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1.
Int J Biol Macromol ; 150: 737-745, 2020 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-32027898

RESUMO

The purpose of present work was to investigate the antioxidant activity of oligosaccharides from mountain-cultivated ginseng (MCG) and cultivated ginseng (CG). The antioxidant activity of total oligosaccharides from MCG and CG were compared preliminary. And then, the total oligosaccharides of MCG, which displayed stronger activity than that of CG, were separated by Carbon-Celite column and eluted with water and ethanol of different concentrations (30%, 50%, 70%, 95%, v/v). Five fractions, MCGOS-H2O, MCGOS-30, MCGOS-50, MCGOS-70, MCGOS-95, were obtained. Seven oligosaccharides were purified from MCGOS-30-MCGOS-95. The structure features of oligosaccharides (MCGO-1-MCGO-7) were characterized using high performance liquid chromatography (HPLC), methylation and gas chromatography-mass (GC-MS), as well as nuclear magnetic resonance spectroscopy. ABTS radical scavenging assay, DPPH radical scavenging assay as well as ferric reducing antioxidant power assay were adopted for antioxidant activity of all the different oligosaccharides sub-fraction. The result showed that the fractions of MCGOS-70 and MCGOS-95 exhibited significant radical scavenging activity with DPPH and ABTS. In conclusion, the oligosaccharides from MCG possessed the significant antioxidant activity. Therefore, we propose that the oligosaccharides from Panax ginseng can be developed as natural antioxidants in food and pharmaceutical fields.

2.
Chem Biodivers ; 17(1): e1900516, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31725193

RESUMO

In this study, 13 panaxadiol (PD) derivatives were synthesized via reactions with aromatic compounds and amino acids. Following this, the cytotoxicity of these compounds was evaluated against four cancer cell lines (human hepatoma cells HepG-2, human lung cancer cells A549, human breast cancer cells MCF-7, and human colon cancer cells HCT-116) and one normal cell lines (human gastric epithelial cells GES-1). The results showed that the panaxadiol derivatives 3, 12, and 13 showed significant inhibition of cellular proliferation against cancer cells compared with PD, and the panaxadiol derivative 12 had the lowest IC50 value for A549 (IC50 =18.91±1.03 µm). For MCF-7 cells, most compounds exhibited good inhibition of cellular proliferation, and the panaxadiol derivative 13 showed the strongest inhibitory effect (IC50 =8.62±0.23 µm), which significantly increased the cytotoxicity of PD and was stronger than the positive control (mitomycin). For normal cells, all compounds exhibited low or no toxic effects; thus, these derivatives can be used to develop novel antiproliferative agents.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Ginsenosídeos/química , Ginsenosídeos/farmacologia , Antineoplásicos/química , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Ginsenosídeos/síntese química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
3.
Eur J Med Chem ; 187: 111964, 2020 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-31862444

RESUMO

Two series of novel derivatives of AD-2, an active ginsenoside derived from ginseng were designed and synthesized. Five human cancer cell lines (MGC-803, SGC-7901, A549, MCF-7, PC-3 cells) and one normal ovarian cell IOSE144 were employed to evaluate the anti-proliferative activity. Most of derivatives possessed obvious enhanced activity compared with AD-2. Among them, compound 4c displayed the most excellent activity in all tested cancer cell lines, especially A549 cells with an IC50 value of 1.07 ± 0.05 µM. The underlying mechanism study suggested that 4c induced S-phase arrest and apoptosis in A549 cells. Increasing the level of ROS and inducing collapse of MMP in cells treated with 4c were also proved. Moreover, Western blot analysis showed that the expression level of p53 and p21 were obviously increased. 4c could remarkably up-regulate the expression of cyt c in cytosol, the ratio of Bax to Bcl-2 and activate caspase-3/9/PARP. Besides, the expression level of MDM2 was remarkably decreased. The results indicated that 4c caused apoptosis through the mitochondrial pathway, which ROS generation was probably involved in, and had the potent to serve as anti-proliferative agent.


Assuntos
Antimaláricos/farmacologia , Triterpenos/farmacologia , Antimaláricos/síntese química , Antimaláricos/química , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Estrutura Molecular , Relação Estrutura-Atividade , Triterpenos/síntese química , Triterpenos/química , Células Tumorais Cultivadas
4.
J Agric Food Chem ; 67(36): 10245-10255, 2019 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-31389238

RESUMO

Ginseng has been widely used as a functional food in the world because of its well-defined health benefits. Previous studies have confirmed that AD-1, a new ginsenoside derived from ginseng, can ameliorate thioacetamide-induced liver injury and fibrosis in mice. Simultaneously, amino acid supplementation is getting more attention as an important adjuvant therapy in the improvement of hepatopathy. The aim of this study was to conjugate AD-1 with several selected amino acids and investigate the cytotoxicity of the obtained conjugates in activated t-HSC/Cl-6 cells and normal human liver cells (LO2). Structure-activity relationships of conjugates and underlying mechanisms of the effect are also explored. The results indicated that conjugate 7c remarkably inhibited cell proliferation in activated t-HSC/Cl-6 cells (IC50 = 3.8 ± 0.4 µM) and appeared to be nontoxic to LO2. Besides, conjugate 7c had a relatively good plasma stability. Further study demonstrated that inducing S-phase arrest and activation of mitochondrial-mediated apoptosis were included in the mechanisms underlying the efficiency of conjugate 7c. These findings provided further insight into designing functional foods (ginsenoside and amino acid) for the application in prevention or improvement of liver fibrosis.


Assuntos
Aminoácidos/farmacologia , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Ginsenosídeos/farmacologia , Células Estreladas do Fígado/citologia , Aminoácidos/química , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Ginsenosídeos/química , Células Estreladas do Fígado/efeitos dos fármacos , Humanos , Pontos de Checagem da Fase S do Ciclo Celular/efeitos dos fármacos
5.
Nat Prod Res ; : 1-8, 2019 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-31264473

RESUMO

Two new 23, 27-dihydroxy-oleanane-type triterpenoid saponins named Raddeanoside Rf and Raddeanoside Rg (1 and 2), along with thirteen known triterpenoid saponins (3-15) were isolated from the rhizome of Anemone raddeana Regel. Their structures were determined by chemical and spectral analysis, including 1 D, 2 D NMR data and HRESIMS. The type of aglycone 23, 27-dihydroxy oleanolic acid is extremely rare in natural products. In addition, the anti-cancer activity for all the compounds were evaluated. Compounds 9 and 10 exhibited significant cytotoxicity with IC50 values of 4.47 and 8.97 µM against human pancreatic cancer lines (PANC-1), while compound 6 with IC50 value of 8.19 µM against human lung lines (A549). The possible structure-activity relationships of these triterpenoid saponins were also tentatively discussed.

6.
Fitoterapia ; 137: 104279, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31356850

RESUMO

20(R)-25-hydroxyprotopanaxadiol (25-OH-PPD) is a natural compound showing a variety of anti-tumor effects. In an attempt to search for a new anti-cancer compound with higher antitumor activities, we designed and synthesized a series of 25-OH-PPD derivatives. Cytotoxicity assay of these derivatives towards MCF-7, A549, U87, HO-8901, Hela cancer cell lines and normal IOSE144 cell lines were tested by MTT assay. Results showed that compared with compound 25-OH-PPD, Compounds 4, 5, 6, 10, 11 showed strong anticancer activity, and all compounds showed low toxicity or no toxicity for normal cells. In particular, compound 6 exhibited the best anti-tumor activity in all cancer cell lines (MCF-7, A549, U87, HO-8901, and Hela) with IC50 values of 5.04 µM, 1.36 µM, 3.24 µM, 3.47 µM, 4.57 µM, respectively. Among the five cell lines, all the compounds showed strong inhibition on A549 cells. Further studies showed that Compound 6 significantly inhibited the proliferation of A549 cells by inducing apoptosis. Our results indicate that Compound 6 is a potential anticancer inhibitor and provides a theoretical basis for further research.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Ginsenosídeos/farmacologia , Acilação , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Ginsenosídeos/síntese química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
7.
J Asian Nat Prod Res ; : 1-6, 2019 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-31357881

RESUMO

One new triterpene glycoside, asiaticoside I (1), along with seven known ones (2-8), were isolated from the aerial parts of Cimicifuga dahurica (Turcz.) Maxim. The structure of 1 was elucidated on the basis of extensive spectroscopic methods including 1D-NMR, 2D-NMR and MS data. The structures of known compounds were determined by comparison with the literature data. Compound 1 exhibited moderate cell growth inhibitory activities in vitro against HELF, non-small cell lung cancer A549, and pancreatic cancer PANC-1 cell lines, with IC50 values of 62.97, 43.19, and 60.40 µM, respectively.

8.
Biomed Chromatogr ; 33(10): e4624, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31215046

RESUMO

Cimicifugae Rhizoma (sheng ma) is a well-known traditional Chinese medicine, which has been demonstrated to possess anti-inflammatory, antipyretic and analgesic activities. In the present study, a simple and efficient HPLC-DAD (high-performance liquid chromatography coupled with diode array detection) method was developed and validated for simultaneous quantification of 19 chemical components (including 16 phenolic acids, one coumarin and two alkaloids) in Cimicifugae Rhizoma. The result indicated that this method could effectively evaluate the quality of Cimicifugae Rhizoma and provide a valuable reference for further study. Additionally, the antioxidant activity of Cimicifugae Rhizoma was evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging assay. The results showed that the content of phenolic acids and antioxidant activity exhibited significant correlation coefficients.


Assuntos
Antioxidantes , Cromatografia Líquida de Alta Pressão/métodos , Cimicifuga/química , Medicamentos de Ervas Chinesas , Alcaloides/análise , Alcaloides/isolamento & purificação , Alcaloides/metabolismo , Antioxidantes/análise , Antioxidantes/isolamento & purificação , Antioxidantes/metabolismo , Compostos de Bifenilo/metabolismo , Cumarínicos/análise , Cumarínicos/isolamento & purificação , Cumarínicos/metabolismo , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/química , Radicais Livres/análise , Radicais Livres/isolamento & purificação , Radicais Livres/metabolismo , Hidroxibenzoatos/análise , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/metabolismo , Limite de Detecção , Modelos Lineares , Picratos/metabolismo , Reprodutibilidade dos Testes
9.
J Sep Sci ; 42(15): 2550-2560, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31168953

RESUMO

Cimicifuga dahurica (Turcz.) Maxim. exerts significant antioxidative due to its high phenolic constituent content. In this study, the extraction condition of the phenolic constituents and antioxidant effect was optimized by the Box-Behnken design and response surface methodology. Eleven main bioactive analytes of Cimicifuga dahurica (Turcz.) Maxim. were simultaneously quantified by high-performance capillary electrophoresis with diode-array detector to assess the effect of extraction technology. The optimal extraction parameters were determined as: the concentration of ethanol 56.21%, liquid/solid ratio 14.65:1, and extraction time 1.64 h for 2.67 times. According to the results, a maximal value of total phenolic acids (3.67 mg/g) was obtained. Meanwhile, the influence of different extraction technology on antioxidant activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl, 2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonate), ferric reducing antioxidant power and hydroxyl radical scavenging method. The results presented here showed that the content of phenolic acid and antioxidant effect was much higher than the European Pharmacopoeia. Altogether, this method successfully applied response surface methodology to optimize the Cimicifuga dahurica (Turcz.) Maxim. extract with high antioxidant activities.


Assuntos
Cimicifuga/química , Fenóis/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Conformação Molecular , Fenóis/química , Extratos Vegetais/química , Estereoisomerismo , Propriedades de Superfície
10.
Bioorg Chem ; 88: 102961, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31075741

RESUMO

20(R)-25-methoxyl-dammarane-3ß,12ß,20-triol (AD-1, CN Patent: 201010107476.7) is a novel derivative of dammarane-type ginsenoside. AD-1 has been shown to inhibit cancer cell proliferation without significant host toxicity in vivo, and has excellent development potential as a new anti-cancer agent. This study was designed systematically to explore the metabolic pathway of ginseng sapogenins. The metabolism of drugs in the body is a complex biotransformation process where drugs are structurally modified to different molecules (metabolites) through various metabolizing enzymes. The compounds responsible for the effects of orally administered ginseng are believed to be metabolites produced in the gastrointestinal tract, so understanding the metabolism of the drug candidate can help to optimize its pharmacokinetics. In this study, faeces samples were collected and extracted after oral administration of AD-1. The 16 metabolites of AD-1 were isolated and identified for the first time with various chromatographic techniques, including semi-preparative high performance liquid chromatography, nuclear magnetic resonance spectroscopy, and mass spectrometry; of these 16 metabolites, 10 were novel compounds. We first discovered the biotransformation of dammarane-type sapogenins into oleanane-type sapogenins in rats and found a series of metabolites that changed, mainly at C-25 and C-29. This study provides new ideas for the metabolic pathway of ginseng sapogenins. The isolated compounds were screened for their effect on the viability and proliferation against cancer cell lines (Human A549, MCF-7, HELA, HO-8901 and U87). The discovery of novel active metabolites 3ß,12ß,21α,22ß-Hydroxy-24-norolean-12-ene (M6) may lead to a new or improved drug candidate. For one, M6 could inhibit the growth of all the tested cancer cells. Among the tested cell lines, M6 exhibited the most remarkable inhibitory effect on ovarian cancer HO-8901 cells, with IC50 value of 2.086 µM. On this basis, we studied the anticancer mechanisms of M6. The results indicated that the pro-apoptotic feature of M6 acts via a mitochondrial pathway. Our results indicated that M6 exhibited a higher inhibitory effect on cancer-cell proliferation than AD-1 by inducing cell apoptosis. Our work provides data for future investigations on the metabolic mechanism of AD-1 in vivo and the potential for future research on developing a new drug.

11.
Phytochemistry ; 162: 232-240, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30953910

RESUMO

Five previously undescribed monoterpenoid indole alkaloids were isolated from the roots of Gelsemium elegans. Their structures with absolute configurations were elucidated by HRESIMS, X-ray diffraction, ECD spectra, and molecular modeling. 19,20-Epoxyhumantenine is a humantenine-type alkaloid with an epoxypropyl group at the C-20 position, (4R)-19-oxo-gelsevirine N4-oxide is a gelsemine-related alkaloid, and gelsedethenine is a gelsedine-type alkaloid with a butenyl group at the C-20 position. Moreover, 10,11-dimethoxy-N1-demethoxy-gelsemamide is an open-loop indole alkaloid and 11-demethoxy-gelsemazonamide is an aromatic azo-linked dimeric indole alkaloid. Among the five alkaloids, (4R)-19-oxo-gelsevirine N4-oxide and 10,11-dimethoxy-N1-demethoxy-gelsemamide exhibited significant inhibitory effects on nitric oxide production in lipopolysaccharide-induced RAW 264.7 macrophage cells, with IC50 values of 6.18 ±â€¯1.07 and 12.2 ±â€¯1.02 µM, respectively.


Assuntos
Gelsemium/química , Alcaloides Indólicos/química , Animais , Alcaloides Indólicos/farmacologia , Concentração Inibidora 50 , Camundongos , Modelos Moleculares , Conformação Molecular , Óxido Nítrico/antagonistas & inibidores , Células RAW 264.7
12.
Int J Biol Macromol ; 133: 324-336, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-30943421

RESUMO

Ginseng Radix et Rhizome, which originated from Panax ginseng C. A. Meyer, has been used as traditional medicine in Asian for >2000 years. It is famous for its healthcare and therapeutic effects. Phytochemistry studies revealed that the major components of P. ginseng are: ginsenosides, polysaccharides, small peptides and essential oil. Modern research has proved that polysaccharide is one of the most important active ingredients in P. ginseng, which also takes up the largest slice of the chemical components. However, the past research was heavily oriented towards the small molecular ginsenosides. Thus, the main purpose of the present review is to summarize the preparation process, structure and biological functions of P. ginseng polysaccharides for further science research and application in medicine.


Assuntos
Produtos Biológicos/química , Produtos Biológicos/farmacologia , Panax/química , Polissacarídeos/química , Polissacarídeos/farmacologia , Animais , Produtos Biológicos/isolamento & purificação , Humanos , Polissacarídeos/isolamento & purificação
13.
Nat Prod Res ; : 1-8, 2019 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-30810364

RESUMO

Two new triterpenoid saponins, tomentoside T1 (1) and tomentoside T2 (2), together with eleven known compounds (3-13) were obtained from ethyl acetate extracts of Anemone tomentosa (Maxim.) Pei by bioactivity-guided isolation. Their structures were elucidated by chemical and spectral analysis, including 1D, 2D NMR data and HRESIMS. The cytotoxic activity of all isolated saponins was evaluated on MDA-MB-231 and PC-3 cell lines. Compounds 5 and 7 showed significant cytotoxicity against with MDA-MB-231 cell and PC-3 cell with IC50 values of 3.73-4.21 µM and 3.53-5.37 µM, respectively.

14.
J Food Drug Anal ; 26(3): 1113-1121, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29976404

RESUMO

Anemone raddeana Regel, a Traditional Chinese Medicine, has been demonstrated to possess cytotoxicity and anti-inflammatory activities. The purpose of this study is to establish analytical methods to identify and quantify the major active constituents in Anemone raddeana. A high-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (HPLC-ESI-Q/TOF-MS) was used to identify the components in the title plant material. To quantify the major components, a HPLC-UV method was developed and validated. The results showed that 37 compounds were identified based on the MS data and retention times. The contents of eight main bioactive compounds were determined by HPLC simultaneously. These methods could be used to effectively evaluate the quality of A. raddeana and provide a valuable reference for further study. In addition, the cytotoxicity activity of the different fractions of A. raddeana was determined. Hederacolchiside A1 (f) showed promising activity against ten human cancer cell lines with IC50 values from 0.29 to 3.48 µM.


Assuntos
Anemone/química , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Espectrometria de Massas em Tandem/métodos , Terpenos/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Medicina Tradicional Chinesa , Rizoma/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Terpenos/farmacologia
15.
J Food Drug Anal ; 26(2): 796-806, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-29567251

RESUMO

Epimedium koreanum Nakai is a famous Chinese herbal medicine for the treatment of impotence, osteoporosis, immune suppression and cardiovascular diseases. Drying is the most common and fundamental procedure in post-harvest processing of E. koreanum, which contributes to the variations of flavonoid content, especially prenylflavonoids, the bioactive components. In present study, effect of drying processes on flavonoid content and antioxidant activity were investigated. High performance liquid chromatography coupled with diode-array detection and electrospray ionization quadrupole time-of-flight tandem mass spectrometry methods were employed. Twenty seven compounds were identified and 11 of them, including eight prenylflavonoids and three other types of flavonoids, were further quantified. The antioxidant activity of E. koreanum was evaluated by the 2,2-diphenyl-1-picrylhydrazyl free radical scavenging method. The results showed that content of the eight prenylflavonoids exhibited significant variations after different drying processes, especially icariin and baohuoside I. The variation tendency of antioxidant activity was positively correlated with the content of total flavonoid, afzelin and icariin.


Assuntos
Antioxidantes/química , Dessecação/métodos , Medicamentos de Ervas Chinesas/química , Epimedium/química , Flavonoides/química , Tecnologia Farmacêutica/métodos , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas por Ionização por Electrospray
16.
Nat Prod Res ; 32(11): 1303-1306, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28651437

RESUMO

A rapid method had been used for comparative study on Artemisia halodendron Turcz. and its two related plants by gas phase-mass spectrometry (GC-MS). The comparison of the volatile oils obtained in three plants by GC-MS were similar in 20 compositions. However, n-Hexadecanoic acid (10.40%), Biphenyl (7.867%) and 9,12-Octadecadienoic acid (7.25%) were the predominant in the volatile oils of A. halodendron Turcz., whereas these constituents did not exist in the other two plants. And the study investigated the effect of three plants against CCl4-induced hepatotoxicity in mice. 70% ethanol extracts of A. halodendron Turcz. showed weaker protective effect than the other two plants. It suggested that they provide a basis for the identification of the A. halodendron Turcz. from the other two plants and the ethanol extract from three plants exerted a protecting effect against hepatotoxicity.


Assuntos
Artemisia/química , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Substâncias Protetoras/farmacologia , Animais , Compostos de Bifenilo/análise , Tetracloreto de Carbono/toxicidade , Cromatografia Gasosa-Espectrometria de Massas/métodos , Ácido Linoleico/análise , Masculino , Camundongos , Óleos Voláteis/análise , Óleos Voláteis/química
17.
Biomed Chromatogr ; 32(2)2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28677911

RESUMO

Bupleuri Radix is a commonly used herb in clinic, and raw and vinegar-baked Bupleuri Radix are both documented in the Pharmacopoeia of People's Republic of China. According to the theories of traditional Chinese medicine, Bupleuri Radix possesses different therapeutic effects before and after processing. However, the chemical mechanism of this processing is still unknown. In this study, ultra-high-performance liquid chromatography with quadruple time-of-flight mass spectrometry coupled with multivariate statistical analysis including principal component analysis and orthogonal partial least square-discriminant analysis was developed to holistically compare the difference between raw and vinegar-baked Bupleuri Radix for the first time. As a result, 50 peaks in raw and processed Bupleuri Radix were detected, respectively, and a total of 49 peak chemical compounds were identified. Saikosaponin a, saikosaponin d, saikosaponin b3 , saikosaponin e, saikosaponin c, saikosaponin b2 , saikosaponin b1 , 4''-O-acetyl-saikosaponin d, hyperoside and 3',4'-dimethoxy quercetin were explored as potential markers of raw and vinegar-baked Bupleuri Radix. This study has been successfully applied for global analysis of raw and vinegar-processed samples. Furthermore, the underlying hepatoprotective mechanism of Bupleuri Radix was predicted, which was related to the changes of chemical profiling.


Assuntos
Bupleurum/química , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/química , Espectrometria de Massas/métodos , Raízes de Plantas/química , Ácido Acético , Composição de Medicamentos , Temperatura Alta , Modelos Estatísticos , Análise Multivariada
18.
J Nat Prod ; 80(11): 2893-2904, 2017 11 22.
Artigo em Inglês | MEDLINE | ID: mdl-29131616

RESUMO

Inspired by the intriguing structures and bioactivities of dimeric alkaloids, 11 new thalifaberine-type aporphine-benzylisoquinoline alkaloids, thalicultratines A-K, a tetrahydroprotoberberine-aporphine alkaloid, thalicultratine L, and five known ones were isolated from the roots of Thalictrum cultratum. Their structures were defined on the basis of NMR and HRESIMS data. The antiproliferative activities of compounds 1-17 were evaluated against human leukemia HL-60 and prostate cancer PC-3 cells. Most alkaloids showed potent cytotoxicity against selected cancer cells. Preliminary SARs are discussed. The most active new compound (3), with an IC50 value of 1.06 µM against HL-60 cells, was selected for mechanism of action studies. The results revealed that compound 3 induced apoptosis and arrested the HL-60 cell cycle at the S phase with the loss of mitochondria membrane potential. The nuclear morphological Hoechst 33258 staining assay was also carried out, and the results confirmed apoptosis.


Assuntos
Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Aporfinas/isolamento & purificação , Aporfinas/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Raízes de Plantas/química , Thalictrum/química , Alcaloides/química , Antineoplásicos Fitogênicos/química , Aporfinas/química , Alcaloides de Berberina , Medicamentos de Ervas Chinesas/química , Células HL-60 , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Relação Estrutura-Atividade
19.
Molecules ; 22(11)2017 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-29099046

RESUMO

Four new special compounds with character of an iriflophene unit and a flavonoid unit connecting via a furan ring were isolated from the roots of Sedum aizoon L. Their corresponding structures were elucidated on the basis of spectroscopic analysis. The in vitro anti-proliferative activities against BXPC-3, A549, and MCF-7 tumor cell lines were evaluated. Compounds 3 and 4 exhibited moderate cytotoxic activities with IC50 ranging from 24.84 to 37.22 µmol L-1, which was capable for further drug exploration.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Flavonoides/farmacologia , Furanos/farmacologia , Sedum/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Flavonoides/química , Flavonoides/isolamento & purificação , Furanos/química , Furanos/isolamento & purificação , Humanos , Células MCF-7 , Espectroscopia de Ressonância Magnética , Estrutura Molecular
20.
Molecules ; 22(10)2017 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-29057809

RESUMO

Fulminant hepatic failure (FHF), associated with high mortality, is characterized by extensive death of hepatocytes and hepatic dysfunction. There is no effective treatment for FHF. Several studies have indicated that flavonoids can protect the liver from different factor-induced injury. Previously, we found that the extracts of Elaeagnus mollis leaves had favorable protective effects on acute liver injury. However, the role and mechanisms behind that was elusive. This study examined the hepatoprotective mechanisms of kaempferol-3-O-α-l-arabinopyranosyl-7-O-α-l-rhamnopyra-noside (KAR), a major flavonol glycoside of E. mollis, against d-galactosamine (GalN) and lipopolysaccharide (LPS)-induced hepatic failure. KAR reduces the mouse mortality, protects the normal liver structure, inhibits the serum aspartate aminotransferase (AST) and alamine aminotransferase (ALT) activity and decreases the production of malondialdehyde (MDA) and reactive oxygen species (ROS) and inflammatory cytokines, TNF-α, IL-6, and IL-1ß. Furthermore, KAR inhibits the apoptosis of hepatocytes and reduces the expression of TLR4 and NF-κB signaling pathway-related proteins induced by GalN/LPS treatment. These findings suggest that the anti-oxidative, anti-inflammatory, and anti-apoptotic effects of KAR on GalN/LPS-induced acute liver injury were performed through down-regulating the activity of the TLR4 and NF-κB signaling pathways.


Assuntos
Glicosídeos/administração & dosagem , Quempferóis/administração & dosagem , Falência Hepática Aguda/tratamento farmacológico , Fígado/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Alanina Transaminase/sangue , Animais , Apoptose/efeitos dos fármacos , Aspartato Aminotransferases/sangue , Elaeagnaceae/química , Galactosamina/toxicidade , Regulação da Expressão Gênica/efeitos dos fármacos , Lipopolissacarídeos/toxicidade , Fígado/metabolismo , Fígado/patologia , Falência Hepática Aguda/sangue , Falência Hepática Aguda/induzido quimicamente , Falência Hepática Aguda/patologia , Malondialdeído/sangue , Camundongos , NF-kappa B/genética , Extratos Vegetais/química , Espécies Reativas de Oxigênio/sangue , Transdução de Sinais/efeitos dos fármacos , Receptor 4 Toll-Like/genética
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