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1.
Arch Pharm (Weinheim) ; 356(4): e2200470, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36707412

RESUMO

Licorice flavonoids (LCFs) have been widely used in food care and medical treatment due to their significant antioxidant activities. However, the molecular mechanism of their antioxidant activity remains unclear. Therefore, network pharmacology, ADMET, density functional theory (DFT), molecular docking, and molecular dynamics (MD) simulation were employed to explore the molecular mechanism of the antioxidant effects of LCF. The network pharmacology and ADMET studies showed that the active molecules of kumatakenin (pKa = 6.18), licoflavonol (pKa = 6.86), and topazolin (pKa = 6.21) in LCF are key antioxidant components and have good biosafety. Molecular docking and MD simulation studies demonstrated that active molecules interacted with amino acid residues in target proteins to form stable protein-ligand complexes and exert their antioxidant effects. DFT studies showed that the antioxidant activity of LCF could be significantly modulated under the solvent-mediated effect. In addition, based on the derivation of the Henderson-Hasselbalch and van't Hoff formulas, the functional relationships between the reaction-free energy (ΔG) of LCF and the pH and pKa values were established. The results showed that active molecules with larger pKa values will be more conducive to the improvement of their antioxidant activity under solvent-mediated effects. In conclusion, this study found that increasing the pKa value of LCF would be an effective strategy to improve their antioxidant activity under the effect of solvent mediation. The pKa value of an LCF will be a direct standard to evaluate its solvent-mediated antioxidant activity. This study will provide theoretical guidance for the development of natural antioxidants.


Assuntos
Antioxidantes , Glycyrrhiza , Solventes , Antioxidantes/farmacologia , Antioxidantes/química , Flavonoides/farmacologia , Flavonoides/química , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
2.
Pharmacol Res ; 178: 106175, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-35283301

RESUMO

Obesity is a significant public health problem worldwide that is characterized by abnormal or excessive fat accumulation. Unfortunately, the application of available weight-loss drugs has been restricted because of their serious adverse effects. Browning of white adipose tissue (WAT), which refers to the transformation of white adipocytes to beige adipocytes under certain stimulations, is regarded as a new strategy to solve the obesity problem. Numerous studies have recently evidenced that traditional Chinese medicine (TCM) could promote browning of WAT with multi-component and multi-target characteristics. This article summarizes natural constituents from TCM with stimulatory effects on browning of WAT in the past two decades. The active ingredients can be generally divided into polyphenols, saponins, alkaloids, terpenoids, phenylpropanoids and others, such as resveratrol, quercetin, curcumin, genistein, capsaicin, epigallocatechin gallate (EGCG), berberine, menthol, emodin and ginsenosides. Simultaneously, the chemical structures, source, model, efficacy and mechanism of these monomeric compounds are also described. And the mechanisms of these active ingredients are mainly involved in the regulation of PRDM16, PGC-1α, PPARγ, SIRT1, AMPK, ß3-adrenergic receptors, TRPV1 and TRPM8 channels, FGF21 and miRNAs. The present article opens opportunities for developing novel drugs or supplements from TCM with wide acceptability to prevent obesity progression and its associated metabolic disorders.


Assuntos
Tecido Adiposo Branco , Medicamentos de Ervas Chinesas , Suplementos Nutricionais , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Medicina Tradicional Chinesa , Obesidade/tratamento farmacológico
3.
ACS Omega ; 9(25): 27002-27016, 2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-38947843

RESUMO

Liriodendron chinense has been widely utilized in traditional Chinese medicine to treat dispelling wind and dampness and used for alleviating cough and diminishing inflammation. However, the antioxidant, antimicrobial, and anti-inflammatory effects of L. chinense leaves and the key active constituents remained elusive. So, we conducted some experiments to support the application of L. chinense in traditional Chinese medicine by investigating the antioxidant, antibacterial, and anti-inflammatory abilities, and to identify the potential key constituents responsible for the activities. The ethanol extract of L. chinense leaves (LCLE) was isolated and extracted, and assays measuring ferric reducing antioxidant power, total reducing power, DPPH•, ABTS•+, and •OH were used to assess its in vitro antioxidant capacities. Antimicrobial activities of LCLE were investigated by minimal inhibitory levels, minimum antibacterial concentrations, disc diffusion test, and scanning electron microscope examination. Further, in vivo experiments including macro indicators examination, histopathological examination, and biochemical parameters measurement were conducted to investigate the effects of LCLE on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice. LCLE was further isolated and purified through column chromatography, and LPS-induced RAW264.7 cells were constructed to assess the diminished inflammation potential of the identified chemical composites. ABTS•+ and •OH radicals were extensively neutralized by the LCLE treatment. LCLE administration also presented broad-spectrum antimicrobial properties, especially against Staphylococcus epidermidis by disrupting cell walls. LPS-induced ALI in mice was significantly ameliorated by LCLE intervention, as evidenced by the histological changes in the lung and liver tissues as well as the reductions of nitric oxide (NO), TNF-α, and IL-6 production. Furthermore, three novel compounds including fragransin B2, liriodendritol, and rhamnocitrin were isolated, purified, and identified from LCLE. These three compounds exhibited differential regulation on NO accumulation and IL-10, IL-1ß, IL-6, TNF-α, COX-2, and iNOS mRNA expression in RAW264.7 cells induced by LPS. Fragransin B2 was more effective in inhibiting TNF-α mRNA expression, while rhamnocitrin was more powerful in inhibiting IL-6 mRNA expression. LCLE had significant antioxidant, antimicrobial, and anti-inflammatory effects. Fragransin B2, liriodendritol, and rhamnocitrin were probably key active constituents of LCLE, which might act synergistically to treat inflammatory-related disorders. This study provided a valuable view of the healing potential of L. chinense leaves in curing inflammatory diseases.

4.
Food Chem ; 454: 139788, 2024 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-38810459

RESUMO

Licochalcone A (LCA) is extracted from licorice plants and used as a food additive. Citric acid (CA) and alanine (Ala) are food additives with good regulatory functions. This study aims to investigate the formation and in vitro release mechanism of the LCA eutectogel using supramolecular self-assembly technology. The mechanism of self-assembly indicates that the resulting eutectogel has strong intermolecular interactions. The formation mechanism of LCA eutectogel suggests that LCA is dispersed in nano form in the DES solution before self-assembly and dispersed in molecular form in the eutectogel after self-assembly. Mesoscopic MD simulation studies indicate that the interaction energy between LCA Ala-CA(5:5) eutectogel and the solvent interface is relatively low, suggesting it may have a better drug release rate, consistent with the in vitro release results. In conclusion, the study successfully prepares LCA eutectogel and provides theoretical guidance for the development and application of novel eutectogel for food application.


Assuntos
Chalconas , Glycyrrhiza , Chalconas/química , Glycyrrhiza/química , Aditivos Alimentares/química , Géis/química , Extratos Vegetais/química , Liberação Controlada de Fármacos , Simulação de Dinâmica Molecular
5.
J Ethnopharmacol ; 301: 115837, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36252875

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: During the Eastern Han Dynasty, Zhang Zhongjing first recorded the Gancao Fuzi decoction (GCFZD) formula in the "Synopsis of the Golden Chamber", which is reportedly an effective and safe treatment for rheumatoid arthritis (RA). However, the mechanism underlying the observed improvement in the T helper 17 (Th17)/regulatory T (Treg) cell imbalance in RA obtained with GCFZD has not been reported. AIM OF THE STUDY: This study aimed to demonstrate whether GCFZD ameliorated RA by modulating the Th17/Treg imbalance in RA mice. MATERIALS AND METHODS: Collagen was used to induce a model of collagen-induced arthritis (CIA) in mice. GCFZD was administered by gavage, and the arthritis index score, imaging and histopathological changes of the ankle joints, and the levels of the immunoglobulin G (IgG) class antibodies and proinflammatory factors in serum were determined. In addition, the frequencies of Th17 and Treg cells, the levels of relevant transcription factors and functional factors and the miR-34a gene in the spleen and the levels of interleukin-17A (IL-17A) and IL-10 in serum were determined. RESULTS: GCFZD significantly reduced the arthritis score, improved joint swelling and bone damage, reduced the pathological score, and decreased the serum levels of IgG class antibody (IgG and IgG2a) and proinflammatory factor [tumour necrosis factor-alpha (TNF-α), IL-1ß and IL-6]. Moreover, the Th17-cell proportion, the expression level of the Th17-specific transcription factor retinoic acid-related orphan receptor γt (RORγt) and functional factor IL-17A in the spleen, and the serum IL-17A level were decreased, whereas the Treg cell proportion, expression levels of the Treg-specific transcription factor forkhead box P3 (Foxp3) and functional factor IL-10 in the spleen, and the serum IL-10 level were increased. Furthermore, GCFZD inhibited miR-34a gene expression while promoting Foxp3 protein expression. CONCLUSIONS: The findings of this study demonstrate the therapeutic effect of GCFZD on mice with CIA, and the mechanism is related to an improvement in the Th17/Treg cell imbalance by targeting Foxp3 via miR-34a.


Assuntos
Artrite Experimental , Artrite Reumatoide , MicroRNAs , Camundongos , Animais , Linfócitos T Reguladores , Interleucina-17/metabolismo , Interleucina-10/metabolismo , Células Th17 , Artrite Reumatoide/patologia , Artrite Experimental/patologia , MicroRNAs/genética , MicroRNAs/metabolismo , Imunoglobulina G , Fatores de Transcrição/metabolismo , Fatores de Transcrição Forkhead/genética , Fatores de Transcrição Forkhead/metabolismo
6.
Int J Pharm ; 644: 123298, 2023 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-37558146

RESUMO

Isoliquiritigenin (ISL) is a natural medicinal product with extensive pharmacological activities. However, its low solubility limits its application. Therefore, this study aimed to explore the solubilization and release mechanism of the ISL using deep eutectic solvents (DESs). The choline chloride (ChCl) and oxalic acid (OA)/malic acid (MA)/gallic acid (GA) were used to synthesize ChCl-OA/MA/GA DESs, and the solubility of ISL in these DESs was studied to explore the solubilization mechanism of ISL. The thermodynamic properties of DESs were characterized using differential scanning calorimetry (DSC). The molecular interactions in DESs were studied using spectroscopy and molecular dynamics (MD) simulations. The relative density of DESs was measured using a pycnometric method, its accuracy was validated by comparing it with the MD simulation. The release of ISL from ChCl-OA/MA/GA eutectogels was studied using Carbomer 940 as the thickener, and the release mechanism of ISL in the eutectogels was explored by the drug release kinetic model. The solubility study found that the solubility of ISL in ChCl-OA/MA/GA DESs is 30073, 5055, and 68,103 times higher than that in an aqueous solution. In addition, further studies using MD simulations revealed that enhancing the interactions between ISL and solvent molecules can improve the solubility of ISL in DESs. In vitro release studies showed that the release of ISL in ChCl-OA/MA/GA eutectogels followed a first-order release model, with correlation coefficients of 0.9812, 0.9916, and 0.9961, respectively. In conclusion, the study of the solubilization and release mechanism of ISL in DESs provides new ideas and methods for the study of poorly soluble drugs, which is expected to improve the efficacy and clinical application value of drugs.


Assuntos
Chalconas , Solventes Eutéticos Profundos , Solventes/química , Água/química , Colina/química
7.
Heliyon ; 9(12): e22421, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38076040

RESUMO

Melasma is a pigmentation disease with refractory and high recurrence risk. Therefore, finding effective treatment has become the focus of research. This study aimed to reveal the mechanism of Licorice rose beverage (LRB) in treating melasma from the perspective of network pharmacology and in vitro and in vivo experimental techniques. Network pharmacological studies have shown that Isolicoflavonol, quercetin, and kaempferol are the main active components of anti-melasma and tyrosinase is the main target. Molecular docking studies have shown that these compounds have a good affinity for these targets. In vitro tyrosinase inhibition experiments showed that LRB could significantly inhibit tyrosinase activity. In vivo studies showed that LRB could significantly improve skin damage and skin pigmentation, reduce the activities of serum and skin tyrosinase in model mice, increase the activity of SOD in serum, and reduce the content of MDA in mice, showing a good effect of anti-melasma. In conclusion, these findings reveal the molecular mechanism of LRB in treating melasma and provide the scientific basis for this product's development and clinical application.

8.
Colloids Surf B Biointerfaces ; 215: 112511, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35483256

RESUMO

Salvia miltiorrhiza and Carthamus tinctorius are traditional Chinese medicines that have been widely used for the treatment of cardiovascular disease. Salvianic acid A (SAA), salvianic acid B (SAB), protocatechuic aldehyde (PCA) and hydroxysafflor yellow A (HSYA) are the major hydrophilic polyphenols of Salvia miltiorrhiza and Carthamus tinctorius, all of which have been documented as active compounds for the prevention and treatment of atherosclerosis (AS). However, high aqueous solubility, low permeability and poor stability properties of the four hydrophilic polyphenols might influence their bioavailability and thus hinder their clinical potential. In this work, we introduced a green and highly efficient method for the efficient delivery of the four hydrophilic components via metal-phenolic network. The four coordination polymers of SAA, SAB, PCA and HSYA were successfully fabricated, and confirmed by UV-vis, FTIR, XPS, ICP-MS and dynamic light scattering analysis. We found all of them displayed potent antioxidant activity, good biocompatibility and stability. Impressively, the four coordination polymers showed remarkably enhanced anti-atherosclerotic effect compared with free drugs. Collectively, metal-phenolic network-based coordination polymer might show great potential for safe and efficient delivery of the hydrophilic polyphenols of Salvia miltiorrhiza and Carthamus tinctorius for anti-atherosclerotic therapy.


Assuntos
Aterosclerose , Carthamus tinctorius , Medicamentos de Ervas Chinesas , Salvia miltiorrhiza , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Polímeros , Polifenóis/farmacologia
9.
J Food Biochem ; 46(10): e14315, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35855584

RESUMO

Excessive oxygen free radicals can lead to aging, cancer, and other diseases. Therefore, searching for effective antioxidants to scavenge oxygen free radicals has become the focus of modern medicine. In this study, the molecular mechanism of Licorice Green Tea Beverage (LGTB) in scavenging oxygen free radicals was investigated by means of network pharmacology, molecular docking and experimental verification. Network pharmacology studies have shown that paeonol, eugenol, cinnamaldehyde, swertisin, rutin, glycyrrhetinic acid, oleic, pelargonidin-3-O-glucoside and quercetin, kaferempol were the main active components of LGTB, and SOD and CAT are important targets for LGTB in scavenging oxygen free radicals. The results of molecular docking showed that these representative compounds had good affinity to SOD and CAT target proteins. In vitro free radical scavenging experiments showed that LTGB had significant scavenging effects on both DPPH and ABTS radicals, and had strong total reducing power. In vitro cell experiments showed that LGTB could protect HaCaT cells from oxidative stress induced by H2 O2 . The mechanism of LGTB was related to the increase of SOD and CAT activity. Western blotting showed that LGTB could inhibit PI3K/AKT/HIF-1 signaling pathway and improve the antioxidant capacity of HaCaT cells. In vivo experiments showed that LGTB could significantly increase mouse visceral index, increase serum SOD and GSH-Px activity, decrease the content of MDA, and improve liver and kidney pathological state. This study reported the molecular mechanism of LTGB scavenging oxygen free radicals, which provided scientific basis for the treatment and clinical research of aging and other diseases caused by excessive free radicals. PRACTICAL APPLICATIONS: Free radicals are produced by the normal response of cells during aerobic respiration and perform various functions, such as signaling and providing protection against infection. However, excessive free radicals can lead to aging, cancer, and other diseases. The antioxidant can overcome the harm caused by excessive free radicals. In this study, we investigated the molecular mechanism of scavenging oxygen free radicals of Licorice Green Tea Beverage (LGTB) through network pharmacology and molecular docking, and its efficacy was verified by free radical scavenging experiment in vitro, HaCaT cell oxidative stress injury induced by H2 O2 , D-galactose to establish an aging model in mice and Western blotting experiment. It not only elucidates its mechanism at the system level, but also proves its validity at the biological level. It provides the theoretical basis and experimental evidence for the follow-up research and promotion of the product.


Assuntos
Ácido Glicirretínico , Glycyrrhiza , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Eugenol/farmacologia , Radicais Livres/metabolismo , Galactose , Glucosídeos , Glycyrrhiza/metabolismo , Camundongos , Simulação de Acoplamento Molecular , Farmacologia em Rede , Fosfatidilinositol 3-Quinases , Extratos Vegetais/farmacologia , Proteínas Proto-Oncogênicas c-akt , Quercetina , Rutina , Superóxido Dismutase/metabolismo , Chá
10.
Front Pharmacol ; 13: 832088, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35211023

RESUMO

Acne vulgaris is one of the most common inflammatory dermatoses in dermatological practice and can affect any gender or ethnic group. Although in previous studies, we had found that licorice flavonoids (LCF) play an anti-acne role by inhibiting PI3K-Akt signaling pathways and mitochondrial activity, the mechanism of LCF regulating skin metabolism, serum metabolism and skin microbes is still unclear. Here, we performed a full spectrum analysis of metabolites in the skin and serum using UHPLC-Triple TOF-MS. The results showed that LCF could treat acne by regulating the metabolic balance of amino acids, lipids and fatty acids in serum and skin. Similarly, we performed Illumina Hiseq sequencing of DNA from the skin microbes using 16S ribosomal DNA identification techniques. The results showed that LCF could treat acne by regulating the skin microbes to interfere with acne and make the microecology close to the normal skin state of rats. In summary, this study confirmed the anti-acne mechanism of LCF, namely by regulating metabolic balance and microbial balance. Therefore, this discovery will provide theoretical guidance for the preparation development and clinical application of the drug.

11.
Front Chem ; 10: 843970, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35308797

RESUMO

Licorice flavonoids (LCFs) are natural flavonoids isolated from Glycyrrhiza which are known to have anti-melanoma activities in vitro. However, the molecular mechanism of LCF anti-melanoma has not been fully understood. In this study, network pharmacology, 3D/2D-QSAR, molecular docking, and molecular dynamics (MD) simulation were used to explore the molecular mechanism of LCF anti-melanoma. First of all, we screened the key active components and targets of LCF anti-melanoma by network pharmacology. Then, the logIC50 values of the top 20 compounds were predicted by the 2D-QSAR pharmacophore model, and seven highly active compounds were screened successfully. An optimal 3D-QSAR pharmacophore model for predicting the activity of LCF compounds was established by the HipHop method. The effectiveness of the 3D-QSAR pharmacophore was verified by a training set of compounds with known activity, and the possible decisive therapeutic effect of the potency group was inferred. Finally, molecular docking and MD simulation were used to verify the effective pharmacophore. In conclusion, this study established the structure-activity relationship of LCF and provided theoretical guidance for the research of LCF anti-melanoma.

12.
Int J Pharm ; 625: 122109, 2022 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-35973589

RESUMO

Alopecia affected approximately 16.6% of all people in China, however, treatment options remain limited due to the side effects. Plant bioactive compound baicalin (BC) possesses hair growth-promotion activity, but poor water solubility and unsuitable log P value restrict its topical application, and natural Glycyrrhizin (GL) can exactly overcome these drawbacks. Here, BC was encapsulated in GL to form GL-BC micelles for alopecia treatment. Simultaneously, tween 80 (TW) as carriers was incorporated in the GL-BC to form GL-TW-BC micelles. The topical penetration, penetration pathways, cellular uptake and the underlying mechanisms behind the hair loss reconstruction of the GL micelles were investigated. We found the optimal GL-BC and GL-TW-BC formulations significantly improved the penetration and accumulation of BC in the porcine skin predominantly through the hair follicles pathways without causing skin irritation, which resulted in a targeted treatment. The proliferation of human dermal papilla cells (hDPCs) and effective cellular uptake was also enhanced. Moreover, the activation of the Wnt/ß-catenin pathway, up-expression of vascular endothelial growth factor (VEGF), α-melanocyte-stimulating hormone (α-MSH) and interleukin-10 (IL-10) were the mechanisms of micelles for the hair recovery. Interestingly, GL and BC exhibited a synergistic treatment of alopecia. Collectively, GL-BC and GL-TW-BC can be used as promising approaches for the treatment of alopecia.


Assuntos
Folículo Piloso , Micelas , Alopecia/tratamento farmacológico , Alopecia/metabolismo , Flavonoides , Ácido Glicirrízico/metabolismo , Folículo Piloso/metabolismo , Humanos , Fator A de Crescimento do Endotélio Vascular/metabolismo
13.
ACS Biomater Sci Eng ; 7(11): 5048-5063, 2021 11 08.
Artigo em Inglês | MEDLINE | ID: mdl-34648280

RESUMO

Specific delivery of NCEH1 plasmid is a promising approach to boost the cholesterol removal from lipid-laden macrophages for antiatherosclerosis. Polyethylenimine (PEI) is one of the most efficient gene carriers among nonviral vectors. However, the high transfection activity of PEI is always accompanied by profound cytotoxicity. To tackle the paradox between transfection efficiency and safety, we constructed a novel ATP-responsive multifunctional supramolecular polymer by cross-linking functionalized low-molecular-weight PEI via a boronic ester bond for NCEH1 plasmid delivery. The supramolecular polymer could condense NCEH1 plasmids to form stable nanosized polyplexes when the w/w ratios of the polymer and gene were higher than 2. ATP-triggered degradation of the polymer and pDNA release were characterized by a series of studies, including 1H NMR, 31P NMR, XPS, agarose gel electrophoresis, and ethidium bromide exclusion tests. In addition, the changes in particle size and morphology were observed in the presence of ATP. Interestingly, the supramolecular polymer showed broad spectrum antioxidant activities by measuring the elimination rates of different reactive oxygen species. In addition, the supramolecular polymer displayed a high buffering capability and good cytocompatibility as demonstrated by the results of the buffering capacity, a hemolysis assay, and a cytotoxicity test. Importantly, it was revealed that the supramolecular polymer/NCEH1 plasmid polyplex formulated at a w/w ratio of 20 was most effective in enhancing cholesterol removal from lipid-laden macrophages and reducing the accumulation of lipid droplets as evidenced by transfection study, cholesterol efflux assay, and oil red O staining studies. Collectively, the ATP-responsive multifunctional supramolecular polymer holds great potential for safe and efficient gene delivery for antiatherosclerosis.


Assuntos
DNA , Polímeros , Trifosfato de Adenosina , Colesterol , DNA/genética , Macrófagos
14.
Phytomedicine ; 90: 153634, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34225246

RESUMO

BACKGROUND: Excess lipid accumulation can accelerate the development of various metabolic diseases. Blossoms of Citrus aurantium L. var. amara Engl. (CAVA) have been reported to possess inhibitory capacities on lipid deposition. However, the constituents responsible for the observed bioactivity and the underlying mechanisms are still not clearly understood. PURPOSE: To screen constituents from blossoms of CAVA with inhibitory effects on lipid accumulation and to explore the action mechanism. METHODS: The chloroform (CHL) extracts are prepared from blossoms of CAVA by fractional extraction and are characterized using LC-MS assay. 3T3-L1 preadipocytes are induced with differentiation medium (DMI) and treated with CHL extracts. High fat diet (HFD)-induced obese mice are further established and administrated with CHL extracts for 12 weeks. Hematoxylin and eosin (HE) staining, Oil Red O staining, ELISA, RT-qPCR, western blot and 16S rRNA gene sequence methods are employed. RESULTS: 14 compounds are identified in CHL extracts and trigonelline hydrochloride, nobiletin and 7-demethylsuberosin are most abundant. CHL extracts treatment significantly inhibit differentiation of 3T3-L1 cells by regulating expression of preadipocyte factor-1 (Pref-1), fatty acid synthase (FAS) and CCAAT/enhancer binding protein α (C/EBPα). CHL extracts intervention also significantly attenuate features of obesity and improved plasma biochemical profiles in HFD-fed mice. HFD-triggered hepatic steatosis and epididymal adipose tissues (EATs) hypertrophy are also reversed by CHL extracts administration through enhancing antioxidant responses and modulating lipogenesis and energy expenditure-related genes and proteins. 16S rRNA gene sequence data further show that CHL extracts enhance the diversity of gut microbiota. CHL extracts at lower concentrations reduce the ratio of Firmicutes to Bacteroidetes and the abundance of Erysipelotrichaceae. CHL extracts at higher doses markedly increase the abundance of Lachnospiraceae. CONCLUSION: These findings suggest that CHL extracts probably suppress lipid accumulation through inhibiting differentiation of 3T3-L1 cells and attenuating metabolic syndromes in HFD-fed mice.


Assuntos
Adipogenia/efeitos dos fármacos , Citrus , Metabolismo dos Lipídeos/efeitos dos fármacos , Extratos Vegetais , Células 3T3-L1 , Animais , Clorofórmio , Citrus/química , Dieta Hiperlipídica , Microbioma Gastrointestinal , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Obesos , Extratos Vegetais/farmacologia , RNA Ribossômico 16S
15.
J Ethnopharmacol ; 208: 138-148, 2017 Aug 17.
Artigo em Inglês | MEDLINE | ID: mdl-28602868

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Oviductus Ranae (OR) is a traditional Chinese medicine derived from Rana temporaria chensinensis David, and is known to have a wide variety of pharmacological effects. AIM OF THE STUDY: To investigate the function and mechanism of OR-containing serum in protecting rat ovarian granulosa cells from hydrogen peroxide (H2O2)-induced oxidative damage. MATERIALS AND METHODS: H2O2-treated granulosa cells were pretreated with OR-containing serum, and viability and proliferation assays were carried out using Cell Counting Kit-8 (CCK-8). Apoptotic granulosa cells were observed microscopically using 4',6-diamidino-2-phenylindole (DAPI), and the apoptotic ratio was quantified via Annexin V/ propidium iodide (PI) staining combined with flow cytometry. The levels of reactive oxygen species (ROS) and mitochondrial membrane potential (ΔΨm) in the cells were measured using 2,7-dichlorofluorescein diacetate (DCFH-DA) and rhodamine 123, respectively, and analyzed by flow cytometry. Mitogen-activated protein kinases (MAPKs), including ERK1/2, JNK, and p38, and other apoptosis-related proteins (p53, Bcl-2, Bax, caspase-9, caspase-3), were detected by western blot analysis, and the related mRNA levels were detected using reverse transcriptase-polymerase chain reaction (RT-PCR). RESULTS: The results revealed that treatment with OR-containing serum reduced apoptosis and mitochondrial membrane damage in H2O2-treated granulosa cells. The OR-containing serum interfered with H2O2-induced intracellular generation of ROS and loss of ΔΨm, which typically lead to apoptosis. Furthermore, the OR-containing serum down-regulated pro-apoptotic proteins such as p53, Bax, caspase-9, and caspase-3, while up-regulating the anti-apoptotic protein Bcl-2. Finally, the OR-containing serum increased phosphorylation of ERK1/2, and reduced JNK and p38 phosphorylation. CONCLUSIONS: OR-containing serum protected rat ovarian granulosa cells against H2O2-induced apoptosis, by reducing ROS production and improving mitochondrial membrane potential, through down-regulation of negative regulators of proliferation, activation of ERK1/2, and inhibition of the activity of JNK and p38.


Assuntos
Células da Granulosa/efeitos dos fármacos , Materia Medica/farmacologia , Ovário/citologia , Estresse Oxidativo/efeitos dos fármacos , Animais , Apoptose/efeitos dos fármacos , Proteínas Reguladoras de Apoptose/genética , Proteínas Reguladoras de Apoptose/metabolismo , Células Cultivadas , Regulação para Baixo , Feminino , Células da Granulosa/metabolismo , Peróxido de Hidrogênio/farmacologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Proteínas Quinases Ativadas por Mitógeno/genética , Proteínas Quinases Ativadas por Mitógeno/metabolismo , RNA Mensageiro/metabolismo , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/metabolismo , Soro
16.
Zhong Yao Cai ; 28(1): 27-9, 2005 Jan.
Artigo em Zh | MEDLINE | ID: mdl-15934239

RESUMO

The chemical constituents of Salacia hainanensis were studied for the first time. Five compounds were isolated from the roots of the plant by silica-gel column chromatography and reverse phase preparative chromatography. Four of them have been identified as friedelin, beta-sitosterol, ursolic acid and mangiferin.


Assuntos
Plantas Medicinais/química , Salacia/química , Sitosteroides/isolamento & purificação , Triterpenos/isolamento & purificação , China , Cromatografia em Camada Fina/métodos , Estrutura Molecular , Raízes de Plantas/química , Sitosteroides/química , Triterpenos/química , Xantonas/química , Xantonas/isolamento & purificação , Ácido Ursólico
17.
Nan Fang Yi Ke Da Xue Xue Bao ; 26(9): 1337-40, 2006 Sep.
Artigo em Zh | MEDLINE | ID: mdl-16982450

RESUMO

OBJECTIVE: To study the factors affecting cyclodextrin (CD) inclusion of the volatile components in compound traditional Chinese medicines and evaluate the stability of the inclusion compound. METHODS: This study took Gengnian compound as an example to examine the factors affecting the inclusion process according to the inclusion compound utilization ratio. Orthogonal design method was employed optimize the parameters in the inclusion process. The moisture absorption rate of the beta-CD inclusion compound was determined in different humidity and Q10 was used to predict its. RESULTS: The inclusion method, inclusion compound dosage, temperature, inclusion time, and the drying method could all obviously influence the inclusion process. The results of orthogonal design study showed that the optimal beta-CD inclusion of Gengnian compound volatile components could be achieved by adding 8-fold volume of beta-CD and stirring for 3 h at room temperature. Stability experiment showed that the humility did not significantly influence the inclusion compound, which can be stable for 1.26 years. CONCLUSION: This study comprehensively examines the factors affecting the inclusion process and the stability of the inclusion compound, and provides experimental basis for application and study of the inclusion technology.


Assuntos
Medicamentos de Ervas Chinesas/química , Óleos Voláteis/química , Tecnologia Farmacêutica/métodos , beta-Ciclodextrinas/química , Combinação de Medicamentos , Estabilidade de Medicamentos , Óleos Voláteis/análise , Óleos Voláteis/isolamento & purificação
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