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1.
J Nat Prod ; 82(2): 407-411, 2019 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-30724564

RESUMO

Chloraserrtone A (1), a new sesquiterpenoid dimer with two lindenane-type sesquiterpenoid monomers bridged by two six-membered rings, was obtained from Chloranthus serratus. A combination of UV, IR, NMR, HRESIMS, and X-ray diffraction data were used to elucidate the structure of 1. Compound 1 represents the first lindenane-type sesquiterpenoid dimer with extremely unique C-15-C-15', C-4-C-6', and C-6-C-11' linkages to form two six-membered rings between the monomeric units. A plausible biosynthesis toward chloraserrtone A is proposed. This new compound (1), together with the known lindenane dimers (2-11), were assessed for their inhibitory effects on lipopolysaccharide-induced NO production in RAW264.7 cells. Compound 6 showed activity with an IC50 value of 3.7 µM.

2.
J Diabetes Res ; 2018: 9216791, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29977927

RESUMO

Diabetic retinopathy is the leading cause of blindness, yet its treatment is very limited. Anti-VEGF drug has been widely applied in ocular disease, but its effects on diabetic retinopathy and the underlying mechanism have remained to be fully explored. To elucidate the role of anti-VEGF treatment, we sought to determine the effects of bevacizumab on diabetic neurovascular changes extending from the 3rd to 9th week with induced diabetes in adult rats. The retinal neurovascular changes included increased expression of VEGF, nNOS, iNOS, eNOS, and NO in the course of diabetes progression. In diabetic rats given bevacizumab injection, the ganglion cell loss and alterations of retinal thickness were ameliorated. In this connection, the immunofluorescence labeling of the above biomarkers was noticeably decreased. Along with this, Western blotting confirmed that bevacizumab treatment was associated with a decrease of VEGF, Flk-1, and cAMP response element binding and protein kinase C protein expression. The present results suggest that bevacizumab treatment in the early stage of the retinopathy may ameliorate the lesions of retinopathy, in which VEGF/Flk-1 signaling has been shown here to play an important role.


Assuntos
Inibidores da Angiogênese/uso terapêutico , Bevacizumab/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Retinopatia Diabética/tratamento farmacológico , Inibidores da Angiogênese/administração & dosagem , Animais , Bevacizumab/administração & dosagem , Diabetes Mellitus Experimental/metabolismo , Retinopatia Diabética/metabolismo , Injeções Intravítreas , Masculino , Ratos , Ratos Sprague-Dawley , Retina/efeitos dos fármacos , Retina/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismo
3.
Bioresour Technol ; 264: 391-394, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29934120

RESUMO

This short communication analyzed enzymolysis kinetics and estimated the resource conversion efficiency of corn cobs. Three pretreatments were applied, and enzymatic hydrolysis was performed to obtain solid residues. The enzymolysis process was fit to a modified logistic formula. The kinetics of enzymolysis were similar for all pretreatments, and all kinetics fit the modified logistic formula. Resource conversion efficiency and saccharification efficiency were estimated for the following pretreatments: 69% and 86% for acid steam explosion, 59% and 73% for alkali soaking, 41% and 51% for water steam explosion, respectively. It can be concluded that pretreatment has a minor effect on the enzymolysis process of corn cobs and a greater effect on saccharification efficiency or resource conversion efficiency.


Assuntos
Zea mays/metabolismo , Álcalis , Reatores Biológicos , Explosões , Hidrólise , Cinética , Vapor , Água
4.
Acta Pharmacol Sin ; 39(9): 1483-1492, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29849130

RESUMO

Liver fibrosis is excessive accumulation of extracellular matrix proteins that results from various chronic liver diseases. Hepatic stellate cells (HSCs) play an essential role in the pathogenesis of liver fibrosis. Danggui Buxue Tang (DBT) is a classic formula of Chinese traditional medicine. We previously showed that DBT could ameliorate liver fibrosis in rats. However, the bioactive components of DBT in the treatment of liver fibrosis remain unknown. In this study we evaluated 14 ingredients from DBT in human hepatic stellate cell line LX-2, and found that astragaloside I (A), levistilide A (L) and calycosin (C) produced synergistic proliferation inhibition on LX-2 cells and TGF-ß1-activated LX-2 cells. Thus, we prepared a mixture of them, and named this combination as ALC formula. Using high-content screening and Western blot assay we revealed that the ALC formula significantly reduced the expression of α-SMA and collagen I in LX-2 cells. The in vivo anti-fibrosis effects of ALC formula were evaluated in a liver fibrosis model in C57BL/6 mice established through injection of dimethylnitrosamine (DMN 2 mg/kg, ip) for 4 weeks. In the third week, the nice were injected with ALC formula (astragaloside I 44.21 mg/kg per day, levistilide A 6 mg/kg per day and calycosin 3.45 mg/kg per day; ip) or sorafenib, a positive control drug (6 mg/kg per day, ip) for 2 weeks. We found that administration of the ALC formula markedly decreased collagen deposition, hydroxyproline (Hyp) content and α-SMA expression levels in the liver tissues compared to the model mice. In conclusion, the present study demonstrates for the first time that astragaloside I, levistilide A and calycosin may be the 3 main bioactive components in DBT; their combination exerts anti-liver fibrosis effects in vitro and in vivo.

5.
Clin Chim Acta ; 483: 249-255, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29752912

RESUMO

OBJECTIVE: In this study we determined the frequency of the most prevalent human papillomavirus (HPV) types in China and evaluated the association between viral loads of different oncogenic HPV types and the severity of disease. METHODS: We enrolled 15,518 women for this study and 3199 of them (20.61%) were identified as positive by a PCR assay, that can simultaneously quantify and genotype HPV. RESULTS: The viral loads of HPV 16, 31, 35, 52, 58, 39, and 56 were lower for women with normal cytology compared to those with disease progression; viral loads were not appreciable for HPV 33, 18, 45, 59, 68, 53, 66, and 51. The viral load of species 9 appeared significantly higher for women with cervical intraepithelial neoplasia (CIN) 2/CIN 3 relative to women with normal/low grade squamous intraepithelial lesion (LSIL)/CIN1 (P < 0.001), and significantly lower compared to those with cervical cancer (P < 0.001). The viral load of HPV species 6 was slightly higher for women with CIN2/CIN 3 compared to women with normal/LSIL/CIN1 (P = 0.002), and not significantly different from women with cervical cancer (P = 0.548). In addition, no statistically significant difference was found in HPV species 5 or species 7 (P = 0.898; P = 0.136). CONCLUSIONS: The HPV viral load-associated risk for developing into CIN and cervical cancer is likely to be species-dependent and primarily restricted to species 9 (types phylogenetically close to HPV16).


Assuntos
Papillomaviridae , Neoplasias do Colo do Útero/virologia , Carga Viral , Adulto , Idoso , Neoplasia Intraepitelial Cervical/patologia , Neoplasia Intraepitelial Cervical/virologia , China , Progressão da Doença , Feminino , Humanos , Pessoa de Meia-Idade , Papillomaviridae/genética , Especificidade da Espécie , Neoplasias do Colo do Útero/patologia
6.
J Asian Nat Prod Res ; : 1-6, 2018 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-29683345

RESUMO

Five fractions prepared from the crude extract of Leonurus japonicus were examined in order to determine their cytotoxic potential. Under the bioassay guidance, a new labdane-type diterpenoid (1), and nine known ones (2-10) along with a seco-labdane (11) were isolated from the aerial parts of Leonurus japonicus. The structure elucidation was primarily based on comprehensive spectroscopic analyses, including HRESIMS, IR, and 1D and 2D NMR methods. Compound 4 (6ß-hydroxy-15,16-epoxylabda-8,13(16),14-trien-7-one) exhibited potential cytotoxicity against HeLa cell line (IC50 = 23.75 µM).

7.
Nat Prod Res ; 32(19): 2312-2318, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29199463

RESUMO

A new C-glycosyl flavone, Chrysin-8-C-(2″-O-ß-6-deoxy-glucopyranosyl)-ß-D-glucopyranoside (1), a new neolignan glycoside, citrusin G (2), as well as 15 known compounds (3-17) were isolated from the peel of Passiflora edulis Sims. The structure determinations were primarily based on comprehensive spectroscopic analyses, and the absolute configuration of 2 were unequivocally determined by the CD experiment and chemical transformation. Compound 1 represents the rare examples of the flavonoid featuring a deoxy glucose sugar moiety. Compounds 5, 7 and 9 exhibited moderate inhibitory effects on nitric oxide (NO) production stimulated by lipopolysaccharide (LPS) in RAW 264.7 cells, with IC50 values of 34.92, 16.12 and 26.67 µM, respectively.


Assuntos
Flavonas/isolamento & purificação , Glicosídeos/isolamento & purificação , Passiflora/química , Animais , Flavonas/química , Glicosídeos/química , Lipopolissacarídeos/farmacologia , Camundongos , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Extratos Vegetais/química , Células RAW 264.7 , Análise Espectral
8.
Nat Prod Res ; 32(8): 885-891, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28817970

RESUMO

Four fractions were prepared from the crude extract of Caesalpinia minax Hance and the inhibitory activity of nitric oxide (NO) production release of RAW 264.7 cells stimulated by lipopolysaccharide (LPS) was evaluated. The ethyl acetate (EtOAc) fraction showed obvious inhibitory effect. Bioassay-guided fractionation led to the isolation of three new cassane diterpenes, caesalmin X (1), caesalmin Y (2) and caesalmin Z (3), together with 19 known cassane diterpenoids (4-22). Their structures were mainly characterised on the basis of extensive spectroscopic analyses and comparison with reported data. Moreover, three compounds (20-22) which possessed furanditerpenoid 7,17-lactone structures, displayed moderate activities, with IC50 value of 29.85, 27.38 and 25.40 µM, respectively.


Assuntos
Caesalpinia/química , Diterpenos/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Linhagem Celular , Diterpenos/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Concentração Inibidora 50 , Lipopolissacarídeos/farmacologia , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Sementes/química , Espectrofotometria Infravermelho
9.
Exp Biol Med (Maywood) ; 242(9): 974-985, 2017 05.
Artigo em Inglês | MEDLINE | ID: mdl-28440736

RESUMO

Levistilide A (C24H28O4, molecular weight = 380.48) derived from Angelica sinensis (Danggui) has been reported to inhibit hepatic stellate cell proliferation. This study investigated the effects of levistilide A on liver fibrosis relating to angiogenesis, particularly on the characteristic change in liver sinusoidal endothelial cells. LX-2 cells were activated by TGF-ß1, and the human hepatic sinusoidal endothelial cells (HHSECs) were induced by endothelial cell growth supplement. Cell viability was detected using a methylthiazoldiphenyl-tetrazolium bromide assay; F-actin was visualized through the fluorescence probe method; cell proliferation was examined using the EdU kit; antiangiogenesis activity was assessed using the tube formation assay and transgenic zebrafish model. To verify the results in vivo, rats were subcutaneously injected with CCl4 twice a week for six weeks to duplicate the liver fibrosis model and then treated with 10 mL/kg of normal saline, 4 mg/kg of sorafenib, and 3 and 6 mg/kg of levistilide A for three weeks from the fourth week. Collagen deposition was detected through Sirius Red staining; liver microvasculature was examined through vWF labeling and X-ray 2D imaging; sinusoidal fenestrations were observed through scanning electron microscopy; collagen I, α-SMA, CD31, vascular endothelial growth factor (VEGF), and VEGF-R2 were detected through Western blotting. Our results indicated that levistilide A attenuated LX-2 cell activation and HHSEC proliferation. The ability of HHSECs to form tubelike structures in Matrigel was inhibited, and the number of functional vessels in transgenic zebrafish decreased. In in vivo experiments, levistilide A reduced collagen deposition and the number of new microvessels; ameliorated sinusoid capillarization; and downregulated the expression of CD31, VEGF, and VEGF-R2. These findings suggest that levistilide A can inhibit liver fibrosis through antiangiogenesis by alleviating sinusoid capillarization via the VEGF signaling pathway. Impact statement Levistilide A has been reported to inhibit hepatic stellate cell (HSC) proliferation. In this study, we further investigated the mechanisms of levistilide A on liver fibrosis relating to angiogenesis, particularly on the characteristic change in liver sinusoidal endothelial cells. The cell models of HSC and liver sinusoidal endothelial cell and CCl4 induced liver fibrosis model were used. These results suggest that levistilide A can inhibit liver fibrosis through antiangiogenesis by alleviating sinusoid capillarization via the vascular endothelial growth factor signaling pathway. The effect of levistilide A on liver fibrosis was confirmed, and its detailed mechanism was also discussed. These findings suggest that levistilide A may be a great potential drug for treating liver fibrosis through antiangiogenesis, and this effect will be verified in other fibrotic animal model studies or by clinical trials.


Assuntos
Fármacos Gastrointestinais/administração & dosagem , Compostos Heterocíclicos de Anel em Ponte/administração & dosagem , Cirrose Hepática/tratamento farmacológico , Cirrose Hepática/patologia , Neovascularização Patológica/patologia , Animais , Modelos Animais de Doenças , Fígado/patologia , Cirrose Hepática/induzido quimicamente , Niacinamida/administração & dosagem , Niacinamida/análogos & derivados , Compostos de Fenilureia/administração & dosagem , Ratos , Sorafenibe , Resultado do Tratamento , Peixe-Zebra
10.
Nat Prod Res ; 31(7): 810-816, 2017 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-27809603

RESUMO

Solanerioside A (1), the first example of a diterpenoid glucoside featuring a 14,15-dinor-cyclophytane scaffold, together with three known terpene glucosides (2-4) were isolated from the methanol extract of the leaves of Solanum erianthum (Solanaceae). The structure of 1 was mainly characterised on the basis of extensive spectroscopic analyses, especially from the 2D NMR spectra. In addition, the spectroscopic data of (6E, 10E)-5,12-dihydroxy-ß-nerolidol 5-O-ß-D-glucopyranoside (3) were reported for the first time. However, these compounds did not display obvious inhibition of LPS-induced NO release in RAW264.7 cells and anti-tumour activity against A549, HepG2, Hela and MCF-7 cells in vitro.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Diterpenos/isolamento & purificação , Glucosídeos/isolamento & purificação , Folhas de Planta/química , Solanum/química , Animais , Linhagem Celular Tumoral , Diterpenos/química , Diterpenos/farmacologia , Glucosídeos/química , Glucosídeos/farmacologia , Humanos , Lipopolissacarídeos/farmacologia , Espectroscopia de Ressonância Magnética , Camundongos , Óxido Nítrico/metabolismo , Extratos Vegetais/química , Células RAW 264.7 , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Infravermelho
11.
Biochem Biophys Res Commun ; 479(2): 358-364, 2016 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-27644881

RESUMO

The aortic medial degeneration is the key histopathologic feature of Thoracic aortic dissection (TAD). The aim of this study was to identify the change of autophagic activity in the aortic wall during TAD development, and to explore the roles of autophagy on regulating functional properties of smooth muscle cells (SMCs). Firstly, compared with control group (n = 11), the increased expression of autophagic markers Beclin1 and LC3 was detected in the aortic wall from TAD group (n = 23) by immunochemistry and western blot. We found that more autophagic vacuoles were present in the aortic wall of TAD patients using Transmission electron microscopy. Next, autophagic activity was examined in AD mice model established by ß-aminopropionitrile fumarate (BAPN) and angiotensin II. Immunochemistry proved that autophagic activity was dynamically changed during AD development. Beclin1 and LC3 were detected up-regulated in the aortic wall in the second week after BAPN feeding, earlier than the fragmentation or loss of elastic fibers. When AD occurred in the 4th week, the expression of Beclin1 and LC3 began to decrease, but still higher than the control. Furthermore, autophagy was found to inhibit starvation-induced apoptosis of SMCs. Meanwhile, blockage of autophagy could suppress PDGF-induced phenotypic switch of SMCs. Taken together, autophagic activity was dynamically changed in the aortic wall during TAD development. The abnormal autophagy could regulate the functional properties of aortic SMCs, which might be the potential pathogenesis of TAD.


Assuntos
Aneurisma Dissecante/patologia , Aorta Torácica/patologia , Autofagia , Miócitos de Músculo Liso/metabolismo , Aminopropionitrilo/análogos & derivados , Aminopropionitrilo/química , Angiotensina II/química , Animais , Aorta Torácica/metabolismo , Apoptose , Proteína Beclina-1/metabolismo , Diferenciação Celular , Proliferação de Células , Elasticidade , Humanos , Imuno-Histoquímica , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Microscopia Eletrônica de Transmissão , Proteínas Associadas aos Microtúbulos/metabolismo , Fenótipo , Regulação para Cima
12.
J Nat Prod ; 79(9): 2257-63, 2016 09 23.
Artigo em Inglês | MEDLINE | ID: mdl-27588583

RESUMO

Bioassay-guided fractionation of an ethanolic extract of Chloranthus japonicus led to the isolation of the known lindenane-type sesquiterpenoid chlojaponilactone B (1). This compound exhibited pronounced inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Further anti-inflammatory assays showed that 1 suppressed the levels of some key inflammation mediators, such as iNOS, TNF-α, and IL-6, in a dose-dependent manner, and reduced the ear thickness and neutrophil infiltration in 12-O-tetradecanoylphorbol-13-acetate (TPA)-stimulated mice. A mechanistic study revealed that compound 1 exerted its anti-inflammatory effects via the suppression of the NF-κB signaling pathway, which inhibited NF-κB-dependent transcriptional activity, IκBα phosphorylation, and p65 nuclear translocation. In contrast, chlojaponilactone B (1) was found to exert little influence on the MAPK signaling pathway.


Assuntos
NF-kappa B/antagonistas & inibidores , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Ciclo-Oxigenase 2/metabolismo , Citocinas/metabolismo , Inflamação/induzido quimicamente , Mediadores da Inflamação , Interleucina-6/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Fosforilação/efeitos dos fármacos , Sesquiterpenos/química , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição RelA , Fator de Necrose Tumoral alfa/farmacologia
13.
Oncotarget ; 7(34): 54263-54273, 2016 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-27472464

RESUMO

While the molecular chaperone heat shock protein 90 (HSP90) is involved in a multitude of physiological and pathological processes, its role relating to pulmonary arterial hypertension (PAH) remains unclear. In the present study, we investigated the effect in which HSP90 improves pulmonary arteriole remodeling, and explored the therapeutic utility of targeting HSP90 as therapeutic drug for PAH. By Elisa and immunohistochemistry, HSP90 was found to be increased in both plasma and membrane walls of pulmonary arterioles from PAH patients. Moreover, plasma HSP90 levels positively correlated with mean pulmonary arterial pressure and C-reactive protein. In a monocrotaline-induced rat model of PH, we found that 17-AAG, a HSP90-inhibitor, alleviated the progress of PH, demonstrated by lower pulmonary arterial pressure and absence of right ventricular hypertrophy. Immunohistochemical staining demonstrated that 17-AAG improved pulmonary arteriole remodeling on the basis of reduced wall thickness and wall area. The inflammatory response attributed to PH could be attenuated by 17-AAG through reduction of NF-κB signaling. Moreover, 17-AAG was found to suppress PDGF-stimulated proliferation and migration of pulmonary artery smooth muscle cells (PASMCs) through induction of cell cycle arrest in the G1 phase. In conclusion, HSP90 inhibitor 17-AAG could improve pulmonary arteriole remodeling via inhibiting the excessive proliferation of PASMCs, and inhibition of HSP90 may represent a therapeutic avenue for the treatment of PAH.


Assuntos
Benzoquinonas/farmacologia , Proteínas de Choque Térmico HSP90/antagonistas & inibidores , Hipertensão Pulmonar/tratamento farmacológico , Lactamas Macrocíclicas/farmacologia , Artéria Pulmonar/fisiopatologia , Remodelação Vascular/efeitos dos fármacos , Adulto , Arteríolas/efeitos dos fármacos , Arteríolas/fisiopatologia , Quinase 4 Dependente de Ciclina/análise , Feminino , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Proteínas de Choque Térmico HSP90/análise , Proteínas de Choque Térmico HSP90/fisiologia , Humanos , Hipertensão Pulmonar/fisiopatologia , Masculino , Pessoa de Meia-Idade , Músculo Liso Vascular/efeitos dos fármacos , Músculo Liso Vascular/fisiopatologia , Miócitos de Músculo Liso/efeitos dos fármacos , Miócitos de Músculo Liso/fisiologia , Artéria Pulmonar/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos
14.
Appl Biochem Biotechnol ; 180(5): 945-953, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27220515

RESUMO

Levulinic acid production, directly from lignocellulosic biomass, resulted in low yields due to the poor substrate accessibility and occurrence of side reactions. The effects of reaction conditions, enzymatic pretreatment, and inhibitor addition on the conversion of steam-exploded rice straw (SERS) short fiber to levulinic acid catalyzed by solid superacid were investigated systematically. The results indicated that the optimal reaction conditions were temperature, time, and solid superacid concentration combinations of 200 °C, 15 min, and 7.5 %. Enzymatic pretreatment improved the substrate accessibility to solid superacid catalyst, and p-hydroxyanisole inhibitor reduced the side reactions during reaction processes, which helped to increase levulinic acid yield. The levulinic acid yield reached 25.2 % under the optimal conditions, which was 61.5 % higher than that without enzymatic pretreatment and inhibitor addition. Therefore, enzymatic pretreatment coupled with the addition of p-hydroxyanisole increased levulinic acid production effectively, which contributed to the value-added utilization of lignocellulosic biomass.


Assuntos
Anisóis/farmacologia , Celulase/metabolismo , Ácidos Levulínicos/metabolismo , Oryza/química , Vapor , Resíduos , Biocatálise/efeitos dos fármacos , Biomassa , Lignina/metabolismo , Oryza/efeitos dos fármacos , Temperatura Ambiente , Fatores de Tempo
15.
Bioorg Med Chem Lett ; 26(13): 3163-3166, 2016 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-27177824

RESUMO

Eight new lindenane sesquiterpenoid dimers, chlojapolides A-H (1-8), along with 11 known analogues were isolated from the whole plant of Chloranthus japonicus. Their structures including absolute configurations were elucidated by spectral and chemical methods. All the compounds were examined for their inhibitory effects on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW 264.7 macrophages, and compounds 1, 11, 13, and 17 exhibited pronounced inhibition with IC50 values in the range of 6.91-15.75µM, being more active than the positive control, quercetin (IC50=15.90µM).


Assuntos
Produtos Biológicos/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Magnoliopsida/química , Óxido Nítrico/antagonistas & inibidores , Sesquiterpenos/farmacologia , Animais , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Linhagem Celular , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade
16.
Anal Chim Acta ; 921: 77-83, 2016 05 19.
Artigo em Inglês | MEDLINE | ID: mdl-27126792

RESUMO

We have developed a ratiometric fluorescent probe BRT based on boron dipyrromethene (BODIPY) and rhodamine-thiohydrazide Förster resonance energy transfer (FRET) platform for sensing hypochlorous acid (HOCl) with high selectivity and sensitivity. The probe can detect HOCl in 15 s with the detection limit of 38 nM. Upon mixing with HOCl the fluorescence colour of probe BRT changed from green to orange. Moreover, probe BRT was applied to successfully monitor HOCl in living RAW 264.7 cells.


Assuntos
Compostos de Boro/química , Transferência Ressonante de Energia de Fluorescência/métodos , Corantes Fluorescentes/química , Ácido Hipocloroso/análise , Porfobilinogênio/análogos & derivados , Rodaminas/química , Animais , Limite de Detecção , Camundongos , Imagem Óptica/métodos , Porfobilinogênio/química , Células RAW 264.7 , Espectrometria de Fluorescência/métodos
17.
Chirality ; 28(3): 259-63, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-26781827

RESUMO

One pair of new C-8-C-3'/C-7-O-C-4' linked neolignan enantiomers (1a/1b) and one new guaiane sesquiterpene (2) first featuring the 1(2),9(10)-conjugated double bond were isolated from the stems of Solanum erianthum (Solanceae). Their structures were characterized on the basis of extensive spectroscopic analyses, especially from their 2D nuclear magnetic resonance (NMR) spectra. The absolute configurations of 1a/2b were rigorously elucidated by electronic circular dichroism (ECD) experiments combined with the reversed helicity rule for the 2,3-dihydrobenzo[b]furan chromophore, and compound 2 is the first report on the sterochemical assignment of a guaiane sesquiterpene by using the allylic axial chirality rule for the conjugated diene chromophore in combination with the calculated ECD spectrum.


Assuntos
Lignanas/química , Sesquiterpenos/química , Solanum/química , Benzofuranos/química , Dicroísmo Circular , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Sesquiterpenos de Guaiano/química , Estereoisomerismo
18.
Bioresour Technol ; 203: 204-10, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-26724552

RESUMO

Physical structure changes of solid medium were investigated to reveal effects of steam explosion sterilization on solid-state fermentation (SSF). Results indicated that steam explosion changed the structure of solid medium at both molecular and three-dimensional structural levels, which exposed hydrophilic groups and enlarged pores and cavities. It was interesting to find that pores where capillary water located were the active sites for SSF, due to the close relationship among capillary water relaxation time, specific surface area and fermentation performance. Therefore, steam explosion sterilization increased the effective contact area for microbial cells on solid medium, which contributed to improving SSF performance. Combined with the previous research, mechanisms of SSF improvement by steam explosion sterilization contained both chemical and physical effects.


Assuntos
Técnicas de Cultura Celular por Lotes/instrumentação , Fermentação , Técnicas de Síntese em Fase Sólida/instrumentação , Vapor , Esterilização/métodos , Bacillus subtilis/crescimento & desenvolvimento , Fenômenos Mecânicos , Esterilização/instrumentação , Propriedades de Superfície , Água
19.
Nat Prod Res ; 30(13): 1459-63, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-26158392

RESUMO

Two new glycosides (1, 2) and two saponins (3, 4) were isolated from the fruits of Sapindus mukorossi Gaertn. The two glycosides were designated as sapindoside G (1) and 4'',4'''''-O-diacetylmukurozioside IIa (2). All four compounds exhibited inhibitory effects against A549 human lung adenocarcinoma cells with inhibition rates up to 69.2-83.3% at a concentration of 100 µg/mL. Flow cytometric analysis revealed that compounds 1-4 could suppress A549 cell growth by promoting cell apoptosis, which was related to the activation of caspase-3.


Assuntos
Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Glicosídeos/isolamento & purificação , Neoplasias Pulmonares/tratamento farmacológico , Extratos Vegetais/farmacologia , Sapindus/química , Linhagem Celular Tumoral , Ativação Enzimática , Frutas/química , Glicosídeos/farmacologia , Humanos , Neoplasias Pulmonares/enzimologia , Neoplasias Pulmonares/patologia , Saponinas/farmacologia
20.
Zhongguo Zhong Yao Za Zhi ; 41(2): 279-284, 2016 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-28861974

RESUMO

To investigate the effect of schisantherin A on liver sinusoid endothelial cell function and angiogenesis. Different dosages (0-40 µmol•L⁻¹) of schisantherin A were incubated 24 h with SK-HEP-1 cells, and the toxicity of SK-HEP-1 cells was assayed by MTT method. The proliferation of SK-HEP-1 cells were induced by the vascular endothelial growth factor (VEGF), with receptor tyrosine kinase inhibitor sorafenib as the control, at the same time, set up the control group, 2, 20 µmol•L⁻¹ schisantherin A were incubated with SK-HEP-1 cells, cell proliferation was analyzed by EdU DNA cell proliferation kit. Fluorescence probe method was used to assay the intracellular NO levels and NOS activity. Tube formation was observed using cell migration and a matrigel tube formation assay. Rat aortic ring assay was performed to observe the sprouting vessels from aortic ring. The fluorescence vessels, the number of functional blood vessels, and intersegmental vessel changes of transgenic zebrafish were also observed. Compared with control group, the proliferation of SK-HEP-1 cells induced by VEGF increased and and the level of NO and NOS activity induced; compared with model group, 2, 20 µmol•L⁻¹ schisantherin A and sorafenib inhibited the proliferation of SK-Hep-1 cells induced by VEGF, and reduced the level of NO and NOS activity. At the dosage of 20 µmol•L⁻¹, schisantherin A attenuated the migration and tube formation of SK-HEP-1 cells induced by VEGF, and also inhibition the formation of rat aortic rings and intersegmental vessel changes of transgenic zebrafish, and significantly reduce the number of vessels in zebrafish. Schisantherin A has potential effects on function of endothelial cell proliferation and angiogenesis.


Assuntos
Inibidores da Angiogênese/administração & dosagem , Capilares/efeitos dos fármacos , Ciclo-Octanos/administração & dosagem , Dioxóis/administração & dosagem , Lignanas/administração & dosagem , Cirrose Hepática/tratamento farmacológico , Fígado/irrigação sanguínea , Animais , Capilares/metabolismo , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Células Endoteliais/efeitos dos fármacos , Células Endoteliais/metabolismo , Humanos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Cirrose Hepática/genética , Cirrose Hepática/metabolismo , Neovascularização Patológica/tratamento farmacológico , Neovascularização Patológica/genética , Neovascularização Patológica/metabolismo , Ratos , Ratos Sprague-Dawley , Fator A de Crescimento do Endotélio Vascular/genética , Fator A de Crescimento do Endotélio Vascular/metabolismo , Peixe-Zebra
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