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1.
J Ethnopharmacol ; 247: 112283, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31605736

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Bulbus Fritillaria cirrhosa D. Don (BFC) is a Chinese traditional herbal medicine that has long been used as an indispensable component in herbal prescriptions for bronchopulmonary diseases due to its well-established strong anti-inflammation and pulmonary harmonizing effects. Interestingly, there are few case reports in traditional Chinese medicine available where they found it to contribute in anti-tumor therapies. Imperialine is one of the most favored active substances extracted from BFC and has been widely recognized as an anti-inflammatory agent. AIM OF THE STUDY: The aim of the current work is to provide first-hand evidences both in vitro and in vivo showing that imperialine exerts anti-cancer effects against non-small cell lung cancer (NSCLC), and to explore the molecular mechanism of this anti-tumor activity. It is also necessary to examine its systemic toxicity, and to investigate how to develop strategies for feasible clinical translation of imperialine. MATERIALS AND METHODS: To investigate anti-NSCLC efficacy of imperialine using both in vitro and in vivo methods where A549 cell line were chosen as in vitro model NSCLC cells and A549 tumor-bearing mouse model was constructed for in vivo study. The detailed underlying anti-cancer mechanism has been systematically explored for the first time through a comprehensive set of molecular biology methods mainly including immunohistochemistry, western blot and enzyme-linked immunosorbent assays. The toxicity profile of imperialine treatments were evaluated using healthy nude mice by examining hemogram and histopathology. An imperialine-loaded liposomal drug delivery system was developed using thin film hydration method to evaluate target specific delivery. RESULTS: The results showed that imperialine could suppress both NSCLC tumor and associated inflammation through an inflammation-cancer feedback loop in which NF-κB activity was dramatically inhibited by imperialine. The NSCLC-targeting liposomal system was successfully developed for targeted drug delivery. The developed platform could favorably enhance imperialine cellular uptake and in vivo accumulation at tumor sites, thus improving overall anti-tumor effect. The toxicity assays revealed imperialine treatments did not significantly disturb blood cell counts in mice or exert any significant damage to the main organs. CONCLUSIONS: Imperialine exerts anti-cancer effects against NSCLC both in vitro and in vivo, and this previously unknown function is related to NF-κB centered inflammation-cancer feedback loop. Imperialine mediated anti-cancer activity is not through cytotoxicity and exhibit robust systemic safety. Furthermore, the liposome-based system we commenced would dramatically enhance therapeutic effects of imperialine while exhibiting extremely low side effects both on cellular and in NSCLC model. This work has identified imperialine as a promising novel anti-cancer compound and offered an efficient target-delivery solution that greatly facilitate practical use of imperialine.


Assuntos
Alcaloides/administração & dosagem , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Cevanas/administração & dosagem , Medicamentos de Ervas Chinesas/administração & dosagem , Fritillaria/química , Neoplasias Pulmonares/tratamento farmacológico , Células A549 , Alcaloides/efeitos adversos , Alcaloides/química , Alcaloides/isolamento & purificação , Animais , Contagem de Células Sanguíneas , Carcinoma Pulmonar de Células não Pequenas/imunologia , Carcinoma Pulmonar de Células não Pequenas/patologia , Cevanas/efeitos adversos , Cevanas/química , Cevanas/isolamento & purificação , Medicamentos de Ervas Chinesas/efeitos adversos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Retroalimentação Fisiológica/efeitos dos fármacos , Humanos , Lipossomos , Neoplasias Pulmonares/imunologia , Neoplasias Pulmonares/patologia , Masculino , Camundongos , NF-kappa B/antagonistas & inibidores , NF-kappa B/imunologia , Testes de Toxicidade , Ensaios Antitumorais Modelo de Xenoenxerto
2.
J Sep Sci ; 42(23): 3579-3588, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31617304

RESUMO

The quantification of three alkaloids is important because quantitative study is a means of assessing the reliability of the experimental method, and three alkaloids of peimine, peiminine, and peimisine are main active ingredients in Chinese Pharmacopoeia 2015. An effective method based on the matrix solid-phase dispersion microextraction was developed for the extraction of alkaloid compounds in Fritillariae Thunbergii Bulbus. Target analytes were analyzed by capillary electrophoresis coupled with quadrupole time-of-flight mass spectrometry. The optimized experimental condition was that 50 mg Fritillariae Thunbergii Bulbus was blended homogeneously with 10 mg citric acid for 5 min. Two hundred microliters of water acidized by 1 mol/L hydrochloric acid (pH = 4.5) was selected to elute tested alkaloids. The results demonstrated that the investigated method had low limits of detection (1.32-1.59 ng/mL), good recoveries (86.63-98.12%), and reproducibility (relative standard deviations of peak areas < 0.87%). The proposed matrix solid-phase dispersion microextraction coupled with capillary electrophoresis combined with quadrupole time-of-flight mass spectrometry was successfully applied for the extraction of alkaloids in plants.


Assuntos
Alcaloides/análise , Alcaloides/isolamento & purificação , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/isolamento & purificação , Eletroforese Capilar/métodos , Microextração em Fase Sólida/métodos , Espectrometria de Massas em Tandem/métodos , Cevanas/análise , Cevanas/isolamento & purificação , Limite de Detecção
3.
Phytochem Anal ; 30(4): 447-455, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30916852

RESUMO

INTRODUCTION: The Chinese medicine formulation, tumour-shrinking decoction (TSD, FM1523), which consists of 15 natural medicines, is used for uterine fibroids (UFs) therapy and possesses excellent clinical therapeutic effect. OBJECTIVE: To develop a sensitive and validated analytical method for the simultaneous quantification of four crucial bioactive compounds including isorhamnetin-3-O-neohesperidoside, curcumin, peimine and tetrahydropalmatine in the principal formulation of this decoction. METHODS: An ultra-performance liquid chromatography coupled tandem mass spectrometry (UPLC-MS/MS) with an electrospray ionisation (ESI) source in multiple reaction monitoring (MRM) mode was conducted to investigate these bioactive compounds in the TSD. The chromatographic separation was performed on a C18 column when the flow rate was adjusted at 0.2 mL/min with gradient elution of acetonitrile-water with 0.1% formic acid. Accelerated solvent extraction (ASE) method with higher extraction efficiency was employed for TSD sample pre-treatment. RESULTS: The linearity, limit of detection (LOD) and limit of quantification (LOQ) were determined for this analytical method. The mean recoveries of the compounds were determined between 100.23% and 104.02% with satisfactory relative standard deviation (RSD) in the ranges of 2.65% to 3.81%. The precision was evaluated by intra-day and inter-day tests, which revealed RSD within the ranges of 1.21% to 2.14% and 1.24% to 2.32%, respectively. CONCLUSION: The bioactive compounds of TSD samples were successfully quantified via UPLC-MS/MS with MRM mode. This study could help to evaluate the pharmacokinetic study of TSD during clinical applications and present a facile strategy for quantifying bioactive compounds in traditional Chinese Medicine decoction.


Assuntos
Alcaloides de Berberina/química , Cevanas/química , Medicamentos de Ervas Chinesas/química , Leiomioma/tratamento farmacológico , Compostos Fitoquímicos/química , Alcaloides de Berberina/isolamento & purificação , Cevanas/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Humanos , Limite de Detecção , Compostos Fitoquímicos/isolamento & purificação , Espectrometria de Massas em Tandem
4.
Phytomedicine ; 23(2): 95-104, 2016 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-26926170

RESUMO

BACKGROUND: The bulb of Fritillaria thunbergii has been utilised as mucoregulators and expectorants for controlling the airway inflammatory diseases in folk medicine. HYPOTHESIS/PURPOSE: We investigated whether verticine, ebeiedine and suchengbeisine isolated from the bulbs of Fritillaria thunbergii inhibit the gene expression and production of MUC5AC mucin from human airway epithelial cells. STUDY DESIGN: Confluent NCI-H292 cells were pretreated with verticine, ebeiedine or suchengbeisine for 30 min and then stimulated with EGF, PMA or TNF-α for 24h. The MUC5AC mucin gene expression was measured by RT-PCR. Production of MUC5AC mucin protein was measured by ELISA. RESULTS: (1) Verticine, ebeiedine or suchengbeisine inhibited the expression of MUC5AC mucin gene induced by EGF, PMA or TNF-α; (2) The production of MUC5AC mucin protein induced by EGF, PMA or TNF-α were also inhibited by treatment of verticine, ebeiedine or suchengbeisine. CONCLUSION: These results suggest that verticine, ebeiedine and suchengbeisine isolated from the bulbs of Fritillaria thunbergii inhibit the gene expression and production of MUC5AC mucin, by directly acting on airway epithelial cells, and the results are consistent with the traditional use of Fritillaria thunbergii as remedy for diverse inflammatory pulmonary diseases.


Assuntos
Alcaloides/química , Cevanas/química , Células Epiteliais/efeitos dos fármacos , Fritillaria/química , Mucina-5AC/metabolismo , Esteroides/química , Alcaloides/isolamento & purificação , Linhagem Celular Tumoral , Cevanas/isolamento & purificação , Fator de Crescimento Epidérmico/farmacologia , Células Epiteliais/metabolismo , Expressão Gênica/efeitos dos fármacos , Humanos , Estrutura Molecular , Mucina-5AC/genética , Extratos Vegetais/química , Raízes de Plantas/química , Esteroides/isolamento & purificação , Fator de Necrose Tumoral alfa/farmacologia
5.
Fitoterapia ; 103: 213-21, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25869849

RESUMO

The major biological active ingredients of Bulbus Fritillariae cirrhosae (BFC) are steroidal alkaloids, such as peimisine, imperialine-3ß-D-glucoside, and peimine. The bulbus of Fritillaria unibracteata var. wabuensis (FUW) was officially recorded in the National Pharmacopoeia of China (2010 edition) as one of the sources of BFC because of its positive therapeutic effects and few side effects. The endophytic fungus strain 6WBY3 was isolated from the fresh bulbus of FUW that had been cultivated for six years. Based on morphological methods and the phylogenetic analysis of internal transcribed spacer (ITS) sequences, this strain was identified as Fusarium redolens. Using color reaction analysis, high performance liquid chromatography with evaporative light scattering detection (HPLC-ELSD), and mass spectrometry (MS), it was demonstrated that F. redolens 6WBY3 could produce peimisine and imperialine-3ß-D-glucoside, similar to its host plant. The yields of peimisine and imperialine-3ß-D-glucoside were 16.0 µg·l(-1) and 18.8 µg·l(-1), respectively, in one week of culture. These results indicate that F. redolens 6WBY3 is a promising candidate for the large scale production of peimisine and imperialine-3ß-D-glucoside. In addition, the results from the strain 6WBY3 lay the foundation for further study into the mechanism of Fritillaria alkaloids biosynthesis in fungi.


Assuntos
Alcaloides/química , Fritillaria/microbiologia , Fusarium/química , Glucosídeos/química , Alcaloides/isolamento & purificação , Cevanas/química , Cevanas/isolamento & purificação , Endófitos/química , Endófitos/isolamento & purificação , Fusarium/classificação , Fusarium/isolamento & purificação , Glucosídeos/isolamento & purificação
6.
Zhong Yao Cai ; 38(10): 2105-8, 2015 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-27254925

RESUMO

OBJECTIVE: To establish an assay method for simultaneous determination of peimine, peiminine, peimissine and hupehenine and to make a comparative analysis of the content of four alkaloids in Fritillaria hupehensis and Fritillaria ebeiensis var. purpurea for the first time. METHODS: A Unitary C18 column(250 mm x 4.6 mm, 5 µm) was chosen with acetonitrile-water (containing 0.05% diethylamine) as mobile phase in a gradient program. The column temperature was 35 degrees C and the flow-rate was 1.0 mL/min. RESULTS: There was high content of peiminine and the content of peimissine was inferior to peiminine in Fritillaria hupehensis. Relatively speaking, peimine and hupehenine were much lower than the other two ingredients. Fritillaria ebeiensis var. purpurea also contained high levels of peiminine, the minimum content of peimine and equivalent content of peimissine comparing with Fritillaria hupehensis. In addition, it didn't contain hupehenine in Fritillaria ebeiensis var. purpurea. CONCLUSION: This method is simple and fast, and it has good separation, reproducibility and reliable results. Also, it can be used as basis for the quality evaluation of Fritillaria hupehensis and Fritillaria ebeiensis var. purpurea.


Assuntos
Alcaloides/isolamento & purificação , Cevanas/isolamento & purificação , Fritillaria/química , Reprodutibilidade dos Testes , Fritillaria/classificação , Plantas Medicinais/química
7.
Phytomedicine ; 21(8-9): 1104-9, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24854573

RESUMO

Steroidal alkaloids, as the major biologically active components in Bulbus Fritillariae, possess a variety of toxicological and pharmacological effects on humans. The objective of this work was to determine whether endophytic fungi isolated from fresh bulbs of Fritillaria unibracteata var. wabensis can produce one or more alkaloids like its host plant. Four classical reagents including Wagner's, iodine-potassium iodide, Mayer's and improved Dragendorff's were used for primary screening. Then thin-layer chromatography (TLC) and high performance liquid chromatography-evaporative light scattering detection (HPLC-ELSD) were employed to identify the fermentation products of the selected strains. The results showed that extract from one stain (WBS007) has positive reactions in process of primary screening. A further TLC scan and HPLC-ELSD showed that strain WBS007 had two components with the same TLC relative front (Rf) value and HPLC retention time (RT) as authentic peimisine and peiminine. In addition, strain WBS007 was identified as Fusarium sp. based on phylogenetic analysis of ITS sequences. Thus, strain WBS007 produced the bioactive ingredient peimisine and peiminine, as does its host plant, and could be used for the production of peimisine and peiminine by fermentation.


Assuntos
Alcaloides/farmacologia , Cevanas/farmacologia , Fritillaria/microbiologia , Fusarium/química , Alcaloides/química , Alcaloides/isolamento & purificação , Cevanas/química , Cevanas/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Delgada , Análise por Conglomerados , Fusarium/genética , Fusarium/isolamento & purificação
8.
J Nat Med ; 67(3): 647-51, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22886818

RESUMO

A novel steroidal alkaloid, suchengbeisine (1), along with two known steroidal alkaloids, N-oxide of verticinone (2) and zhebeininoside (3), were isolated from the bulbs of Fritillaria shuchengensis S. C. Chen et S. F. Yin. The structures of these compounds were elucidated by intensive spectroscopic methods, including NMR, IR, CD and MS.


Assuntos
Alcaloides/isolamento & purificação , Fritillaria/química , Fitosteróis/isolamento & purificação , Esteroides/isolamento & purificação , Alcaloides/química , Alcaloides/farmacologia , Células CACO-2 , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cevanas/isolamento & purificação , Relação Dose-Resposta a Droga , Células HeLa , Células Hep G2 , Humanos , Concentração Inibidora 50 , Células MCF-7 , Estrutura Molecular , Fitosteróis/química , Fitosteróis/farmacologia , Raízes de Plantas/química , Plantas Medicinais , Esteroides/química , Esteroides/farmacologia
9.
Yao Xue Xue Bao ; 48(12): 1836-43, 2013 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-24689243

RESUMO

To study the in situ intestinal absorption kinetics and compatibility influence of peimine and peiminine in rats, the absorption of peimine and peiminine in small intestine (duodenum, jejunum and ileum) and colon of rats was investigated using in situ single-pass perfusion method and the drug content was measured by HPLC-ELSD. Perfusion rate, pH, concentration of drug, gender and bile duct ligation can significantly affect the absorption of peimine and peiminine, the Ka, and Papp values in the condition of pH 6.8 and pH 7.4 had significant difference (P<0.01), as drug concentration irlcreased, the absorption parameters of peimine and peiminine decreased, Ka and Papp between low concentrations and middle concentrations was significant difference (P<0.01). Verapamil can not affect Ka and Papp of peimine and peiminine which are in the extract (P> 0.05). Bitter almonds and licorice can significantly reduce the absorption of peimine and peiminine with the usual dose (P<0.01), extracted separately and together had no significant difference on Ka and Papp (P> 0.05). Experimental results show that the absorption features of peimine and peiminine are basically the same, both of them could be absorbed at all segments of the intestine in rats and had no special absorption window, and with significant differences between male and female individuals. The absorption of peimine and peiminine complies with the active transport and facilitated diffusion in the general intestinal segments. Bitter almond and licorice can reduce the intestinal absorption rate ofpeimine and peiminine.


Assuntos
Cevanas/farmacocinética , Fritillaria/química , Absorção Intestinal , Animais , Cevanas/administração & dosagem , Cevanas/isolamento & purificação , Colo/metabolismo , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Feminino , Glycyrrhiza/química , Ácido Glicirrízico/isolamento & purificação , Ácido Glicirrízico/farmacologia , Absorção Intestinal/efeitos dos fármacos , Intestino Delgado/metabolismo , Masculino , Perfusão , Raízes de Plantas/química , Plantas Medicinais/química , Prunus dulcis/química , Ratos , Ratos Sprague-Dawley , Fatores Sexuais
10.
Electrophoresis ; 33(14): 2152-8, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22821492

RESUMO

A simple and inexpensive CE method was developed for the determination of peimine and peiminine. Because of the lack of an UV chromophore of peimine and peiminine, the detection method chosen was indirect UV detection, with N-(1-naphthyl)ethylenediamine dihydrochloride (NED) as the UV absorbing probe. It was thought that NED, a chromophoric ion, may form hydrogen bonding pairs with the analytes to cause significant changes in separation selectivity. Additionally, the hydrophobic interactions between analytes and the probe also play a crucial role in achieving a resolution between the two analytes. The analyses were carried out with a background electrolyte composed of 66% MeOH-ACN (1:1, v/v), 34% aqueous buffer containing 15 mM NaH2PO4, 2.5 mM NED, 4 mM H3PO4. MeOH-ACN mixtures used as organic modifiers can not only reduce the adsorption of NED to the capillary wall, but also decrease the baseline noise and drift. The method provided a linear response ranging from 5 to 200 µg/mL. The limits of detection (LODs) for peimine and peiminine were 3.9 and 4.1 µg/mL, respectively. The repeatabilities (n = 3) reached relative standard deviation values (RSDs) of 3.4 and 4.1% for the peak areas, 4.0 and 4.4% for the peak heights, and 0.29 and 0.30% for the migration time of peimine and peiminine, respectively. Regression equations revealed linear relationships (r = 0.9995-0.9996) between the peak area of each analyte and the concentration. The method developed was successfully applied to quantify peimine and peiminine in chloroform extracts of the ground Bulbus Fritillariae Thunbergii.


Assuntos
Cevanas/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Eletroforese Capilar/métodos , Etilenodiaminas/química , Fritillaria/química , Limite de Detecção , Raízes de Plantas/química , Raios Ultravioleta
11.
Chem Biodivers ; 5(2): 259-66, 2008 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-18293439

RESUMO

Phytochemical investigation of the bulbs of Fritillaria hupehensis resulted in the isolation and structural elucidation of four new steroidal penta- and hexacyclic veratraman- and cevan-based alkaloids, respectively, compounds 1-4. They were obtained together with the known constituents ebeinine (5) and zhebeinine (6), which were isolated for the first time from this plant. The structures of the new isolates were established by spectroscopic and mass-spectrometric analyses, in combination with chemical methods. All compounds were assayed for their cytotoxic effects towards HeLa and HepG2 cell lines. Compounds 1 and 2 showed significant inhibitory effects against both types of tumor cells, with IC(50) values in the range 2.52-0.23 microM, similar as those for 5-fluorouracil used as positive control.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Fritillaria/química , Tubérculos/química , Alcaloides/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cevanas/química , Cevanas/isolamento & purificação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HeLa , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética/métodos , Espectroscopia de Ressonância Magnética/normas , Conformação Molecular , Padrões de Referência , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrofotometria Infravermelho/métodos , Estereoisomerismo , Relação Estrutura-Atividade
12.
Z Naturforsch C J Biosci ; 63(11-12): 789-93, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-19227824

RESUMO

Ten strains of endophytic fungi were isolated from the bulbs of the traditional Chinese medicinal plant Fritillaria ussuriensis. The extract from one of them, Fu7, showed a positive reaction with Dragendorff's reagent and the same Rf value in thin-layer chromatography (TLC) analysis as authentic sipeimine. A further TLC scan and high-performance liquid chromatography-evaporative light-scattering detection (HPLC-ELSD) showed that one ingredient of the extract of strain Fu7 had a similar absorption curve in the range 200-700 nm and the same retention time as authentic sipeimine. Thus, the fungus produces the bioactive ingredient sipeimine, as does its host plant, and could be used for the production of sipeimine by fermentation.


Assuntos
Cevanas/isolamento & purificação , Cevanas/metabolismo , Fritillaria/metabolismo , China , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Delgada , Medicamentos de Ervas Chinesas/isolamento & purificação , Filtração , Fritillaria/química , Fritillaria/crescimento & desenvolvimento , Raízes de Plantas/química
13.
Zhongguo Zhong Yao Za Zhi ; 32(16): 1609-14, 2007 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-18027648

RESUMO

In this review, we described the taxonomic study of the Fritillaria medicinal plant in the recent years. The taxonomic study of the Fritillaria medicinal plant was carried out from three main aspects: the traditional morphological character, the characteristic constituents of the plant and genotyping and species identification of Fritillaria by DNA chips. By comparison, we concluded that the DNA chip technology can provide a rapid, high throughput for genotyping and quality assurance of the plant species verification. It is the most prosperous method of species identification of the plant.


Assuntos
Fritillaria/classificação , Plantas Medicinais/classificação , Cevanas/isolamento & purificação , Flores/anatomia & histologia , Flores/química , Flores/genética , Fritillaria/anatomia & histologia , Fritillaria/genética , Genótipo , Análise de Sequência com Séries de Oligonucleotídeos , Folhas de Planta/anatomia & histologia , Folhas de Planta/química , Folhas de Planta/genética , Plantas Medicinais/anatomia & histologia , Plantas Medicinais/genética
14.
Yao Xue Xue Bao ; 42(3): 274-8, 2007 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-17520826

RESUMO

To search for potential drugs with potent antitussive, expectorant, antiasthmatic activities and low toxicity, a series of verticinone-bile acids salts were prepared based on the clearly elucidated antitussive, expectorant and antiasthmatic activities of verticinone in bulbs of Fritillaria and different bile acids in Snake Bile. The antitussive, expectorant and antiasthmatic activities of these verticinone-bile acid salts were then screened with different animal models. Ver-CA (verticinone-cholic acid salt) and Ver-CDCA (verticinone-chenodeoxycholic acid salt) showed much more potent activities than other compounds. The bioactivities of Ver-CA and Ver-CDCA are worthy to be intensively studied, and it is also deserved to pay much attention to their much more potent antitussive effects than codeine phosphate. In order to elucidate whether they have synergistic effect and attenuated toxicity, their activities will be continuously compared with single verticinone, cholic acid and chenodeoxycholic acid at the same doses on different animal models. The application of "combination principles" in traditional Chinese medicinal formulations may be a novel way in triditional Chinese medicine research and discovery.


Assuntos
Antiasmáticos/farmacologia , Antitussígenos/farmacologia , Ácidos e Sais Biliares/farmacologia , Cevanas/farmacologia , Expectorantes/farmacologia , Animais , Antiasmáticos/química , Antitussígenos/química , Asma/prevenção & controle , Ácidos e Sais Biliares/química , Cevanas/química , Cevanas/isolamento & purificação , Ácido Quenodesoxicólico/química , Ácido Quenodesoxicólico/farmacologia , Ácido Cólico/química , Ácido Cólico/farmacologia , Tosse/prevenção & controle , Combinação de Medicamentos , Composição de Medicamentos/métodos , Sinergismo Farmacológico , Expectorantes/química , Feminino , Fritillaria/química , Cobaias , Masculino , Camundongos , Plantas Medicinais/química , Distribuição Aleatória , Serpentes
15.
Planta Med ; 72(9): 814-8, 2006 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-16881015

RESUMO

18 alkaloids were successfully isolated from five Fritillaria species and 5 derivatives were synthesized. Their effects on the bioactivity of human whole blood cholinesterase (ChE) were assessed. The results showed that N-demethylpuqietinone, hupeheninoside, ebeiedinone, yibeinoside A and chuanbeinone inhibited the bioactivity of human whole blood ChE at the concentration of 1.0 x 10 ( - 4) M, with the inhibitory effects of 55.5 +/- 2.7 %, 66.8 +/- 2.0 %, 69.0 +/- 1.7 %, 71.2 +/- 1.8 % and 70.7 +/- 3.3 %, respectively. The effects of the five alkaloids on human red blood cell (RBC) acetylcholinesterase (AChE) and human plasma butyrylcholinesterase (BChE) were further studied, and their IC (50) values for human RBC AChE were 6.4 +/- 0.003 microM, 16.9 +/- 0.018 microM, 5.7 +/- 0.004 microM, 6.5 +/- 0.013 microM and 7.7 +/- 0.001 microM, respectively, and the IC50 values for human plasma BChE were 12.5 +/- 0.026 microM, 2.1 +/- 0.005 microM, 5.2 +/- 0.002 microM, 7.3 +/- 0.005 microM and 0.7 +/- 0.001 microM, respectively. These data suggest, therefore, that N-demethylpuqietinone, hupeheninoside, ebeiedinone, yibeinoside A and chuanbeinone have both anti-RBC AChE and anti-plasma BChE activities, N-demethylpuqietinone is a selective inhibitor of AChE, whereas hupeheninoside and chuanbeinone are the selective inhibitors of BChE.


Assuntos
Alcaloides/farmacologia , Inibidores da Colinesterase/farmacologia , Fritillaria/química , Esteroides/farmacologia , Alcaloides/química , Células Sanguíneas/metabolismo , Cevanas/química , Cevanas/isolamento & purificação , Cevanas/farmacologia , Inibidores da Colinesterase/química , Glucosídeos/química , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Humanos , Esteroides/química
16.
Yao Xue Xue Bao ; 39(5): 348-50, 2004 May.
Artigo em Chinês | MEDLINE | ID: mdl-15338876

RESUMO

AIM: To investigate the chemical constituents of the bulbs of Fritillaria wabuensia. METHODS: Chromatography techniques were used to isolate the chemical constituents. EI-MS, 1HNMR, 13 CNMR and DEPT were used to determine the structures of the isolated constituents. RESULTS: Three alkaloids were isolated from the bulbs of Fritillaria wabuensia, and were identified as imperialine (I), imperialine-beta-N-oxside (II), isoverticine-beta-N-oxide (III). CONCLUSION: Isoverticine-beta-N-oxide was isolated from the bulbs of Fritillaria wabuensia for the first time. Isoverticine-beta-N-oxide is a new alkaloid.


Assuntos
Óxidos N-Cíclicos/isolamento & purificação , Fritillaria/química , Plantas Medicinais/química , Triterpenos/isolamento & purificação , Cevanas/química , Cevanas/isolamento & purificação , Óxidos N-Cíclicos/química , Estrutura Molecular , Triterpenos/química
17.
Nat Prod Res ; 18(3): 205-9, 2004 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-15143828

RESUMO

The structure of a new crystalline base (melting point (mp) 167-169 degrees C) obtained from Fritillaria imperialis was elucidated as (20R, 25R)-5alpha,17beta-cevanine-3beta,6beta-diol, X-ray diffraction analysis of the mono-hydrate. The base was found to be identical with persicanidine B and also with harepermine.


Assuntos
Cevanas/química , Cevanas/isolamento & purificação , Fritillaria/química , Cristalização , Difração de Raios X
18.
Zhongguo Zhong Yao Za Zhi ; 29(4): 331-4, 2004 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-15706870

RESUMO

OBJECTIVE: To study the chemical constituents of hybridized Bulbus Fritillariae Ussuriensis. METHOD: The chemical constituents were isolated by silica column chromatography and their structures were identified by physical and chemical eveidences and spectral analysis (IR, 1H-NMR, 13C-NMR, 2D-NMR, MS). RESULT: Seven compounds were obtained and identified as (20S,25S)5alpha, 14alpha, 17beta-cevanine-6beta-hydroxy-3-one (hupehenirine, ZF1), (20S,25S)5alpha, 14alpha, 17beta-cevanine-3beta-hydroxy-6-one (hupehenizine, ZF2), (20R,25S)5alpha, 14alpha-cevanine-3beta,20beta-dihydroxy-6-one (peiminine, verticinone, ZF3), (20S,25S)5alpha, 14alpha, 17beta-cevanine-3beta, 6beta-dihydroxy (hupehenine, ZF4), (20R,25S)5alpha, 14alpha-cevanine-3beta, 6beta, 20beta-trihydroxy (isoverticine, ZF5), (20R,25S)5alpha, 14alpha-cevanine-3beta, 6alpha, 20beta-trihydroxy (peimine, verticine, ZF6), (20S,25S)5alpha, 14alpha, 17beta-evanine-6beta-hydroxy-3beta-O-beta-D-glucoside (hupeheninoside, ZF7). CONCLUSION: Compounds ZF1-7 were isolated from hybridized Bulbus Fritillariae Ussuriensis for the first time.


Assuntos
Cevanas/isolamento & purificação , Fritillaria/química , Glucosídeos/isolamento & purificação , Plantas Medicinais/química , Cevanas/química , Fritillaria/classificação , Fritillaria/genética , Glucosídeos/química , Hibridização Genética , Estrutura Molecular , Raízes de Plantas/química , Plantas Medicinais/classificação , Plantas Medicinais/genética
19.
Phytochem Anal ; 13(3): 158-61, 2002.
Artigo em Inglês | MEDLINE | ID: mdl-12099106

RESUMO

The extraction procedure and quantitative determination by HPLC-evaporative light scattering detection (ELSD) of the main bioactive components, namely, imperialine (1) and imperialine-3 beta-glucoside (2), of bulbs of Fritillaria pallidiflora Schrenk have been investigated. The most efficient method for the simultaneous extraction of 1 and 2 involved pre-treatment of the bulb powder with ammonia, followed by reflux with dichloromethane:methanol at 90 degrees C for 4 h. Simultaneous determination of non-chromophoric 1 and 2 by HPLC-ELSD employed a Kromasil C18 column eluted with acetonitrile:water:diethylamine. The assay was accurate and reproducible with an overall variation lower than 4% and a sample recovery higher than 98%. The methods described have been successfully used to evaluate the quality of three batches of the crude traditional Chinese medicinal herb derived from the bulbs of F. pallidiflora.


Assuntos
Alcaloides/isolamento & purificação , Cevanas/isolamento & purificação , Fritillaria/química , Glucosídeos/isolamento & purificação , Alcaloides/química , Cevanas/química , Cromatografia Líquida de Alta Pressão , Glucosídeos/química , Luz , Estruturas Vegetais/química , Espalhamento de Radiação
20.
Planta Med ; 64(2): 172-4, 1998 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-9525109

RESUMO

In order to check the structure-activity relationship and prepare more potent derivatives of imperialine with anticholinergic activity, imperialinol (2), 3 beta-acetoxyimperialine (3), 3 beta-propionoxyimperialine (4), and 3 beta-butyroxyimperialine (5) were prepared. Compounds 4 and 5 displayed better anticholinergic activity against muscarinic receptors of the heart and brain than imperialine (1). The decrease in activity in 2 showed the importance of the 6-keto functionality in imparting the anticholinergic activity.


Assuntos
Alcaloides/química , Cevanas/química , Antagonistas Colinérgicos/química , Coração/fisiologia , Hipocampo/fisiologia , Plantas Medicinais , Receptores Muscarínicos/efeitos dos fármacos , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Animais , Cevanas/isolamento & purificação , Cevanas/farmacologia , Antagonistas Colinérgicos/isolamento & purificação , Antagonistas Colinérgicos/farmacologia , Cobaias , Coração/efeitos dos fármacos , Átrios do Coração , Hipocampo/efeitos dos fármacos , Técnicas In Vitro , Estrutura Molecular , Receptores Muscarínicos/fisiologia , Relação Estrutura-Atividade
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