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1.
Zhongguo Zhong Yao Za Zhi ; 44(23): 5191-5197, 2019 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-32237357

RESUMO

This study aims to investigate the PPARγ agonists isolated from the aqueous extract of Siegesbeckia pubescens( SPA) and their anti-inflammatory activities in vitro. The 293 T cells transfected transiently with PPARγ recombinant plasmid were used as a screening model to guide the isolation of PPARγ activitating components,and then PPARγ activities were measured by double luciferase reporter gene assay. The chemical structures were identified by chromatography or spectroscopic techniques. Furthermore,a UC inflammatory model in vitro was established on HT-29 cells by stimulating with TNF-α. The mRNA levels and secretion of proinflammatory cytokines on HT-29 cells,such as IL-1ß,TNF-α,IL-8,were detected by RT-PCR and ELISA. The results showed that five diterpenoids were obtained from the fraction D_(50) with the strongest PPARγ activity among others in SPA,and determined as kirenol( 1),darutigenol( 2),enantiomeric-2-ketone-15,16,19-three hydroxypinomane-8( 14)-ene-19-O-ß-D-glucoside( 3),darutoside( 4),enantiomeric-2-ß,15,16,19-four hydroxypinomane-8( 14)-ene-19-O-ß-D-glucoside( 5),respectively. All the compounds exhibited active effects on PPARγ in a concentration-dependent manner( P<0. 01). In addition,compound 1 significantly inhibited the expression of IL-1ß mRNA and secretion of IL-8 on HT-29 cells inflammation model( P<0. 001); both compounds 2 and 3 effectively inhibited the expression of IL-1ß,TNF-α,IL-8 mRNA and secretion of IL-8( P<0. 01 or P<0. 001),although at different extent; compound 4 significantly inhibited the expression of IL-1ß and TNF-α mRNA( P<0. 01 or P<0. 001),while compound 5 inhibited the expression of IL-1ß mRNA obviously( P<0. 001). In conclusion,the diterpenoids 1-5 isolated from S. pubescens have the PPARγ activation activities and potential effects of anti-UC in vitro.


Assuntos
Anti-Inflamatórios/farmacologia , Asteraceae/química , Diterpenos/farmacologia , PPAR gama/agonistas , Colite Ulcerativa , Citocinas/imunologia , Células HT29 , Humanos , Fator de Necrose Tumoral alfa
2.
Cancer Lett ; 420: 195-207, 2018 04 28.
Artigo em Inglês | MEDLINE | ID: mdl-29425683

RESUMO

Uncontrolled excessive activation of Hedgehog (Hh) signaling pathway is linked to a number of human malignant tumorigenesis. To obtain valuable Hh pathway inhibitors from natural product, in present study, a pair of novel epimers, Cynanbungeigenin C (CBC) and D (CBD) from the plant Cynanchum bungei Decne were chemically characterized by multiple spectroscopic data and chemical derivatization, and evaluated for their inhibition on Hh pathway. Mechanistically, CBC and CBD block Hh pathway signaling not through targeting Smo and Sufu, but at the level of Gli. In addition, both eipmers significantly suppress Hh pathway-dependent Ptch+/-; p53-/- medulloblastoma in vitro and in vivo. Furthermore, both CBC and CBD inhibited two Smo mutants induced Hh pathway activation, which suggested that they are potential compounds for the treatment of medulloblastoma with primary or acquired resistance to current Smo inhibitors. These results highlight the potential of CBC and CBD as effective lead compounds in the treatment of medulloblastoma and other Hh-dependent malignancy.


Assuntos
Neoplasias Cerebelares/tratamento farmacológico , Cynanchum/química , Meduloblastoma/tratamento farmacológico , Fitosteróis/administração & dosagem , Fitosteróis/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos , Animais , Neoplasias Cerebelares/metabolismo , Células HEK293 , Proteínas Hedgehog/metabolismo , Humanos , Meduloblastoma/metabolismo , Camundongos , Células NIH 3T3 , Fitosteróis/química , Fitosteróis/farmacologia , Extratos Vegetais/análise , Ensaios Antitumorais Modelo de Xenoenxerto , Proteína GLI1 em Dedos de Zinco/metabolismo
3.
Nat Prod Commun ; 11(6): 747-8, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27534107

RESUMO

Two new 13, 14/14, 15-disecopregnane-type skeleton C21 steroidal aglycones, neocynapanogenin G (1) and neocynapanogenin H (2), were isolated from the hydrolyzed extract of the CHCl3 soluble extract of the roots of Cynanchun paniculatum. Their structures were determined on the basis of chemical evidence and extensive spectroscopic methods, including 1D and 2D NMR spectroscopy. Compound 1 displayed signifidant inhibition of the Hedgehog signaling pathway in vitro.


Assuntos
Cynanchum/química , Medicamentos de Ervas Chinesas/química , Iridoides/química , Raízes de Plantas/química , Esteroides/química , Animais , Linhagem Celular , Ouriços-Cacheiros/genética , Ouriços-Cacheiros/metabolismo , Humanos , Estrutura Molecular , Transdução de Sinais/efeitos dos fármacos
4.
Eur J Pharmacol ; 789: 370-384, 2016 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-27448502

RESUMO

Stephanthraniline A (STA), a C21 steroid isolated from Stephanotis mucronata (Blanco) Merr., was previously shown to inhibit T cells activation and proliferation in vitro and in vivo. The purpose of this study was to further evaluate the in vivo immunosuppressive activity of STA and to elucidate its potential mechanisms. The results showed that pretreatment with STA significantly attenuated concanavalin A (Con A)-induced hepatitis and reduced CD4(+) T cells activation and aggregation in hepatic tissue in mice. STA directly suppressed the activation and proliferation of Con A-induced CD4(+) T cells, and inhibited NFAT, NFκB and MAPK signaling cascades in activated CD4(+) T cells in vitro. Moreover, it was proved that STA inhibited T cells activation and proliferation through proximal T cell-receptor (TCR) signaling- and Ca(2+) signaling-independent way. The molecular docking studies predicted that STA could tight bind to PKCθ via five hydrogen. The further findings indicated STA directly inhibited PKCθ kinase activity, and its phosphorylation in activated CD4(+) T cells in vitro. Collectively, the present study indicated that STA could protect against CD4(+) T cell-mediated immunological hepatitis in mice through PKCθ and its downstream NFAT, NFκB and MAPK signaling cascades. These results highlight the potential of STA as an effective leading compound for use in the treatment of CD4(+) T cell-mediated inflammatory and autoimmune diseases.


Assuntos
Linfócitos T CD4-Positivos/efeitos dos fármacos , Linfócitos T CD4-Positivos/imunologia , Diterpenos/farmacologia , Hepatite/tratamento farmacológico , Hepatite/imunologia , Isoenzimas/antagonistas & inibidores , Ativação Linfocitária/efeitos dos fármacos , Proteína Quinase C/antagonistas & inibidores , Animais , Sinalização do Cálcio/efeitos dos fármacos , Domínio Catalítico , Agregação Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Diterpenos/metabolismo , Diterpenos/uso terapêutico , Feminino , Hepatite/metabolismo , Hepatite/patologia , Isoenzimas/química , Isoenzimas/metabolismo , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Camundongos , Simulação de Acoplamento Molecular , NF-kappa B/metabolismo , Fatores de Transcrição NFATC/metabolismo , Fosforilação/efeitos dos fármacos , Proteína Quinase C/química , Proteína Quinase C/metabolismo , Proteína Quinase C-theta , Proteínas Quinases/metabolismo
5.
Nat Prod Commun ; 11(12): 1797-1800, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30508336

RESUMO

Two new 8, 14-seco skeleton C(21) steroidal aglycones, cynanbungeigenin A (1) and cynanbungeigenin B (2), were isolated from the hydrolyzed extract of the EtOAc soluble extract of the roots of Cynanchum bungei. Their structures were determined on the basis of chemical evidence and extensive spectroscopic methods, including 1D and 2D NMR spectroscopy.


Assuntos
Cynanchum/química , Pregnanos/isolamento & purificação , Animais , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Proteínas Hedgehog/antagonistas & inibidores , Camundongos , Células NIH 3T3 , Extratos Vegetais/química , Raízes de Plantas/química , Pregnanos/química , Pregnanos/farmacologia , Espectroscopia de Prótons por Ressonância Magnética
6.
Nat Prod Commun ; 9(2): 155-6, 2014 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-24689277

RESUMO

Two novel steroidal aglycones, together with four known ones, were isolated from the hydrolysis extract of the CHCl3 soluble extract of the stems of Marsdenia tenacissima. Their structures were determined on the basis of chemical evidence and extensive spectroscopic methods, including 1D and 2D NMR spectroscopy. These compounds displayed inhibition of the Hedgehog signaling pathway in vitro.


Assuntos
Proteínas Hedgehog/antagonistas & inibidores , Marsdenia/química , Transdução de Sinais/efeitos dos fármacos , Esteroides/isolamento & purificação , Extratos Vegetais/análise , Caules de Planta/química , Esteroides/farmacologia
8.
Chem Biodivers ; 8(6): 1121-31, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21674784

RESUMO

The total crude polysaccharides (CADPs), isolated from the roots of Angelica dahurica by H(2) O extraction, EtOH precipitation, and dialysis, and the four fractions ADP1, ADP2, ADP3, and ADP4, obtained by gel filtration of the CADPs, were analyzed to characterize their composition and evaluated for their antioxidant activity using different in vitro tests such as the malondialdehyde (MDA)-production, the ferrous ion (Fe(2+) )-chelating, and the HO(.) radical-scavenging assays. The predominant neutral monosaccharides in the four fractions were identified as arabinose, galactose, and glucose, while the composition and ratio of the monosaccharides were different between the fractions. The CADPs and its fractions were found to significantly inhibit lipid peroxidation, chelate Fe(2+) , and scavenge HO(.) radicals, indicating that these polysaccharides possessed antioxidant activity. Among the four fractions, ADP4 exhibited the strongest antioxidant activity, which was stronger than that of the control antioxidant vitamin E (Vit E). Taken together, the chemical composition of these polysaccharides might affect their antioxidant activity, and ADP4 could be explored as a source of potential novel natural antioxidants for food and pharmaceutical purposes.


Assuntos
Angelica/química , Depuradores de Radicais Livres/química , Polissacarídeos/química , Cromatografia em Gel , Depuradores de Radicais Livres/isolamento & purificação , Depuradores de Radicais Livres/farmacologia , Quelantes de Ferro/química , Quelantes de Ferro/isolamento & purificação , Quelantes de Ferro/farmacologia , Malondialdeído/metabolismo , Raízes de Plantas/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia
9.
J Ethnopharmacol ; 125(2): 310-7, 2009 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-19559777

RESUMO

AIM OF THE STUDY: The roots of Actinidia eriantha Benth (Actinidiaceae) have been used for cancers in the Chinese folk medicine. The present study aimed at evaluating the antitumor potentials of the polysaccharides from the roots of Actinidia eriantha and elucidating their immunological mechanisms by determining the effects on the growth of tumor transplanted in mice and the immune response in tumor-bearing mice. MATERIALS AND METHODS: The total polysaccharide AEP and fours purified polysaccharides AEPA, AEPB, AEPC and AEPD were isolated and purified from the roots of Actinidia eriantha by hot water extraction, ethanol precipitation, dialysis and gel filtration. Their effects on the growth of mouse transplantable tumor, splenocyte proliferation, the activity of natural killer (NK) cells and cytotoxic T lymphocytes (CTL), production of cytokines from splenocytes, and serum antigen-specific antibody levels in tumor-bearing mice were measured. RESULTS: AEP and four purified polysaccharides could not only significantly inhibit the growth of mouse transplantable tumor, but also remarkably promote splenocytes proliferation, NK cell and CTL activity, IL-2 and IFN-gamma production from splenocytes, and serum antigen-specific antibody levels in tumor-bearing mice. CONCLUSIONS: The antitumor activity of AEP and four purified polysaccharides might be achieved by improving immune response, and the composition of the monosaccharides, uronic acid contents and molecular weight could affect their antitumor and immunomodulatory activity.


Assuntos
Actinidia/química , Antineoplásicos Fitogênicos/uso terapêutico , Citocinas/metabolismo , Fatores Imunológicos/uso terapêutico , Linfócitos/metabolismo , Neoplasias Experimentais/tratamento farmacológico , Polissacarídeos/uso terapêutico , Animais , Anticorpos/sangue , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Fatores Imunológicos/isolamento & purificação , Fatores Imunológicos/farmacologia , Interferon gama/metabolismo , Interleucina-2/metabolismo , Células Matadoras Naturais/metabolismo , Masculino , Camundongos , Transplante de Neoplasias , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Raízes de Plantas , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Sarcoma 180 , Baço/citologia , Linfócitos T Citotóxicos/metabolismo
10.
Zhongguo Zhong Yao Za Zhi ; 33(20): 2356-8, 2008 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-19157127

RESUMO

OBJECTIVE: To study the chemical constituents from n-BuOH fraction of the roots of Stephanotis mucronata. METHOD: The compounds were separated by chromatographic methods. A combination of UV, MS, and NMR spectroscopic methods was applied to identify structure of these compounds. RESULT: Four oleane saponins were isolated and identified as sitakisoside VII (1), sitakisoside VI (2), sitakisoside II (3), and sitakisoside I (4). CONCLUSION: These four compounds were obtained for the first time from this plant.


Assuntos
Apocynaceae/química , Medicamentos de Ervas Chinesas/química , Raízes de Plantas/química , Saponinas/química , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular
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