Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 71
Filtrar
1.
Zhongguo Zhong Yao Za Zhi ; 49(6): 1526-1539, 2024 Mar.
Artículo en Chino | MEDLINE | ID: mdl-38621936

RESUMEN

This study aims to investigate the component variations and spatial distribution of ginsenosides in Panax quinquefolium roots during repeated steaming and drying. Ultra performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry(UPLC-Q-TOF-MS/MS) was employed to identify the ginsenosides in the root extract. Matrix-assisted laser desorption/ionization mass spectrometry imaging(MALDI-MSI) was employed to visualize the spatial distribution and spatiotemporal changes of prototype ginsenosides and metabolites in P. quinquefolium roots. The UPLC results showed that 90 ginsenosides were identified during the steaming process of the roots, and polar ginsenosides were converted into low polar or non-polar ginsenosides. The content of prototype ginsenosides decreased, while that of rare ginsenosides increased, which included 20(S/R)-ginsenoside Rg_3, 20(S/R)-ginsenoside Rh_2, and ginsenosides Rk_1, Rg_5, Rs_5, and Rs_4. MALDI-MSI results showed that ginsenosides were mainly distributed in the epidermis and phloem. As the steaming times increased, ginsenosides were transported to the xylem and medulla. This study provides fundamental information for revealing the changes of biological activity and pharmacological effect of P. quinquefolium roots that are caused by repeated steaming and drying and gives a reference for expanding the application scope of this herbal medicine.


Asunto(s)
Ginsenósidos , Panax , Ginsenósidos/análisis , Espectrometría de Masas en Tándem , Espectrometría de Masa por Láser de Matriz Asistida de Ionización Desorción/métodos , Panax/química , Cromatografía Líquida de Alta Presión/métodos , Raíces de Plantas/química
2.
Biomed Pharmacother ; 174: 116521, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38593700

RESUMEN

AIM: American ginseng berries, grown in the aerial parts and harvested in August, are a potentially valuable material. The aim of the study was to analyze the specific polysaccharides in American ginseng berries, and to demonstrate the anti-inflammation effect through in vitro and in vivo experiments and molecular docking. METHODS: After deproteinization and dialysis, the extracted crude polysaccharide was separated and purified. The structure of the specific isolated polysaccharide was investigated by Fourier Transform infrared spectroscopy (FT-IR), GC-MS and nuclear magnetic resonance (NMR), and anti-inflammatory activity was evaluated using in vitro and in vivo models (Raw 264.7 cells and zebrafish). Molecular docking was used to analyze the binding capacity and interaction with cyclooxygenase-2 (COX-2). RESULTS: A novel neutral polysaccharide fraction (AGBP-A) was isolated from American ginseng berries. The structural analysis demonstrated that AGBP-A had a weight-average molecular weight (Mw) of 122,988 Da with a dispersity index (Mw/Mn) value of 1.59 and was composed of arabinose and galactose with a core structure containing →6)-Gal-(1→ residues as the backbone and a branching substitution at the C3 position. The side-chains comprised of α-L-Ara-(1→, α-L-Ara-(1→, →5)-α-L-Ara-(1→, ß-D-Gal-(1→. The results showed that it significantly decreased pro-inflammatory cytokines in the cell model. In a zebrafish model, AGBP-A reduced the massive recruitment of neutrophils to the caudal lateral line neuromast, suggesting the relief of inflammation. Molecular docking was used to analyze the combined capacity and interaction with COX-2. CONCLUSION: Our study indicated the potential efficacy of AGBP-A as a safe and valid natural anti-inflammatory component.


Asunto(s)
Antiinflamatorios , Panax , Polisacáridos , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Frutas , Simulación del Acoplamiento Molecular , Panax/química , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Polisacáridos/farmacología , Espectroscopía Infrarroja por Transformada de Fourier , Células RAW 264.7 , Animales , Ratones
3.
Int J Biol Macromol ; 259(Pt 2): 129394, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38218277

RESUMEN

In this study, the green synthesis of chitosan/glutamic acid/agarose/Ag (Chi/GA/Aga/Ag) nanocomposite hydrogel was obtained via in situ reduction of Ag ions during the crosslinking process of chitosan-agarose double network hydrogels. The rich hydroxyl, carboxyl and amino groups in both agarose, chitosan, and glutamic acid can effectively control the growth, dispersion and immobilization of nearly spherical Ag nanoparticles (70 nm) in the Chi/GA/Aga/Ag composite hydrogel. Glutamic acids can act as the structure-directing agents to induce the formation of chitosan/glutamic acid hydrogel. The mechanical strength of the Chi/GA/Aga/Ag composite hydrogel can be enhanced by the introduction of chitosan-agarose double network hydrogels, which guarantees that it can be directly used as a visual test strip of the Cu ions with a lower detection limit of 1 µM and an active catalyst for the reduction of 4-nitrophenol within 18 min. The quantitative and semi-quantitative measurement of Cu ions can be carried out by UV-visible absorption spectroscopy and visual measurement, which provided a convenient, portable, and "naked-eye" solid-state detection methodology.


Asunto(s)
Antígenos de Grupos Sanguíneos , Quitosano , Nanopartículas del Metal , Nitrofenoles , Sefarosa/química , Plata/química , Nanogeles , Quitosano/química , Ácido Glutámico , Nanopartículas del Metal/química , Colorimetría , Hidrogeles/química
4.
J Sep Sci ; 46(20): e2300306, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37654052

RESUMEN

Bergenia ciliata (haw.) Sternb, the renowned pharmaceutical plant in Jammu and Kashmir of Pakistan, is widely applied in treating different illnesses including diabetes, diarrhea, and vomiting. This work employed an efficient one-step inner-recycling counter-current chromatography for preparative separating and purifying compounds with similar partition coefficients from the rhizome of Bergenia ciliate (haw.). Five compounds, including quercetin rhamnodiglucoside (1), quercetin-3-O-rutinoside (2), bergenine (3), kaempferol (4), and palmatic acid (5), were successfully separated using the optimized biphasic solvent system that contained ter-butylmetylether/n-butanol/acetonitrile/water (2:2:1:5, v/v) with the purities over 98%. Mass spectrometry and nuclear magnetic resonance were conducted for structural identification. As a result, our proposed strategy might be applied in separating compounds with similar partition coefficients, which was advantageous with regard to the less solvent and time consumption, and the increased number of theoretical plates.


Asunto(s)
Distribución en Contracorriente , Plantas Medicinales , Distribución en Contracorriente/métodos , Extractos Vegetales/análisis , Rizoma/química , Solventes/análisis , Cromatografía Líquida de Alta Presión
5.
J Sep Sci ; 46(19): e2300238, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37548129

RESUMEN

Gynostemma pentaphyllum (Thunb.) Makino represents the popular health food and supplemental product with broad pharmacological activities. The highly polar glycosides, including flavonoids and saponins, are major effective active components that contain diverse sugar positions and quantities, which result in diverse chemical polarities, making it challenging to separate and isolate these components. The present work described the rapid and efficient linear gradient counter-current chromatography to preparatively separate glycosides from aboveground parts of G. pentaphyllum. Besides, the ethyl acetate and n-butanol binary mobile phases were achieved through adjusting associated proportions. Six glycosides, including quercetin-3-O-neohesperidoside (1), kaempferol-3-O-robinobioside (2), kaempferol-3-O-neohesperidoside (3), gypenoside LVI (4), ginsenoside Rb3 (5), and gypenoside XLVI (6), were isolated at the purities greater than 98%. Moreover, electrospray ionization mass spectrometry and nuclear magnetic resonance tandem mass spectrometry were conducted for structural identification. According to our findings, the established linear gradient counter-current chromatography was an efficient approach to separate the highly polar glycosides from aboveground parts of G. pentaphyllum. Our proposed strategy can be used to separate active compounds from other complex natural products.

6.
ACS Omega ; 8(28): 25582-25591, 2023 Jul 18.
Artículo en Inglés | MEDLINE | ID: mdl-37483222

RESUMEN

The refractive index (RI) is an important physiochemical property of deep eutectic solvents (DESs) for application in the optical identification of specific substances or measuring the concentration of solutes in solutions. However, the available data on the RI of DESs is limited. Here, a systematic investigation on the RI of 48 typical DESs and 30 mixtures with water was conducted under atmospheric pressure. The effect of temperature in the range 293.15-338.15 K, hydrogen-bonding donors (HBDs), and hydrogen-bonding acceptors (HBAs) on RI was investigated. Furthermore, the RI of DESs as a function of mass percentage in the range of 20-80% water was also studied. It was found that the RI of DESs and its aqueous binary mixtures decreases linearly with the increase of temperature. HBDs and HBAs had a significant influence on the RI of DESs. Among them, the RI of choline chloride (ChCl)/phenol and ChCl/o-cresol were obviously higher than those of other DESs. It was also found that the addition of water would decrease the RI of DESs, and the RI of DES content in percentage (wt %) of water binary mixtures increases linearly as a function of mass percentage of DESs for 20 DESs. However, for the other 10 DESs, there is no linear relationship between the RI and the DES content.

7.
Int J Biol Macromol ; 248: 125586, 2023 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-37379950

RESUMEN

American ginseng, a precious classic herbal medicine, is used extensively in China for life prolongation purpose. This study aimed to elucidate the structure and anti-inflammatory activity of a neutral polysaccharide isolated from American ginseng (AGP-A). Nuclear magnetic resonance in conjunction with gas chromatography-mass spectrometry were used to analyze AGP-A's structure, whereas Raw264.7 cell and zebrafish models were employed to assess its anti-inflammatory activity. According to the results, AGP-A has a molecular weight of 5561 Da and is primarily consisted of glucose. Additionally, linear α-(1 â†’ 4)-glucans with α-D-Glcp-(1 â†’ 6)-α-Glcp-(1→ residues linked to the backbone at C-6 formed the backbone of AGP-A. Furthermore, AGP-A significantly decreased pro-inflammatory cytokines (IL-1ß, IL-6 and TNF-α) in Raw264.7 cell model. AGP-A in zebrafish model significantly lower the massive recruitment of neutrophils to the neuromast of the caudal lateral line. Inflammation may be relieved by the AGP-A component in American ginseng based on these results. In conclusion, our study shows the structural characterization, remarkable anti-inflammatory properties of AGP-A and its potential curative efficacy as a safe, valid natural anti-inflammatory medicine.


Asunto(s)
Panax , Pez Cebra , Ratones , Animales , Extractos Vegetales/química , Polisacáridos/química , Antiinflamatorios/química , Células RAW 264.7 , Panax/química , Peso Molecular
8.
J Sep Sci ; 46(16): e2300053, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37376800

RESUMEN

In this work, the preparative separation of quinolyridine alkaloids from seeds of T. lanceolata by conventional and pH-zone-refining counter-current chromatography. Traditional counter-current chromatography separation was performed by a flow-rate changing strategy with a solvent system of ethyl acetate-n-butanol-water (1:9:10, v/v) and 200 mg sample loading. Meanwhile, the pH-zone-refining mode was adopted for separating 2.0 g crude alkaloid extracts with the chloroform-methanol-water (4:3:3, v/v) solvent system using the stationary and mobile phases of 40 mM hydrochloric acid and 10 mM triethylamine. Finally, six compounds, including N-formylcytisine (two conformers) (1), N-acetycytisine (two conformers) (2), (-)-cytisine (3), 13-ß-hydroxylthermopsine (4), N-methylcytisine (5), and thermopsine (6) were successfully obtained in the two counter-current chromatography modes with the purities over 96.5%. Moreover, we adopted nuclear magnetic resonance and mass spectrometry for structural characterization. Based on the obtained findings, the pH-zone-refining mode was the efficient method to separate quinolyridine alkaloids relative to the traditional mode.


Asunto(s)
Alcaloides , Extractos Vegetales , Extractos Vegetales/química , Distribución en Contracorriente/métodos , Concentración de Iones de Hidrógeno , Cromatografía Líquida de Alta Presión/métodos , Alcaloides/análisis , Solventes/química , Agua , Semillas/química
9.
Front Pharmacol ; 14: 1149191, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37251325

RESUMEN

Nanohydrogels show great potential as efficient drug carriers due to their biocompatibility, low toxicity, and high water absorbability. In this paper, we prepared two O-carboxymethylated chitosan (OCMC)-based polymers functionalized with ß-cyclodextrin (ß-CD) and amino acid. The structures of the polymers were characterized by Fourier Transform Infrared (FTIR) Spectroscopy. Morphological study was carried out on a Transmission Electron Microscope (TEM), and the results indicated that the two polymers had irregular spheroidal structure with some pores distributed on their surface. The average particle diameter was below 500 nm, and the zeta potential was above +30 mV. The two polymers were further used for preparing nanohydrogels loaded with anticancer drugs lapatinib and ginsenoside Rg1, and the resulting nanohydrogels showed high drug loading efficiency and pH-sensitive (pH = 4.5) drug release behavior. In vitro cytotoxicity investigation revealed that the nanohydrogels exhibited high cytotoxicity against lung cancer (A549) cells. In vivo anticancer investigation was performed in a transgenic Tg(fabp10:rtTA2s-M2; TRE2:EGFP-kras V12) zebrafish model. The results showed that the synthesized nanohydrogels significantly inhibited the expression of EGFP-kras v12 oncogene in zebrafish liver, and the L-arginine modified OCMC-g-Suc-ß-CD nanohydrogels loading lapatinib and ginsenoside Rg1 showed the best results.

10.
J Sep Sci ; 46(10): e2300042, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-36939191

RESUMEN

Cyperus rotundus L. has been extensively used in ancient medication for the treatment of different disorders worldwide, in which sesquiterpenes are the most representative components. In this study, sesquiterpenes were effectively purified by two-dimensional counter-current chromatography in combination with continuous injection and inner-recycling mode with a solvent system of n-hexane/ethyl acetate/methanol/water (1:0.2:1:0.2, v/v/v/v). For one-dimension separation, continuous injection mode was used with three times injection and the inner-recycling mode was adopted for the separation of two mixtures for two-dimensional separation. Finally, four sesquiterpenoids, including scariodione (1), cyperenoic acid (2), scariodione (3), and α-cyperone (4), were obtained with purities over 98%. Mass spectrometry and nuclear magnetic resonance were applied to identify their structures. The results from the anti-inflammation effect with zebrafish demonstrated that cyperenoic acid exhibited stronger anti-inflammation activity. Molecular docking results suggested that cyperenoic acid possessed lower binding energies -9.4545 kcal/mol with 1CX2 to form formed hydrogen bond interaction with ARG120. In general, all the obtained findings proved that the strong anti-inflammation capacity of cyperenoic acid can have the potential of being adopted for treating diseases resulting from inflammation.


Asunto(s)
Cyperus , Sesquiterpenos , Animales , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Cyperus/química , Distribución en Contracorriente/métodos , Rizoma , Pez Cebra , Antiinflamatorios
11.
J Sep Sci ; 46(9): e2300046, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-36853146

RESUMEN

As a famous health food, roots of Panax quinquefolium L. possessed immune regulation and enhancement of the central nervous system, in which ginsenosides are the main active component with different numbers and positions of sugars, causing different chemical polarities with a challenge for the separation and isolation. In this study, a fast and effective bilinear gradient counter-current chromatography was proposed for preparative isolation ginsenosides with a broad partition coefficient range from roots of Panax quinquefolium L. In terms of the established method, the mobile phases comprising n-butanol and ethyl acetate were achieved by adjusting the proportion. Coupled with the preparative HPLC, eleven main ginsenosides were successfully separated, including ginsenoside Rg1 (1), Re (2), acetyl ginsenoside Rg1 (3), Rb1 (4), Rc (5), Rg2 (6), Rb3 (7), quinquefolium R1 (8), Rd (9), gypenoside X VII (10) and notoginsenoside Fd (11), with purities exceeding 95% according to the HPLC results. Tandem mass spectrometry and electrospray ionization mass spectrometry were adopted for recognizing the isolated compound architectures. Our study suggests that linear gradient counter-current chromatography effectively separates the broad partition coefficient range of ginsenosides compounds from the roots of Panax quinquefolium L. In addition, it can apply to active compound isolation from other complicated natural products.


Asunto(s)
Ginsenósidos , Panax , Ginsenósidos/química , Cromatografía Líquida de Alta Presión/métodos , Panax/química , Distribución en Contracorriente/métodos , Raíces de Plantas/química
12.
Nat Prod Res ; 37(6): 919-927, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35793441

RESUMEN

Four new isolates including one new butanediamide glycoside (1), one new flavonoid glycoside (2) and two new flavonone glycosides (3, 4) were identified from the leaves and stems of Panax quinquefolius, among which 1 possessed the firstly reported N,N'-(5-hydroxy-1,3-phenylene) butanediamide skeleton with an unique 6/9 ranged dual-ring structure. The structures were elucidated by the NMR data, ECD analysis and chemical acid hydrolysis. All the compounds (1-4) were tested for their cytotoxicity against two human cancer cell lines of HepG2, A549 and HCT116 by the MTT method. Outstandingly, compound 1 exhibited targeted inhibitory proliferation of HCT116 cell with IC50 value of 12.1 µM, whereas compounds 3 and 4 exhibited targeted inhibitory proliferation of HepG2 cell with IC50 values of 15.3 and 17.3 µM, as well as no obvious cytotoxicity of compounds 1-4 against A549.


Asunto(s)
Antineoplásicos , Panax , Humanos , Panax/química , Flavonoides/química , Glicósidos/química , Antineoplásicos/análisis , Hojas de la Planta/química , Estructura Molecular
13.
J Ethnopharmacol ; 305: 116110, 2023 Apr 06.
Artículo en Inglés | MEDLINE | ID: mdl-36581162

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Hyperlipidemia is the systemic manifestation of abnormal lipid metabolism, characterized by elevated circulating levels of cholesterol and triglyceride and a high risk of cardiovascular events. Radix Bupleuri (RB) is a traditional Chinese herbal product used to treat liver diseases. Our previous study demonstrated that Saikosaponins (SSs), the most potent bioactive ingredients in RB, ameliorate hepatic steatosis. However, whether SSs have anti-hyperlipidemia effects and plausible underlying mechanisms remain elusive. AIM OF THE STUDY: To comprehensively evaluate the lipid-lowering potential of SSs against hyperlipidemia in rats. MATERIALS AND METHODS: RNA sequencing and untargeted metabolomics approaches were applied to analyze the changes in the liver transcriptome and serum lipid profile in long-term high-fat diet feeding-induced hyperlipidemia rats in response to SSs or positive drug simvastatin (SIM) intervention. RESULTS: Our data revealed that SSs significantly alleviated HFD-induced hypertriglyceridemia and hypercholesterolemia. Combined with the analysis of gene ontology enrichment analysis and gene set enrichment analysis, we found that SSs remarkably repaired the unbalanced blood lipid metabolic spectrum in a dose-dependent manner by increasing the hepatic uptake of circulating fatty acids and facilitating mitochondrial respiration in fatty acid oxidation, comparable to SIM group. In addition, SSs markedly modulated cholesterol clearance by promoting intracellular cholesterol efflux, HDL remodeling, LDL particle clearance, and bile acid synthesis. SSs also efficiently protected the liver from lipid overload-related oxidative stress and lipid peroxidation, as well as substantially exaggerated inflammatory response. CONCLUSION: Our research not only unraveled the intricate mechanisms underlying the lipid-lowering functions of SSs but also provided novel perspectives on developing an SSs-based therapeutic strategy for the treatment of hyperlipidemia. CLASSIFICATION: Metabolism.


Asunto(s)
Hiperlipidemias , Hígado , Ratas , Animales , Ratas Sprague-Dawley , Hiperlipidemias/tratamiento farmacológico , Hiperlipidemias/metabolismo , Metabolismo de los Lípidos , Lípidos , Colesterol , Dieta Alta en Grasa/efectos adversos
14.
Curr Cancer Drug Targets ; 23(4): 251-264, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36278447

RESUMEN

The previous year's worldview for cancer treatment has advanced from general to more precise therapeutic approaches. Chemotherapies were first distinguished as the most reliable and brief therapy with promising outcomes in cancer patients. However, patients could also suffer from severe toxicities resulting from chemotherapeutic drug usage. An improved comprehension of cancer pathogenesis has led to new treatment choices, including tumor-targeted therapy and immunotherapy. Subsequently, cancer immunotherapy and targeted therapy give more hope to patients since their combination has tremendous therapeutic efficacy. The immune system responses are also initiated and modulated by targeted therapies and cytotoxic agents, which create the principal basis that when targeted therapies are combined with immunotherapy, the clinical outcomes are of excellent efficacy, as presented in this review. This review focuses on how immunotherapy and targeted therapy are applicable in cancer management and treatment. Also, it depicts promising therapeutic results with more extensive immunotherapy applications with targeted therapy. Further elaborate that immune system responses are also initiated and modulated by targeted therapies and cytotoxic agents, which create the principal basis that this combination therapy with immunotherapy can be of great outcome clinically.


Asunto(s)
Inmunoterapia , Neoplasias , Humanos , Terapia Combinada , Neoplasias/tratamiento farmacológico , Citotoxinas
15.
J Pharm Anal ; 12(5): 743-754, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-36320604

RESUMEN

Lipidomics coverage improvement is essential for functional lipid and pathway construction. A powerful approach to discovering organism lipidome is to combine various data acquisitions, such as full scan mass spectrometry (full MS), data-dependent acquisition (DDA), and data-independent acquisition (DIA). Caenorhabditis elegans (C. elegans) is a useful model for discovering toxic-induced metabolism, high-throughput drug screening, and a variety of human disease pathways. To determine the lipidome of C. elegans and investigate lipid disruption from the molecular level to the system biology level, we used integrative data acquisition. The methyl-tert-butyl ether method was used to extract L4 stage C. elegans after exposure to triclosan (TCS), perfluorooctanoic acid, and nanopolystyrene (nPS). Full MS, DDA, and DIA integrations were performed to comprehensively profile the C. elegans lipidome by Q-Exactive Plus MS. All annotated lipids were then analyzed using lipid ontology and pathway analysis. We annotated up to 940 lipids from 20 lipid classes involved in various functions and pathways. The biological investigations revealed that when C. elegans were exposed to nPS, lipid droplets were disrupted, whereas plasma membrane-functionalized lipids were likely to be changed in the TCS treatment group. The nPS treatment caused a significant disruption in lipid storage. Triacylglycerol, glycerophospholipid, and ether class lipids were those primarily hindered by toxicants. Finally, toxicant exposure frequently involved numerous lipid-related pathways, including the phosphoinositide 3-kinase/protein kinase B pathway. In conclusion, an integrative data acquisition strategy was used to characterize the C. elegans lipidome, providing valuable biological insights into hypothesis generation and validation.

16.
J Nat Prod ; 85(6): 1503-1513, 2022 06 24.
Artículo en Inglés | MEDLINE | ID: mdl-35687347

RESUMEN

Aurora kinases (Aurora A, B, and C) are a family of serine/threonine kinases that play critical roles during mitotic initiation and progression. Aurora A and B kinases are ubiquitously expressed, and their overexpression and/or amplification in many cancers have been associated with poor prognosis. Several inhibitors that target Aurora kinases A, B, or both have been developed during the past decade with efficacy in different in vitro and in vivo models for a variety of cancers. Recent studies have also identified Aurora A as a synthetic lethal target for different tumor suppressors, including RB1, SMARCA4, and ARID1A, which signifies the need for Aurora-A-selective inhibitors. Here, we report the screening of a small library of quinones (nine naphthoquinones, one orthoquinone, and one anthraquinone) in a biochemical assay for Aurora A kinase that resulted in the identification of several quinones as inhibitors. IC50 determination against Aurora A and B kinases revealed the inhibition of both kinases with selectivity toward Aurora A. Two of the compounds, natural quinone naphthazarin (1) and a pseudo anthraquinone, 2-(chloromethyl)quinizarin (11), potently inhibited the proliferation of various cancer cell lines with IC50 values ranging from 0.16 ± 0.15 to 1.7 ± 0.06 and 0.15 ± 0.04 to 6.3 ± 1.8 µM, respectively. Treatment of cancer cells with these compounds for 24 h resulted in abrogated mitosis and apoptotic cell death. Direct binding of both the compounds with Aurora A kinase was also confirmed through STD NMR analysis. Docking studies predicted the binding of both compounds to the ATP binding pocket of Aurora A kinase. We have, therefore, identified quinones as Aurora kinase inhibitors that can serve as a lead for future drug discovery endeavors.


Asunto(s)
Aurora Quinasa A , Aurora Quinasa B , Neoplasias , Inhibidores de Proteínas Quinasas , Quinonas , Antraquinonas , Aurora Quinasa A/antagonistas & inhibidores , Aurora Quinasa B/antagonistas & inhibidores , Línea Celular Tumoral , ADN Helicasas , Humanos , Proteínas Nucleares , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/farmacología , Quinonas/química , Quinonas/farmacología , Factores de Transcripción
17.
J Ginseng Res ; 46(2): 225-234, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35509817

RESUMEN

Background: Ginseng, officially known as Panax ginseng Meyer, has been traditionally used as a medicinal herb, particularly in Asia. Ginseng is propagated from seeds; however, seed germination is challenging, especially in its natural environment on farms. The seeds typically exhibit morphophysiological dormancy and require release from both morphological and physiological dormancy before germination. Although some studies have proposed methods for increasing seed germination rates, the underlying mechanisms of its dormancy release process remain unclear. Here, we investigated metabolic alterations during dehiscence in P. ginseng to determine their potential roles in dormancy release. Methods: We compared the ginseng seed metabolome before and after dehiscence and the ginsenoside and phytosterol compositions of the seeds in both periods in the presence of related enzymes. Results: After seed dehiscence, the sugar, amino acid, and squalene concentrations were significantly altered, phytosterols associated with the stigmasterol biosynthesis pathway were increased, while ginsenoside and brassinosteroid levels were not significantly altered. In addition, squalene epoxidase, cycloartenol synthase, 24-methylenesterol C-methyltransferase, and the stigmasterol biosynthesis pathway were activated. Conclusion: Overall, our findings suggest that morphological activities that facilitate ginseng seed growth are the primary phenomena occurring during the dehiscence process. This study improves the understanding of P. ginseng germination processes and promotes further research of its germination and cultivation.

18.
Int J Nanomedicine ; 17: 1647-1657, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35418754

RESUMEN

Background: The leaves of L. japonica (LLJ) are widely used as medicine in China. It is rich in caffeoylquinic acids, flavonoids and iridoid glycosides and has strong reducing capacities. Therefore, it can be used as a green material to synthesize silver nanoparticles. Methods: LLJ was used as a reducing agent to produce the LLJ-mediated silver nanoparticles (LLJ-AgNPs). The structure and physicochemical properties of LLJ-AgNPs were characterized by ultraviolet spectroscopy (UV-Vis), scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), and x-ray powder diffraction (XRD). Antioxidant activity of LLJ-AgNPs was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging. Antibacterial activity was determined by 96 well plates (AGAR) gradient dilution, while the anticancer potential was determined by MTT assay. Results: The results showed LLJ-AgNPs had a spherical structure with the maximum UV-Vis absorption at 400 nm. In addition, LLJ-AgNPs exhibited excellent antioxidant properties, where the free radical scavenging rate of LLJ-AgNPs was increased from 39% to 92% at concentrations from 0.25 to 1.0 mg/mL. Moreover, LLJ-AgNPs displayed excellent antibacterial properties against E. coli and Salmonella at room temperature, with minimum inhibitory values of 10-6 and 10-5 g/L, respectively. In addition, the synthetic LLJ-AgNPs exhibited a better inhibition effect in the proliferation of cancer cells (HepG2, MDA-MB -231, and Hela cells). Conclusion: The present study provides a green approach to synthesize LLJ-AgNPs. All those findings illustrated that the produced LLJ-AgNPs can be used as an economical and efficient functional material for further applications in food and pharmaceutical fields.


Asunto(s)
Lonicera , Nanopartículas del Metal , Antibacterianos/química , Antibacterianos/farmacología , Antioxidantes/química , Escherichia coli , Células HeLa , Humanos , Nanopartículas del Metal/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Plata/química , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X
19.
Talanta ; 243: 123391, 2022 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-35325750

RESUMEN

Rare ginsenoside Rg3 is a main active ingredient in ginseng, which is more easily absorbed by human body and plays its role. Determination of Rg3 in edible and medicinal samples is a key factor for quality evaluation and effective monitoring of adulteration. In this study, an electrochemical sensor was developed based on molecularly imprinted polymer (MIP) and nanomaterial amplification. MIP was achieved by electro-polymerization with Rg3 as the template molecule and the functional monomer was o-phenylenediamine. Multi-walled carbon nanotubes (MWCNT) and titanium carbide (Ti3C2Tx) nanocomposites formed an excellent porous structure, which exhibited the advantages of increasing the specific surface area and electrical conductivity. The prepared sensor presented a great linear relation of Rg3 in the range of 10-2000 µg mL-1 with a limit of detection (LOD) of 0.34 µg mL-1. Importantly, the sensor was successfully utilized to detect ginsenoside Rg3 in different real samples.


Asunto(s)
Impresión Molecular , Nanocompuestos , Nanotubos de Carbono , Técnicas Electroquímicas , Electrodos , Ginsenósidos , Humanos , Límite de Detección , Polímeros Impresos Molecularmente , Nanocompuestos/química , Nanotubos de Carbono/química , Polímeros/química , Titanio
20.
J Sep Sci ; 45(11): 1856-1865, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35338696

RESUMEN

Paeonia lactiflora Pall., one of the most famous classical herbal medicine, has been used to treat diseases for over 1200 years. In this research, the functional ingredients were purified by online-switch two-dimensional high-speed counter-current chromatography combined with inner-recycling and continuous injection mode. The antioxidant activity was evaluated by investigating the 2,2'-azobis (2-amidinopropane) dihydrochloride-induced oxidant damage in vitro and confirmed through molecular docking. n-Butanol/ethyl acetate/water (2:3:5, v/v) solvent system was used for the first-dimensional separation and optimized the sample loading. Two pure compounds and a polyphenol-enriched fraction were separated. The polyphenol-enriched fraction was separated with a solvent system n-hexane/ethyl acetate/methanol/water (2:8:4:6, v/v) with continuous injection mode. Five compounds were successfully separated, including gallic acid (1), methyl gallate (2), albiflorin (3), paeoniflorin (4), and ethyl gallate (5). Their structures were identified by mass spectrometry and NMR spectroscopy. The results from the antioxidant effect showed that albiflorin had stronger antioxidant activity. Molecular docking results indicated that the affinity energy of the identified compounds ranged from -3.79 to -8.22 kcal/mol and albiflorin showed the lowest affinity energy. Overall, all those findings suggested that the strong antioxidant capacity of albiflorin can be potentially used for the treatment of diseases caused by oxidation.


Asunto(s)
Paeonia , Antioxidantes/farmacología , Cromatografía Líquida de Alta Presión/métodos , Distribución en Contracorriente/métodos , Simulación del Acoplamiento Molecular , Paeonia/química , Polifenoles , Solventes , Agua
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...