacologia , Distribuição Aleatória , Carga Tumoral/efeitos dos fármacos , Ensaios Antitumorais Modelo de Xenoenxerto
20.
Microb Pathog ; 124: 152-162, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30142463

RESUMO

The Alpinia purpurata inflorescence contains a lectin (ApuL), which has immunomodulatory activities on human cells. In the present work, it was evaluated the antibacterial and antifungal effects of ApuL against human pathogens. ApuL showed bacteriostatic activity against non-resistant (UFPEDA-02) and an oxacillin-resistant isolate (UFPEDA-672) of Staphylococcus aureus with minimal inhibitory concentrations (MIC50) of 50 and 400 µg/mL, respectively. In addition, it showed bactericidal effect on the non-resistant isolate (minimal bactericidal concentration: 200 µg/mL). For Candida albicans and Candida parapsilosis, ApuL showed fungistatic effect (MIC50: 200 and 400 µg/mL, respectively). The lectin was able to impair the viability of the microorganism cells, as indicated by propidium iodide (PI) staining. Analysis of growth curves, protein leakage, and ultrastructural changes supported that ApuL acts through distinct mechanisms on S. aureus isolates. Ultrastructural analysis of ApuL-treated Candida cells revealed malformations with elongations and bulges. ApuL-oxacillin combination showed synergistic effect on the oxacillin-resistant isolates UFPEDA-670 and 671, which were not sensitive to lectin alone. Synergism was also detected for ApuL-ceftazidime against a multidrug-resistant isolate of Pseudomonas aeruginosa. Synergistic action of ApuL-fluconazole was detected for C. parapsilosis, which was insensitive to the drug alone. Biofilm formation by S. aureus non-resistant isolate and C. albicans was remarkably inhibited by ApuL at sub-inhibitory concentrations. In conclusion, ApuL showed differential effects on non-resistant and resistant bacterial isolates, was active against Candida species, and showed synergistic action in combination with antibiotics.


Assuntos
Alpinia/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Biofilmes/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Lectinas/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Candida albicans/crescimento & desenvolvimento , Candida albicans/fisiologia , Sinergismo Farmacológico , Lectinas/isolamento & purificação , Testes de Sensibilidade Microbiana , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Staphylococcus aureus/crescimento & desenvolvimento , Staphylococcus aureus/fisiologia
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