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1.
Carbohydr Res ; 484: 107777, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31446303

RESUMO

Four new triterpene glycosides, named salaciacochinosides A-D (1-4) were isolated from the 90% ethanol extract of Salacia cochinchinensis, together with five known compounds 2α,3ß,23-trihydroxyurs-12,18-dien-28-oic acid 28-O-ß-d-glucopyranoside (5), racemiside (6), alangiplatanoside (7), acantrifoside E (8), and syringin (9). The structures of the four new triterpenoids were characterized by chemical methods and MS, IR, 1D and 2D NMR spectral analyses. The α-glucosidase inhibitory activities of the nine compounds were assessed, compounds 6 and 7 showed remarkable α-glucosidase inhibitory activities, with IC50 values of 0.44 and 0.75 µM, respectively. Compounds 1-5 exhibited moderate α-glucosidase inhibitory activities, and compounds 8 and 9 showed none α-glucosidase inhibitory activity in our current experiments.


Assuntos
Inibidores de Glicosídeo Hidrolases/química , Glicosídeos/química , Salacia/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Glicosídeos/farmacologia , Concentração Inibidora 50 , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Triterpenos/química , Triterpenos/farmacologia
2.
J Asian Nat Prod Res ; : 1-8, 2019 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-31131622

RESUMO

Two new isopimarane diterpenoids, named 1α-hydroxy-7-oxoisopimara-8, 15-diene (1), 11ß-hydroxy-7-oxoisopimara-8(14), 15-diene (2), together with six known compounds (3-8), were isolated from the medicinal plant Salacia cochinchinensis. All isolates were assayed for their cytotoxicity and α-glucosidase inhibitory activity. Results suggested compounds 1, 3 possessed significant cytotoxic activity against HepG2, HL60, and Hela cell lines with IC50 values ranging from 0.23 to 0.35 µM, and compounds 7, 8 exhibited noticeable α-glucosidase inhibitory ability with IC50 values of 0.25 and 0.31 µM, respectively.

3.
Fitoterapia ; 130: 152-155, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30172827

RESUMO

Two new terpenoids, named biperovskatone B (1) and 1α- hydroxyl demethylsalvicanol quinine (2), were isolated from the cultured Perovskia atriplicifolia. Their structures were elucidated by comprehensive analyses of the MS, IR, 1D and 2D NMR spectra. Compound 1 was a novel diterpenoid dimer, containing two different rearranged 9(10 → 20)-abeoabietane type diterpenoid fragments. Compound 2 was a new icetexane diterpenoid with characteristic ortho-quinone carbonyl groups. Both compounds were assayed for their anti-HBV activity in vitro. Results suggested compounds 1 and 2 showed noticeable anti- anti-HBV activity, inhibiting the replication of HBV DNA with IC50 values of 10.78 and 8.61 µM, respectively.


Assuntos
Antivirais/farmacologia , Vírus da Hepatite B/efeitos dos fármacos , Salvia/química , Terpenos/farmacologia , Antivirais/isolamento & purificação , China , Células Hep G2 , Humanos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Terpenos/isolamento & purificação
4.
Zhongguo Zhong Yao Za Zhi ; 43(13): 2705-2712, 2018 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-30111020

RESUMO

In order to establish a more perfect evaluation system for dryness effect of Atractylodis Rhizoma, determine the main dry parts of Atractylodis Rhizoma,and further define the mechanism of stir-baked Atractylodis Rhizoma in reducing the dryness. The healthy rats were given with different doses of water extract and volatile oil of raw Atractylodis Rhizoma and stir-baked Atractylodis Rhizoma for 21 days. Based on the theory of the dry-dry and dryness-induced Yin deficiency, the amount of drinking water, tissue morphology of submandibular glands, urine volume and the expression of aquaporin 2 (AQP2) in the kidneys, as well as blood rheology, ratio of cAMP/cGMP in serum and the content of Na⁺-K⁺-ATP enzyme were selected as the evaluation indexes. The results indicated that the rats with high dose volatile oil from raw Atractylodis Rhizoma had a significant increase in the amount of drinking water, urine volume, blood viscosity, ratio of cAMP/cGMP and content of Na⁺-K⁺-ATP enzyme in the serum(P<0.05)as compared with the soybean oil group; meanwhile, atrophy of submandibular acinar gland was obvious,and the expression of aquaporin 2 was reduced significantly(P<0.05). There were significant differences between volatile oil high dose group of raw Atractylodis Rhizoma and volatile oil high dose group of stir-baked Atractylodis Rhizoma. There was no significant difference between the water extract groups of raw and stir-baked Atractylodis Rhizoma and the saline group. A comprehensive evaluation system for the dryness effect of Atractylodis Rhizoma was established. It was confirmed that the volatile oil part was the main dry part of Atractylodis Rhizoma. It revealed that the mechanism of dryness effect of Atractylodis Rhizoma was not only related to the decrease of the total content of the volatile oil, but also may be related to the transformation of dryness components in the volatile oil. It provides references for the study of material basis of Atractylodis Rhizoma dryness, provides an experimental basis for the clinical application of Atractylodis Rhizoma, further clarifies the mechanism of stir-baked Atractylodis Rhizoma in reducing the dryness, and provides thoughts for the evaluation of other dry traditional Chinese medicines.


Assuntos
Atractylodes , Medicamentos de Ervas Chinesas , Animais , Aquaporina 2 , Ratos , Rizoma , Deficiência da Energia Yin
5.
Chem Biodivers ; 14(7)2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28419767

RESUMO

Four new diterpene glucosides, namely perovskiaditerpenosides A - D (1 - 4), were isolated from the BuOH extract of Perovskia atriplicifolia. Their structures were well elucidated by chemical methods and comprehensive spectroscopic analyses including MS, IR, and NMR (1D and 2D). The newly isolated compounds were screened for their cytotoxic activity against HepG2, NB4, HeLa, K562, MCF7, PC3, and HL60. The obtained results indicated that the new compounds possessed considerable cytotoxic activity.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Diterpenos/isolamento & purificação , Glucosídeos/isolamento & purificação , Lamiaceae/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Butanóis , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Extratos Vegetais , Análise Espectral
6.
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
7.
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
8.
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
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