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1.
Phytochemistry ; 169: 112178, 2019 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-31669819

RESUMO

In the present work, we take advantage of the characteristic NMR signal (δC-10 = 96.0-99.9) for guiding the isolation of schinortriterpenoids (SNTs) from n-butanol fraction of stems of Kadsura heteroclita which is a Tujia ethnomedicine with trivial name "Xuetong". This effort resulted in the identification of three unreported 3,4:9,10-disecocycloartane triterpenoids xuetongdilactones A-C and three undescribed SNTs xuetongdilactones D-F, along with two known SNTs, namely, wuweizidilactone B and micrandilactone B. The structures of the unreported compounds were established based on 1D, and 2D NMR, HRESIMS, and ECD spectroscopic data analysis. The absolute stereochemistry of xuetongdilactone A was determined by X-ray diffraction analysis along with ECD calculation. The antioxidant and cytotoxic activities were evaluated for all the isolated compounds.

2.
Fitoterapia ; 138: 104276, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31351128

RESUMO

Binglang, the fruit of Areca catechu L, has a long history as an important Chinese herbal medicine. Two new alkaloids (1 and 2), along with forty-one known compounds (3-43) were isolated from the dried fruit of Areca catechu L. The structures were elucidated on basis of the IR, UV, MS and 1D, 2D NMR spectroscopic data. Compounds 26 and 33 showed weak cytotoxicity against human gastric cancer cell line (BGC-823) with IC50 of 15.91 µM and 20.13 µM, respectively.

3.
Molecules ; 24(9)2019 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-31035334

RESUMO

As part of our continual efforts to exploit 'Tujia Ethnomedicine' for their pharmacophoric functionalities, we herein investigated Kadsura heteroclita collected from a deep Wulin mountain area in northern Hunan province. The current study resulted in the isolation of three new sesquiterpenes: 6α,9α,15-trihydroxycadinan-4-en-3-one (1), (+)-3,11,12-trihydroxycalamenene (2), (-)-3,10,11,12-tetrahydroxy-calamenene (3), along with four known sesquiterpenes (4-7), and a cytochalasin H (8). Their chemical structures were elucidated by 1D-, and 2D-NMR spectroscopy, and HRESI-MS, CD spectrometry. The antioxidant, and cytotoxic activities of the compounds were evaluated. Compound 8 exhibited a strong antioxidant effect with an IC50 value of 3.67 µM on isolated human polymorphonuclear cells or neutrophils.


Assuntos
Kadsura/química , Extratos Vegetais/química , Caules de Planta/química , Sesquiterpenos/química , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Estrutura Molecular , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia
4.
J AOAC Int ; 102(4): 1102-1111, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-30616712

RESUMO

Background: QishenYiqi dripping pills (QSYQ), consisting of Salvia miltiorrhiza, Astragalus membranaceus, Panax notoginseng, and Dalbergia odorifera, is a widely used to treat ischemic cerebrovascular and hemorrhagic cerebrovascular in China. Objective: In this study, a rapid and sensitive ultra-HPLC coupled with a triple quadrupole MS (UHPLC-QQQ-MS) method was established for the simultaneous quantification of 19 bioactive components. Methods: Chromatographic separation was performed on an Agilent Eclipse Plus C18 Rapid Resolution High Definition (RRHD) column (2.1 × 50 mm, 1.8 µm) with a mobile phase composed of a 0.1% (v/v) formic acid aqueous solution and acetonitrile in a gradient elution manner. A QQQ-MS was used in positive and negative ionization mode with multiple reactions monitoring for quantitative analysis. Results: The established methods were validated with linearity, precision, repeatability, stability, recovery, and matrix effect. All calibration curves exhibited excellent linear relationship with the correlation coefficient (r) >0.9985 for each analyte within the test range. This method was successfully applied to quantify target compounds of different structural types in 12 batches of QSYQ. Conclusions: The results suggest that the established method is rapid, sensitive, and reliable. The developed UHPLC-QQQ-MS method can provide scientific basis and reference to quality control and consistency evaluation of QSYQ sample and other formulations. Highlights: A rapid, sensitive, and reliable UHPLC-QQQ-MS method has been developed and validated for simultaneous determination of 19 compounds including phenolic acids, saponins, isoflavonoids, and tanshinones in QSYQ for the first time.

5.
Nat Prod Res ; : 1-8, 2018 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-30582363

RESUMO

Twenty-four compounds were isolated from the roots of Polygonatum cyrtonema Hua, including a new octopamine dimer, named trans-bis(N-feruloyl)octopamine (1). The structure was established on the basis of spectroscopic and chemical methods. All the extracts and compounds were evaluated for cytotoxic and antioxidant activities by using MTT and chemiluminescence assay. The extracts showed activity against MCF-7 and HepG-2 cell lines from IC50 0.30 to 1.01 mg mL-1. Compound 3 exhibited activity against HepG-2 cell lines with IC50 8.99 µM. Compound 7 exhibited activity against Hela cell lines with IC50 2.53 µM and BGC-823 cell lines with IC50 7.77 µM. Moreover, compound 7 showed antioxidant with IC50 12 µM compared to the positive control with IC50 77 µM. Compound 16 exhibited activity against HepG-2 cell lines with IC50 1.05 µM and MCF-7 cell lines with IC50 1.89 µM. These results indicated that this plant might be potential in natural medicine and healthy food.

6.
Anal Bioanal Chem ; 2018 Jun 22.
Artigo em Inglês | MEDLINE | ID: mdl-29934853

RESUMO

As an essential phosphate group hydrolase, alkaline phosphatase (ALP), whose level in serum is correlated with bone disease, liver dysfunction, and cancer, could be used as a biomarker for clinical diagnosis and biomedical studies. Hence, developing a convenient and sensitive method for ALP assay has importance in disease diagnosis, drug treatment, and prognosis assessment. In this work, using a hairpin DNA strand as the substrate, we developed an ultrasensitive and simple fluorescence method for quantitative ALP assay based on the binding difference of reduced graphene oxide (rGO) with different DNA strands coupled with λ exonuclease (λ exo) cleavage. Under the optimal conditions, the limit of detection (LOD) of ALP is estimated to be 0.01 U/L with the linear region from 0.5 U/L to 70 U/L. Furthermore, the proposed assay was used to detect ALP in complicated cell-free extracts and evaluate the inhibitory effects of two well-known inhibitors of ALP activity. Finally, the method was used to investigate the effect of natural compounds on ALP activity and five compounds with different inhibitory capability were screened. In summary, we propose that the new method for ALP assay can be applied for therapeutic drug monitoring (TDM) and high-throughput compound screening in combination with multiwell plate technology.

7.
Fitoterapia ; 121: 170-174, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28754541

RESUMO

Four new benzophenone glycosides named as aquilaside A-D (1-4) along with five known compounds (5-9) were isolated from the methanol extract of the flower buds of Aquilaria sinensis. Their structures were elucidated on the basis of 1D and 2D NMR and mass spectroscopic analyses. All purified compounds were evaluated for their anti-inflammatory and cytotoxic activities. Aquilasides B and C displayed moderate cytotoxicity against SK-MEL cells with IC50 of 17.0 and 12.0µM and weak NF-κB inhibitive activity at 100µM with 30% and 60%, respectively.


Assuntos
Benzofenonas/química , Flores/química , Glicosídeos/química , Thymelaeaceae/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Benzofenonas/isolamento & purificação , Linhagem Celular Tumoral , Glicosídeos/isolamento & purificação , Humanos , Camundongos , Estrutura Molecular , NF-kappa B/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Células RAW 264.7
8.
J Microbiol Biotechnol ; 27(8): 1409-1418, 2017 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-28621110

RESUMO

Two typical microbial communities from Chinese rice wine fermentation collected in Yichang city and Suzhou city in China were investigated. Both communities could ferment glutinous rice to rice wine in 2 days. The sugar and ethanol contents were 198.67 and 14.47 mg/g, respectively, for rice wine from Yichang city, and 292.50 and 12.31 mg/g, respectively, for rice wine from Suzhou city. Acetic acid and lactic acid were the most abundant organic acids. Abundant fungi and bacteria were detected in both communities by high-throughput sequencing. Saccharomycopsis fibuligera and Rhizopus oryzae were the dominant fungi in rice wine from Suzhou city, compared with R. oryzae, Wickerhamomyces anomalus, Saccharomyces cerevisiae, Mucor indicus, and Rhizopus microsporus in rice wine from Yichang city. Bacterial diversity was greater than fungal diversity in both communities. Citrobacter was the most abundant genus. Furthermore, Exiguobacterium, Aeromonas, Acinetobacter, Pseudomonas, Enterobacter, Bacillus, and Lactococcus were highly abundant in both communities.


Assuntos
Bactérias/classificação , Bactérias/isolamento & purificação , Biota , Fungos/classificação , Fungos/isolamento & purificação , Vinho/microbiologia , Ácidos Carboxílicos/análise , China , Cidades , Etanol/análise , Fermentação , Oryza , Açúcares/análise , Vinho/análise
9.
Nat Prod Res ; 31(15): 1725-1732, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28278632

RESUMO

The present study investigated the chemical constituents of aerial part of Polygonum pubescens Blume. Twenty-two compounds 1-22 were obtained from petroleum ether and ethyl acetate extracts of aerial part of P. pubescens, including a new phenylpropanoide esters 1 and 21 known compounds. The structures were determined on the basis of spectroscopic and chemical methods. Sixteen compounds were assessed for their cytotoxic and anti-inflammatory activities. Several compounds showed effects on different targets.


Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Extratos Vegetais/química , Polygonum/química , Animais , Anti-Inflamatórios/química , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Cinamatos/química , Cinamatos/isolamento & purificação , Cinamatos/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Humanos , Estrutura Molecular , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia
10.
Nat Prod Res ; 31(19): 2211-2217, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28287272

RESUMO

Two new sesquiterpene lactone glycosides, namely melitensin 15-O-ß-D-glucoside (1) and 11ß,13-dihydrosalonitenolide 15-O-ß-D-glucoside (2), along with eight known compounds (3-10) were isolated from the aerial part of Cnicus benedictus L. Their structures were elucidated from analyses of extensive spectroscopic data. Compounds 1-6 all possessed an α-methyl-γ-lactone moiety. Moreover, compound 5 exhibited moderate activity against the growth of Aspergillus fumigatus, with IC50 values of 17.67 µg mL-1.


Assuntos
Cnicus/química , Glicosídeos/isolamento & purificação , Sesquiterpenos/isolamento & purificação , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Aspergillus fumigatus/efeitos dos fármacos , Centaurea , Glicosídeos/química , Concentração Inibidora 50 , Lactonas/química , Lactonas/isolamento & purificação , Estrutura Molecular , Sesquiterpenos/química
11.
Nat Prod Res ; 31(17): 2053-2057, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28000515

RESUMO

Fourteen compounds including vanicoside B (1), vanicoside F (2), vanicoside E (3) and 5,6-dehydrokawain (4), aniba-dimer-A (5), 6,6'-((1α,2α,3ß,4ß)-2,4-diphenylcyclobutane-1,3-diyl)bis(4-methoxy-2H-pyran-2-one) (6), (+)-ketopinoresinol (7), isorhamnetin (8), 3,7-dihydroxy-5,6-dimethoxy-flavone (9), isalpinin (10), cardamomin (11), pinosylvin (12), 2-desoxy-4-epi-pulchellin (13) and ß-sitosterol (14) were isolated from dichloromethane-soluble portion of Polygonum hydropiper. By using Alamar blue assay, compounds 2, 7, 8, 11 and 12 were found to be active against Trypanosoma brucei with IC50 values in the range of 0.49-7.77 µg/mL. Cardamomin (11) had most significant activity against T. brucei with IC50/IC90 values of 0.49/0.81 µg/mL compared to the positive control DFMO (IC50/IC90: 3.02/8.05 µg/mL). Furthermore, in antimalarial, antimicrobial, anti-inflammatory, PPAR and cytotoxic assays, some compounds have demonstrated moderate inhibitory potentials.


Assuntos
Anti-Infecciosos/farmacologia , Antimaláricos/farmacologia , Polygonum/química , Tripanossomicidas/farmacologia , Trypanosoma brucei brucei/efeitos dos fármacos , Anti-Infecciosos/química , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Antimaláricos/química , Chalconas/farmacologia , Cinamatos/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Testes de Sensibilidade Microbiana , Estrutura Molecular , PPAR gama/genética , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Sitosteroides/farmacologia , Tripanossomicidas/química
12.
Sci Rep ; 6: 28611, 2016 06 23.
Artigo em Inglês | MEDLINE | ID: mdl-27334428

RESUMO

EGFR is a potential therapeutic target for treating bladder cancer, but has not been approved for clinical use yet. Metformin is a widely used antidiabetic drug and has demonstrated interesting anticancer effects on various cancer models, alone or in combination with chemotherapeutic drugs. The efficacy of gefitinib, a well-known EGFR tyrosine kinase inhibitor, combined with metformin was assessed on bladder cancer and underlying mechanisms were explored. This drug combination induced a strong anti-proliferative and anti-colony forming effect and apoptosis in bladder cancer cell lines. Gefitinib suppressed EGFR signaling and inhibited phosphorylation of ERK and Akt. Metformin amplified this inhibitory effect and enhanced gefitinib-induced activation of AMPK signaling pathway. In vivo intravesical treatment of metformin and gefitinib on syngeneic orthotopic mice confirmed the significant inhibitory effect on bladder tumor growth. These two drugs may be an excellent combination for the treatment of bladder cancer through intravesical instillation.


Assuntos
Proliferação de Células/efeitos dos fármacos , Receptores ErbB/metabolismo , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Metformina/farmacologia , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Quinazolinas/farmacologia , Neoplasias da Bexiga Urinária/tratamento farmacológico , Administração Intravesical , Animais , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Feminino , Gefitinibe , Humanos , Camundongos , Camundongos Endogâmicos C57BL , Fosforilação/efeitos dos fármacos , Inibidores de Proteínas Quinases/farmacologia , Transdução de Sinais/efeitos dos fármacos , Neoplasias da Bexiga Urinária/metabolismo
13.
J Asian Nat Prod Res ; 17(3): 232-8, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25379867

RESUMO

Investigation on the EtOAc extract of the bark of Zanthoxylum simulans led to the isolation of four new lignans including zanthoxylumin A (1), zanthoxylumin B (2), ( - )-magnolin (3), and ( - )-pinoresinol-di-3,3-dimethylallyl ether (4). Their structures were established by comprehensive analysis of the spectral data, especially 1D and 2D NMR spectra.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Lignanas/isolamento & purificação , Zanthoxylum/química , Medicamentos de Ervas Chinesas/química , Lignanas/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Casca de Planta/química
14.
Zhong Yao Cai ; 36(11): 1792-5, 2013 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-24956821

RESUMO

OBJECTIVE: To study the chemical constituents of Zanthoxyli Cortex. METHODS: The chemical constituents were isolated and purified by silica gel and HP-20, MCI gel, Sephadex LH -20 column chromatography, RP-18 and PTLC. Their structures were elucidated by the analysis of spectral data and chemical properties. RESULTS: Ten compounds were isolated from EtOAc extract and their structures were identified as: asarinin (I), fargesin (II), eudesmin (III), (1R, 2R, 5R, 6S)-2-(3,4-dimethoxyphenyl)-6-(3,4-dihydroxyphenyl)-3,7-dioxabicyclo[3.3.0]-octane(IV), dimethoxysamin(V), rel-(1R,5R,6S)-6-(3,4-dimethoxyphen-yl)-3,7-dioxabicyclo-[3.3.0]-octan-2-one(VI), Magnone A(VII), beta-sitoste-rol( VIII), beta-armyrin(IX), beta-amyrone(X). CONCLUSION: These compounds isolated from Zanthoxyli Cortex's Ethyl acetate extract are all known compounds. Fargesin(II) and beta-amyrone(X) are isolated from Zanthoxyli Cortex for the first time.


Assuntos
Casca de Planta/química , Extratos Vegetais/isolamento & purificação , Rutaceae/química , Acetatos , Benzodioxóis/química , Benzodioxóis/isolamento & purificação , Dioxóis/química , Dioxóis/isolamento & purificação , Furanos/química , Furanos/isolamento & purificação , Lignanas/química , Lignanas/isolamento & purificação , Espectroscopia de Ressonância Magnética , Extratos Vegetais/química , Triterpenos/química , Triterpenos/isolamento & purificação
15.
Arch Pharm Res ; 31(10): 1325-9, 2008 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-18958424

RESUMO

A new ferulic acid ester, 1'-methyl-2'-hydroxyethyl ferulate (1), together with methylcaffeate (2), 4-hydroxy cinnamic acid (3), ferulic acid (4), caffeic acid (5), diosmetin (6), luteolin (7), 5,3',4'-trihydroxy-3,7-dimethoxyflavone (8), eriodictyol (9), kaempferol (10), quercetin (11), acacetin-7-O-glcopyranoside (12), 4-(beta-glucopyranosyloxy) benzoic acid (13), luteolin-7-O-(6''-feruloyl) glucopyranoside (14), luteolin-7-O-glucopyranoside (15), kaempferide-3-O-rhamnopyranoside (16), quercitrin (17), kaempferol-3-O-glucopyranoside (18), prunasin (19), quercetin-7-O-glucopyranoside (20), quercetin-3-O-glucopyranoside (21), plantaginin (22), linarin (23), luteolin-7-O-rutinoside (24), and chlorogenic acid (25) were isolated from the aerial parts of Dacocephalum peregrinum. The structure of 1 was elucidated on the basis of spectroscopic and HR-ESI-MS analyses. In addition, compound 1 exhibited mild inhibitory effect on NO production in LPS-stimulated RAW264.7 cells.


Assuntos
Ácidos Cumáricos/química , Lamiaceae/química , Animais , Cromatografia em Camada Delgada , Ácidos Cumáricos/isolamento & purificação , Dimetil Sulfóxido , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Espectroscopia de Ressonância Magnética , Camundongos , Óxido Nítrico/biossíntese , Extratos Vegetais/química , Solventes , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Ultravioleta , Sais de Tetrazólio , Tiazóis
16.
Zhong Yao Cai ; 26(12): 867-9, 2003 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-15058205

RESUMO

OBJECTIVE: To find the active constituents of Rosa bracteata Wendl. to antagonize withdrawal syndrome in morphinedependent mice. METHODS: The constituents were isolated and purified by silica gel chromatography repeatedly. Their structures were made clear by chemical reactions and on the evidence of spectroscopy. RESULTS AND CONCLUSIONS: Five compounds were isolated from the fruits and four of them were determined as trimethly citrate, dimethyl 3-carboxyl-3-hydroxypentanedioate, 3-hydroxy-3-methoxycarbonyl-pentanedioic acid, calcium citrate, which were found from the Rose genus plant for the first time.


Assuntos
Citrato de Cálcio/isolamento & purificação , Citratos/isolamento & purificação , Plantas Medicinais/química , Rosa/química , Citrato de Cálcio/análise , Citratos/análise , Medicamentos de Ervas Chinesas/química , Frutas/química , Cromatografia Gasosa-Espectrometria de Massas , Peso Molecular , Espectrofotometria Ultravioleta
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