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1.
Int Immunopharmacol ; 128: 111565, 2024 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-38262161

RESUMO

Activation of NOD-like receptor protein 3 (NLRP3) inflammasome exacerbates liver inflammation and fibrosis in nonalcoholic steatohepatitis (NASH), suggesting that development of inflammasome inhibitor can become leading candidate to ameliorate NASH. Panax ginseng (P. ginseng) contains numerous bioactive natural components to reduce inflammation. This study aims to identify inhibitory components of P. ginseng for NLRP3 inflammasome activation. We separated polar and non-polar fractions of P. ginseng and tested modulation of NLRP3 inflammasome, and then identified pure component for inflammasome inhibitor which ameliorates diet-induced NASH. Non-polar P. ginseng fractions obtained from ethyl acetate solvent attenuated IL-1ß secretion and expression of active caspase-1. We revealed that panaxydol (PND) is pure component to inhibit NLRP3 inflammasome activation. PND blocked inflammasome cytokines release, pyroptotic cell death, caspase-1 activation and specking of inflammasome complex. Inhibitory effect of PND was specific to NLRP3-dependent pathway via potential interaction with ATP binding motif of NLRP3. Moreover, in vivo studies showed that PND plays beneficial roles to reduce tissue inflammations through disruption of NLRP3 inflammasome and to ameliorate the development of NASH. These results provide new insight of natural products, panaxydol, for NLRP3 inflammasome inhibitor and could offer potential therapeutic candidate for reliving NASH.


Assuntos
Doença Hepática Crônica Induzida por Substâncias e Drogas , Di-Inos , Álcoois Graxos , Hepatopatia Gordurosa não Alcoólica , Panax , Humanos , Animais , Camundongos , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Inflamassomos/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Proteínas NLR , Panax/metabolismo , Inflamação , Caspases , Camundongos Endogâmicos C57BL
2.
Phytochemistry ; 187: 112782, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33915418

RESUMO

Six undescribed compounds (1-6) were isolated from the leaves of Viburnum erosum along with four known compounds 7-10. The structures were determined by NMR and MS spectroscopic analyses, and their absolute configurations were established by chemical and spectroscopic methods. Compounds 1-6 were α-glucosidic hydroquinone derivatives with different linear monoterpenoid structures. Compounds 1-10 were also evaluated for their tyrosinase inhibitory activities, and 10 showed potent inhibition of tyrosinase enzyme with IC50 value of 37.9 µM compared to 47.6 µM of the positive control (ß-arbutin).


Assuntos
Viburnum , Arbutina/farmacologia , Glucosídeos , Hidroquinonas/farmacologia , Monofenol Mono-Oxigenase
3.
Immune Netw ; 20(4): e32, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32895619

RESUMO

Influenza virus is the major cause of seasonal and pandemic flu. Currently, oseltamivir, a potent and selective inhibitor of neuraminidase of influenza A and B viruses, is the drug of choice for treating patients with influenza virus infection. However, recent emergence of oseltamivir-resistant influenza viruses has limited its efficacy. Morin hydrate (3,5,7,2',4'-pentahydroxyflavone) is a flavonoid isolated from Morus alba L. It has antioxidant, anti-inflammatory, neuroprotective, and anticancer effects partly by the inhibition of the NF-кB signaling pathway. However, its effects on influenza virus have not been studied. We evaluated the antiviral activity of morin hydrate against influenza A/Puerto Rico/8/1934 (A/PR/8; H1N1) and oseltamivir-resistant A/PR/8 influenza viruses in vitro. To determine its mode of action, we carried out time course experiments, and time of addition, hemolysis inhibition, and hemagglutination assays. The effects of the co-administration of morin hydrate and oseltamivir were assessed using the murine model of A/PR/8 infection. We found that morin hydrate reduced hemagglutination by A/PR/8 in vitro. It alleviated the symptoms of A/PR/8-infection, and reduced the levels of pro-inflammatory cytokines and chemokines, such as TNF-α and CCL2, in infected mice. Co-administration of morin hydrate and oseltamivir phosphate reduced the virus titers and attenuated pulmonary inflammation. Our results suggest that morin hydrate exhibits antiviral activity by inhibiting the entry of the virus.

4.
ACS Omega ; 5(37): 23989-23995, 2020 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-32984720

RESUMO

Small Molecular Accurate Recognition Technology (SMART 2.0) has recently been introduced as a NMR-based machine learning tool for the discovery and characterization of natural products. We attempted targeted isolation of sesquiterpene lactones from Eupatorium fortunei with the aid of structural annotation by SMART 2.0 and chemical profiling. Eight germacrene-type (1-7 and 10) and two eudesmane-type sesquiterpene lactones (8 and 9) were isolated from the whole plant of Eupatorium fortunei. With the guidance of the results of the subfractions from E. fortunei obtained by SMART 2.0, their cytotoxic activities were evaluated against five cancer cells (SKOV3, A549, PC3, HEp-2, and MCF-7). Compounds 4 and 8 exhibited IC50 values of 3.9 ± 1.2 and 3.9 ± 0.6 µM against prostate cancer cells, PC3, respectively. Compound 7 showed good cytotoxicity with IC50 values of 5.8 ± 0.1 µM against breast cancer cells, MCF-7. In the present study, the rapid annotation of the mixture of compounds in a fraction by the NMR-based machine learning tool helped the targeted isolation of bioactive compounds from natural products.

5.
Int J Anal Chem ; 2020: 3830258, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32831841

RESUMO

The husks and fruits of Zanthoxylum species (Rutaceae) are the popular pungent and spicy ingredients of foods and the traditional medicines in many countries. Three Zanthoxylum species, Z. bungeanum, Z. schinifolium, and Z. piperitum, are distributed and intermixed with each other as "Zanthoxyli Pericarpium" in Korean markets. In the present study, we analyzed the ethyl acetate-soluble and nonpolar fractions of Zanthoxylum samples by 1H NMR spectrometry and performed a multivariate analysis for finding the discriminant markers between three species. Xanthoxylin was identified as the metabolic marker for the discrimination of Zanthoxylum species and quantified by the qNMR approach.

6.
J Ethnopharmacol ; 225: 31-41, 2018 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-29958960

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The herbal composition Gyeongshingangjeehwan 18 (GGEx18), composed of Rheum palmatum L. (Polygonaceae), Laminaria japonica Aresch (Laminariaceae), and Ephedra sinica Stapf (Ephedraceae), is used as an antiobesity drug in Korean clinics. The constituents of GGEx18 have traditionally been reported to inhibit obesity and related metabolic diseases such as insulin resistance and dyslipidemia. OBJECTIVE: This study investigated the effects of GGEx18 on nonalcoholic fatty liver disease (NAFLD) in mice fed a high-fat diet (HFD) and the underlying cellular and molecular mechanisms involved. METHODS: C57BL/6 J mice were fed either a low-fat diet (LFD), an HFD, or an HFD supplemented with GGEx18 (125, 250, or 500 mg/kg of body weight/day). After 13 weeks, blood analyses, histology, immunohistochemistry, and real-time PCR were performed to assess NAFLD development in these mice. RESULTS: Mice fed an HFD had increases in body weight, epididymal adipose tissue mass, adipocyte size, and adipose expression of inflammation-related genes compared with those fed an LFD. These increases were ameliorated in mice treated with 500 mg/kg/day GGEx18 without affecting food consumption profiles. GGEx18 not only decreased serum levels of triglycerides, free fatty acids, and alanine aminotransferase, but also decreased hepatic lipid accumulation, numbers of mast cells and α-smooth muscle actin-positive cells, and collagen levels induced by an HFD. Consistent with the histological data, the hepatic expression of lipogenesis-, inflammation-, and fibrosis-related genes was lower, while hepatic fatty acid ß-oxidation-related gene expression was higher, in mice receiving GGEx18 compared to mice fed only the HFD. DISCUSSION AND CONCLUSION: These results indicate that GGEx18 attenuates visceral obesity and NAFLD, in part by altering the expression of genes involved in hepatic steatosis and fibroinflammation in HFD-induced obese mice. These findings suggest that GGEx18 may be effective for preventing and treating NAFLD associated with visceral obesity.


Assuntos
Anti-Inflamatórios/uso terapêutico , Fármacos Antiobesidade/uso terapêutico , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Obesidade Abdominal/tratamento farmacológico , Preparações de Plantas/uso terapêutico , Animais , Dieta Hiperlipídica , Ephedra sinica , Regulação da Expressão Gênica/efeitos dos fármacos , Laminaria , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Camundongos Endogâmicos C57BL , Hepatopatia Gordurosa não Alcoólica/genética , Hepatopatia Gordurosa não Alcoólica/patologia , Obesidade Abdominal/genética , Obesidade Abdominal/patologia , Fitoterapia , Extratos Vegetais , Rheum
7.
Pharmacogn Mag ; 14(54): 162-166, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29720825

RESUMO

BACKGROUND: DF formula is a herbal preparation comprised three medicinal herbs, namely, Ephedra intermedia, Rheum palmatum, and Lithospermum erythrorhizon, which is being used for the treatment of obesity and liver fibrosis in Korean local clinics. OBJECTIVE: Since the abovementioned three herbs exist with different proportions in DF formula and their chemical markers have different physiochemical properties; it is quite challenging to develop an analytical methodology for the determination of these chemical markers. MATERIALS AND METHODS: For the analysis of the three herbs, five chemicals, (+)-pseudoephedrine (1) and (-)-ephedrine (2) for E. intermedia, aloe-emodin (3), and chrysophanol (4) for R. palmatum, and shikonin (5) for L. erythrorhizon, were selected for method validation of DF formula, and the analytical conditions were optimized and validated using high-performance liquid chromatography coupled with an ultraviolet detector (HPLC-UV). RESULTS: The specificities for the five compounds 1-5 were determined by their UV absorption spectra (1-4: 215 nm and 5: 520 nm). Their calibration curves showed good linear regressions with high correlation coefficient values (R2 > 0.9997). The limits of detection of these five markers were in the range 0.4-2.1 ng/mL, with the exception of 5 (12.7 ng/mL). The intraday variability for all the chemical markers was less than a Relative standard deviation (RSD) of 3%, except for 5 (RSD = 12.6%). In the case of interday analysis, 1 (1.0%), 2 (3.1%), and 4 (3.7%) showed much lower variabilities (RSD < 5%) than 3 (7.6%) and 5 (8.2%). Moreover, the five chemical markers showed good recoveries with good accuracies in the range of 90%-110%. CONCLUSIONS: The developed HPLC-UV method for the determination of the five chemical markers of the components of DF formula was validated. SUMMARY: DF formula, the herbal composition of Ephedra intermedia, Rheum palmatum and Lithospermum erythrorhizonFive chemical markers in DF formula were (+)-pseudoephedrine (1) and (-)-ephedrine (2) for E. intermedia, aloe-emodin (3) and chrysopanol (4) for R. palmatum, and shikonin (5) for L. erythrorhizon, with quite different physico-chemical propertiesFive chemical markers in DF formula were determined by HPLC-UV Abbreviations used: EP: (-)-ephedrine; PSEP: (+)-pseudoephedrine; HPLC: High-performance liquid chromatography; UV: Ultraviolet; LOD: Limit of detection; LOQ: Limit of quantification; RSD: Relative standard deviation.

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