RESUMO
Objective: To investigate the chemical constituents of Thalictrum fortunei. Methods: Compounds were separated and purified by chromatographic methods and the structures were identified by their physicochemical properties and spectroscopic data. Results: Ten compounds were isolated and identified as bergenin( 1),1-( 4-hydroxy-3-methoxy)-phenyl-2-[4-( 1,2,3-trihydroxypropyl)-2-methoxy]-phenoxym-1,3-propandiol( 2) ã4-( 2-hydroxyethyl)-2-methoxyphenyl-O-ß-D-glucopyranoside( 3),meliasendanin D( 4),2-( 4-hydroxy-3-methoxyphenyl)-ethyl-O-ß-D-glucopyranoside( 5),kizutasaponin C( 6),2-( 3-hydroxy-4-methoxyphenyl)-ethyl-O-ß-Dglucopyranoside( 7),ß-sitosterol( 8),3-O-ß-D-glucopyranosyl( 1â6)-ß-D-glucopyranosyl( 22 S,24Z)-cycloart-24-en-3ß,22,30-tetraol-26-O-ß-D-glucopyranoside( 9) and 3-O-ß-D-quinovopyranosyl( 1â6)-ß-D-glucopyranosyl( 1â4)-ß-D-fucopyranosyl( 22 S,24Z)-cycloart-24-en-3ß,22,26-triaol-26-O-ß-D-glucopyranoside( 10). Conclusion: Compounds 1 ~ 6 are isolated form this plant for the first time.
Assuntos
Thalictrum , Cromatografia , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos VegetaisRESUMO
OBJECTIVE: To study the protective effects of ginkgolide N against glutamte-induced injury in PC12 cells and its mechanisms. METHODS: The injury model was established by treating PC12 cells with glutamate, and PC12 cells were treated with different concentrations of ginkgolide N with ginkgolide B as control. The cells activity was analyzed by MTT assay. The apoptosis of PC12 cells were examined by acridine orange( AO) staining, the reactive oxygen species and mitochondrial membrane potential of PC12 cells were examined by flow cytometry. Western blot method was used to examine the expression of Cleaved Caspase-3 protein. RESULTS: Ginkgolides N of 2-8 µgmol/L inhibited PC12 cells apoptosis and ROS accumulation induced by glutamate,stabilized membrane potential of damaged PC12, and reduced the expression of Cleaved Caspase-3 protein. CONCLUSION: Ginkgolide N has a protective effect on PC12 cells injury induced by glutamate, and the mechanism may be associated with reducing ROS generation, stabilizing membrane potential and inhibiting the expression of Cleaved Caspase-3 protein.
Assuntos
Ginkgolídeos/farmacologia , Ácido Glutâmico/efeitos adversos , Potencial da Membrana Mitocondrial , Substâncias Protetoras/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Animais , Apoptose , Caspase 3/metabolismo , Células PC12/efeitos dos fármacos , RatosRESUMO
Microctis Folium, the leaves of Microcos paniculata L., is a commonly used herbal tea material. The methanol extract of Microctis Folium and its principle compounds vitexin (1), isovitexin (2) and isorhamnetin 3-O-ß-D-rutinoside (3) were investigated for their α-glucosidase inhibitory effects. The extract showed strong α-glucosidase inhibitory effect (IC50 = 61.30 µg/mL) and the three flavonoid glycosides 1-3 exerted satisfactory α-glucosidase inhibitory effects, with IC50 values of 244.0 µM, 266.2 µM and 275.4 µM, respectively. A simple and reliable HPLC-DAD method was developed for the quantification of the three flavonoid glycosides in Microctis Folium and applied successfully to determine contents of these components in samples collected from different locations. This study suggested that Microctis Folium may be a promising candidate for development of herbal antidiabetes drugs, and vitexin, isovitexin and isorhamnetin 3-O-ß-D-rutinoside can be the biomarkers and chemical markers for this plant substance.
Assuntos
Flavonoides/farmacologia , Inibidores de Glicosídeo Hidrolases , Glicosídeos/farmacologia , Poaceae/química , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Ativação Enzimática/efeitos dos fármacos , Flavonoides/química , Glicosídeos/química , Concentração Inibidora 50 , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Reprodutibilidade dos TestesRESUMO
Ypsilandra thibetica belongs to the family Liliaceae. Its whole plant has the medicinal functions of heat-clearing and detoxifying, relieving congestion and other effects, and is used as the folk medicine to cure scrofula, dysuria embolism and other symptoms. Previous chemical studies revealed that its major and active ingredient is steroidal saponin. Up to now, more than fifty steroidal saponins, mainly composed of spirostan and furostanol types, have been described. Pharmacological and clinical studies have demonstrated that Y. thibetica has anti-tumor, uterine contractions, hemostatic and antibacterial activities, in particular for the treatment of a variety of gynecological hemorrhagic diseases. In an effort to provide references for the advanced research and development of this species, this paper summarized the research progress on its pharmacognosy, including botany and authentication, its isolated secondary metabolites, biological activities and pharmacological applications. In addition, some advantages of this species which could be potentially used as a substitute for Paridis Rhizoma, one of ingredients of the well-known drug "Yunnan Baiyao", together with the future prospect are also briefly included.
Assuntos
Medicamentos de Ervas Chinesas/química , Liliaceae/química , Plantas Medicinais/química , Animais , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Estrutura MolecularRESUMO
Two new cycloartane glycosides were isolated from the aerial parts of Thalictrum fortunei (Ranunculaceae). The chemical structures of these compounds were elucidated as 3-O-ß-D-glucopyranosyl (1 â 4)-ß-d-fucopyranosyl-(22S,24Z)-cycloart-24-en-3ß,22,26,30-tetraol 26-O-ß-D-glucopyranoside and 3-O-ß-D-glucopyranosyl (1 â 4)-ß-D-fucopyranosyl-(22S,24Z)-cycloart-24-en-3ß,22,26,29-tetraol 26-O-ß-D-glucopyranoside by extensive 1D and 2D NMR methods, HR-ESI-MS, and hydrolysis. Their cytotoxic activities toward human hepatoma Bel-7402 cells, human colon carcinoma LoVo cells, and human non-small-cell lung cancer NCIH-460 cells were evaluated by MTT assay, respectively.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Saponinas/isolamento & purificação , Thalictrum/química , Triterpenos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Saponinas/química , Saponinas/farmacologia , Triterpenos/química , Triterpenos/farmacologiaRESUMO
OBJECTIVE: To study the pharmacokinetics of ginkgolide B injection in Beagle dogs. METHODS: Determined the serum concentration of ginkgolide B by LC-MS and calculated its parameter of pharmacokinetics via DAS 2.0 software. RESULTS: After intravenous drips of 0.62, 2.07 and 10.35 mg/kg ginkgolide B, parameters of pharmacokinetics of ginkgolide B were as follows: Tmax were 0.444, 1, 1 h; Cmax were 0.764, 3.024, 11.013 mg/L; AUC(0-1) were 1.007, 3.644, 16.646 mg x h/Lo. CONCLUSION: Ginkgolide B has two compartment model in Beagle dogs.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Ginkgo biloba/química , Ginkgolídeos/farmacocinética , Lactonas/farmacocinética , Fator de Ativação de Plaquetas/antagonistas & inibidores , Fator de Ativação de Plaquetas/farmacocinética , Animais , Área Sob a Curva , Disponibilidade Biológica , Cães , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/farmacocinética , Feminino , Fibrinolíticos/administração & dosagem , Ginkgolídeos/administração & dosagem , Ginkgolídeos/sangue , Injeções Intravenosas , Lactonas/administração & dosagem , Lactonas/sangue , Masculino , Modelos Animais , Fator de Ativação de Plaquetas/administração & dosagem , Distribuição Aleatória , Fatores de TempoRESUMO
OBJECTIVE: To study the pharmacokinetics of ginkgolide B for injection in rats. METHODS: The serum concentration of ginkgolide B was determined by LC-MS and calculate its parameter of pharmacokinetics via DAS2.0 software. RESULTS: After intravenous of 0.75, 3.75 and 14.0 mg/kg ginkgolide B, parameters of pharmacokinetics of ginkgolide B were: Tmax were all (0.083 +/- 0) h, Cmax were (422.312 +/- 14.203), (1608.467 +/- 226.677), (1987.036 +/- 237.202) microg/L, AUC0-1 were (533.833 +/- 114.943), (1786.029 +/- 137.066), (1943.44 +/- 415.892) microg x h/L. CONCLUSION: Ginkgolide B has three compartment model in rats.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Fibrinolíticos/farmacocinética , Ginkgo biloba/química , Ginkgolídeos/farmacocinética , Lactonas/farmacocinética , Animais , Área Sob a Curva , Feminino , Fibrinolíticos/administração & dosagem , Fibrinolíticos/sangue , Ginkgolídeos/administração & dosagem , Ginkgolídeos/sangue , Injeções Intravenosas , Lactonas/administração & dosagem , Lactonas/sangue , Masculino , Espectrometria de Massas , Fator de Ativação de Plaquetas/antagonistas & inibidores , Distribuição Aleatória , Ratos , Ratos Wistar , Fatores de TempoRESUMO
Two previously undescribed triterpenoids (1-2), along with thirteen known compounds (3-15) were isolated from a CHCl3-soluble extract of the leaves of Cyclocarya paliurus. Their structures were established on the basis of chemical and spectroscopic approaches. These compounds were assessed for their therapeutic effects on diabetic nephropathy (DN)-evoked fibrosis through High-Glucose and transforming growth factor-ß1 (TGF-ß1) challenged HK-2 cells. Among them, compounds 3, 5 and 8 could remarkedly decrease the level of fibronectin to relieve DN with 27.66 ± 2.77%, 6.09 ± 0.57% and 17.74 ± 5.83% inhibition rate at 10 µM, 10 µM and 1 µM, respectively.
Assuntos
Juglandaceae , Triterpenos , Juglandaceae/química , Extratos Vegetais/química , Folhas de Planta/química , Triterpenos/químicaRESUMO
OBJECTIVE: To develop a HPLC- ELSD method for determination the contents of geniposide, crocin and crocetin in different processing products of Fructus Gardeniae. METHODS: The separation was performed in the HyperClone ODS C18 column (250 mm x 4. 6 mm, 5 microm) with linear gradient elution using methanol-water and 0.05% phosphoric acid in water, the flowing rate was 0.8 mL/min, the column temperature was 30 degrees C, and the ELSD parameter was as follow: 70 degrees C as atomization temperature and 2.0 L/min as the gas flowing rate. RESULTS: The contents of geniposide and crocin in raw, yellowish, carbocoal and scorched Fructus Gardeniae decreased with the deepening of processing degree. However, the content of crocetin in carbocoal and scorched Fructus Gardeniae increased comparing with the raw one. CONCLUSION: This is a simple and credible quality control method, and can be used for the quality control and comprehensive evaluation for different processed products of Fructus Gardeniae.
Assuntos
Carotenoides/análise , Cromatografia Líquida de Alta Pressão/métodos , Gardenia/química , Iridoides/análise , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Frutas/química , Controle de Qualidade , Reprodutibilidade dos Testes , Tecnologia Farmacêutica/métodos , Vitamina A/análogos & derivadosRESUMO
A new decalin derivative, monascusic acid A (1), together with a new natural product (2), was isolated from the ethanol extract of red yeast rice. Their structures were elucidated by spectroscopic methods.
Assuntos
Produtos Biológicos/química , Medicina Tradicional Chinesa , Naftalenos/isolamento & purificação , Estrutura Molecular , Naftalenos/química , Ressonância Magnética Nuclear BiomolecularRESUMO
Six new cycloartane triterpenoid saponins, thalisides A-F (1-6), along with four known ones (7-10), were isolated from Thalictrum fortunei. The new structures were elucidated by using spectroscopic data (NMR, IR, UV, and MS). Compounds 1-10 were examined for their in vitro cytotoxicity against two human cancer cell lines (HepG2, A549) and antiviral activity against influenza A virus (H1N1) and found to be inactive.
Assuntos
Saponinas/química , Saponinas/farmacologia , Thalictrum/química , Triterpenos/química , Células A549 , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antivirais/química , Antivirais/isolamento & purificação , Antivirais/farmacologia , Células Hep G2 , Humanos , Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos , Saponinas/isolamento & purificaçãoRESUMO
A rapid and validated method using ultra high-performance liquid chromatography coupled with a triple quadrupole mass spectrometry (UHPLC-QQQ MS) was developed for simultaneous determination of four active steroidal saponins, i.e., dichotomin ( 1: ), pennogenin 3-O-α-l-arabinofuranosyl-(1â4)-[α-l-rhamnopyranosyl-(1â2)]-ß-d-glucopyranoside ( 2: ), pennogenin 3-O-α-l-rhamnopyranosyl-(1â2)-[α-l-rhamnopyranosyl-(1â4)-α-l-rhamnopyranosyl-(1â4)]-ß-d-glucopyranoside ( 3: ) and diosgenin 3-O-α-l-rhamnopyranosyl-(1â2)-[α-l-rhamnopyranosyl-(1â4)-α-l-rhamnopyranosyl-(1â4)]-ß-d-glucopyranosidein ( 4: ), in Ypsilandra thibetica Franch. The optimized sample preparation and UHPLC-QQQ MS conditions were chosen for quantitative analysis. The separation was performed on an Agilent Zorbax Eclipse Plus C18 column (2.1 mm × 50 mm, 1.8 µm) with gradient elution of acetonitrile-0.1% formic acid in water. All calibration curves showed good linear regression (r> 0.9985) within the test range. The limits of detection and quantification were in the range of 0.02-4.40 and 0.04-22.0 ng/mL, respectively. The proposed method was applied to analyze two batches of Y. thibetica samples for target compounds within 10 min. This work promoted the quality control method for raw material or preparations of Y. thibetica.
Assuntos
Técnicas de Química Analítica/métodos , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas , Melanthiaceae/química , Saponinas/análise , Limite de Detecção , TempoRESUMO
OBJECTIVE: To study the chemical constituents from rhizome of Pulsatilla dahurica. METHOD: The constituents were isolated and purified by various chromatographic methods. AR compounds were identified on the basis of spectral analysis and physico-chemical characters. RESULT: Six compounds were isolated from the 70% alcohol extract of the rhizome identified as hederagenin ( I ), hederagenin 3-O-alpha-L-arabinopyranoside (II), hederagenin 3-O-beta-D-glucopyranosyl(1-->2)-alpha-L-arabinopyranoside (III), hederagenin 3-O-beta-D-glucopyranosyl(1 -->2) [beta-D-glucopyranosyl(1-->4)]-alpha-L-arabinopyranoside (IV), beta-sitosterol (V) and daucosterol (VI), respectively. CONCLUSION: Compounds I approximately VI were isolated from this plant for the first time.
Assuntos
Ácido Oleanólico/análogos & derivados , Plantas Medicinais/química , Pulsatilla/química , Saponinas/isolamento & purificação , Ácido Oleanólico/química , Ácido Oleanólico/isolamento & purificação , Rizoma/química , Saponinas/química , Sitosteroides/química , Sitosteroides/isolamento & purificaçãoRESUMO
Four new cycloartane glycosides, 3-O-ß-D-xylopyranosyl-(1 â 6)-ß-D-glucopyranosyl-(1 â 4)-ß-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3ß,22,26-triol 26-O-(6-O-acetyl)-ß-D-glucopyranoside (1), 3-O-α-L-arabinopyranosyl-(1 â 6)-ß-D-glucopyranosyl-(1 â 4)-ß-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3ß,22,26-triol 26-O-(6-O-acetyl)-ß-D-glucopyranoside (2), 3-O-ß-D-glucopyranosyl (24S)-cycloartane-3ß,16ß,24,25,30-pentaol 25-O-ß-D-glucopyranosyl-(1 â 6)-ß-D-glucopyranoside (3) and 3-O-ß-D-glucopyranosyl (24S)-cycloartane-3ß,16ß,24,25,30-pentaol 25-O-ß-D-glucopyranosyl-(1 â 4)-ß-D-glucopyranoside (4), were isolated from the aerial parts of Thalictrum fortunei. Their structures were established on the basis of extensive NMR and HR-ESI-MS analyses, along with acid hydrolysis.
Assuntos
Glicosídeos/química , Componentes Aéreos da Planta/química , Thalictrum/química , Triterpenos/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
Four new cycloartane glycosides were isolated from the aerial parts of Thalictrum fortunei (Ranunculaceae). The chemical structures of these new glycosides were elucidated as 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3beta,22,26-triol 26-O-beta-D-glucopyranoside, 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3beta,22,26-triol 26-O-beta-D-quinovopyranosyl-(1-->6)-beta-D-glucopyranoside, 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3beta,22,26-triol 26-O-beta-D-xylopyranosyl-(1-->6)-beta-D-glucopyranoside, and 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3beta,22,26-triol 26-O-alpha-L-arabinopyranosyl-(1-->6)-beta-D-glucopyranoside by extensive NMR methods, HR-ESI-MS, and hydrolysis. This is the first report of (22S,24Z)-3beta,22,26-trihydroxycycloartan-24-ene (thelictogenin A, 5) being glycosylated at C-26.