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1.
Bioorg Med Chem Lett ; 30(2): 126791, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31740251

RESUMO

Neddylation modification is often over-expressed in a variety of human tumor cells. Therefore, targeting neddylation pathway may represent a potential approach to the treatment of human tumors. Herein, we describe the discovery of a hit scaffold from our in-house library and further structure-based optimizations. In this work, compound V11 could block the neddylation and inhibit the activity of NAE (with an EC50 value of 3.56 µM), and a dose-dependent reduction of the Ubc12-NEDD8 conjugations was also observed. Molecular docking results suggest compound V11 could bind tightly to NAE via hydrogen bonds and hydrophobic interactions. Compound V11 showed the best antiproliferative ability with an IC50 value of 8.22 µM against gastric cancer MGC-803 cells. Further anticancer activity studies suggested that compound V11 inhibited MGC-803 cell growth, caused a cell cycle arrestment at G2/M phase and induced apoptosis via extrinsic and intrinsic apoptosis pathways. All the findings suggest that 1,2,4-triazine scaffold might provide a novel scaffold for the further development of neddylation inhibitors and compound V11 might be a potential neddylation inhibitor with anticancer activity.

2.
Oncol Res ; 2019 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-31711559

RESUMO

MicroRNAs (miRNAs) play crucial roles in tumorigenesis and tumor progression. MiR-561 has been reported to be downregulated in gastric cancer and affects cancer cell proliferation and metastasis. However, the role and underlying molecular mechanism of miR-561 in human non-small-cell lung cancer (NSCLC) remain unknown and need to be further elucidated. In this study, we discovered that miR-561 expression was downregulated in human NSCLC tissues and cell lines. The overexpression of miR-561 inhibited NSCLC cell proliferation and cell cycle G1-S transition and induced apoptosis. The inhibition of miR-561 facilitated cell proliferation and G1-S transition and suppressed apoptosis. MiR-561 expression was inversely correlated with P-REX2a expression in NSCLC tissues. P-REX2a was confirmed to be a direct target of miR-561 by using a luciferase reporter assay. The overexpression of miR-561 decreased P-REX2a expression, and the suppression of miR-561 increased P-REX2a expression. Particularly, P-REX2a silencing recapitulated the cellular and molecular effects observed upon miR-561 overexpression, and P-REX2a overexpression counteracted the effects of miR-561 overexpression on NSCLC cells. Moreover, both exogenous expression of miR-561 and silencing of P-REX2a resulted in suppression of the PTEN/AKT signaling pathway. Our study demonstrates that miR-561 inhibits NSCLC cell proliferation and G1-S transition and induces apoptosis through suppression of the PTEN/AKT signaling pathway by targeting P-REX2a. These findings indicate that miR-561 plays a significant role in NSCLC progression and serves as a potential therapeutic target for NSCLC.

3.
Eur J Med Chem ; 183: 111731, 2019 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-31577977

RESUMO

With the expectation to find out new anti-gastric cancer agents with high efficacy and selectivity, a series of novel tertiary sulfonamide derivatives were synthesized and the anti-cancer activity was studied in three selected cancer cell lines (MGC-803, PC-3, MCF-7) in vitro. Some of the synthesized compounds could significantly inhibit the proliferation of these tested cancer cells and were more potent than the positive control (5-Fu). The structure-activity relationship of tertiary sulfonamide derivatives was explored in this report. Among the tested compounds, compound 13g containing benzimidazole moiety showed the best anti-proliferation activities against MGC-803 cells (IC50 = 1.02 µM), HGC-27 cells (IC50 = 1.61 µM), SGC-7901 (IC50 = 2.30 µM) cells as well as the good selectivity between the cancer and normal cells. Cellular mechanism studies elucidated compound 13g inhibited the colony formation of gastric cancer cell lines. Meanwhile, compound 13g arrested cell cycle at G2/M phase and induced cell apoptosis. Mechanistically, compound 13g markedly decreased p-Akt and p-c-Raf expression, which revealed that compound 13g targeted gastric cancer cell lines via interfering with AKT/mTOR and RAS/Raf/MEK/ERK pathways. All the findings suggest that compound 13g might be a valuable lead compound for the anti-gastric cancer agents.


Assuntos
Antineoplásicos , Benzimidazóis/química , Neoplasias Gástricas/tratamento farmacológico , Sulfonamidas , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Desenho de Drogas , Humanos , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química , Sulfonamidas/farmacologia
4.
Bioorg Chem ; 92: 103190, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31465969

RESUMO

A series of novel indoline derivatives were synthesized and evaluated for antiproliferative activity against four selected cancer cell lines (Hela, A549, HepG2 and KYSE30). Among them, compound 20 displayed the potent inhibition activity against esophageal cancer cells (Kyse30, Kyse450, Kyse510 and EC109). Cellular mechanism studies in esophageal squamous cell carcinoma (ESCC) cells elucidated compound 20 inhibited cell growths in vitro and in vivo, reduced colony formation, arrested cell cycle at M phase, and induced Noxa-dependent apoptosis in ESCC. Importantly, compound 20 was identified as a novel Noxa mediated apoptosis inducer. These results suggested that compound 20 might be a promising anticancer agent with potential for development of further clinical applications.

5.
Genomics Proteomics Bioinformatics ; 17(1): 52-63, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-31028880

RESUMO

Proton pump inhibitors (PPIs) are commonly used to lessen symptoms in patients with gastroesophageal reflux disease (GERD). However, the effects of PPI therapy on the gastrointestinal microbiota in GERD patients remain unclear. We examined the association between the PPI usage and the microbiota present in gastric mucosal and fecal samples from GERD patients and healthy controls (HCs) using 16S rRNA gene sequencing. GERD patients taking PPIs were further divided into short-term and long-term PPI user groups. We showed that PPI administration lowered the relative bacterial diversity of the gastric microbiota in GERD patients. Compared to the non-PPI-user and HC groups, higher abundances of Planococcaceae, Oxalobacteraceae, and Sphingomonadaceae were found in the gastric microbiota from the PPI-user group. In addition, the Methylophilus genus was more highly abundant in the long-term PPI user group than in the short-term PPI-user group. Despite the absence of differences in alpha diversity, there were significant differences in the fecal bacterial composition of between GERD patients taking PPIs and those not taking PPIs. There was a higher abundance of Streptococcaceae, Veillonellaceae, Acidaminococcaceae, Micrococcaceae, and Flavobacteriaceae present in the fecal microbiota from the PPI-user group than those from the non-PPI-user and HC groups. Additionally, a significantly higher abundance of Ruminococcus was found in GERD patients on long-term PPI medication than that on short-term PPI medication. Our study indicates that PPI administration in patients with GERD has a significant effect on the abundance and structure of the gastric mucosal microbiota but only on the composition of the fecal microbiota.


Assuntos
Refluxo Gastroesofágico/tratamento farmacológico , Refluxo Gastroesofágico/microbiologia , Microbioma Gastrointestinal/efeitos dos fármacos , Inibidores da Bomba de Prótons/uso terapêutico , Adulto , Idoso , Bactérias/genética , Bactérias/isolamento & purificação , Fezes/microbiologia , Feminino , Mucosa Gástrica/microbiologia , Humanos , Masculino , Microbiota , Pessoa de Meia-Idade , RNA Ribossômico 16S/genética
6.
Bioorg Chem ; 86: 375-385, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30763884

RESUMO

Novel chalcone-dithiocarbamate hybrids were designed, synthesized and evaluated for antiproliferative activity against selected cancer cell lines (MGC803, MCF7, and PC3). Among these analogues, (E)-2-oxo-2-((4-(3-(3,4,5-trimethoxyphenyl)acryloyl)phenyl)amino)ethyl-4-(2-hydroxyethyl)piperazine-1-carbodithioate (12d) showed the best inhibitory activity against PC3 cells (IC50 = 1.05 µM). Cellular mechanism studies elucidated 12d could inhibit colony formation, arrest cell cycle at G2/M phase and induce DNA damage against PC3 cells. Compound 12d also induced mitochondrial apoptosis by caspase activation, MMP decrease, ROS production and catalase (CAT) inhibition. Importantly, 12d inhibited epithelial-mesenchymal transition (EMT) process by regulating EMT-related proteins (E-cadherin, N-cadherin, Vimentin, MMP2, MMP9). These results indicated that 12d is a promising lead compound and deserves further investigation for prevention and treatment of human prostate cancer.

7.
Sci Rep ; 7(1): 12788, 2017 10 06.
Artigo em Inglês | MEDLINE | ID: mdl-28986548

RESUMO

We have synthesized a series of new ß-lactam-azide derivatives as orally active anti-tumor agents by targeting tubulin colchicine binding site and examined their structure activity relationship (SAR). Among them, compound 28 exhibited the most potent antiproliferative activity against MGC-803 cells with an IC50 value of 0.106 µM by induction of G2/M arrest and apoptosis and inhibition of the epithelial to mesenchymal transition. 28 acted as a novel inhibitor of tubulin polymerization by its binding to the colchicine site. SAR analysis revealed that a hydrogen atom at the C-3 position of the ß-lactam was required for the potent antiproliferative activity of ß-lactam-azide derivatives. Oral administration of compound 28 also effectively inhibited MGC-803 xenograft tumor growth in vivo in nude mice without causing significant loss of body weight. These results suggested that compound 28 is a promising orally active anticancer agent with potential for development of further clinical applications.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Azidas/farmacologia , Colchicina/farmacologia , Tubulina (Proteína)/metabolismo , beta-Lactamas/química , beta-Lactamas/farmacologia , Administração Oral , Animais , Antineoplásicos/administração & dosagem , Apoptose/efeitos dos fármacos , Azidas/administração & dosagem , Azidas/química , Caderinas/metabolismo , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Colchicina/química , Regulação para Baixo/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Camundongos Endogâmicos BALB C , Camundongos Nus , Relação Estrutura-Atividade , Regulação para Cima/efeitos dos fármacos , Proteína da Zônula de Oclusão-1/metabolismo , beta-Lactamas/administração & dosagem
8.
Molecules ; 22(9)2017 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-28872607

RESUMO

A series of sulfanilamide-1,2,3-triazole hybrids were designed by a molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, MCF-7 and PC-3). The detailed structure-activity relationships for these sulfanilamide-1,2,3-triazole hybrids were investigated. All these sulfanilamide-1,2,3-triazole hybrids exhibited moderate to potent activity against all cell lines. In particular 4-methyl-N-((1-(3-phenoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)benzenesulfonamide (11f) showed the most potent inhibitory effect against PC-3 cells, with an IC50 value of 4.08 µM. Furthermore, the tubulin polymerization inhibitory activity in vitro of compound 11f was 2.41 µM. These sulfanilamide hybrids might serve as bioactive fragments for developing more potent antiproliferative agents.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Sulfanilamidas/síntese química , Sulfanilamidas/farmacologia , Moduladores de Tubulina/síntese química , Moduladores de Tubulina/farmacologia , Antineoplásicos/administração & dosagem , Linhagem Celular Tumoral , Desenho de Drogas , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Relação Estrutura-Atividade , Sulfanilamidas/administração & dosagem , Triazóis/administração & dosagem , Triazóis/síntese química , Triazóis/farmacologia , Tubulina (Proteína)/metabolismo , Moduladores de Tubulina/administração & dosagem
9.
Eur J Med Chem ; 138: 1076-1088, 2017 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-28763643

RESUMO

A series of 5,6-diaryl-1,2,4-triazines hybrids bearing a 1,2,3-triazole linker were synthesized by molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, EC-109 and PC-3). The first structure-activity relationship (SAR) for these 5,6-diaryl-1,2,4-triazines is explored in this report with evaluation of 15 variants of the structural class. Among these chemical derivatives, 3-(((1-(4-fluorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)thio)-5,6-diphenyl-1,2,4-triazine (11E) showed the more potent inhibitory effect against three cell lines than 5-Fu. Cellular mechanism studies in MGC-803 cells elucidated 11E inhibited colony formation and arrested cell cycle at G2/M phase. Furthermore, compound 11E caused morphological changes, decreased mitochondrial membrane potential, and induced apoptosis through the apoptosis-related proteins in MGC-803 cells. It was the first time, to our knowledge, that 5,6-diaryl-1,2,4-triazines bearing a 1,2,3-triazole linker were used as potential apoptosis inducers.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Descoberta de Drogas , Triazinas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Triazinas/síntese química , Triazinas/química
10.
Mol Divers ; 21(4): 933-942, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28785928

RESUMO

Novel phenothiazine-dithiocarbamate analogues were designed by molecular hybridization strategy and synthesized and evaluated for their anticancer activity in vitro against three selected cancer cell lines (EC-109, MGC-803, and PC-3). The preliminary structure-activity relationship (SAR) for this phenothiazine-dithiocarbamate hybrids is explored. Among all analogues, 2-oxo-2-(10H-phenothiazin-10-yl)ethyl 4-ethylpiperazine-1-carbodithioate (8a) showed the most potent inhibitory activity with an [Formula: see text] value of [Formula: see text] against PC-3 cells. In addition, compound 8a could arrest the cell cycle at the G1 phase and regulate the expression of G1 checkpoint-related proteins, suggesting that phenothiazine-dithiocarbamate hybrids might be useful as cell cycle blockers.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Desenho de Drogas , Fenotiazinas/síntese química , Fenotiazinas/farmacologia , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Técnicas de Química Sintética , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Fenotiazinas/química , Relação Estrutura-Atividade
11.
Oncotarget ; 8(12): 20011-20024, 2017 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-28212553

RESUMO

BACKGROUND: Conflicting evidence exists regarding the effects of platelet/lymphocyte ratio (PLR) and lymphocyte/monocyte ratio(LMR) on the prognosis of colorectal cancer (CRC) patients. This study aimed to evaluate the roles of the PLR and LMR in predicting the prognosis of CRC patients via meta-analysis. METHODS: Eligible studies were retrieved from the PubMed, Embase,andChina National Knowledge Infrastructure (CNKI) databases, supplemented by a manual search of references from retrieved articles. Pooled hazard ratios (HR) with 95% confidence intervals (95% CI) were calculated using the generic inverse variance and random-effect model to evaluate the association of PLR and LMR with prognostic variables in CRC, including overall survival (OS), cancer-specific survival (CSS) and disease-free survival (DFS). RESULTS: Thirty-three studies containing 15,404 patients met criteria for inclusion. Pooled analysis suggested that elevated PLR was associated with poorer OS (pooled HR = 1.57, 95% CI: 1.41 - 1.75, p< 0.00001, I2=26%) and DFS (pooled HR = 1.58, 95% CI: 1.31 - 1.92, p< 0.00001, I2=66%). Conversely, high LMR correlated with more favorable OS (pooled HR = 0.59, 95% CI: 0.50 - 0.68, p< 0.00001, I2=44%), CSS (pooled HR = 0.54, 95% CI: 0.40 - 0.72, p< 0.00001, I2=11%) and DFS (pooled HR = 0.82, 95% CI: 0.71- 0.94,p=0.005, I2=29%). CONCLUSIONS: Elevated PLR was associated with poor prognosis, while high LMR correlated with more favorable outcomes in CRC patients. Pretreatment PLR and LMR could serve as prognostic predictors in CRC patients.


Assuntos
Plaquetas/patologia , Neoplasias Colorretais/patologia , Linfócitos/patologia , Monócitos/patologia , Contagem de Células Sanguíneas , Neoplasias Colorretais/terapia , Humanos , Prognóstico
12.
Eur J Med Chem ; 127: 87-99, 2017 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-28038329

RESUMO

A series of novel formononetin-dithiocarbamate derivatives were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell line (MGC-803, EC-109, PC-3). The first structure-activity relationship (SAR) for this formononetin-dithiocarbamate scaffold is explored in this report with evaluation of 14 variants of the structural class. Among these analogues, tert-butyl 4-(((3-((3-(4-methoxyphenyl)-4-oxo-4H-chromen-7-yl)oxy)propyl)thio)carbonothioyl)piperazine-1-carboxylate (8i) showed the best inhibitory activity against PC-3 cells (IC50 = 1.97 µM). Cellular mechanism studies elucidated 8i arrests cell cycle at G1 phase and regulates the expression of G1 checkpoint-related proteins in concentration-dependent manners. Furthermore, 8i could inhibit cell growth via MAPK signaling pathway and inhibit migration via Wnt pathway in PC-3 cells.


Assuntos
Movimento Celular/efeitos dos fármacos , Desenho de Drogas , Isoflavonas/química , Isoflavonas/farmacologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Tiocarbamatos/química , Via de Sinalização Wnt/efeitos dos fármacos , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Técnicas de Química Sintética , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Sinergismo Farmacológico , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Humanos , Isoflavonas/síntese química , Relação Estrutura-Atividade
13.
Bioorg Med Chem Lett ; 26(16): 3918-22, 2016 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-27423479

RESUMO

A series of novel dithiocarbamate-chalcone derivates were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell lines (EC-109, SK-N-SH and MGC-803). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds II2 and II5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03µM and 2.46µM, respectively. Further mechanism studies revealed that compound II2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase.


Assuntos
Antineoplásicos/síntese química , Chalcona/análogos & derivados , Desenho de Drogas , Tiocarbamatos/química , Antineoplásicos/química , Antineoplásicos/toxicidade , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Chalcona/síntese química , Chalcona/toxicidade , Ensaios de Seleção de Medicamentos Antitumorais , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Humanos , Relação Estrutura-Atividade , Tiocarbamatos/síntese química , Tiocarbamatos/toxicidade , Proteína Supressora de Tumor p53/metabolismo
14.
Molecules ; 21(5)2016 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-27213317

RESUMO

A series of novel chalcone-1,2,3-triazole-azole hybrids were designed, synthesized and evaluated for their antiproliferative activity against three selected cancer cell lines (SK-N-SH, EC-109 and MGC-803). Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Particularly, compound I-21 showed the most excellent antiproliferative activity with an IC50 value of 1.52 µM against SK-N-SH cancer cells. Further mechanism studies revealed that compound I-21 induced morphological changes of SK-N-SH cancer cells possibly by inducing apoptosis. Novel chalcone-1,2,3-triazole-azole derivatives in this work might be a series of promising lead compounds to develop anticancer agents for treating neuroblastoma.


Assuntos
Azóis/química , Azóis/farmacologia , Linhagem Celular Tumoral , Humanos , Relação Estrutura-Atividade
15.
Fitoterapia ; 104: 41-4, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25964187

RESUMO

Two new compounds, 2S-hydroxyl-jiadifenolide (1) and jiadifenlactone acid (2), and eight known compounds were isolated from the fruits of Illicium jiadifengpi. Their structures were analysed using several spectroscopic techniques, including 1D-, 2D-NMR and HR-ESI-MS experiments. The anti-hepatitis B virus (HBV) activities of the isolates were evaluated via HBV transfection of the Hep G2.2.15 cell line. The inhibitory rates of the most active compounds, compounds 4 and 5, on the HBeAg and HBsAg expression were 28.85±3.15% and 17.53±1.81% and 37.93±2.74% and 23.47±9.52% at concentrations of 64.94µM and 61.35µM, respectively.


Assuntos
Antivirais/farmacologia , Vírus da Hepatite B/efeitos dos fármacos , Illicium/química , Sesquiterpenos/farmacologia , Antivirais/química , Frutas/química , Células Hep G2 , Humanos , Estrutura Molecular , Sesquiterpenos/química
16.
Nat Prod Res ; 29(9): 800-6, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25466282

RESUMO

This article marks the first report on high-performance liquid chromatography (HPLC) coupled with diode-array detection (DAD) and quadruple time-of-flight mass spectrometry (Q-TOF/MS) for the identification and quantification of main bioactive constituents in Baeckea frutescens. In total, 24 compounds were identified or tentatively characterised based on their retention behaviours, UV profiles and MS fragment information. Furthermore, a validated method with good linearity, sensitivity, precision, stability, repeatability and accuracy was successfully applied for simultaneous determination of five flavonoids and one chromone in different plant parts of B. frutescens collected at different harvest times, and their dynamic contents revealed the appropriate harvest times. The established HPLC-DAD-Q-TOF/MS using multi-bioactive markers was proved to be a validated strategy for the quality evaluation on both raw materials and related products of B. frutescens.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Cromonas/análise , Flavonoides/análise , Myrtaceae/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Estrutura Molecular , Reprodutibilidade dos Testes
17.
Chin J Nat Med ; 12(6): 477-80, 2014 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-24969530

RESUMO

AIM: To study the chemical constituents of the fruits of Illicium henryi. METHOD: Chromatographic separations on silica gel, Sephadex LH-20 gel and MCI gel were used to isolate the compounds. The structures were elucidated based on extensive spectroscopic data analyses. RESULTS: Seven compounds were obtained and their structures were identified as 10-benzoyl-cycloparvifloralone (1), cycloparvifloralone (2), 2α-hydroxycycloparviforalone (3), henrylactone B (4), merrillianone (5), henrylactone C (6) and 7, 14-ortholactone- 3-hydroxyfloridanolide (7). CONCLUSION: Compound 1 is a new sesquiterpene lactone. The tested compounds showed weak anti-HBV activities on HBV surface antigen (HBsAg) secretion and HBV e antigen (HBeAg) secretion using Hep G2.2.15 cell line.


Assuntos
Frutas/química , Illicium/química , Extratos Vegetais/química , Sesquiterpenos/isolamento & purificação , Antivirais/química , Antivirais/isolamento & purificação , Antivirais/farmacologia , Células Hep G2 , Vírus da Hepatite B/efeitos dos fármacos , Humanos , Estrutura Molecular , Extratos Vegetais/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia
18.
Curr Cancer Drug Targets ; 14(2): 181-200, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24467530

RESUMO

There is an emerging paradigm shift in oncology that seeks to emphasize molecularly targeted approaches for cancer prevention and therapy. Chalcones (1,3-diphenyl-2-propen-1-ones), naturally-occurring compounds with widespread distribution in spices, tea, beer, fruits and vegetables, consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α, ß-unsaturated carbonyl system. Due to their structural diversity, relative ease of chemical manipulation and reaction of α, ß-unsaturated carbonyl moiety with cysteine residues in proteins, some lead chalcones from both natural products and synthesis have been identified in a variety of screening assays for modulating important pathways or molecular targets in cancers. These pathways and targets that are affected by chalcones include MDM2/p53, tubulin, proteasome, NF-kappa B, TRIAL/death receptors and mitochondria mediated apoptotic pathways, cell cycle, STAT3, AP-1, NRF2, AR, ER, PPAR-γ and ß-catenin/Wnt. Compared to current cancer targeted therapeutic drugs, chalcones have the advantages of being inexpensive, easily available and less toxic; the ease of synthesis of chalcones from substituted benzaldehydes and acetophenones also makes them an attractive drug scaffold. Therefore, this review is focused on molecular targets of chalcones and their potential implications in cancer prevention and therapy.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Chalconas/uso terapêutico , Terapia de Alvo Molecular , Neoplasias/tratamento farmacológico , Animais , Morte Celular/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos , Humanos , Estrutura Molecular , Neoplasias/metabolismo , Neoplasias/patologia , Fitoterapia , Plantas Medicinais , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
19.
Artigo em Inglês | MEDLINE | ID: mdl-24212142

RESUMO

A sensitive and accurate method based on the use of liquid chromatography-tandem mass spectrometry (LC-MS/MS) was developed for the simultaneous determination of eight illegal synthetic dyes (Sudan (I-IV), Para Red, Rhodamine B, Chrysoidin and Auramine O) in chili products. A simple sample treatment procedure entailing the use of an extraction step with acetonitrile/H2O (9/1) without further cleanup was developed. HPLC was performed on a C18 column using a multistep gradient elution with 5mM ammonium acetate (pH 3.0 with formic acid) and methanol as the mobile phase. Mass spectral acquisition was done in multiple reaction monitoring (MRM) mode using positive electrospray ionization (ESI). Linear calibrations were obtained with correlation coefficients R(2)>0.99. Limit of detection (LOD) and limit of quantification (LOQ) for the studied dyes were in the ranges of 0.05-0.6µgkg(-1) and 0.3-3.0µgkg(-1) depending on matrices, respectively. The recoveries of the eight synthetic dyes in five matrices ranged from 70.5% to 119.2%. The intra- and inter-day precisions (RSDs) were between 2.3-15.8% and 5.7-15.6%, respectively. The applicability of the method to the determination of eight banned dyes in chili products was demonstrated.


Assuntos
Capsicum/química , Cromatografia Líquida/métodos , Corantes/análise , Contaminação de Alimentos/análise , Espectrometria de Massas em Tandem/métodos , Capsicum/normas , China , Contaminação de Alimentos/legislação & jurisprudência , Limite de Detecção , Modelos Lineares , Reprodutibilidade dos Testes
20.
Molecules ; 18(10): 11866-72, 2013 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-24077171

RESUMO

Two new monoterpenes, p-mentha-1(7),8-dien-2-O-ß-D-glucoside and trans-2,4-dihydroxy-2,4-dimethyl-trans-1-acetic acid γ-lactone were isolated from the fruits of Illicium lanceolatum along with trans-2,4-dihydroxy-2,4-dimethyl-cis-1-acetic acid γ-lactone, (1R,2R,4R)-8-p-menthen-1,2-diol, trans-sobrerol, (1S,2S,4R)-p-menthane-1,2,8-triol and (1S, 2S, 4R, 8R)-p-menthane-1,2,9-triol. The structures of the isolates were confirmed by spectroscopic analysis and they showed no inhibitory effects on the in vitro growth of microbial organisms (Escherichia coli, Staphyloccocus aureus, Bacillus subtilis) at less than 1.0 mg/mL.


Assuntos
Frutas/química , Illicium/química , Monoterpenos/química , Extratos Vegetais/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Bacillus subtilis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Modelos Químicos , Modelos Moleculares , Conformação Molecular , Peso Molecular , Monoterpenos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Espectrometria de Massas por Ionização por Electrospray , Staphylococcus aureus/efeitos dos fármacos
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