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1.
Fitoterapia ; : 104516, 2020 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-32081701

RESUMO

A new bilobalide isomer (1), together with two flavonol glycosides (2, 3), have been isolated and elucidated from the extract of Ginkgo biloba leaves. Significantly, 1 was a new sesquiterpene lactone with two lactone ring groups, both 2 and 3 were two flavonol glycosides with a same cis-coumaroylated fragment. Their chemical structures were elucidated by NMR and MS spectroscopic date and the absolute configuration of 1 was specific established by Cu-Kα X-ray crystallographic analyses. However, 1-3 showed no obvious anti-platelet aggregation activity.

2.
Fitoterapia ; 141: 104454, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31857181

RESUMO

Three rare squiterpene lactone dimers lineariifolianoids M-O (1-3) were isolated from Inula lineariifolia for the first time. Their structures and absolute configuration were established on the basis of by NMR and MS spectroscopic data and X-ray crystallography. Furthermore, those three compounds exhibited significant inhibitory activity against LPS-induced NO production in RAW 264.7 macrophages with IC50 values of 1.421, 1.087 and 1.243 µM, respectively.

3.
Nat Prod Bioprospect ; 2019 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-31786736

RESUMO

Eight new triterpenoids were isolated from Ainsliaea latifolia. The structures of these compounds were elucidated by interpretation of spectroscopic data, including HRESIMS and NMR data. Compounds 4-6 are identified as rare trinorcucurbitane or tetranorcucurbitane triterpenoids. The absolute configurations of compounds 1 and 2 were confirmed by Snatzke's method. All compounds were evaluated for their inhibition against cyclooxyenase-2 (COX-2), in which compound 4 showed significant inhibitory effect against COX-2 with IC50 value of 3.98 ± 0.32 µM, comparable to that of positive control NS-398 (IC50 4.14 ± 0.28 µM).

4.
Phytomedicine ; 64: 153073, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31542661

RESUMO

BACKGROUND: Ginkgo biloba (Gb) extracts have been used as a traditional Chinese medicine. Gb contains flavonoids, which are considered to be its active ingredients and have been used in the treatment of a variety of diseases. However, few scientific research studies on the side effects of flavonoid in Gb have been reported. PURPOSE: The present study aimed to investigate the effect of bilobetin on the kidney of Sprague-Dawley (SD) rats. STUDY DESIGN AND RESULT: In this study, rats were injected with 50 mg/kg of bilobetin, a biflavone isolated from Gb, for 7 days and aristolochic acid was used as positive controls. The results showed that the body weight and urine output of the rats were dramatically decreased, and urinary protein increased after the intraperitoneal injection of bilobetin compared with the control group. Bilobetin treatment showed vacuolar degeneration in the renal tubular epithelium, glomerular atrophy by histostaining, and podocyte fusion by electron microscopy. This study further showed that bilobetin promoted the trafficking of aquaporin 2 (AQP-2) onto the plasma membrane to achieve the function of urine concentration by in vivo study in rats and in vitro study in IMCD-3 cells. The redistribution of AQP-2 is due to increased expression of cGMP in IMCD-3 cells, which in turn promoted the phosphorylation of AQP-2 at site Ser-256. The proteinuria caused by bilobetin may be attributed to podocyte cell cycle arrest at G2/M transition, which is may associated with AKT and MAPK signaling. CONCLUSIONS: The current study showed that bilobetin has some side effects on kidneys at a dose of 50 mg/kg in SD rats and provides insight into the potential detrimental effects of monomeric ingredients in Gb.

5.
Sci Rep ; 9(1): 12673, 2019 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-31481699

RESUMO

MADS-box transcription factors possess many functions in plant reproduction and development. However, few MADS-box genes related to secondary metabolites regulation have been identified. In Hevea brasiliensis, natural rubber is a representative cis-polyisoprenoids in secondary metabolism which occurs in the rubber laticifer cells, the molecular regulation basis of natural rubber biosynthesis is not clear. Here, a total of 24 MADS-box genes including 4 type I MADS-box genes and 20 type II MADS-box genes were identified in the transcriptome of rubber tree latex. The phylogenetic analysis was performed to clarify the evolutionary relationships of all the 24 rubber tree MADS-box proteins with MADS-box transcription factors from Arabidopsis thaliana and Oryza sativa. Four type I MADS-box genes were subdivided into Mα (3 genes) and Mß (1 gene). Twenty type II MADS-box genes were subclassified into MIKC* (8 genes) and MIKCc (12 genes). Eight MADS-box genes (HblMADS3, 5, 6, 7, 9, 13, 23, 24) were predominant expression in laticifers. ABA up-regulated the expression of HblMADS9, and the expression of HblMADS3, HblMADS5, HblMADS24 were up-regulated by MeJA. The function of HblMADS24 was elucidated. HblMADS24 bound HbFPS1 promoter in yeast and HblMADS24 activated HbFPS1 promoter in tobacco plants. Moreover, we proposed that HblMADS24 is a transcription activator of HbFPS1 which taking part in natural rubber biosynthesis.

6.
Genet Mol Biol ; 2019 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-31441928

RESUMO

Histone methylation plays a crucial role in various biological processes including from heterochromatin formation to transcriptional regulation. Currently, no information is available regarding histone methylation modifiers in the important rubber-producing plant Hevea brasiliensis. Here, we identified 47 histone methyltransferase (HMT) genes and 25 histone demethylase (HDM) genes, as possible members of the histone methylation modifiers in the rubber tree genome. According to the structural features of HMT and HDM, the HbHMTs were classified to two groups (HbPRMs and HbSDGs), the HbHDMs have two groups (HbLSDs and HbJMJs). The expression patterns of HbHMTs and HbHDMs were analyzed in five different tissues and at different phases of somatic embryogenesis. HbSDG10, 21, 25, 33, HbJMJ2, 18, 20 were with high expression at different phases of somatic embryogenesis. HbSDG10,14, 20, 21, 3 and HbPRMT4 were expressed highly in anther, HbSDG14, 20, 21, 22, 23, 33, 35 and HbPRMT1 HbJMJ7 and HbLSD1, 2, 3, 4 showed a high expression level in callus. HbSDG1, 7, 10, 13, 14, 18, 19, 21, 22, 23, 35, HbPRMT1, 8, HbJMJ5, 7, 11, 16, 20 and HbLSD2, 3, 4 were expressed highly in somatic embryo. HbSDG10, 21, 25, 33, HbLSD2, 3 3 were expressed highly in bud of regenerated plant. The expression analyses reveal that HbHMTs and HbHDMs exhibit different expression patterns at different phases during somatic embryogenesis and imply that some HbHMTs and HbHDMs play important roles during somatic embryogenesis. This study will provide fundamental to further study on regulations of histone metylation in Hevea brasiliensis.

7.
Org Lett ; 20(23): 7567-7570, 2018 12 07.
Artigo em Inglês | MEDLINE | ID: mdl-30421929

RESUMO

Vlasoulamine A (1), an unprecedented sesquiterpene lactone dimer featuring a fully hydrogenated pyrrolo[2,1,5- cd]indolizine core, and vlasoulones A and B (2 and 3), a pair of epimeric dimers formed from a proposed Diels-Alder [4 + 2] cycloaddition between a germacrane sesquiterpene lactone and a eudesmane sesquiterpene, were isolated from the roots of Vladimiria souliei. Their structures and absolute configurations were established by NMR, MS, and single-crystal X-ray spectroscopic analysis. Moreover, 1 exhibited neuroprotective activity when evaluated for glutamate-induced cytotoxicity, nuclear Hoechst 33258 staining, and measuring intracellular reactive oxygen species levels, using a rat pheochromocytoma PC12 cell-based model system.


Assuntos
Antineoplásicos/farmacologia , Asteraceae/química , Lactonas/farmacologia , Fármacos Neuroprotetores/farmacologia , Raízes de Plantas/química , Sesquiterpenos/farmacologia , Animais , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Ácido Glutâmico/farmacologia , Lactonas/química , Lactonas/isolamento & purificação , Modelos Moleculares , Estrutura Molecular , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Células PC12 , Ratos , Espécies Reativas de Oxigênio/análise , Espécies Reativas de Oxigênio/metabolismo , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade
8.
Fitoterapia ; 130: 156-162, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30172826

RESUMO

Five new podocarpane trinorditerpenes (1-5) and a dimeric trinorditerpene with an unprecedented skeleton bearing a 1,4-benzodioxane moiety (6) along with seven known compounds (7-13) were isolated from the stems of Celastrus angulatus (Celastraceae). These compounds' structures were elucidated by comprehensive spectroscopic analysis. In addition, the absolute configuration of 1 was determined by single crystal X-ray diffraction analysis. Compounds 3, 4, 7, and 12 exhibited moderate inhibitory activity against LPS-induced NF-κB activation in murine macrophage RAW264.7 cells at IC50 values of 25.08, 18.64, 15.33 and 3.89 µM, respectively. However, compound 6 exhibited potent cytotoxicity against the A549 and MDA-MB-231 human tumour cell lines with IC50 values of 4.47 µM and 5.86 µM, respectively. Compound 9 exhibited potent cytotoxicity against the HCT116 and BEL7404 human tumour cell lines with IC50 values of 6.77 µM and 9.45 µM, respectively.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Celastrus/química , Diterpenos/farmacologia , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , China , Diterpenos/isolamento & purificação , Humanos , Camundongos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Caules de Planta/química , Células RAW 264.7
9.
Int J Biol Macromol ; 118(Pt B): 2216-2223, 2018 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-30009906

RESUMO

Reduction of lipid absorption has been recognized as an attractive approach for the discovery of new drugs to treat obesity and overweight. The leave extract of Ginkgo biloba has been widely used for the treatment of metabolic diseases (such as hyperlipidemia) in both eastern and western countries, but the bioactive compounds in Ginkgo biloba and the underlying mechanism have not been fully characterized. This study aimed to investigate the inhibition potentials and mechanism of major biflavones from G. biloba on pancreatic lipase (PL), a key target regulating lipid absorption. The results clearly demonstrated that all tested biflavones in G. biloba including isoginkgetin, bilobetin, ginkgetin and sciadopitysin, displayed strong to moderate inhibitory effects on PL with the IC50 values ranging from 2.90 µM to 12.78 µM. Further investigations on both inhibition kinetic analyses and docking simulations demonstrated that isoginkgetin, bilobetin and ginkgetin were potent PL inhibitors (Ki < 2.5 µM), which could create strong interactions with the catalytic triad of PL via hydrogen bonding. These findings provided a new powerful evidence for explaining the hypolipidemic effects of G. biloba, while these newly identified PL inhibitors from G. biloba could serve as lead compounds for the development of biflavonoid-type PL inhibitors.


Assuntos
Biflavonoides/farmacologia , Inibidores Enzimáticos/farmacologia , Ginkgo biloba/química , Lipase/antagonistas & inibidores , Pâncreas/enzimologia , Animais , Biflavonoides/química , Inibidores Enzimáticos/química , Concentração Inibidora 50 , Cinética , Lipase/metabolismo , Simulação de Acoplamento Molecular , Sus scrofa , Termodinâmica
10.
Fitoterapia ; 127: 396-401, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29641986

RESUMO

Six new chromane and chromene meroterpenoids rubiginosins A-F (1-2, and 4-7), together with three known ones, rubiginosin G (3) and anthopogochromenes A and B (8-9),were isolated from the flowers of Rhododendron rubiginosum Franch. var. rubiginosum. Among them, 1-4 were the chromane ones derived from an intramolecular [2 + 2] cycloaddition of their respective chromene precursors, making a 6/6/6/4- or 6/6/5/4-ring fused scaffold. The absolute configuration of the chiral center at C-2 of 1-9 was determined as S by chromane/chromene helicity rule and X-ray crystallograph. Notably, more attention should be paid to 6-carboxyl derivatives, since the 6-carboxyl derivatives showed an abnormal diagnostic Cotton effect (CE) with respect to their normal diagnostic CE. Compounds 1-9 were tested for cytotoxicity against four cell lines (A549, HCT116, SK-HEP-1, and HL-60), and only 1, 3, 5, and 9 showed moderate cytotoxicity, while others were inactive, discovering the 6-carboxyl is crucial for their low cytotoxicity.


Assuntos
Benzopiranos/isolamento & purificação , Flores/química , Rhododendron/química , Terpenos/isolamento & purificação , Linhagem Celular Tumoral , Cromanos/isolamento & purificação , Humanos , Estrutura Molecular
11.
Zhongguo Zhong Yao Za Zhi ; 43(1): 100-108, 2018 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-29552818

RESUMO

Application of a combination of various chromatographic techniques including column chromatography over silica gel, Sephadex LH-20, macroporous adsorbent resin, and reversed-phase HPLC, led to the isolation of 173 compounds including irdidoids, monoterpenes, sesquiterpenes, triterpenes, lignans, flavonoids, and simple aromatic derivatives from the ethyl acetate-soluble fraction of the whole plants of Valeriana jatamansi(Valerianaceae), and their structures were elucidated by spectroscopic methods including 1D, 2D NMR UV, IR, and MS techniques. Among them, 77 compounds were new. In previous reports, we have described the isolation, structure elucidation, and bioactivities of 68 new and 25 known compounds. As a consequence, we herein reported the isolation and structure elucidation of the remaining 9 new and 71 known compounds, the structure revision of valeriotriate A(8a), as well as cytotoxicity of some compounds.


Assuntos
Extratos Vegetais/química , Valeriana/química , Acetatos , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Iridoides/análise , Lignanas/análise , Estrutura Molecular , Monoterpenos/análise , Compostos Fitoquímicos/análise , Sesquiterpenos/análise , Triterpenos/análise
12.
J Exp Bot ; 69(8): 1903-1912, 2018 04 09.
Artigo em Inglês | MEDLINE | ID: mdl-29432591

RESUMO

Hevea brasiliensis is a key commercial source of natural rubber (cis 1,4-polyisoprene). In H. brasiliensis, rubber transferase is responsible for cis-1,4-polymerization of isoprene units from isopentenyl diphosphate and thus affects the yield of rubber. Little is known about the regulatory mechanisms of the rubber transferase gene at a molecular level. In this study we show that the 5'UTR intron of the promoter of the rubber transferase gene (HRT2) suppresses the expression of HRT2. A H. brasiliensis RING zinc finger protein (designated as HbRZFP1) was able to interact specifically with the HRT2 promoter to down-regulate its transcription in vivo. A 14-3-3 protein (named as HbGF14a) was identified as interacting with HbRZFP1, both in yeast and in planta. Transient co-expression of HbGF14a and HbRZFP1-encoding cDNAs resulted in HbRZFP1-mediated HRT2 transcription inhibition being relieved. HbGF14a repressed the protein-DNA binding of HbRZFP1 with the HRT2 promoter in yeast. We propose a regulatory mechanism by which the binding of HbGF14a to HbRZFP1 interferes with the interaction of HbRZFP1 with the HRT2 promoter, thereby repressing the protein-DNA binding between them. This study provides new insights into the role of HbGF14a in mediating expression of the rubber transferase gene in Hevea brasiliensis.


Assuntos
Proteínas 14-3-3/metabolismo , Regulação Enzimológica da Expressão Gênica , Hevea/metabolismo , Proteínas de Plantas/metabolismo , Transferases/genética , Proteínas 14-3-3/química , Proteínas 14-3-3/genética , Sequência de Aminoácidos , Regulação da Expressão Gênica de Plantas , Hevea/química , Hevea/classificação , Hevea/genética , Filogenia , Proteínas de Plantas/química , Proteínas de Plantas/genética , Regiões Promotoras Genéticas , Ligação Proteica , Domínios RING Finger , Borracha/metabolismo , Alinhamento de Sequência , Transferases/química , Transferases/metabolismo , Dedos de Zinco
13.
Fitoterapia ; 125: 117-122, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29307850

RESUMO

Five rare sesquiterpene lactone dimers, vlasouliolides E-I, were isolated from Vladimiria souliei. Their chemical structures were elucidated by spectroscopic analysis. Furthermore, 2 and 4 were unambiguously confirmed by Cu-Kα X-ray crystallographic analysis. Compounds 1, 2, 4 and 5 exhibited significant anti-inflammatory activity against LPS-induced NO production in RAW 264.7 cells with IC50 values of 1.88, 4.89, 7.24 and 2.46µM, respectively. Additionally, compounds 1 and 2 were revealed with potent inhibitory activity of the phosphorylation progress of NF-κB P65.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Asteraceae/química , Lactonas/isolamento & purificação , Sesquiterpenos/isolamento & purificação , Animais , Anti-Inflamatórios/farmacologia , Lactonas/farmacologia , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Raízes de Plantas/química , Células RAW 264.7 , Sesquiterpenos/farmacologia , Fator de Transcrição RelA/metabolismo
14.
J Plant Res ; 131(3): 555-562, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29234988

RESUMO

Dracaena cambodiana is a traditional medicinal plant used for producing dragon's blood. The plants and dragon's blood of D. cambodiana contain a rich variety of steroidal saponins. However, little is known about steroidal saponin biosynthesis and its regulation in D. cambodiana. Here, 122 genes encoding enzymes involved in steroidal saponin biosynthesis were identified based on transcriptome data, with 29 of them containing complete open reading frames (ORF). Transcript expression analysis revealed that several genes related to steroidal saponin biosynthesis showed distinct tissue-specific expression patterns; the expression levels of genes encoding the key enzymes involved in the biosynthesis and early modification of steroidal saponins were significantly down-regulated in the stems in response to the inducer of dragon's blood, exhibiting positive correlations with the content of steroidal saponins. These results provide insights on the steroidal saponins biosynthetic pathway and mechanisms underlying induced formation of dragon's blood in D. cambodiana.


Assuntos
Dracaena/genética , Saponinas/biossíntese , Transcriptoma , Vias Biossintéticas , Dracaena/química , Dracaena/metabolismo , Perfilação da Expressão Gênica , Anotação de Sequência Molecular , Extratos Vegetais/biossíntese , Extratos Vegetais/química , Saponinas/química
15.
Front Plant Sci ; 8: 1974, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29187861

RESUMO

MYB transcription factors hold vital roles in the regulation of plant secondary metabolic pathways. Laticifers in rubber trees (Hevea brasiliensis) are of primary importance in natural rubber production because natural rubber is formed and stored within these structures. To understand the role of MYB transcription factors in the specialized cells, we identified 44 MYB genes (named HblMYB1 to HblMYB44) by using our previously obtained transcriptome database of rubber tree laticifer cells and the public rubber tree genome database. Expression profiles showed that five MYB genes were highly expressed in the laticifers. HblMYB19 and HblMYB44 were selected for further study. HblMYB19 and HblMYB44 bound the promoters of HbFDPS1, HbSRPP, and HRT1 in yeast. Furthermore, the transient overexpression of HblMYB19 and HblMYB44 in tobacco plants significantly increased the activity of the promoters of HbFDPS1, HbSRPP, and HRT1. Basing on this information, we proposed that HblMYB19 and HblMYB44 are the regulators of HbFDPS1, HbSRPP, and HRT1, which are involved in the biosynthesis pathway of natural rubber.

16.
Shanghai Kou Qiang Yi Xue ; 26(4): 409-413, 2017 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-29199336

RESUMO

PURPOSE: To investigate the expression of Smad4, Smad7 and Caveolin-1 in the process of carcinogenesis of oral mucosa in Wistar rats, and to understand the changes of TGF-ß/Smad signaling pathway and Caveolin-1 in oral cancer. METHODS: Palatal mucosal carcinogenesis specimens of Wistar rats were obtained from School of Stomatology, Zhengzhou University, which included 5 samples of normal mucosa, 10 samples of simple hyperplasia mucosa, 6 samples of mild mucosal dysplasia, 7 samples of moderate mucosal dysplasia, 13 samples of mucosa severe mucosal dysplasia, and 28 samples of oral cancer tissue. The expression of Smad4, Smad7 and Caveolin-1 was detected by immunohistochemistry. SPSS15.0 software package was used for statistical analysis. RESULTS: The expression of Smad4 decreased in normal and hyperplastic epithelia, dysplasticepithelia and oral cancer gradually, the difference of the expression among the three groups was significant (P<0.05). The expression of Smad7 and Caveolin-1 increased in normal and hyperplastic epithelia, dysplasticepithelia and oral cancer gradually, respectively; the difference of the expression among the 3 groups was significant (P<0.05). Spearman correlation analysis showed that Smad4 was negatively correlated with Smad7, Smad4 was negatively correlated with caveolin-1, Smad7 was positively correlated with Caveolin-1 (P<0.05). CONCLUSIONS: Synergistic effects may exist among Smad4, Smad7 and caveolin-1 in carcinogenesis of oral cancer.


Assuntos
Caveolina 1 , Mucosa Bucal , Neoplasias Bucais , Proteína Smad4 , Proteína Smad7 , Animais , Carcinogênese , Caveolina 1/genética , Caveolina 1/metabolismo , Mucosa Bucal/metabolismo , Neoplasias Bucais/genética , Neoplasias Bucais/metabolismo , Ratos , Ratos Wistar , Transdução de Sinais , Proteína Smad4/metabolismo , Proteína Smad7/metabolismo , Fator de Crescimento Transformador beta
17.
Fitoterapia ; 119: 90-99, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28408269

RESUMO

Two new eudesmane sesquiterpenoids, chlorajaponols A-B (1-2), two new guaiane sesquiterpenoids, chlorajaponols C-D (3-4), a new germacrane sesquiterpenoid, chlorajaponol E (5), and a new lindenane sesquiterpenoid, chlorajaponol F (6), along with 8 known sesquiterpenoids and 6 known disesquiterpenoids, were isolated from the whole plant of Chloranthus japonicus. Their structures were established by extensive analysis of NMR spectroscopic data in combination with mass spectrometry. The structures of compounds 1-4 were confirmed by single crystal X-ray diffraction (CuKα radiation). The possible biogenetic pathways of compounds 1-6 were discussed. Chlorajaponol B (2) showed significant inhibition against nitric oxide (NO) release in LPS-induced RAW264.7 macrophages with the IC50 value of 9.56±0.71µM, comparable to that of positive control amino guanidine (8.50±0.35µM). Shizukaol C (18) strongly suppressed the proliferation of three human tumor cell lines MGC803, HepG2, and HL-60 with IC50 values of 4.60±1.05µM, 3.17±0.66µM, and 1.57±0.27µM, respectively.


Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Magnoliopsida/química , Sesquiterpenos de Eudesmano/farmacologia , Sesquiterpenos de Guaiano/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Humanos , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Células RAW 264.7 , Sesquiterpenos de Eudesmano/isolamento & purificação , Sesquiterpenos de Guaiano/isolamento & purificação
18.
Sci Rep ; 7: 45157, 2017 03 23.
Artigo em Inglês | MEDLINE | ID: mdl-28332623

RESUMO

Abscisic acid (ABA) is an essential phytohormone involved in diverse physiological processes. Although genome-wide analyses of the ABA receptor PYR/PYL/RCAR (PYL) protein/gene family have been performed in certain plant species, little is known about the ABA receptor protein/gene family in the rubber tree (Hevea brasiliensis). In this study, we identified 14 ABA receptor PYL proteins/genes (designated HbPYL1 through HbPYL14) in the most recent rubber tree genome. A phylogenetic tree was constructed, which demonstrated that HbPYLs can be divided into three subfamilies that correlate well with the corresponding Arabidopsis subfamilies. Eight HbPYLs are highly expressed in laticifers. Five of the eight genes are simultaneously regulated by ABA, jasmonic acid (JA) and ethylene (ET). The identification and characterization of HbPYLs should enable us to further understand the role of ABA signal in the rubber tree.


Assuntos
Proteínas de Arabidopsis/genética , Regulação da Expressão Gênica de Plantas , Hevea/genética , Hevea/metabolismo , Família Multigênica , Reguladores de Crescimento de Planta/metabolismo , Motivos de Aminoácidos , Sequência de Aminoácidos , Sequência Conservada , Evolução Molecular , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Estudo de Associação Genômica Ampla , Hevea/classificação , Filogenia , Reguladores de Crescimento de Planta/farmacologia , Regiões Promotoras Genéticas , Borracha/metabolismo , Transcriptoma
19.
Sci Rep ; 7: 43837, 2017 03 03.
Artigo em Inglês | MEDLINE | ID: mdl-28256560

RESUMO

Vlasouliolides A-D (1-4), four rare sesquiterpene lactone dimers, were isolated from Vladimiria souliei. The common structural characteristic of 1-4 is the C32 skeleton comprising two sesquiterpene lactone units linked by a C11-C13' single bond with one acetyl connected to the C-13 position of one of the two sesquiterpene lactone units. The stereochemistries of 1-4 were assigned by a combination of NOESY correlations and Cu-Κα X-ray crystallographic analyses. Compounds 1-4 strongly inhibited the production of NO in LPS-stimulated RAW 264.7 cells. Furthermore, 1 and 2 inhibited the activation of NF-κB in LPS-induced 293T cells.


Assuntos
Anti-Inflamatórios/farmacologia , Asteraceae/química , Lactonas/farmacologia , Sesquiterpenos/farmacologia , Animais , Anti-Inflamatórios/química , Cristalografia por Raios X , Dimerização , Células HEK293 , Humanos , Lactonas/química , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Células RAW 264.7 , Sesquiterpenos/química
20.
J Ethnopharmacol ; 196: 39-46, 2017 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-27988396

RESUMO

BACKGROUNDS: Inula helenium L. is an herb with anti-inflammatory properties. Sesquiterpene lactones (SLs), mainly alantolactone (AL) and isoalantolactone (IAL), are considered as its active ingredients. However, the anti-inflammatory effects of SL-containing extracts of I. helenium have not been explored. Here we prepared total SLs from I. helenium (TSL-IHL), analyzed its chemical constituents, and performed cellular and animal studies to evaluate its anti-inflammatory activities. MATERIALS AND METHODS: The chemical profile of TSL-IHL was analyzed by HPLC-UV. Its in vitro effects on the activation of signaling pathways and expression of inflammatory genes were examined by western blotting and quantitative real-time PCR, respectively, and compared with those of AL and IAL. Its in vivo anti-inflammatory effects were evaluated in adjuvant- and collagen-induced arthritis rat models. RESULTS: Chemical analysis showed that AL and IAL represent major constituents of TSL-IHL. TSL-IHL, as well as AL and IAL, could inhibit TNF-α-induced activation of NF-κB and MAPK pathways in b. End3 cells, suppress the expressions of MMP-3, MCP-1, and IL-1 in TNF-α-stimulated synovial fibroblasts, and IL-1, IL-6, and iNOS in LPS-activated RAW 264.7 cells in a dose-dependent manner in the range of 0.6-2.4µg/mL. Oral administration of TSL-IHL at 12.5-50mg/kg could dose-dependently alleviate the arthritic severity and paw swelling in either developing or developed phases of arthritis of rats induced by adjuvant or collagen CONCLUSIONS: These results indicated potentials of TSL-IHL in prevention and therapy of rheumatoid arthritis.


Assuntos
Anti-Inflamatórios/uso terapêutico , Artrite Experimental/tratamento farmacológico , Artrite Reumatoide/tratamento farmacológico , Inula , Lactonas/uso terapêutico , Sesquiterpenos/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Artrite Experimental/metabolismo , Artrite Experimental/prevenção & controle , Artrite Reumatoide/metabolismo , Artrite Reumatoide/prevenção & controle , Linhagem Celular , Citocinas/genética , Citocinas/metabolismo , Lactonas/farmacologia , Masculino , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , NF-kappa B/metabolismo , Raízes de Plantas , Células RAW 264.7 , Ratos Wistar , Sesquiterpenos/farmacologia
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