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1.
Phytochemistry ; 174: 112337, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32163787

RESUMO

Four undescribed sulfur-containing indole alkaloids, isatisindigoticanines H, I and isatindigosides F, G along with three known analogues were obtained from Isatis tinctoria L. roots. Isatisindigoticanines H and I contained an unusual 1-(thiazol-4-yl)butane-1,2,3,4-tetraol moiety while isatindigosides F and G possessed a new 3-[3-(1H-indole-2-yl)azet-2-yl]-1H-indole skeleton. The putative biosynthetic pathways of isatisindigoticanines H, I and isatindigosides F, G are proposed. The isolated compounds showed nitric oxide inhibitory effects with IC50 values ranging from 4.3 to 70.3 µM.


Assuntos
Isatis , Alcaloides Indólicos , Estrutura Molecular , Óxido Nítrico , Raízes de Plantas , Enxofre
2.
Chemosphere ; 239: 124523, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31499308

RESUMO

Arsenic (As) is a toxic metalloid that severely hampers plant growth and also poses health risks for humans through the food chain. Although nitric oxide (NO) is known to improve plant resistance to multiple stresses including metal toxicity, little is known about its role in the As tolerance of hyperaccumulator plants. This study investigates the role of the exogenously applied NO donor, sodium nitroprusside (SNP), in improving the As tolerance of Isatis cappadocica, which has been reported to hyperaccumulate As. Exposure to toxic As concentrations significantly increases NO production and damages the cell membrane, as indicated by increased hydrogen peroxide (H2O2) and malondialdehyde (MDA) concentrations, thereby reducing plant growth. However, the addition of SNP improves growth and alleviates As-induced oxidative stress by enhancing the activity of superoxide dismutase (SOD), ascorbate peroxidase (APX), glutathione reductase (GR), glutathione S-transferase (GST), glutathione (GSH), as well as proline and thiol concentrations, thereby confirming the beneficial role played by NO in increasing As stress tolerance. Furthermore, the As-induced decrease in growth and the increase in oxidative stress were more marked in the presence of bovine hemoglobin (Hb; a NO scavenger) and N(G)-nitro-l-arginine methyl ester (l-NAME; a NO synthase inhibitor), thus demonstrating the protective role of NO against As toxicity. The reduction in NO concentrations by l-NAME suggests that NOS-like activity is involved in the generation of NO in response to As in I. cappadocica.


Assuntos
Antioxidantes/metabolismo , Arsênico/toxicidade , Isatis/efeitos dos fármacos , Óxido Nítrico/metabolismo , Nitroprussiato/farmacologia , Animais , Ascorbato Peroxidases/metabolismo , Bovinos , Membrana Celular/patologia , Glutationa/metabolismo , Glutationa Redutase/metabolismo , Peróxido de Hidrogênio/metabolismo , Isatis/metabolismo , Malondialdeído/metabolismo , Doadores de Óxido Nítrico , Estresse Oxidativo/efeitos dos fármacos , Superóxido Dismutase/metabolismo
3.
Planta Med ; 85(17): 1374-1382, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31801158

RESUMO

Six pairs of alkaloid enantiomers including 11 new alkaloids (1A: /1B: -5A: /5B, 6A: ) were isolated from the leaves of Isatis tinctoria. Their structures were established by extensive spectroscopic analyses. Enantiomers were separated successfully by chiral chromatographic column and the absolute configurations of all isolates were determined by comparison of experimental and calculated electronic circular dichroism spectra. The isolated alkaloids were evaluated for their neuroprotective activities against H2O2-induced cell injury in human neuroblastoma SH-SY5Y cells. The results showed that 5A/5B: and 6A/6B: exhibited potent neuroprotective activities at 50 µM compared with the H2O2-treated group.


Assuntos
Isatis/química , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Linhagem Celular Tumoral , Humanos , Peróxido de Hidrogênio , Isomerismo , Estrutura Molecular , Neuroblastoma , Neurônios/efeitos dos fármacos , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
4.
Molecules ; 24(22)2019 Nov 07.
Artigo em Inglês | MEDLINE | ID: mdl-31703370

RESUMO

As our ongoing research project on Ban Lan Gen (Isatis tinctoria roots), a total of 23 alkaloids were obtained. Compounds 1 and 2 contain an unusual C-C bond between the 2(1H)-quinolinone moiety and the phenol moiety and between the 2(1H)-quinolinone moiety and the 1H-indole moiety, respectively. Compound 3 possesses an unusual carbon skeleton and its putative biosynthetic pathway was discussed, and Compound 23 was deduced as a new indole alkaloid glycoside. Compounds 4-7 were identified as four new natural products by extensive spectroscopic experiments. Additionally, the anti-inflammatory activity was assessed based on nitric oxide (NO) production using Lipopolysaccharide-stimulated RAW264.7 macrophages. Compounds 9, 15, and 17 showed inhibitory effects with IC50 values of 1.2, 5.0, and 74.4 µM.


Assuntos
Alcaloides/química , Alcaloides/isolamento & purificação , Isatis/química , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/química , Raízes de Plantas/química
5.
Anim Reprod Sci ; 210: 106178, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31635774

RESUMO

Liquid preservation of boar semen is a preferred method in pig husbandry, and antioxidants to protect against sperm oxidative stress during periods of storage have become the focus of recent research. Through its antioxidant activity, Isatis root polysaccharide (IRPS), a plant extract, can effectively reduce the cellular lipid peroxidation caused by the accumulation of reactive oxygen species inside mitochondria. In the present study, there was examination of the effects of no supplementation (Control) of a semen extender with or supplementation in different concentrations of IRPS (0.2, 0.4, 0.6, 0.8, and 1.2 mg/mL) on sperm quality variables and antioxidant capacity during liquid storage. The results indicate that after prolonged storage (≥ 3 days), the sperm motility was greater in the group supplemented with 0.6 mg/mL IRPS than in the other groups (P < 0.05). The use of this IRPS concentration also resulted in maintanence of acrosome integrity, plasma membrane integrity, mitochondrial membrane potential, and antioxidant capacity of the sperm (P < 0.05). Furthermore, the results of an in vitro fertilization study indicate IRPS at 0.6 mg/mL markedly increased the sperm fertilization capacity (P < 0.01) and embryonic development to the blastocyst stage (P < 0.05). The addition of 0.6 mg/mL IRPS enhanced the antioxidant capacity of boar sperm, resulting in greater preservation of sperm motility and fertilization capacity during liquid storage. These findings indicate that IRPS has the potential to be used as a component of a semen-preserving diluent to maintain sperm quality during storage.


Assuntos
Isatis/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Polissacarídeos/farmacologia , Espermatozoides/efeitos dos fármacos , Suínos , Animais , Membrana Celular/efeitos dos fármacos , Fertilização In Vitro/veterinária , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Extratos Vegetais/química , Polissacarídeos/química , Preservação do Sêmen/veterinária , Motilidade Espermática/efeitos dos fármacos
6.
Molecules ; 24(17)2019 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-31470525

RESUMO

Five pairs of alkaloid enantiomers (1a/1b-5a/5b) were obtained from Isatis indigotica (I. indigotica) roots. Among them, 1a/1b, 2a/2b and 3a/3b were determined as three pairs of new alkaloid enantiomers. Their structures were elucidated by physicochemical properties and spectroscopic methods. The absolute configurations were deduced by comparison of their experimental circular dichroism (CD) and calculated electronic circular dichroism (ECD) spectra, as well as by single-crystal X-ray crystallography using anomalous scattering of Cu Kα radiation. Alkaloids 1a and 1b possess an unpresented carbon skeleton and their putative biosynthetic pathways are discussed. Moreover, all of the alkaloids were tested for their nitric oxide (NO) inhibitory effects in RAW 264.7 cells, and 4a and 4b showed inhibitory effects with IC50 values of 76.97 µM and 65.88 µM, respectively.


Assuntos
Alcaloides/química , Anti-Inflamatórios/química , Isatis/química , Lipopolissacarídeos/antagonistas & inibidores , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Relação Dose-Resposta a Droga , Lipopolissacarídeos/farmacologia , Camundongos , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Extratos Vegetais/química , Raízes de Plantas/química , Células RAW 264.7 , Estereoisomerismo
7.
Phytochemistry ; 166: 112058, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31280093

RESUMO

Isatis indigotica Fortune is a popular herb in traditional Chinese medicine, and various types of metabolites are the basis for its pharmacological efficacy. The biosynthesis and accumulation of these metabolites are closely linked to nitrogen availability; the benefits of low nitrogen application on the environment and herb quality are increasingly prominent. To analyze metabolic changes in the leaves and roots of I.indigotica in nitrogen deficiency conditions, and to identify the pathways and metabolites induced by low nitrogen availability, we used untargeted liquid chromatography coupled with mass spectrometry (UHPLC-TripleTOF) to obtain metabolomics profiling of I.indigotica under two N-deficiency treatments (0 kg/hm2; 337.5 kg/hm2) and normal nitrogen treatment (675 kg/hm2). A total of 447 metabolites were annotated. Principal component analysis separated the three nitrogen treatments. A greater diversity of metabolites was observed in roots than in leaves under N-deficiency treatments, suggesting that roots have a more important function in low N tolerance. Differential metabolites were mainly enriched in purine metabolism, phenylpropanoid biosynthesis, the shikimate pathway, tryptophan metabolism, and flavonoid biosynthesis that notably induced only in leaves in low nitrogen stress. Moderate N-deficiency benefits carbohydrate accumulation, whereas accumulation of most amino acids decreases. Uniquely, L-tryptophan was maintained at a high concentration in N-deficiency conditions. Low nitrogen stress induced the accumulation of some specialized metabolites (matairesinol, dictamnine, 5-hydroxyindoleacetate (serotonin) in roots and vitexin, xanthohumol, sinapyl alcohol in leaves). N-deficiency also increased the accumulation of adenosine and quality indicators of I.indigotica (indirubin-indigo, epigoitrin and anthranilic acid) in a certain degree. Our findings showed that nitrogen deficiency modified roots and leaves conditions of I.indigotica, affecting both the primary and secondary metabolism. Moderate nitrogen reduction was beneficial to the accumulation of active ingredients. Our methods and analysis are expected to provide an insight regarding the diversity of metabolites and regulation of their synthesis in low nitrogen application, and better investigate the nitrogen deficiency effect on I.indigotica.


Assuntos
Isatis/metabolismo , Metabolômica , Nitrogênio/deficiência , Cromatografia Líquida , Espectrometria de Massas
8.
Gene ; 713: 143974, 2019 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-31301484

RESUMO

An orthologous gene of SEPALLATA1, designated as IiSEP1, was isolated from Isatis indigotica. The genomic DNA of IiSEP1 is 3.1 Kb in length. The full-length cDNA of IiSEP1 is 1481 bp and contains a 756 bp ORF encoding a 251-amino-acid protein. Sequence comparison revealed that IiSEP1 belonged to the MADS-box gene family. IiSEP1 contains 7 exons and 6 introns, showing similar exon-intron structure with Arabidopsis SEP1. Phylogenetic analysis suggested that IiSEP1 belonged to AGL2/SEP subfamily and was likely to be an I. indigotica ortholog of Arabidopsis SEP1. Quantitative real-time PCR showed that IiSEP1 was predominantly expressed in the reproductive organs. Ectopic expression of IiSEP1 in Arabidopsis resulted in early flowering, accompanied with the reduction of inflorescence number and the production of terminal flower on the top of the main stems. Moreover, IiSEP1 overexpressing flowers generated numerous variations in phenotype. The sepals were changed into petal-sepal mosaic structures or displayed carpelloid features, and transparent ovules were formed in internal surface of these sepals. In addition, some flowers were constituted by sepals and pistil, but lacked petals and stamens. Taken together, IiSEP1 might play important roles in reproductive growth of I. indigotica and could affect the morphogenesis of flowers and fruits.


Assuntos
Arabidopsis/crescimento & desenvolvimento , Flores/crescimento & desenvolvimento , Fatores de Transcrição Forkhead/genética , Isatis/crescimento & desenvolvimento , Proteínas de Plantas/genética , Plantas Geneticamente Modificadas/crescimento & desenvolvimento , Proteínas de Schizosaccharomyces pombe/genética , Sequência de Aminoácidos , Arabidopsis/genética , Flores/genética , Regulação da Expressão Gênica de Plantas , Isatis/genética , Proteínas de Domínio MADS/genética , Fenótipo , Plantas Geneticamente Modificadas/genética , Homologia de Sequência
9.
Fitoterapia ; 137: 104189, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31158429

RESUMO

Seventeen lignans (1-17) were obtained from the roots of Isatis indigotica (I. indigotica). Among them, isatindigosesquilignans A-C (1-3) were deduced as three undescribed sesquilignans, which possess unusual carbon skeleton of aryltetralin unit connected with a C6-C3 moiety via a five-membered ring of C-3-C-8″-C-7″-O-C-4. Isatindigosesquilignans B and C were determined as the first examples of its glycosides from a natural source and a plausible biosynthetic pathway was proposed. Moreover, all of the isolated lignans were assayed regarding their inhibitory effects on nitric oxide (NO) production in RAW 264.7 cells and compounds 1, 2 and 7 showed inhibitory effects with IC50 values ranging from 19.46 µM to 64.82 µM.


Assuntos
Isatis/química , Lignanas/farmacologia , Macrófagos/efeitos dos fármacos , Óxido Nítrico/metabolismo , Animais , China , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Lignanas/isolamento & purificação , Camundongos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Raízes de Plantas/química , Células RAW 264.7
10.
Environ Sci Pollut Res Int ; 26(21): 21704-21716, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31129904

RESUMO

A hydroponic experiment was conducted to explore the interactive effects of selenium (Se) supplementation (0, 5, and 10 µM) and arsenic (As) toxicity (0, 200, and 400 µM) on the growth, accumulation, and oxidative damage along with defense mechanisms of metallicolous (MP) and non-metallicolous population (NMP) of Isatis cappadocica, an As-hyperaccumulator, and Brassica oleracea as reference brassica. The results revealed that As stress significantly hampered plant growth particularly in B. oleracea. It reduced plant growth due to enhanced oxidative load of As-stressed plants. Between the two Isatis populations, metallicolous plants accumulated significantly higher As, however with considerably low growth defects. Furthermore, Se supplementation counteracted the adverse effects of stress on growth and physiological performance of all studied plants. Addition of Se, particularly at higher dose (10 µM), significantly suppressed root As uptake and slightly its accumulation in shoots of B. oleracea plants treated with 400 µM As, and thus improved growth characteristics of stressed plants. Under As stress, Se supplementation increased the activities of enzymatic (peroxidase (POD) and glutathione reductase (GR)) and non-enzymatic (anthocyanins and total flavonoids) antioxidants, thereby suggesting relieved As stress by reduced oxidative damage. Taken together, these results support the beneficial role of Se in the regulation of As stress by improving growth, physiology, and antioxidant capacity, and highlight its significance for plants grown on such metal-contaminated soils.


Assuntos
Arsênico/toxicidade , Brassica/fisiologia , Isatis/fisiologia , Selênio/metabolismo , Poluentes do Solo/toxicidade , Antioxidantes/metabolismo , Brassica/metabolismo , Glutationa Redutase/metabolismo , Oxirredução , Peroxidase
11.
Dermatol Ther ; 32(4): e12939, 2019 07.
Artigo em Inglês | MEDLINE | ID: mdl-30990240

RESUMO

Objective of this open, noninterventional, noncontrolled study was to investigate the tolerability and performance of a woad extract containing cream in subjects with dry, pruritic skin after twice daily application over 2 weeks. Assessments included sensorial characteristics, skin condition, pruritus (numeric rating scale [NRS], dynamic pruritus score [DPS]), skin dryness (itch-controlled days [ItchCD], overall dry skin [ODS]), transepidermal water loss (TEWL), skin hydration and quality of life (5PLQ, DLQI). All sensorial characteristics were well perceived (>4), with tolerability (4.77 ± 0.47) and no negative skin feelings (4.73 ± 0.74) achieving the highest scores (0-5 scale). Dry skin and symptoms improved significantly (p < .001) for all variables: NRS (from 4.8 ± 1.74 to 1.83 ± 2.18), ItchCD (from 8.23 ± 4.40 to 4.81 ± 4.07), ODS (from 1.80 ± 0.85 to 0.65 ± 0.65), hydration (23.33 ± 1.33 to 40.70 ± 1.86), and quality of life (5PLQ: from 7.12 ± 4.25 to 4.24 ± 3.67; DLQI: from 5.29 ± 4.79 to 3.00 ± 3.98). The DPS revealed a moderate antipruritic effect. The TEWL decreased slightly (p = .511). No side effects were reported. The study suggests that, the cream is effective, and well tolerated in treating dry, irritated, and pruritic skin.


Assuntos
Isatis/química , Extratos Vegetais/administração & dosagem , Prurido/tratamento farmacológico , Dermatopatias/tratamento farmacológico , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Extratos Vegetais/efeitos adversos , Estudos Prospectivos , Prurido/patologia , Qualidade de Vida , Creme para a Pele , Dermatopatias/patologia , Resultado do Tratamento
12.
Phytochemistry ; 163: 89-98, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31035058

RESUMO

The pharmacologically active dichloromethane extracts of dried woad leaves (Isatis tinctoria L.), and the methanol extracts of comparable fresh leaves of the same plants, were analyzed by LC-MSn. The fresh leaf metabolite profile revealed a complex pattern of indolic compounds. Besides the known indigo precursors, isatan A, isatan B and indican, seven previously unreported indole derivatives were characterized: acetylindican, malonylindican, two dioxindole glucosides, dioxindole malonylglucoside, 6-hydroxyindole-3-carboxylic acid 6-O-glucoside and 6-hydroxyindole-3-carboxylic acid glucose ester. The integration of 122 compounds in fresh leaves and of five selected compounds (indoxyl, isatin, indigo, indirubin, and tryptanthrin) in dried leaves, formed the input data for a stepwise modelling procedure generating five predictive linear models. The structure of the predictive models and a cross validation provide evidence that the models could predict well or moderately well the accumulation of the selected lipophilic compounds, and were simple enough to be used in a woad cultivation program. PLS regression models relating each of the five selected dry leaf indolics to the fresh leaf metabolome were then fitted in order to deduct potential precursors and mechanisms leading to the formation of these lipophilic indolics in drying woad leaves. The models suggested glucobrassicin, isatan A and isatan B as the main candidate precursors of these compounds, besides a minor contribution of other fresh leaf indolics, including malonylindican, actylindican and dioxindole malonylglucoside. Dioxindole malonylglucoside was identified here as isatan C. The models further suggested that the accumulation of phenylpropanoid antioxidants in woad leaves has a negative impact on the formation of indoxyl, isatin, indigo, indirubin and tryptanthrin.


Assuntos
Alcaloides Indólicos/metabolismo , Isatis/química , Folhas de Planta/química , Biomarcadores/análise , Biomarcadores/metabolismo , Interações Hidrofóbicas e Hidrofílicas , Alcaloides Indólicos/análise , Isatis/metabolismo , Estrutura Molecular , Folhas de Planta/metabolismo
13.
BMC Mol Biol ; 20(1): 9, 2019 03 25.
Artigo em Inglês | MEDLINE | ID: mdl-30909859

RESUMO

BACKGROUND: Isatis indigotica, a traditional Chinese medicine, produces a variety of active ingredients. However, little is known about the key genes and corresponding expression profiling involved in the biosynthesis pathways of these ingredients. Quantitative real-time polymerase chain reaction (qRT-PCR) is a powerful, commonly-used method for gene expression analysis, but the accuracy of the quantitative data produced depends on the appropriate selection of reference genes. RESULTS: In this study, the systematic analysis of the reference genes was performed for quantitative real-Time PCR normalization in I. indigotica. We selected nine candidate reference genes, including six traditional housekeeping genes (ACT, α-TUB, ß-TUB, UBC, CYP, and EF1-α), and three newly stable internal control genes (MUB, TIP41, and RPL) from a transcriptome dataset of I. indigotica, and evaluated their expression stabilities in different tissues (root, stem, leaf, and petiole) and leaves exposed to three abiotic treatments (low-nitrogen, ABA, and MeJA) using geNorm, NormFinder, BestKeeper, and comprehensive RefFind algorithms. The results demonstrated that MUB and EF1-α were the two most stable reference genes for all samples. TIP41 as the optimal reference gene for low-nitrogen stress and MeJA treatment, while ACT had the highest ranking for ABA treatment and CYP was the most suitable for different tissues. CONCLUSIONS: The results revealed that the selection and validation of appropriate reference genes for normalizing data is mandatory to acquire accurate quantification results. The necessity of specific internal control for specific conditions was also emphasized. Furthermore, this work will provide valuable information to enhance further research in gene function and molecular biology on I. indigotica and other related species.


Assuntos
Perfilação da Expressão Gênica/normas , Regulação da Expressão Gênica de Plantas/genética , Genes Essenciais/genética , Isatis/genética , Reação em Cadeia da Polimerase em Tempo Real/normas , Padrões de Referência
14.
J Exp Clin Cancer Res ; 38(1): 49, 2019 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-30717771

RESUMO

BACKGROUND: The JAK2-STAT signaling pathway plays a critical role in myeloproliferative neoplasms (MPN). An activating mutation in JAK2 (V617F) is present in ~ 95% of polycythemia vera, essential thrombocythemia, and primary myelofibrosis cases. This study aims to explore the selective JAK2V617F inhibitor, evaluate the efficacy and possible mechanism of ZT55 on MPN. METHODS: HTRF assays were conducted to evaluate the selective inhibition of ZT55 for JAKs. Cell apoptosis, proliferation, and cycle arrest assays were performed to examine the effect of ZT55 on HEL cell line with JAK2V617F mutation in vitro. Western analysis was used to monitor the expression and activity of proteins on JAK2/STAT pathway. A mice xenograft model was established to evaluate the antitumor efficacy of ZT55 in vivo. Peripheral blood samples from patients with the JAK2V617F mutation were collected to estimate the effect of ZT55 on erythroid colony formation by colony-forming assay. RESULTS: We found that ZT55 showed a selective inhibition of a 0.031 µM IC50 value against JAK2. It exhibited potent effects on the cellular JAK-STAT pathway, inhibiting tyrosine phosphorylation in JAK2V617F and downstream STAT3/5 transcription factors. ZT55 inhibited the proliferation of the JAK2V617F-expressing HEL cell line, leading to cell cycle arrest at the G2/M phase and induction of caspase-dependent apoptosis. Notably, ZT55 also significantly suppressed the growth of HEL xenograft tumors in vivo. Further evaluation indicated that ZT55 blocked erythroid colony formation of peripheral blood hematopoietic progenitors from patients carrying the JAK2V617F mutation. CONCLUSION: These results suggest that ZT55 is a highly-selective JAK2 inhibitor that can induce apoptosis of human erythroleukemia cells by inhibiting the JAK2-STAT signaling.


Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Janus Quinase 2/antagonistas & inibidores , Transtornos Mieloproliferativos/tratamento farmacológico , Inibidores de Proteínas Quinases/uso terapêutico , Animais , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/farmacologia , Feminino , Humanos , Isatis/química , Janus Quinase 2/sangue , Janus Quinase 2/genética , Masculino , Camundongos , Camundongos Nus , Transtornos Mieloproliferativos/sangue , Transtornos Mieloproliferativos/genética , Células-Tronco Neoplásicas/efeitos dos fármacos , Mutação Puntual , Inibidores de Proteínas Quinases/administração & dosagem , Inibidores de Proteínas Quinases/farmacologia , Fator de Transcrição STAT3/metabolismo , Fator de Transcrição STAT5/metabolismo , Ensaios Antitumorais Modelo de Xenoenxerto
15.
Chem Biodivers ; 16(3): e1800579, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30557446

RESUMO

Leaves of the plant species Isatis indigotica Fortune ex Lindl. (Chinese woad) produce the metabolites tryptanthrin, indirubin and N-formylanthranilic acid upon spraying with an aqueous solution of copper chloride but not after spraying with water. The antifungal activities of these metabolites against the phytopathogens Alternaria brassicicola, Leptosphaeria maculans and Sclerotinia sclerotiorum established that tryptanthrin is a much stronger growth inhibitor of L. maculans than the phytoalexin camalexin. The biosynthetic precursors of tryptanthrin and N-formylanthranilic acid are proposed based on the deuterium incorporations of isotopically labeled compounds. The overall results suggest that tryptanthrin is a phytoalexin and indirubin and N-formylanthranilic acid are phytoanticipins in the plant species I. indigotica and that chemical diversity and biodiversity are intimately connected.


Assuntos
Alternaria/efeitos dos fármacos , Antifúngicos/farmacologia , Ascomicetos/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Isatis/química , Quinazolinas/farmacologia , ortoaminobenzoatos/farmacologia , Antifúngicos/química , Antifúngicos/isolamento & purificação , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Indóis/química , Indóis/isolamento & purificação , Indóis/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Quinazolinas/química , Quinazolinas/isolamento & purificação , Relação Estrutura-Atividade , ortoaminobenzoatos/química , ortoaminobenzoatos/isolamento & purificação
16.
Org Biomol Chem ; 16(48): 9430-9439, 2018 12 12.
Artigo em Inglês | MEDLINE | ID: mdl-30511067

RESUMO

Four pairs of new spiropyrrolizidine oxindole enantiomers (1a/1b-4a/4b) were isolated from the leaves of Isatis indigotica Fortune. Their structures and absolute configurations were elucidated by a combination of NMR spectroscopic analyses, experimental and calculated electronic circular dichroism (ECD) and the assistance of quantum chemical predictions (QCP) of 13C NMR chemical shifts. Notably, all the isolated spiropyrrolizidine oxindoles are reported as natural products for the first time. The biosynthetic pathway of these unique structures was proposed to be formed by cycloaddition reaction. In addition, all the compounds were evaluated for their inhibitory effects on ß-amyloid aggregation by ThT assay, and the optically pure compounds 1a/1b and 2a/2b exhibited better Aß1-42 aggregation inhibition potency (85.8% and 73.6%, 71.5% and 75.8%, respectively) at a concentration of 20 µM, compared with the positive control curcumin (57.0%). The difference of the inhibitory pattern caused by chirality was also explained by molecular docking studies.


Assuntos
Isatis/química , Oxindois/química , Alcaloides de Pirrolizidina/química , Compostos de Espiro/química , Peptídeos beta-Amiloides/metabolismo , Humanos , Simulação de Acoplamento Molecular , Oxindois/isolamento & purificação , Oxindois/farmacologia , Fragmentos de Peptídeos/metabolismo , Agregados Proteicos/efeitos dos fármacos , Alcaloides de Pirrolizidina/isolamento & purificação , Alcaloides de Pirrolizidina/farmacologia , Compostos de Espiro/isolamento & purificação , Compostos de Espiro/farmacologia , Estereoisomerismo
17.
Zhongguo Zhong Yao Za Zhi ; 43(10): 2091-2096, 2018 May.
Artigo em Chinês | MEDLINE | ID: mdl-29933676

RESUMO

Nineteen compounds were isolated from the roots of Isatis indigotica through silica gel, Sephadex LH-20, ODS and pre-HPLC chromatography technique. Their structures were elucidated by the MS and NMR spectra as 7-hydroxydeoxyvasicinone (1), (1H-indol-3-yl) oxoacetamide (2), 1-methoxy-1H-indole-3-acetonitrile (3), arvelexin (4), 1H-indole-3-acetonitrile (5), 1H-indole-3-aldehyde (6), 1H-indole-3-acetic acid (7), 2,3-dihydro-4-hydroxy-2-oxo-indole-3-acetonitrile (8), deoxyvasicinone (9), indigotiisocoumarin A (10), cycloanthranilylproline (11), quinazoline-2,4(1H,3H)-diones (12), indirubin(13), (+)-pinoresinol (14), (+)-epipinoresinol (15), burselignan (16), (+)-isolariciresinol (17),vanillic acid (18) and 5-hydroxymaltol (19). Among them, compound 1 is a new natural product, and compound 2, 14, 15, 18 and 19 were isolated from the title plant for the first time.


Assuntos
Isatis/química , Compostos Fitoquímicos/análise , Raízes de Plantas/química
18.
Zhongguo Zhong Yao Za Zhi ; 43(11): 2242-2245, 2018 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-29945374

RESUMO

To detect possible pathogenic virus(es) in woad (Isatis tinctoria) cultivated at Institute of Medicinal Plant Development in Beijing, reverse transcription(RT)-PCR was performed using total RNA of symptomatic woad leaves with primers for poty-, polero-, tobamovirus, broad bean wilt virus 2(BBWV2) and cucumber mosaic virus (CMV). A 657 bp fragment was amplified from symptomatic woad using CMV primers. Sequencing and BLAST analysis indicated that this fragment shared 99% nucleotide identity and 100% amino acid identity with CMV-Vi isolate. The isolate was named CMV-Isatis tinctorial (CMV-It). Phylogenetic analysis based on nucleotide sequences of CP genes showed that CMV-It clustered with CMV-K and belonged to subgroup I. To our knowledge, this is first identification of CMV in woad by RT-PCR and the CP gene was analyzed. This work provided data for research and control of woad mosaic disease.


Assuntos
Cucumovirus/classificação , Isatis/virologia , Doenças das Plantas/virologia , Sequência de Bases , Pequim , Cucumovirus/isolamento & purificação , Filogenia
19.
Zhongguo Ying Yong Sheng Li Xue Za Zhi ; 34(1): 57-60, 2018 Jan 08.
Artigo em Chinês | MEDLINE | ID: mdl-29926660

RESUMO

OBJECTIVE: To investigate anti-inflammatory and immunomodulation effects of different ecotype from Isatidis Radix growing in Gansu province. METHODS: Mice were randomly divided into 6 groups (n=11)and used the auricular swelling and paw edema to observe the anti-inflammatory effects of Isatidis Radix; Mice were randomly divided into 7 groups (n=11) and through the gasbag synovitis model to observe the anti-inflammatory effects of Isatidis Radix; Mice were randomly divided into 6 groups (n=11), the immunosuppressed model were established by injection of cyclophosphamide (CTX) to study the effects of Isatidis Radix on index of thymus, blood routine and cytokines. RESULTS: Gansu different ecotype from Isatidis Radix could reduce the swelling of the mice auricle, paw edema and total protein, leukotriene B4(LTB4)and malonaldehyde(MDA) in airbag synovitis exudates, and upgrade serum levels of superoxide dismutase (SOD); Degrade the tumor necrosis factor-α (TNF-α) and upgrade the index of thymus, the number of red and white corpuscles, the level of interferon-γ (IFN-γ), interleukin-4 (IL-4) (P<0.05, 0.01) of mice immunosuppressed model; Above the research of anti-inflammatory and immunomodulation, there were no significant differences between Isatidis Radix of Gansu different ecotype and tetraploid. CONCLUSIONS: Different ecotype of Isatidis Radix has obvious functions in anti-inflammatory and immunomodulation, but there are no significant differences between Gansu different ecotype and tetraploid.


Assuntos
Anti-Inflamatórios/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Imunomodulação/efeitos dos fármacos , Isatis/química , Extratos Vegetais/farmacologia , Animais , China , Citocinas/imunologia , Ecótipo , Camundongos , Distribuição Aleatória
20.
Res Vet Sci ; 119: 91-98, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29890386

RESUMO

Isatis root polysaccharide (IRPS) has gained attention in the field of virology. However, very few studies have evaluated the effects of IRPS on H3N2 swine influenza virus (SIV). The antiviral activities of IRPS against SIV were investigated in vitro through three different modes and in vivo in an experimental mouse model of SIV infection. Mice were treated by oral gavage with various doses of IRPS before being experimentally infected with SIV A/swine/Henan/2010(H3N2). The antiviral effects of IRPS were evaluated by clinical signs, weight, histopathology, cytokine levels in lung homogenates and serum nitric oxide (NO) and IgG levels at 2, 5 and 9 d post-infection. IRPS demonstrated an inhibitory effect on SIV in Madin-Darby canine kidney cells. Additionally, IRPS significantly improved symptoms, reduced pathological changes and enhanced serum levels of NO and IgG in SIV-infected mice. Furthermore, detection of cytokines in lung homogenates showed IRPS could alter cytokine production to improve immune responses and systemic ability to repair inflammation. Moreover, IRPS extenuated the pulmonary inflammatory response. The results show that various concentrations of IRPS exert antiviral effects in vitro and in vivo. In an experimental mouse model of SIV infection, IRPS at a dose of 75 mg/kg was effective.


Assuntos
Antivirais/farmacologia , Vírus da Influenza A Subtipo H3N2 , Isatis/química , Infecções por Orthomyxoviridae/veterinária , Polissacarídeos/farmacologia , Animais , Cães , Vírus da Influenza A Subtipo H1N1 , Camundongos , Infecções por Orthomyxoviridae/tratamento farmacológico , Suínos , Doenças dos Suínos/tratamento farmacológico
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