RESUMO
Six new cyanoglucosides, 2S-cardiospermin-5-benzoate (1), 2R-cardiospermin-5-p-hydroxybenzoate (2), 2S-cardiospermin-5-cis-p-coumarate (3), isocardiospermin-5-p-hydroxybenzoate (4), sutherlandin-5-p-hydroxybenzoate (5), and sutherlandin-5-cis-p-coumarate (6), together with 17 known compounds were isolated from Sorbaria sorbifolia. The structures of the new compounds were elucidated by extensive spectroscopic methods, including 1D and 2D NMR, HR-ESI-MS and ECD experiments. The biosynthetic relationship of 1-9 was also discussed. The cyanoglucosides (1-9) and 15 exhibited moderate inhibitory effect on nitric oxide production of RAW264.7 macrophages stimulated by lipopolysaccharide (LPS).
Assuntos
Glicosídeos/química , Hidroxibenzoatos/química , Leucina/química , Rosaceae/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Ácidos Cumáricos/química , Ácidos Cumáricos/isolamento & purificação , Glicosídeos/isolamento & purificação , Hidroxibenzoatos/isolamento & purificação , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Componentes Aéreos da Planta/química , Células RAW 264.7RESUMO
Two new C(13)-norisoprenoids, named lyratols E and F (1-2), were isolated from the whole plant of Solanum lyratum Thunb, and their structures were elucidated by extensive spectroscopic analyses. In vitro, two new compounds were found to show significant cytotoxicity against selected cancer cells including P-388 and HT-29.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Norisoprenoides/isolamento & purificação , Solanum/química , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Células HT29 , Humanos , Leucemia P388 , Camundongos , Estrutura Molecular , Norisoprenoides/química , Norisoprenoides/farmacologiaRESUMO
Two new ent-clerodane diterpenoids have been isolated from Scutellaria barbata, and their structures were established by detailed spectroscopic analyses as (13R)-6α,7ß-dihydroxy-8ß,13-epoxy-11ß-nicotinyloxy-ent-clerodan-3-en-15,16-olide (scutelinquanine D, 1) and (11E)-6α-acetoxy-7ß,8ß-dihydroxy-ent-clerodan-3,11,13-trien-15,16-olide (6-acetoxybarbatin C, 2). In vitro, the isolated two new compounds showed significant cytotoxic activities against three human cancer cell lines (HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells), and gave IC(50) values in the range of 2.5-6.6 µM.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Diterpenos Clerodânicos/isolamento & purificação , Diterpenos Clerodânicos/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Scutellaria/química , Antineoplásicos Fitogênicos/química , Diterpenos/química , Diterpenos Clerodânicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Células HT29 , Humanos , Concentração Inibidora 50 , Células KB , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , EstereoisomerismoRESUMO
Two new neo-clerodane diterpenoids have been isolated from the whole plant of Scutellaria barbata D. Don, and their structures were established by detailed spectral analyses as scutehenanine H (1) and 6-(2,3-epoxy-2-isopropyl-n-propoxyl)barbatin C (2). In vitro, the isolated two new compounds showed significant cytotoxic activities against three human cancer lines, and gave IC(50) values in the range OF 2.0-4.2 µΜ.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Diterpenos Clerodânicos/isolamento & purificação , Neoplasias/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Scutellaria/química , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/uso terapêutico , Linhagem Celular Tumoral , Diterpenos Clerodânicos/farmacologia , Diterpenos Clerodânicos/uso terapêutico , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologiaRESUMO
This study was carried out to investigate whether rosmarinic acid (RA) has antifibrotic effect on experimental liver fibrosis in vitro and in vivo and its possible mechanism. Culture of hepatic stellate cells (HSCs) determine proliferation and expression of transforming growth factor-beta1 (TGF-beta1), connective transforming growth factor (CTGF) and alpha-smooth muscle actin (alpha-SMA). In carbon tetrachloride (CCL(4))-induced rat liver fibrosis model, determined biochemical indicator, liver fibrosis grade and histopathological changes, immunohistochemical detected liver TGF-beta1 and CTGF expression. The results indicated that RA could inhibit HSCs proliferation, inhibit TGF-beta1, CTGF and alpha-SMA expression in cultured HSCs. It has marked evident in reducing fibrosis grade, ameliorating biochemical indicator and histopathological morphology, reducing liver TGF-beta1 and CTGF expression in CCL(4)-induced liver fibrosis. These findings suggest that RA has potentially conferring antifibrogenic effects.
Assuntos
Antioxidantes/uso terapêutico , Intoxicação por Tetracloreto de Carbono/tratamento farmacológico , Cinamatos/uso terapêutico , Depsídeos/uso terapêutico , Células Estreladas do Fígado/efeitos dos fármacos , Cirrose Hepática/tratamento farmacológico , Fígado/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Actinas/metabolismo , Animais , Antioxidantes/farmacologia , Intoxicação por Tetracloreto de Carbono/complicações , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Cinamatos/farmacologia , Fator de Crescimento do Tecido Conjuntivo/antagonistas & inibidores , Depsídeos/farmacologia , Modelos Animais de Doenças , Fígado/metabolismo , Fígado/patologia , Cirrose Hepática/etiologia , Cirrose Hepática/metabolismo , Masculino , Fitoterapia , Extratos Vegetais/farmacologia , Ratos , Ratos Sprague-Dawley , Fator de Crescimento Transformador beta1/antagonistas & inibidores , Ácido RosmarínicoRESUMO
Astilbin, a flavonoid compound, was isolated from the rhizome of Smilax glabra Roxb. This study was conducted to investigate the efficacy of astilbin on experimental diabetic nephropathy (DN) in vivo and in vitro and its possible mechanisms. Astilbin was added in high glucose stimulated HK-2 cells, streptozotocin-induced experimental DN, randomized to receive intragastric ( I. G.) astilbin to observe its anti-renal lesion effect. Results showed that astilbin inhibited high glucose stimulated HK-2 cell production of transforming growth factor-beta1 (TGF-beta1) and connective tissue growth factor (CTGF) in vitro, especially CTGF; analogic results was also found in vivo. I. G. of astilbin 2.5 mg/kg or 5 mg/kg significantly ameliorated renal function, reduced kidney index, while it increased body weight and survival time in animals. In addition there was no significant difference in blood glucose level between the STZ-treated group and the astilbin groups. Furthermore, astilbin ameliorated the pathological progress of renal morphology. Astilbin can exert an early renal protective role to DN, inhibit production of TGF-beta1 and especially of CTGF. We suggest that astilbin inhibition of CTGF may be a potential target in DN therapy. This work provides the first evidence for astilbin as a new candidate of DN therapeutic medicine.