RESUMO
Two new phenanthrene and 9, 10-dihydrophenanthrene derivatives (1-2) with six known congeners (3-8) were isolated from the extraction of stems of Dendrobium officinale. Compounds 1 and 2 were based on carbon skeleton in which phenanthrene and 9, 10-dihydrophenanthrene moiety were linked with a phenylpropane unit through a dioxane bridge, respectively. Their structures were determined by comprehensive NMR spectroscopic data, the absolute configuration of new compounds were determined by comparing their experimental and calculated ECD for the first time. All the compounds were investigated contains two cancer cell lines (HI-60, THP-1). All the isolates showed cytotoxicity, especially compound 4 showed markedly cytotoxic activities against HI-60 and THP-1 cell lines with IC50 values of 11.96 and 8.92 µM.
Assuntos
Dendrobium/química , Fenantrenos/química , Caules de Planta/química , Humanos , Estrutura MolecularRESUMO
Five selaginellin derivatives, including two new selaginellins termed selaginellins M (1) and N (2), and three previously identified compounds, selaginellin (3), selaginellin A (4), and selaginellin C (5), were isolated from the Selaginella tamariscina (Beauv.) Spring plant. In addition, four known biflavonoids, namely neocryptomerin ( 6), hinokiflavone (7), pulvinatabiflavone (8), and 7''- O-methylamentoflavone (9), were also isolated. The structures of new compounds 1 and 2 were elucidated by spectroscopic analysis. The cytotoxic activity of compounds 1- 9 was evaluated against a small panel of human cancer cell lines, including U251 (human glioma cells), HeLa (human cervical carcinoma cells), and MCF-7 (human breast cancer cells). The two new selaginellins, selaginellins M (1) and N (2), showed medium activity against the human cancer cell lines.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Biflavonoides/farmacologia , Selaginellaceae/química , Compostos de Bifenilo/farmacologia , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Cicloexanonas/farmacologia , Citotoxinas/farmacologia , Glioma/tratamento farmacológico , Células HeLa/efeitos dos fármacos , Humanos , Estrutura Molecular , Fitoterapia , Extratos Vegetais/farmacologiaRESUMO
OBJECTIVE: To study the chemical constituents from aerial parts of Gynura divaricata. METHODS: The constituents were isolated on silica gel column chromatography, preparative TLC and Sephadex LH-20 column chromatography, identified by physicochemical properties and the structures were elucidated by spectral analysis. RESULTS: 10 compounds were isolated and identified as 2-(1', 2', 3', 4'-tetrahydroxybutyl)-6-(2", 3", 4"-trihydroxybutyl)-pyrazine (1), 2-(1', 2', 3', 4'-tetrahydroxybutyl)-5-(2", 3", 4"-trihydroxybutyl) -pyrazine (2), nicotinic acid (3), 5-hydroxy-picolinic acid(4), methyl-5-hydroxy-2- pyridinecarboxylate (5), adenosine (6), uridine (7), stigmasterol-5-O- beta-D-glucoside (8), dibutyl terephthalate (9), methyl chlorogenate (10). CONCLUSION: Compounds 1, 2, 5, 9, 10 are obtained from this genus for the first time, Compounds 3, 4 are obtained from this plant for the first time.
Assuntos
Asteraceae/química , Niacina/isolamento & purificação , Ácidos Picolínicos/isolamento & purificação , Componentes Aéreos da Planta/química , Plantas Medicinais/química , Adenosina/química , Adenosina/isolamento & purificação , Ácido Clorogênico/análogos & derivados , Ácido Clorogênico/química , Ácido Clorogênico/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Niacina/química , Ácidos Picolínicos/química , Uridina/química , Uridina/isolamento & purificaçãoRESUMO
The aim of this study was to investigate the effect of demethylbellidifolin (DMB), a major xanthone compound of Swertia davidi franch, on nitroglycerin (NTG) tolerance. In the in vivo portion of the study, pretreatment of Sprague-Dawley rats with NTG (10 mg/kg) for 8 days caused tolerance to the depressor effect of NTG. This was evident because the depressor effect of NTG (150 microg/kg, I. V.) was almost completely abolished in the tolerant rats. The tolerance could be diminished by treatment with DMB. In the in vitro study, the exposure of aortic rings of Sprague-Dawley rats to NTG (10 microM) for 30 min caused tolerance to the vasodilating effect of NTG. The tolerance is evident because of a substantial right shift of the NTG concentration-relaxation curves. This shift was reduced by pretreatment of the aortic rings with DMB. In cultured human umbilical vein endothelial cells (HUVECs), incubation of NTG for 16 h increased reactive oxygen species (ROS) production, attenuated cyclic guanosine monophosphate (cGMP) levels and decreased the activity of aldehyde dehydrogenase 2 (ALDH-2), the main enzyme responsible for NTG bioactivation. All the effects mentioned above were prevented by co-incubation with DMB. In conclusion, DMB prevents NTG tolerance via increasing ALDH-2 activity through decreasing ROS production.
Assuntos
Aldeído Desidrogenase/metabolismo , Antioxidantes/farmacologia , Tolerância a Medicamentos , Células Endoteliais/efeitos dos fármacos , Proteínas Mitocondriais/metabolismo , Nitroglicerina/uso terapêutico , Swertia/química , Xantenos/farmacologia , Aldeído-Desidrogenase Mitocondrial , Animais , Antioxidantes/isolamento & purificação , Aorta , GMP Cíclico/metabolismo , Interações Ervas-Drogas , Humanos , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/metabolismo , Veias Umbilicais , Vasodilatadores , Xantenos/isolamento & purificaçãoRESUMO
Asymmetric dimethylarginine (ADMA), an endogenous nitric oxide synthase (NOS) inhibitor, has been implicated in vascular inflammation through induction of reactive oxygen species (ROS) and proinflammatory genes in endothelial cells. However, relatively few attentions have been paid to the effect of ADMA on monocytes, one of the important cells throughout all stages of atherosclerosis. In the present study, we found that reinioside C, the main component extracted from Polygala fallax Hemsl., dose-dependently inhibited tumor necrosis factor-alpha (TNF-alpha) production induced by ADMA in monocytes, Furthermore, reinioside C attenuated ADMA-induced generation of reactive oxygen species and activation of nuclear factor-kappaB (NF-kappaB) activity in monocytes in a dose-dependent manner, this effect was inhibited by l-arginine (NOS substrate) and PDTC (inhibitor of NF-kappaB). These data suggest that reinioside C could attenuate the increase of TNF-alpha induced by exogenous ADMA through inhibition ROS/NF-kappaB pathway in monocytes.
Assuntos
Arginina/análogos & derivados , Medicamentos de Ervas Chinesas/farmacologia , Monócitos/efeitos dos fármacos , NF-kappa B/metabolismo , Polygala , Espécies Reativas de Oxigênio/metabolismo , Saponinas/farmacologia , Fator de Necrose Tumoral alfa/metabolismo , Arginina/metabolismo , Linhagem Celular , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/isolamento & purificação , Humanos , Monócitos/metabolismo , NF-kappa B/antagonistas & inibidores , Óxido Nítrico Sintase/metabolismo , Polygala/química , Pirrolidinas/farmacologia , Tiocarbamatos/farmacologiaRESUMO
OBJECTIVE: To investigate the effect of reinioside C (RC) on the expression of lectin-like oxidized low density lipoprotein receptor (LOX)-1 mRNA and LOX-1 protein induced by oxidized low density lipoprotein (ox-LDL) in cultured human umbilical vein endothelial cells (HUVEC). METHODS: HUVECs were cultured with ox-LDL (50 mg/L) for 24 h in the absence or presence of RC (1, 3, and 10 micromol/L). The expressions of LOX-1 mRNA and LOX-1 protein were examined by RT-PCR and Western-blot. RESULTS: Incubation with ox-LDL (50 mg/L) significantly raised the expression of LOX-1 mRNA and LOX-1 protein,which was concentration-dependent. CONCLUSION: RC can inhibit the increased expression of LOX-1 mRNA and LOX-1 protein induced by ox-LDL in HUVECs.
Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Lipoproteínas LDL/farmacologia , Polygala/química , Receptores de LDL/biossíntese , Saponinas/farmacologia , Veias Umbilicais/metabolismo , Células Cultivadas , Endotélio Vascular , Humanos , RNA Mensageiro/biossíntese , RNA Mensageiro/genética , Receptores de LDL/genética , Veias Umbilicais/citologiaRESUMO
A new compound, 2-(1,4-dihydroxy cyclohexanyl )-acetic acid isolated from the seeds of Forsythia suspensa (Thunb.) Vahl, has been assessed for potent antiviral effect on RSV for the first time in vitro by cell morphology methods. Its structure was elucidated on the basis of spectroscopic evidence (IR, MS, 1H-NMR, 13C-NMR). We have trivially named it Rengynic acid.