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1.
Braz. j. biol ; 84: e253616, 2024. tab, graf
Artigo em Inglês | MEDLINE, LILACS, VETINDEX | ID: biblio-1355880

RESUMO

Abstract This study evaluated the effect of the volatile oil of Alpinia zerumbet (VOAz) on caveolin-1 gene expression and muscular fibrosis. The rats were immobilized to induce fibrosis of the gastrocnemius muscle, and they were treated with VOAz. Collagen quality was assessed by histology and the expression of the caveolin-1 (CAV-1) gene was evaluated using qPCR. Histomorphological analysis indicated a significant reduction in the perimeter, width, and intensity of collagen in the treated groups, thus showing that the oil was effective in regulating the quality of collagen at the three concentrations. The results of expression levels suggested a decrease in the lesioned group and in two treatment groups (0.0115 µg/g and 0.009 µg/g). However, with the lowest concentration (0.0065 µg/g), no significant difference was observed, with levels similar to those found in healthy tissue. Therefore, the results showed that VOAz has the potential to be a non-invasive and low-cost alternative to aid in the treatment of muscular fibrosis.


Resumo Este estudo avaliou o efeito do óleo volátil de Alpinia zerumbet (OVAz) na expressão do gene da caveolina-1 e na fibrose muscular. Os ratos foram imobilizados para induzir a fibrose do músculo gastrocnêmio, e foram tratados com OVAz. A qualidade do colágeno foi avaliada com histologia e à expressão do gene caveolina-1 (CAV-1) foi avaliada usando qPCR. A análise histomorfológica indicou uma redução significativa no perímetro, largura e intensidade do colágeno nos grupos tratados. Os resultados dos níveis de expressão sugeriram diminuição nos grupos de lesão e em dois grupos de tratamento (0,0115 µg/g e 0,009 µg/g). No entanto, com a menor concentração (0,0065 µg/g), não foi observada diferença significativa, apresentando níveis semelhantes aos encontrados em tecido saudável. O uso do OVAz foi eficaz para reverter as alterações do colágeno causadas pela fibrose, e sua menor concentração apresentou uma possível tendência de aumento na expressão do CAV-1. Portanto, os resultados mostraram que o OVAz tem potencial para ser uma alternativa não invasiva e de baixo custo para auxiliar no tratamento da fibrose muscular.


Assuntos
Animais , Ratos , Óleos Voláteis/farmacologia , Colágeno/metabolismo , Alpinia/química , Caveolina 1/metabolismo , Músculos/efeitos dos fármacos , Fibrose , Óleos Vegetais/farmacologia , Brasil , Ratos Wistar , Modelos Animais de Doenças , Músculos/patologia
2.
Oncol Rep ; 48(2)2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35730618

RESUMO

Alpinia katsumadai Hayata (AKH), a widely used traditional Chinese medicine, exerts various biological functions, including anti­inflammatory, antioxidant, anti­microbial and anti­asthmatic effects. However, studies on its anticancer activity and associated mechanisms are limited. The present study investigated the effects of ethanol extract from AKH on the viability of various human cancer and normal liver LX­2 cells using Cell Counting Kit­8 assay. Apoptosis was detected by Hoechst 33342/PI staining and Annexin­V­FITC/PI double staining. Autophagy was examined by Ad­GFP­LC3B transfection. The association between AKH­induced autophagy and apoptosis was investigated by pre­treatment of the cells with the autophagy inhibitors, 3­methyladenine (3MA) and bafilomycin A1 (Baf­A1), followed by treatment with AKH. The expression levels of cleaved poly(ADP­ribose) polymerase (PARP), caspase­8, caspase­3, caspase­9, phosphorylated (p­)AMP­activated protein kinase (AMPK), Akt, mTOR and p70S6K were examined using western blot analysis. The in vivo antitumor activity of AKH was investigated in nude mice bearing A549 lung cancer xenografts. The components of AKH were detected by liquid chromatography mass spectrometry­ion trap­time­of­flight mass spectrometry. The results revealed that AKH significantly inhibited the proliferation of various cancer cells with the half maximal inhibitory concentration (IC50) values of 203­284 µg/ml; however, its inhibitory effect was much less prominent against normal liver LX­2 cells with an IC50 value of 395 µg/ml. AKH markedly induced apoptosis and autophagy, and upregulated the protein expression of cleaved­caspase­3, caspase­8, caspase­9 and cleaved PARP in a concentration­dependent manner. Of note, the autophagy inhibitors (3MA and Baf­A1) significantly attenuated its pro­apoptotic effects on human pancreatic cancer Panc­28 and lung cancer A549 cells. Furthermore, AKH significantly increased the levels of p­AMPK, and decreased those of p­Akt, p­mTOR and p­p70S6K in Panc­28 and A549 cells. AKH markedly inhibited the growth of A549 tumor xenografts in vivo. In addition, a total of nine compounds were detected from AKH. The present study demonstrates that AKH markedly inhibits the growth and induces autophagy­related apoptosis in cancer cells by regulating the AMPK and Akt/mTOR/p70S6K signaling pathways. AKH and/or its active fractions may thus have potential to be developed as novel anticancer agents for clinical use.


Assuntos
Alpinia , Neoplasias Pulmonares , Proteínas Quinases Ativadas por AMP/metabolismo , Alpinia/metabolismo , Animais , Apoptose , Autofagia , Caspase 3/metabolismo , Caspase 8/metabolismo , Caspase 9/metabolismo , Linhagem Celular Tumoral , Humanos , Neoplasias Pulmonares/patologia , Camundongos , Camundongos Nus , Inibidores de Poli(ADP-Ribose) Polimerases/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Proteínas Quinases S6 Ribossômicas 70-kDa/metabolismo , Transdução de Sinais , Serina-Treonina Quinases TOR/metabolismo
3.
Biomed Res Int ; 2022: 2824535, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35726318

RESUMO

In traditional medicine, Alpinia oxyphylla Miquel seed has been used to treat gout and hyperuricemia-related symptoms by enhancing kidney functions. Allopurinol is the most commonly used drug to treat hyperuricemia; however, the drug has many adverse effects. Combining allopurinol with another compound could reduce the need for high doses and result in improved safety. We investigated the possible synergistic effects of Alpinia oxyphylla seed extract (AE) and allopurinol in decreasing urate concentrations in rats with potassium oxonate-induced hyperuricemia. This study evaluated the effects of allopurinol combined with AE on levels of serum urate, blood urea nitrogen (BUN), and creatinine in a hyperuricemic rat model. The effects of allopurinol plus AE on xanthine oxidase (XOD) activity and urate uptake were measured. The concomitant administration of allopurinol and AE normalized serum urate and reduced BUN and creatinine. The attenuation of hyperuricemia-induced impaired kidney function was related to downregulation of renal urate transporter 1 and upregulation of renal organic anion transporter 1, with inhibition of serum and hepatic XOD activities. The antihyperuricemic effects of allopurinol were enhanced when combined with AE. These results suggested that the combined use of allopurinol and AE may have clinical efficacy in treating hyperuricemia.


Assuntos
Alopurinol , Alpinia , Medicamentos de Ervas Chinesas , Hiperuricemia , Extratos Vegetais , Alopurinol/uso terapêutico , Alpinia/química , Animais , Creatinina/sangue , Medicamentos de Ervas Chinesas/uso terapêutico , Hiperuricemia/tratamento farmacológico , Rim , Extratos Vegetais/uso terapêutico , Ratos , Sementes/química , Ácido Úrico/sangue , Xantina Oxidase/metabolismo
4.
An Acad Bras Cienc ; 94(2): e20211164, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35703698

RESUMO

The analysis of gait in animals is important for understanding movement disorders in various human pathologies, especially those that develop muscle fibrosis. In the search for treatment alternatives for this problem, essential oils have been studied. Among them, research involving the essential oil of Alpinia zerumbet (EOAz) has been shown to promote relaxation and improve muscle function. Therefore, this study aimed to evaluate the effect of EOAz on gait with muscle fibrosis in immobilized rats. 30 rats (Wistar) were divided into five groups of six animals each: control group (without fibrosis and without treatment), immobilization group (with fibrosis and without treatment), and EOAz treatment groups (with fibrosis and with treatment). The animals were immobilized for 15 days with an ankle plantar flexion orthosis. After this period, they were treated with the oil cutaneously for 30 days. The analysis of behavioral tests before treatment indicated a significant increase in the means of the immobilized groups about to with concerning the control. We conclude that EOAz was effective in improving gait after inducing muscle fibrosis in immobilized rats. Studies are needed to assess the oil's effectiveness in the treatment of muscle fibrosis in human pathologies.


Assuntos
Alpinia , Óleos Voláteis , Animais , Fibrose , Análise da Marcha , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Folhas de Planta , Ratos , Ratos Wistar
5.
Molecules ; 27(9)2022 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-35566064

RESUMO

BACKGROUND: Alpinia officinarum (A. officinarum) is known to exhibit a beneficial effect for anti-inflammatory, anti-oxidant, and anti-hyperlipidemic effects. However, no sufficient research data are available on the cardiovascular effect of A. officinarum. Thus, in this study, we investigate whether A. officinarum extract has direct effects on vascular reactivity. METHODS: To examine whether A. officinarum extract affects vascular functionality, we measured isometric tension in rat mesenteric resistance arteries using a wire myograph. After arteries were pre-contracted with high-K+ (70 mM), phenylephrine (5 µM), or U46619 (1 µM), A. officinarum extract was treated. RESULTS: A. officinarum extract induced vasodilation in a concentration-dependent manner, and this effect was endothelium independent. To further investigate the mechanism, we incubated arteries in a Ca2+-free and high-K+ solution, followed by the cumulative addition of CaCl2 (0.01-2.5 mM) with or without A. officinarum extract (30 µg/mL). Pre-treatment of A. officinarum extract reduced the contractile responses induced by cumulative administration of Ca2+, which suggests that extracellular Ca2+ influx was inhibited by the treatment of A. officinarum extract. These results were associated with a reduction in phosphorylated MLC20 in VSMCs treated with A. officinarum extract. Furthermore, eucalyptol, an active compound of A. officinarum extract, had a similar effect as A. officinarum extract, which causes vasodilation in mesenteric resistance arteries. CONCLUSION: A. officinarum extract and its active compound eucalyptol induce concentration-dependent vasodilation in mesenteric resistance arteries. These results suggest that administration of A. officinarum extract could exert beneficial effects to treat high blood pressure.


Assuntos
Alpinia , Vasodilatação , Animais , Endotélio Vascular , Eucaliptol/farmacologia , Artérias Mesentéricas , Extratos Vegetais/farmacologia , Ratos
6.
Food Chem ; 389: 133011, 2022 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-35500409

RESUMO

The synchronous mitigative effects of Alpinia officinarum Hance (AOH) and curcumin on the generation of methylimidazole and acrylamide in cookies were investigated. Possible mechanisms related to quenching free radicals, reducing lipid oxidation and eliminating carbonyl intermediates were explored by electron paramagnetic resonance (EPR) and HPLC. The total methylimidazole and acrylamide contents raised with an increase in heating temperature and time, and reached a maximum at 200 °C for 11 min. AOH and curcumin reduced methylimidazole and acrylamide simultaneously; the maximum inhibition rates for methylimidazole and acrylamide were 51.55% (0.015% curcumin) and 73.66% (1.5% AOH). Alkyl free radicals and HO· were proved to be the critical free radicals for methylimidazole and acrylamide, AOH and curcumin quenched these radicals in a dose-dependent manner. The lipid oxidation, active carbonyl intermediates glyoxal, methylglyoxal, and acrylaldehyde were also reduced by AOH and curcumin simultaneously, which may be resulted from the quenching of free radicals.


Assuntos
Alpinia , Curcumina , Acrilamida , Espectroscopia de Ressonância de Spin Eletrônica , Radicais Livres , Lipídeos
7.
J Ethnopharmacol ; 295: 115397, 2022 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-35605918

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Alpinia officinarum Hance, a perennial natural medicine-food herb, has been traditionally used to treat colds, stomachache, and diabetes for thousands of years. 1,7-Diphenyl-4E-en-3-heptanone (DPH5), a diarylheptanoid isolated from the rhizome of A. officinarum has been reported to be safe and to have antioxidant and hypoglycemic effects, suggesting its potential in the treatment of insulin resistance (IR). AIM OF THE STUDY: Aim of to investigate the protective effect of DPH5 on IR and elucidate its underlying mechanism of action. MATERIALS AND METHODS: HepG2 cells were used as the research objects. Glucose uptake and reactive oxygen species (ROS) levels in high glucose-induced insulin-resistant HepG2 cells were assessed using flow cytometry. Glucose consumption and the levels of malondialdehyde (MDA) and superoxide dismutase (SOD) were analyzed using the corresponding assay kits. The expression of mRNA and proteins related to insulin signaling, glucose metabolism, and antioxidant factor, including insulin receptor substrate-1 (IRS1), phosphatidylinositol 3-kinase (PI3K), protein kinase B (AKT), translocation of glucose transporter-4, glycogen synthase kinase-3ß (GSK3ß), glucokinase (GCK), pyruvate kinase (PK), phosphoenolpyruvate carboxykinase (PEPCK), glucose-6-phosphatase (G6Pase), nuclear factor-erythroid 2 related factor 2 (Nrf2), heme oxygenase-1 (HO-1), NADPH quinoneoxidoreductase (NQO1), and glutathione peroxidase (GSH-Px) was determined using real-time quantitative polymerase chain reaction and western blotting. Furthermore, molecular docking was performed to determine the spatial mechanism of DPH5 on the key targets PI3K, AKT, Nrf2, and GSK3ß. RESULTS: DPH5 could improve IR that manifested as increased glucose uptake and glucose consumption in insulin-resistant HepG2 cells. Moreover, DPH5 could enhance antioxidant capacity by activating Nrf2/HO-1 elements, including increasing Nrf2, HO-1, SOD, NQO1, and GSH-Px expression and reducing MDA, ROS, and JNK levels, thereby improving oxidative stress and ultimately alleviating IR. Additionally, DPH5 could promote the expression of IRS1, PI3K, AKT, GSK3ß, GCK, and PK, and downregulate the expression of PEPCK and G6pase, thereby accelerating glucose utilization and enhancing insulin sensitivity. The mechanism underlying the effect of DPH5 in alleviating IR was related to the PI3K/AKT- and Nrf2/HO-1-mediated regulation of the GSK3ß signaling pathway, and the results were further confirmed using the specific inhibitors LY294002 and ML385. Results from molecular docking indicated that there were different regulatory sites and interacting forces between DPH5 and PI3K, AKT, Nrf2, and GSK3ß; however, the binding force was relatively strong. CONCLUSIONS: DPH5 improved oxidative stress and glucose metabolism via modulating the PI3K/AKT-Nrf2-GSK3ß pathway, thereby ameliorating IR. Overall, our findings suggest the potential of DPH5 as a natural medicine to treat type-2 diabetes mellitus.


Assuntos
Alpinia , Resistência à Insulina , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Diarileptanoides/farmacologia , Glucose/farmacologia , Glicogênio Sintase Quinase 3 beta/metabolismo , Células Hep G2 , Humanos , Insulina/metabolismo , Simulação de Acoplamento Molecular , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo , Fosfatidilinositol 3-Quinase/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais , Superóxido Dismutase/metabolismo
8.
Molecules ; 27(10)2022 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-35630752

RESUMO

This study aimed to investigate the chemical composition and reveal the selective inhibitory activity of Alpinia galanga (L.) Willd. essential oil (AGO) on acetylcholinesterase (AChE) compared to butyrylcholinesterase (BChE). The chemical composition of AGO was investigated by means of gas chromatography-mass spectrometry. Ellman's method was used to determine the inhibitory activities against AChE and BChE. Microemulsion systems with desirable anticholinesterase effects were developed. Methyl cinnamate and 1,8-cineole were reported as the major component of AGO. The IC50 values of A. galanga oil against AChE and BChE were 24.6 ± 9.6 and 825.4 ± 340.1 µg/mL, respectively. The superior selectivity of AGO on AChE (34.8 ± 8.9) compared to galantamine hydrobromide (6.4 ± 1.5) suggested AGO to be an effective ingredient with fewer side effects for Alzheimer's treatment. Interestingly, the microemulsion of AGO possessed significantly higher anticholinesterase activity than that of native oil alone. Therefore, microemulsion of AGO is a promising alternative approach for the treatment of Alzheimer's disease.


Assuntos
Alpinia , Óleos Voláteis , Acetilcolinesterase , Alpinia/química , Butirilcolinesterase , Inibidores da Colinesterase/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia
9.
Food Chem ; 392: 133314, 2022 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-35636195

RESUMO

This study evaluated drying characteristics, structure and essential oil chemical composition, and biological activity of A. galanga by hot air drying (HAD), vacuum drying (VD), freeze drying (FD). The results showed that HAD had the shortest drying time while FD could better maintain the microstructure and showed a higher essential oil yield than HAD and VD. In addition, E-nose, HS-GC-IMS and HS-SPME-GC-MS could effectively distinguish the essential oil chemical composition of the four samples because different drying methods induced the changes in the profile and content of the compounds. HS-SPME-GC-MS detected 43 compounds, of which alcohols, alkenes, and esters were the main substances in fresh and dry samples. In comparison, HS-SPME-GC-IMS detected 80 compounds, including alcohols, aldehydes, ketones, esters, alkenes. Overall, the FD samples showed more outstanding advantages by evaluating antioxidant properties and antibacterial activities. FD was more suitable for A. galanga drying as it maintains appearance and biological activity.


Assuntos
Alpinia , Óleos Voláteis , Compostos Orgânicos Voláteis , Álcoois , Alcenos , Alpinia/química , Antioxidantes/química , Ésteres , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Compostos Orgânicos Voláteis/química
10.
Int J Mol Sci ; 23(7)2022 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-35409351

RESUMO

Yakuchinone A (1) is a bioactive diarylheptanoid isolated from the dried fruits of Alpinia oxyphylla. Microbial transformation has been recognized as an efficient method to produce new biologically active derivatives from natural products. In the present study, microbial transformation of yakuchinone A was performed with the fungus Mucor hiemalis KCTC 26779, which led to the isolation of nine new metabolites (2, 3a, 3b, and 4-9). Their structures were elucidated as (3S)-oxyphyllacinol (2), (3S,7R)- and (3S,7S)-7-hydroxyoxyphyllacinol (3a and 3b), (3S)-oxyphyllacinol-4'-O-ß-d-glucopyranoside (4), (3S)-4″-hydroxyoxyphyllacinol (5), (3S)-3″-hydroxyoxyphyllacinol (6), (3S)-2″-hydroxyoxyphyllacinol (7), (3S)-2″-hydroxyoxyphyllacinol-2″-O-ß-d-glucopyranoside (8), and (3S)-oxyphyllacinol-3-O-ß-d-glucopyranoside (9) based on the comprehensive spectroscopic analyses and the application of modified Mosher's method. All compounds were evaluated for their cytotoxic activities against melanoma, as well as breast, lung, and colorectal cancer cell lines. Compound 9, which was O-glucosylated on the diarylheptanoid alkyl chain, exhibited the most selective cytotoxic activities against melanoma cell lines with the IC50 values ranging from 6.09 to 9.74 µM, indicating that it might be considered as a possible anti-cancer lead compound.


Assuntos
Alpinia , Melanoma , Alpinia/química , Diarileptanoides , Frutas , Humanos , Estrutura Molecular , Extratos Vegetais/química
11.
Food Chem ; 386: 132759, 2022 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-35339079

RESUMO

This study aimed to investigate the effects of different pretreatment methods on the drying process and quality of catalytic infrared dried ginger slices, particularly the safety quality. Four different pretreatments strategies were used: sample submerged in distilled water, water + US pretreatment, ethanol pretreatment, and ethanol + US pretreatment. The results showed that all pretreatments reduced drying time, and sample pretreatment by ethanol + US had the highest drying efficiency, hardness, highest total phenolic content, and total flavonoid content retention. However, these pretreatments slightly decreased the rehydration ratio and gingerol content. The possible explanation for these results has been put forward by microstructure analysis. CIR-dried ginger samples were pretreated by four methods required by the agricultural standards of China. This study provides a new perspective on the commercial application of ethanol + US pretreatment for CIR-dried ginger slices.


Assuntos
Alpinia , Gengibre , Dessecação/métodos , Etanol/química , Flavonoides/análise , Gengibre/química , Água
12.
J Agric Food Chem ; 70(13): 3989-3999, 2022 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-35321548

RESUMO

Alpinia hainanensis is an important food spice and ethnic medicine in Southwest China. In this study, we found that the EtOAc-soluble fraction (AHE) of the A. hainanensis rhizome ethanol extract could ameliorate dextran sulfate sodium-induced ulcerative colitis (UC). To explore active constituents, five pairs of previously unreported enantiomers (1-5), together with nine known ones (6-14), were obtained. Structural characterization was achieved by comprehensive spectroscopic methods. Compounds 1 and 2 were new curcumin-butyrovanillone hybrids featuring a rare structural fragment of 2,3-dihyrofuran. The anti-inflammatory activities of isolates were evaluated, and the results indicated that compounds (-)-1, (-)-3, 6, 9, 11, and 12 significantly inhibited the nuclear factor-κB signaling pathway. These findings indicate the major active fraction of the A. hainanensis rhizome ethanol extract enriched with diarylheptanoids, flavonoids, phenolics, and their hybrid mixtures, which could be developed as a nutritional and dietary supplement for treating UC.


Assuntos
Alpinia , Colite Ulcerativa , Animais , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Sulfato de Dextrana/efeitos adversos , Modelos Animais de Doenças , Humanos , NF-kappa B/metabolismo , Extratos Vegetais/química , Rizoma
13.
Food Chem ; 385: 132660, 2022 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-35306240

RESUMO

The capacity of Kaempferia galanga L. (KG) and kaempferol to mitigate the formation of free and bound heterocyclic amines (HAs) and advanced glycation end products (AGEs) in roast beef patties was explored. Electron paramagnetic resonance (EPR) and density functional theory (DFT) were used to reveal the possible mechanisms involved in quenching the free radicals. KG (0.5%, 1.0%, 1.5%) and kaempferol (0.005%, 0.010%, 0.015%) reduced HAs and AGEs in a dose-dependent manner. Alkyl free radical, HOO·, and 1O2 were critical to the formation of HAs, and 1O2 was pivotal to AGEs. They were quenched by KG and kaempferol in a dose-dependent manner. DFT indicated that the 3-OH group of kaempferol was most pivotal and quenched the HOO· mainly via H-atom transfer. The active carbonyl intermediates phenylacetaldehyde, glyoxal, and methylglyoxal can also be reduced by KG and kaempferol in a dose-dependent manner, which may be result from the quenching of free radicals.


Assuntos
Alpinia , Produtos Finais de Glicação Avançada , Aminas , Animais , Bovinos , Teoria da Densidade Funcional , Radicais Livres , Quempferóis
14.
Fitoterapia ; 158: 105141, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35124163

RESUMO

Proanthocyanidins (PACs) have various bioactivities, such as being anti-bacterial, anti-cancer, and anti-oxidant. Consequently, they have been vigorously studied for the development of new natural bioactive compounds. Recently, PAC was isolated from leaves and pseudostems of the medicinal plant Alpinia zerumbet (Pers.) B.L. Burtt and R.M. Smith, and it had shown in vitro antiviral activity against influenza A H1N1 viruses (IAVs). The 50% endpoint dilution method indicated that 0.1 mg/mL A. zerumbet-derived PAC (AzPAC) reduced the titer of IAVs by >3 logs. The antiviral activity of AzPAC means that it can interact directly with viral particles since the antiviral activity test was done by coincubation of PAC with and IAVs before viral infection. However, few studies have investigated the preventive mechanism utilized by AzPAC on influenza virus replication. In this study, the composition of AzPAC and the affinity between AzPAC and IAVs was investigated in detail. We found that AzPAC was composed of an epicatechin, which was linked by inter-flavan bonds between the C4 and C8 positions (B2-type) and the C4 and C6 positions (B5-type) in the terminal units. A quenching assay indicated that AzPAC interacted with IAV membrane proteins, hemagglutinin and neuraminidase. Additionally, circular dichroism analysis indicated that AzPAC affected the change in the secondary structure rate of the viral membrane proteins. AzPAC was able to impair the infective process of IAVs via direct interaction with their viral membrane proteins. These results indicate that A. zerumbet is a bioresource for the development of preventive drugs against IAV infection.


Assuntos
Alpinia , Vírus da Influenza A Subtipo H1N1 , Vírus da Influenza A , Proantocianidinas , Alpinia/química , Antivirais/farmacologia , Estrutura Molecular , Proantocianidinas/farmacologia , Replicação Viral
15.
Bioorg Chem ; 120: 105653, 2022 03.
Artigo em Inglês | MEDLINE | ID: mdl-35149263

RESUMO

Ten new diarylheptanoid dimers, katsumadainols C1 - C10 (1-10), were isolated from the seeds of Alpinia katsumada and elucidated by extensive spectroscopic methods, ECD calculations, and single-crystal X-ray diffraction. Their antidiabetic effects were evaluated by the stimulation of GLP-1 secretion in STC-1 cells and inhibition against four diabetes-related enzymes, GPa, α-glucosidase, PTP1B, and DPP4. Compounds 1-5 and 7-10 significantly stimulated GLP-1 secretion by 267.5-433.1% (25.0 µM) and 117.8-348.2% (12.5 µM). Compounds 1-4 exhibited significant inhibition on GPa with IC50 values of 18.0-31.3 µM; compounds 1-5 showed obvious inhibition on α-glucosidase with IC50 values of 6.9-18.2 µM; compounds 1-5 and 10 possessed PTP1B inhibitory activity with IC50 values ranging from 35.5 to 80.1 µM. This investigation first disclosed compounds 1-4 as intriguing GLP-1 secretagogues and GPa, α-glucosidase, and PTP1B inhibitors, which provided valuable clues for searching multiple-target antidiabetic candidates from Zingiberaceae plants.


Assuntos
Alpinia , Alpinia/química , Diarileptanoides/química , Diarileptanoides/farmacologia , Inibidores Enzimáticos/farmacologia , Peptídeo 1 Semelhante ao Glucagon , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/química , Secretagogos , alfa-Glucosidases
16.
Food Funct ; 13(4): 2228-2237, 2022 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-35133383

RESUMO

This study aimed to characterize the structural features of a novel water-soluble polysaccharide (AOHP) extracted from Alpinia officinarum Hance and to verify its regulating effect on mouse immunity. Cellulose DEAE-52 and Sephadex G-100 columns were used to obtain purified AOHP. Techniques including NMR, methylation, monosaccharide composition, FT-IR, and molecular weight determination were applied to investigate the physicochemical properties and structural characterization of AOHP. Then, the influence of AOHP on mice was studied. After oral administration of AOHP, organ indexes, serum biochemistry indexes, and cytokines in the spleens of the mice were analysed. The results showed that AOHP was composed of T-α-D-Glcp, (1,4)-α-D-Glcp and (1,4,6)-α-D-Glcp with a number-average molecular weight of 26.0 kDa and a weight-average molecular weight of 52.8 kDa. Additionally, the innate immune statuses of the mice were improved by treatment with AOHP, while no obvious damage was identified. To conclude, the immunomodulatory activity and biological safety make AOHP a viable candidate as an ingredient for healthcare drugs.


Assuntos
Alpinia , Fatores Imunológicos/farmacologia , Imunomodulação/efeitos dos fármacos , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Administração Oral , Animais , Feminino , Fatores Imunológicos/administração & dosagem , Fatores Imunológicos/química , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Polissacarídeos/administração & dosagem , Polissacarídeos/química , Espectroscopia de Infravermelho com Transformada de Fourier
17.
J Ethnopharmacol ; 288: 114975, 2022 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-35026343

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Alpinia calcarata (Haw.) Roscoe rhizomes are used to treat diabetes, rheumatism, gastrointestinal problems, inflammatory diseases, cough and respiratory problems in traditional practices. The primary objective of the study is to identify and isolate anti-inflammatory bioactive compounds from A.calcarata rhizomes and to assess its molecular mechanism. MATERIALS AND METHODS: The bioassay-guided fractionation of methanolic extract of A. calcarata rhizomes yielded chloroform fraction as the effective fraction and galangin as the bioactive compound identified by NMR studies. The anti-inflammatory action of galangin was evaluated by determining NO and cytokine production in LPS stimulated RAW264.7 cells. Further, its mechanism was studied on the expression levels of mRNA and protein targets by qPCR and Western blot analysis. RESULTS: Based on the MTT assay, the concentration of 3.1-25 µM of galangin was selected for further studies. Galangin reduced the levels of NO and proinflammatory cytokines (TNF-α, IL-1ß and IL-6) production in LPS induced RAW 264.7 cells in a dose-dependent manner. In addition, the qPCR analysis revealed a reduction in the mRNA expression levels of COX-2, IRAK 1 and JAK 1 in galangin treated LPS stimulated RAW 264.7 cells in a dose-dependent manner. Western blot analysis implicated that galangin has markedly reduced the protein expression levels of cell signaling regulators (JAK-1, IRAK-1, MyD88, MAPK (p38 and ERK) and NF-κB p65). CONCLUSION: From the results, it is evident that the inhibition of these cell signaling regulators has contributed to the anti-inflammatory effects of galangin. To our knowledge, we are the first to report IRAK-1 and JAK-1 as therapeutic targets of galangin for its anti-inflammatory effect.


Assuntos
Alpinia/química , Anti-Inflamatórios/farmacologia , Flavonoides/farmacologia , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Relação Dose-Resposta a Droga , Flavonoides/administração & dosagem , Flavonoides/isolamento & purificação , Inflamação/tratamento farmacológico , Inflamação/patologia , Quinases Associadas a Receptores de Interleucina-1/metabolismo , Janus Quinase 1/metabolismo , Lipopolissacarídeos , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Extratos Vegetais/administração & dosagem , Células RAW 264.7 , Rizoma , Fator de Transcrição RelA/metabolismo
18.
Exp Appl Acarol ; 86(2): 313-326, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35024988

RESUMO

Acaricidal activities and acetylcholinesterase (AChE) inhibitory activities were evaluated of active constituents of the essential oil extracted from Alpinia galanga rhizomes cultivated from India and their derivatives against Haemaphysalis longicornis nymphs. In addition, the effect was investigated of active components of A. galanga oil on egg laying of adult females of H. longicornis and egg hatchability. Of the volatile components identified in A. galanga oil, ethyl cinnamate, ethyl methoxycinnamate, and methyl cinnamate at 0.32 mg/cm2 resulted in 100% mortality, respectively, indicating that the acaricidal activity of the A. galanga oil against H. longicornis nymphs could be attributed to these compounds. To evaluate the structure-activity relationship between cinnamate derivatives and their acaricidal activities, allyl cinnamate, benzyl cinnamate, isopropyl cinnamate, isobutyl cinnamate, and isoamyl cinnamate were selected. Among cinnamate derivatives tested, allyl cinnamate exhibited the most potent toxicity (LC50 = 0.055 mg/cm2) against H. longicornis nymphs. The allyl cinnamate was also tested for AChE activity in vivo in H. longicornis nymphs and was found to affect the AChE activity. Allyl cinnamate at 10-50 mg/mL inhibited egg laying of adult females of H. longicornis by 10-43%. Egg hatching was suppressed completely by treatment with allyl cinnamate at 50 mg/mL, whereas allyl cinnamate was minimally toxic against non-target earthworms, Eisenia fetida. These results suggest that allyl cinnamate can be used as an active ingredient for the development of eco-friendly tick acaricides against H. longicornis, a vector for Sever fever with thrombocytopenia syndrome (SFTS) virus.


Assuntos
Acaricidas , Alpinia , Ixodidae , Óleos Voláteis , Acaricidas/farmacologia , Acetilcolinesterase , Animais , Óleos Voláteis/farmacologia , Rizoma
19.
Anticancer Agents Med Chem ; 22(4): 721-730, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34229591

RESUMO

BACKGROUND: Various plant species have been shown to be effective in the prevention or adjuvant therapy of cancer. Alpinia officinarum and its main phytochemicals have also been the subject of several studies for their anticancer properties. OBJECTIVE: The objective of this study is to analyze the extracts of A. officinarum to quantify flavonoids and to evaluate the growth inhibitory effects of the extracts on MCF-7 and LNCaP cells. METHODS: A. officinarum aqueous and hydroalcoholic extracts were analyzed by using High-Performance Liquid Chromatography (HPLC) for the quantification of three flavonoid compounds. Then, MCF-7, LNCaP, and fibroblast cells were treated with several concentrations (25, 50, 100, 200, and 400 µg/mL) of extracts (24, 48 and 72h). Cell viability was assessed using an MTT assay. Flow cytometry was conducted to evaluate apoptosis. RESULTS: Galangin and kaempferol (3.85 and 1.57 mg/g dry extract) were quantified, respectively, in hydroalcoholic and aqueous extracts using a validated method. The hydroalcoholic extract significantly decreased the viability of MCF-7 (IC50: 43.45µg/mL for 48h) and LNCaP cells (IC50: 168 µg/mL for 48h). The aqueous extract reduced cancer cell viability by more than 50% only at 200 and 400 µg/mL (72 h). Treatment of primary fibroblasts with both extracts showed no significant decrease in cell viability (25-100 µg/mL; 24 and 48h). The hydroalcoholic extract induced a significant increase in apoptotic cells in both MCF-7 and LNCaP cells. CONCLUSION: Obtained results demonstrated the cytotoxicity of A. officinarum through apoptosis induction in two cancer cell lines. Further investigations are required to determine the underlying apoptotic cell death mechanisms induced by A. officinarum in cancerous cells.


Assuntos
Alpinia , Neoplasias da Mama , Carcinoma , Alpinia/química , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Cromatografia Líquida de Alta Pressão , Flavonoides/farmacologia , Humanos , Células MCF-7 , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Próstata/patologia
20.
Planta Med ; 88(2): 163-178, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33445186

RESUMO

Estrogen receptor-positive breast cancer patients have a good prognosis, but 30% of these patients will experience recurrence due to the development of resistance through various signaling pathways. This study aimed to evaluate the mode of anticancer effects of 1'-acetoxychavicol acetate, which is isolated from the rhizomes of Alpinia galanga in estrogen receptor positive (MCF7) human epidermal growth factor receptor 2-overexpressed (MCF7/HER2), and endocrine-resistant breast cancer cells (MCF7/LCC2 and MCF7/LCC9). 1'-Acetoxychavicol acetate showed antiproliferation in a concentration- and time-dependent fashion and had higher potency in human epidermal growth factor receptor 2-overexpressed cell lines. This was associated with down-regulation of human epidermal growth factor receptor 2, pERK1/2, pAKT, estrogen receptor coactivator, cyclin D1, and MYC proto-oncogene while in vivo and significant reduction in the tumor mass of 1'-acetoxychavicol acetate-treated zebrafish-engrafted breast cancer groups. The anti-invasive effects of 1'-acetoxychavicol acetate were confirmed in vitro by the matrigel invasion assay and with down-regulation of C - X-C chemokine receptor type 4, urokinase plasminogen activator, vascular endothelial growth factor, and basic fibroblast growth factor 2 genes. The down-regulation of urokinase plasminogen activator and fibroblast growth factor 2 proteins was also validated by molecular docking analysis. Moreover, 1'-acetoxychavicol acetate-treated cells exhibited lower expression levels of the anti-apoptotic Bcl-2 and Mcl-1 proteins in addition to enhanced stress-activated kinases/c-Jun N-terminal kinase 1/2 and poly-ADP ribose polymerase cleavage, indicating apoptotic cell induction by 1'-acetoxychavicol acetate. Moreover, 1'-acetoxychavicol acetate had higher potency in human epidermal growth factor receptor 2-overexpressed cell lines regarding its inhibition on human epidermal growth factor receptor 2, pAKT, pERK1/2, PSer118, and PSer167-ERα proteins. Our findings suggest 1'-acetoxychavicol acetate mediates its anti-cancer effects via human epidermal growth factor receptor 2 signaling pathway.


Assuntos
Alpinia , Apoptose , Álcoois Benzílicos/farmacologia , Neoplasias da Mama , Alpinia/química , Animais , Neoplasias da Mama/tratamento farmacológico , Proliferação de Células , Feminino , Humanos , Células MCF-7 , Simulação de Acoplamento Molecular , Transdução de Sinais , Peixe-Zebra
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