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1.
PLoS One ; 15(3): e0230154, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32150567

RESUMO

To gain better insight into the regulatory networks of anthocyanin biosynthesis, an integrated analysis of the metabolome and transcriptome in purple and green leaves of Tetrastigma hemsleyanum was conducted. Transcript and metabolite profiles were archived by RNA-sequencing data analysis and LC-ESI-MS/MS, respectively. There were 209 metabolites and 4211 transcripts that were differentially expressed between purple and green leaves. Correlation tests of anthocyanin contents and transcriptional changes showed 141 significant correlations (Pearson correlation coefficient >0.8) between 16 compounds and 14 transcripts involved in the anthocyanin biosynthesis pathway. Some novel genes and metabolites were discovered as potential candidate targets for the improvement of anthocyanin content and superior cultivars.


Assuntos
Antocianinas/metabolismo , Metaboloma/genética , Folhas de Planta/metabolismo , Transcriptoma/genética , Vitaceae/genética , Antocianinas/genética , Cor , Biologia Computacional , Perfilação da Expressão Gênica , Regulação da Expressão Gênica de Plantas , Genes de Plantas , Proteínas de Plantas/genética , Espectrometria de Massas em Tandem , Vitaceae/química , Vitaceae/metabolismo
2.
BMC Genomics ; 20(1): 687, 2019 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-31472675

RESUMO

BACKGROUND: Tetrastigma hemsleyanum Diels et Gilg is a valuable medicinal herb, whose main bioactive constituents are flavonoids. Chilling sensitivity is the dominant environmental factor limiting growth and development of the plants. But the mechanisms of cold sensitivity in this plant are still unclear. Also, not enough information on genes involved in flavonoid biosynthesis in T. hemsleyanum is available to understand the mechanisms of its physiological and pharmaceutical effects. RESULTS: The electrolyte leakage, POD activity, soluble protein, and MDA content showed a linear sustained increase under cold stress. The critical period of cold damage in T. hemsleyanum was from 12 h to 48 h. Expression profiles revealed 18,104 differentially expressed genes (DEGs) among these critical time points. Most of the cold regulated DEGs were early-response genes. A total of 114 unigenes were assigned to the flavonoid biosynthetic pathway. Fourteen genes most likely to encode flavonoid biosynthetic enzymes were identified. Flavonols of T. hemsleyanum might play a crucial role in combating cold stress. Genes encoding PAL, 4CL, CHS, ANR, FLS, and LAR were significantly up-regulated by cold stress, which could result in a significant increase in crucial flavonols (catechin, epicatechin, rutin, and quercetin) in T. hemsleyanum. CONCLUSIONS: Overall, our results show that the expression of genes related to flavonol biosynthesis as well as flavonol content increased in T. hemsleyanum under cold stress. These findings provide valuable information regarding the transcriptome changes in response to cold stress and give a clue for identifying candidate genes as promising targets that could be used for improving cold tolerance via molecular breeding. The study also provides candidate genes involved in flavonoid biosynthesis and may be useful for clarifying the biosynthetic pathway of flavonoids in T. hemsleyanum.


Assuntos
Resposta ao Choque Frio/genética , Flavonoides/genética , Vitaceae/genética , Vias Biossintéticas , Flavonoides/química , Flavonoides/metabolismo , Regulação da Expressão Gênica de Plantas , Ontologia Genética , Proteínas de Plantas/genética , RNA-Seq , Transcriptoma , Vitaceae/metabolismo
3.
Int J Biol Macromol ; 141: 611-621, 2019 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-31499109

RESUMO

Tetrastigma hemsleyanum Diels et Gilg, a rare herbal plant native to China, possesses high medicinal value. More researches have focused on the flavones in the tubers of Tetrastigma hemsleyanum whereas polysaccharides attract few attentions. In this study, a purified polysaccharide (TTP-1) with the average molecular weights of 478.33 kDa was extracted from Tetrastigma hemsleyanum and conducted multiple analysis to identify its structural information. In vitro, TTP-1 could suppress the inflammation, cytotoxicity, genotoxicity, mitochondrial dysfunction and oxidative damage induced by LPS in RAW264.7 cells. Meanwhile, TTP-1 could attenuate inflammation via COX-2, iNOS, MAPKs pathways and ameliorate oxidative damage through Nrf2-Keap1, Sirt1-FoxO1 pathways in RAW264.7 cells. In vivo, the inflammation induced by LPS triggered the suppression of survival ratio and growing development, as well as the restrain of athletic ability in Caenorhabditis elegans. The treatment of TTP-1 reversed the situation induced by LPS. In a word, TTP-1 could ameliorate LPS-induced inflammation both in vitro and in vivo.


Assuntos
Caenorhabditis elegans , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Tubérculos/química , Polissacarídeos/farmacologia , Vitaceae/química , Animais , Ciclo-Oxigenase 2/metabolismo , Proteína Forkhead Box O1/metabolismo , Proteína 1 Associada a ECH Semelhante a Kelch/metabolismo , Macrófagos/metabolismo , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Polissacarídeos/uso terapêutico , Células RAW 264.7 , Sirtuína 1/metabolismo
4.
Int J Biol Macromol ; 140: 206-215, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31415856

RESUMO

Tetrastigma hemsleyanum Diels et Gilg (THDG) is used as a Chinese traditional anti-inflammatory medicine for about thousands of years. In this work, Tetrastigma hemsleyanum Diels et Gilg's polysaccharide (TP) can inhibit E. coli's growth in initial dosing period. Compared with the antibacterial effect of Achyranthe's polysaccharide (AP) from their metabolic profile, it's obviously that their metabolic sites for E. coli were inconsistent. Moreover, TP could not only increase the level of fructose-6-phosphate (F6P), decrease the level of fructose-1,6-diphosphate (FBP), but also charge the amount of the two differential metabolic with the change of the concentration and the dosing time. Actually, F6P could transform into FBP by catalyze of 6-phosphofructokinase-1(6-PFK-1), which is an important process in glycolysis. Furthermore, FBP was considered have positively correlated with E. coli's growth rate. Therefore, TP can inhibit the E. coli's proliferation by interfering with the process for glycolysis and gluconeogenesis. Based on the experimental result, we proposed a new mouthwash method to evaluate the anti-bacterial activity. Compared with AP, TP can inhibit the E. coli's growth within 2 h with a low concentration (0.5%) and a short dosing time (5 min). This study extends the applications of THDG and establishes a new assessment method for the pharmacology activity of Chinese herbal medicine.


Assuntos
Achyranthes/química , Antibacterianos/farmacologia , Escherichia coli/efeitos dos fármacos , Metabolômica , Polissacarídeos/farmacologia , Vitaceae/química , Antibacterianos/química , Medicamentos de Ervas Chinesas , Escherichia coli/crescimento & desenvolvimento , Espectrometria de Massas , Medicina Tradicional Chinesa , Folhas de Planta/química , Polissacarídeos/química
5.
Molecules ; 24(9)2019 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-31060200

RESUMO

Leea asiatica (L.) Ridsdale (Leeaceae) is found in tropical and subtropical countries and has historically been used as a traditional medicine in local healthcare systems. Although L. asiatica extracts have been found to possess anthelmintic and antioxidant-related nephroprotective and hepatoprotective effects, little attention has been paid toward the investigation of phytochemical constituents of this plant. In the current study, phytochemical analysis of isolates from L. asiatica led to the identification of 24 compounds, including a novel phenolic glucoside, seven triterpenoids, eight flavonoids, two phenolic glycosides, four diglycosidic compounds, and two miscellaneous compounds. The phytochemical structures of the isolates from L. asiatica were elucidated using spectroscopic analyses including 1D- and 2D-NMR and ESI-Q-TOF-MS. The presence of triterpenoids and flavonoids supports the evidence for anthelmintic and antioxidative effects of L. asiatica.


Assuntos
Compostos Fitoquímicos/análise , Vitaceae/química , Anti-Helmínticos/química , Anti-Helmínticos/isolamento & purificação , Anti-Helmínticos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Medicina Tradicional , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Componentes Aéreos da Planta/química , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
6.
Inflammopharmacology ; 27(6): 1297-1307, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31123967

RESUMO

OBJECTIVE: Tetrastigma hemsleyanum, a rare and endangered medicinal plant, has attracted much attention due to its immunoregulatory and hepatoprotective activities. This study aimed to evaluate the anti-inflammatory effects and underlying mechanisms of total flavonoids from T. hemsleyanum(TFT)on Con A-induced hepatitis in mice. METHODS: TFT (1, 2 and 4 g/kg) and a positive control drug bifendate (200 mg/kg) were administered intragastrically to mice once daily for 10 consecutive days. On the 10th day, the model autoimmune of hepatitis was established by intravenous injection of Con A (20 mg/kg) 1 h after drug administration. Liver injury was assessed by serum levels of alanine amino transferase (ALT and AST) and histopathology 8 h after Con A injection. The levels of pro-inflammatory Th17 cytokines (IL-17, IL-6) and anti-inflammatory Treg cytokines (IL-10, TGF-ß1) in serum were evaluated by ELISA, the levels of Th17 and Treg cells infiltrated into spleen were investigated by flow cytometry methods, and hepatic tissue transcription factor Foxp3 and RORγt mRNA were determined using quantitative real-time PCR. RESULTS: Pretreatment with TFT and bifendate significantly reduced the serum levels of ALT and AST, and attenuated histopathological alterations in Con A-induced liver injury. With respect to samples treated with Con A alone, TFT and bifendate pretreatments differentially attenuated the increase of serum inflammatory factors interleukin (IL)-17 and IL-6 levels, the proportions of Th17 cells in spleen and the expression of RORγt in hepatic tissues. Meanwhile, TFT and bifendate pretreatments could enhance the percentage of Treg cells in spleen and the expression of Foxp3 in hepatic tissues, as well as the levels of transforming growth factor (TGF)-ß1, IL-10 in serum. CONCLUSION: The anti-inflammatory effects of TFT was mediated by regulating Treg/Th17 immune homeostasis, which, therefore, suppressed the inflammatory immune response. This study provided scientific basis for the further researches and clinical applications of Tetrastigma hemsleyanum.


Assuntos
Anti-Inflamatórios/uso terapêutico , Flavonoides/uso terapêutico , Hepatite Autoimune/tratamento farmacológico , Linfócitos T Reguladores/efeitos dos fármacos , Células Th17/efeitos dos fármacos , Vitaceae/química , Animais , Concanavalina A/farmacologia , Citocinas/biossíntese , Flavonoides/farmacologia , Fatores de Transcrição Forkhead/genética , Hepatite Autoimune/imunologia , Hepatite Autoimune/patologia , Homeostase , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Linfócitos T Reguladores/imunologia , Células Th17/imunologia
7.
Free Radic Res ; 53(5): 562-573, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31039619

RESUMO

The main flavonoid components of Radix Tetrastigma (RTF) were extracted and identified by UPLC-TOF/MS. In vitro, RTF prevented inflammation in RAW 264.7 cells by suppressing morphological (both cell and nucleus) changes, and decreasing nitric oxide (NO), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) contents. Exposure to LPS also leads to oxidant damage, and RTF alleviated damage to mitochondria, decreased O2- accumulation, and restored the glutathione level. RTF intervention decreased the expression of c-Jun N-terminal kinase (JNK) and p38 phosphorylation, accompanied by downregulation of nuclear factor erythroid 2-related factor 2 (Nrf2) and forkhead box protein O1 (FoxO1). In vivo, aging of Caenorhabditis elegans (C. elegans) by paraquat (PQ) was observed through lifespan, lipofuscin, and enzyme analysis. RTF protected against damage in N2 worms but not in daf-16 mutants. Gene expression was further assessed, and p38/PMK-1 and Nrf2/SKN-1 expression in worms was suppressed by PQ, which was reversed by RTF treatment. Together, these results suggested that RTF could help ameliorate inflammation-induced damage through JNK, p38 and Nrf2 pathways.


Assuntos
Proteínas de Caenorhabditis elegans/genética , Caenorhabditis elegans/efeitos dos fármacos , Proteínas de Ligação a DNA/genética , Flavonoides/farmacologia , Longevidade/efeitos dos fármacos , Proteínas Quinases Ativadas por Mitógeno/genética , Fatores de Transcrição/genética , Vitaceae/química , Animais , Caenorhabditis elegans/genética , Caenorhabditis elegans/crescimento & desenvolvimento , Caenorhabditis elegans/metabolismo , Proteínas de Caenorhabditis elegans/metabolismo , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Proteínas de Ligação a DNA/metabolismo , Flavonoides/química , Flavonoides/isolamento & purificação , Proteína Forkhead Box O1/genética , Proteína Forkhead Box O1/metabolismo , Regulação da Expressão Gênica , Glutationa/metabolismo , Inflamação , Proteínas Quinases JNK Ativadas por Mitógeno/genética , Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Longevidade/genética , Camundongos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/patologia , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Paraquat/antagonistas & inibidores , Paraquat/farmacologia , Extratos Vegetais/química , Células RAW 264.7 , Espécies Reativas de Oxigênio/antagonistas & inibidores , Espécies Reativas de Oxigênio/metabolismo , Fatores de Transcrição/metabolismo , Proteínas Quinases p38 Ativadas por Mitógeno/genética , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
8.
Zhongguo Zhong Yao Za Zhi ; 44(4): 696-702, 2019 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-30989881

RESUMO

As a rare endangered medical plant that newly cultivated,little experimental information is available for growth and metabolites of Tetrastigma hemsleyanum in response to nitrogen( N). The effects of different levels of N on growth of T. hemsleyanum and the content of phytochemicals( polysaccharide,total flavonoids and phenolics) and antioxidant activity( ABTS and FRAP) in stems and leaves were investigated in this study. A certain amount of N had positive effects on most of biological traits,and excessive dose of N went against growth of T. hemsleyanum. With N levels decreased,the polysaccharide content in stems and leaves had no significant change,while the total flavonoid and phenolic content,and antioxidant activities increased steadily. Antioxidant activities and total flavonoid and phenolic content had significant positive correlation. Excessive N fertilizer should be avoided by cultivation.


Assuntos
Vitaceae , Antioxidantes , Flavonoides , Nitrogênio , Fenóis , Compostos Fitoquímicos , Extratos Vegetais , Folhas de Planta
9.
PLoS One ; 14(3): e0214594, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30921428

RESUMO

The genus Cyphostemma (Planch.) Alston (Vitaceae) includes about 150 species distributed in eastern and southern Africa and Madagascar. Some species are used in traditional medicine and their biological activities, including antiproliferative effects against cancer cell lines, have been demonstrated. To date no investigations on Cyphostemma essential oils have been carried out. Essential oils, which play important roles in plant defenses have been demonstrated to be active in the treatment of several human diseases and to enhance bioavability of other drugs. The aim of this paper was to identify the chemical composition of the essential oil of the leaves of Cyphostemma juttae (Dinter & Gilg) Desc. and to verify some biological activities on two triple negative breast cancer cell lines (MDA-MB-231, SUM 149), characterized by the over-expression of the transcription factor NF-κB. In the essential oil, obtained by hydrodistillation and analysed by gas chromatography-mass spectrometry, 39 compounds were detected and with phytol (30%) dominating the chemical composition. C. juttae essential oil reduced cell growth and showed a pro-oxidant activity in both cell lines. Moreover, C. juttae essential oil caused a substantial decrease of NF-κB activation and consequently a significant reduction of some NF-κB target genes. The present study shows for the first time the cytotoxic properties of C. juttae essential oil and highlight its availability to interfere with NF-κB pathway, suggesting a potential therapeutic use in triple negative breast cancers (TNBCs) of this essential oil.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Neoplasias de Mama Triplo Negativas/patologia , Vitaceae/química , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , NF-kappa B/metabolismo , Folhas de Planta/química , Espécies Reativas de Oxigênio/química , Espécies Reativas de Oxigênio/farmacologia
10.
J Enzyme Inhib Med Chem ; 34(1): 753-760, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30829084

RESUMO

The aerial parts of Tetrastigma hemsleyanum (APTH) have been used as a functional tea in China. The purpose of the current study was to identify the bioactive constituents with inhibitory activity against soluble epoxide hydrolase (sEH) and inducible nitric oxide synthase (iNOS), which are jointly considered potential therapeutic targets for vascular system diseases. In the present study, 39 compounds (1-39) were isolated from the APTH. Among them, compounds 8, 10, 12, 16, 17, 19, and 32 displayed potential activities, with IC50 values ranging from 4.5 to 9.5 µM, respectively, and all in non-competitive inhibition mode. Compounds 5, 10, 12, 19, and 32 displayed potent iNOS inhibitory effects, with IC50 values ranging from 15.6 to 47.3 µM. The results obtained in this work contribute to a better understanding of the pharmacological activities of T. hemsleyanum and its potential application as a functional food.


Assuntos
Epóxido Hidrolases/antagonistas & inibidores , Óxido Nítrico Sintase/antagonistas & inibidores , Fenóis/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/farmacologia , Vitaceae/química , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Epóxido Hidrolases/metabolismo , Camundongos , Modelos Moleculares , Estrutura Molecular , Óxido Nítrico Sintase/metabolismo , Fenóis/química , Fenóis/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Células RAW 264.7 , Solubilidade , Relação Estrutura-Atividade
11.
Microsc Res Tech ; 82(4): 335-344, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30351520

RESUMO

This present study is the first report on the detailed foliar epidermal anatomy and micromorphology of seeds of five species of Vitaceae from Pakistan using light microscopy (LM) and scanning electron microscopy (SEM). The studied species occur at various localities particularly higher altitude. Qualitative and quantitative leaf micromorphological characters investigated here are related to shape and size of epidermal cells, anticlinal wall pattern, stomatal pore, guard cell, stomatal complex, subsidiary cells, and trichomes. Variations in size and shape were observed in the studied species. Irregular, polygonal and elongated epidermal cells with straight or undulate margins, stomata anomocytic type, and trichomes nonglandular, unicellular to multicellular in all the studied plants. Seed micromorphological qualitative characters studied are shape of margins, integument cell, apical notch, chalaza, anticlinal wall thickness, and quantitative characters are number of seeds per berry, length, and width of seed, length to width ratio. The detailed distribution and microscopic characteristics investigated of family Vitaceae has a distinguished role in identification at genus and species level and may provide evidence in the determination of taxonomic rank of the family in the phylogenetic tree. This study possesses potential for plant taxonomists to further evaluate the species for phytochemical studies and physiology. RESEARCH HIGHLIGHTS: Light microscopy and scanning electron microscopy was used for the micromorphological investigation of family Vitaceae Qualitative and quantitative characteristics were studied Variation in microscopic features of leaf epidermis and seeds Identification of species based on micromorphological characters.


Assuntos
Epiderme Vegetal/ultraestrutura , Folhas de Planta/anatomia & histologia , Sementes/ultraestrutura , Vitaceae/anatomia & histologia , Células Epidérmicas/ultraestrutura , Microscopia Eletrônica de Varredura , Paquistão , Estômatos de Plantas/ultraestrutura , Tricomas/ultraestrutura , Vitaceae/classificação
12.
Int J Biol Macromol ; 125: 1033-1041, 2019 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-30500505

RESUMO

In this study, a novel polysaccharide TDGP-3 from Tetrastigma hemsleyanum Diels et Gilg was extracted by enzymolysis-ultrasonic assisted extraction (EUAE) method and its antioxidant and hypolipidemic activities were evaluated. With a molecular weight of 3.31 × 105 Da, TDGP-3 was composed of 1,4-Glcp, 1,4-Glap and 1,3,6-Manp linkage in the main chain. TDGP-3 showed potential effects on relieving hyperlipidemia and preventing oxidative stress, reflecting by regulating blood lipid levels (TC, TG, HDL-C and LDL-C), decreasing the contents of MDA in liver, restoring the activities of hepatic antioxidant enzymes (SOD, GSH-Px and CAT). The results clearly indicated that the TDGP-3 possesses a potent hypolipidemic activity and might be used for hyperlipidaemia treatment.


Assuntos
Antioxidantes/química , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/química , Polissacarídeos/química , Vitaceae/química , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Sequência de Carboidratos , Catalase/metabolismo , HDL-Colesterol/sangue , LDL-Colesterol/sangue , Glutationa Peroxidase/metabolismo , Hiperlipidemias/metabolismo , Hiperlipidemias/fisiopatologia , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Extração Líquido-Líquido/métodos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/fisiopatologia , Testes de Função Hepática , Masculino , Malondialdeído/metabolismo , Camundongos , Camundongos Endogâmicos ICR , Peso Molecular , Estresse Oxidativo , Extratos Vegetais/química , Folhas de Planta/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Sonicação , Superóxido Dismutase/metabolismo , Triglicerídeos/sangue
13.
Int J Biol Macromol ; 123: 775-783, 2019 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-30447363

RESUMO

In the present study, a novel polysaccharide (THDP-3) purified from cane leaves of Tetrastigma hemsleyanum Diels et Gilg was obtained via anion exchange chromatography and the structural analyses of the compound indicated that THDP-3 is a homogenous polysaccharide with molecular weight of 77.98 kDa. Our results show that it consists of rhamnose, arabinose, mannose, glucose and galactose at molar ratio of 1.0: 1.3: 2.5: 2.3:3.1 with main backbones of →4)-α-D-GalAp-(1→, →4)-ß-D-Galp-(1→ and →4)-α-D-Glcp-(1→, and main branches of ß-D-Manp-(1→, →3,6-ß-D-Manp-1→ and α-D-Araf-(1→. In the anti-diabetic assays, THDP-3 showed significant hypoglycemic activity in alloxan-induced diabetic mice. In addition, THDP-3 was found regulating the expression of glucokinase, amp-activated protein kinase, glucose-6-phosphatase and phosphoenolpyruvate carboxykinase. These new findings indicate the high potential in therapeutic mechanisms investigation using THDP-3. Moreover, our results of hypoglycemic activity using THDP-3 demonstrated that the compound could serve as a potential anti-diabetic agent.


Assuntos
Hipoglicemiantes/química , Hipoglicemiantes/uso terapêutico , Polissacarídeos/química , Polissacarídeos/uso terapêutico , Vitaceae/química , Aloxano , Animais , Glicemia/metabolismo , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/genética , Regulação da Expressão Gênica/efeitos dos fármacos , Glicogênio/metabolismo , Hipoglicemiantes/farmacologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos Endogâmicos ICR , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Espectroscopia de Prótons por Ressonância Magnética
14.
Curr Pharm Des ; 24(33): 3972-3979, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30398111

RESUMO

BACKGROUND: Alzheimer disease (AD) can be considered as the most common age related neurodegenerative disorder and also an important cause of death in elderly patients. A number of studies showed the correlation of this disease pathology with BACE1 inhibitor and it is also evident that BACE1 inhibitor can function as a very potent strategy in treating AD. METHODS: In this present study, we aimed to prospect for novel plant-derived BACE1 inhibitors from Leea indica and to realise structural basis of their interactions and mechanisms using combined molecular docking and molecular dynamics based approaches. An extensive library of Leea indica plant derived molecule was compiled and computationally screened for inhibitory action against BACE1 by using virtual screening approaches. Furthermore, induced fit docking and classical molecular dynamics along with steered molecular dynamics simulations were employed to get insight of the binding mechanisms. RESULTS: Two triterpenoids, ursolic acid and lupeol were identified through virtual screening; wherein, lupeol showed better binding free energy in MM/GBSA, MM/PBSA and MM/GBVI approaches. Furthermore classical and steered dynamics revealed the favourable hydrophobic interactions between the lupeol and the residues of flap or catalytic dyadof BACE1; however, ursolic acid showed disfavorable interactions with the BACE1. CONCLUSION: This study therefore unveiled the potent BACE1 inhibitor from a manually curated dataset of Leea indica molecules, which may provide a novel dimension of designing novel BACE1 inhibitors for AD therapy.


Assuntos
Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Inibidores Enzimáticos/farmacologia , Triterpenos Pentacíclicos/farmacologia , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , Vitaceae/química , Secretases da Proteína Precursora do Amiloide/metabolismo , Ácido Aspártico Endopeptidases/metabolismo , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Modelos Moleculares , Triterpenos Pentacíclicos/química , Triterpenos Pentacíclicos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade , Termodinâmica , Triterpenos/química , Triterpenos/isolamento & purificação
15.
BMC Plant Biol ; 18(1): 208, 2018 Sep 24.
Artigo em Inglês | MEDLINE | ID: mdl-30249188

RESUMO

BACKGROUND: Tetrastigma hemsleyanum is of great medicinal importance and used as a model system to address the evolutionary history of warm-temperate evergreen (WTE) forest biomes in East Asia over Neogene time scales. However, further studies on the neutral and adaptive divergence processes of T. hemsleyanum are currently impeded by a lack of genomic resources. In this study, we de novo assembled and annotated a reference transcriptome for two cpDNA lineages (Central-South-East vs. Southwest) of T. hemsleyanum. We further used comparative genomic and multilocus coalescent approaches to investigate the tempo and mode of lineage diversification in T. hemsleyanum. RESULTS: A total of 52,838 and 65,197 unigenes with an N50 of 1,667 and 1,841 bp for Central-South-East (CSE) and Southwest (SW) lineages, respectively, were recovered, and 6,692 putative orthologs were identified between the two lineages. Estimation of Ka/Ks ratios for these orthologs revealed that ten genes had Ka/Ks values significantly greater than 0.5 (P < 0.05), whereas 2,099 (Ka/Ks < 0.5, P < 0.05) were inferred to be under purifying selection. Based on three bioinformatic strategies, we identified a total of 1,018 single-copy nuclear genes (SCNGs) from the orthologs. We successfully designed eight nuclear gene primer pairs with high intraspecific variation (e.g. hT = 0.923, πT = 1.68×10-3), when surveyed across a subset of T. hemsleyanum individuals. Concordant with the previous cpDNA data, the haplotype networks constructed for most nuclear gene loci clearly identified the two lineages. A multilocus coalescence analysis suggested that the separation between the two lineages appears to have occurred during the mid-Pliocene. Despite their ancient divergence, both lineages experienced expansion at rather localized scales and have continued to exchange genes at a low rate. CONCLUSIONS: This study demonstrated the utility of transcriptome sequencing as a basis for SCNG development in non-model species and the advantages of integrating multiple nuclear loci for phylogeographic and phylogenetic studies.


Assuntos
Evolução Biológica , Perfilação da Expressão Gênica , Vitaceae/genética , Adaptação Biológica/genética , DNA de Cloroplastos , Etiquetas de Sequências Expressas , Anotação de Sequência Molecular , Tipagem de Sequências Multilocus , Proteínas de Plantas/genética , Vitaceae/fisiologia
16.
Pak J Pharm Sci ; 31(5): 1813-1816, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30150175

RESUMO

The phytochemical screening and antioxidant potential of bark and stem of Parthenocissus quinquefolia (L.) planch was assessed in order to verify its ethnopharmacological significance. All major secondary metabolites e.g. alkaloids, flavonoids, saponins, terpenoids, tannins, reducing sugars, cardiac glycosides and anthraquinones were present. Antioxidant activity was analysed by using five techniques which included DPPH Free Radical Scavenging Activity, FRAP (Ferric Reducing Antioxidant Power), TAA (Total Antioxidant Activity, TPC (Total Phenolic Content and MC (Metal Chelating) Activity. Ethanolic extract of bark showed the highest scavenging effects of 90.01±0.01%, with IC50 value of 24.32mg/ml. Aqueous stem extract showed best activity with IC50 value of 13.6±0.34mg/ml. The significance antioxidant potential indicates the effectiveness of bark and stem of P. quinquefolia in treatment of many diseases.


Assuntos
Antioxidantes/química , Compostos Fitoquímicos/química , Casca de Planta , Extratos Vegetais/química , Caules de Planta , Vitaceae , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/isolamento & purificação , Depuradores de Radicais Livres/farmacologia , Radicais Livres/antagonistas & inibidores , Radicais Livres/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia
17.
Int J Biol Macromol ; 119: 70-78, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30036623

RESUMO

Four polysaccharides, PTP-1, PTP-2, PTP-3 and PTP-4, were obtained from the water extraction of the stems of P. tricuspidata by anion exchange chromatography and gel filtration. The antioxidant activities of four PTPs were investigated, exhibiting different antioxidant activities, in which PTP-4 performed noticeable, with strong superoxide radical activity (comparable to BHT), high DPPH radical activity (78.53% at 1250 µg/mL), moderate hydroxyl radical scavenging activity and reducing power activity. Furthermore, the chemical structure of PTP-4 was measured by FT-IR, GC, 1H and 13C NMR spectra, indicating its mainly composition of the arabinose, xylose, galactose, glucuronic acid, and mannose. Thus, the stems of P. tricuspidata could be used as a potential source for natural antioxidant.


Assuntos
Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Caules de Planta/química , Polissacarídeos/farmacologia , Vitaceae/química , Antioxidantes/química , Antioxidantes/isolamento & purificação , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/isolamento & purificação , Depuradores de Radicais Livres/farmacologia , Espectroscopia de Ressonância Magnética , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Espectroscopia de Infravermelho com Transformada de Fourier
18.
Molecules ; 23(6)2018 06 14.
Artigo em Inglês | MEDLINE | ID: mdl-29899226

RESUMO

Alkaloids 1⁻10 were isolated from the aerial parts of Tetrastigma hemsleyanum (APTH) and obtained from species of the genus Tetrastigma for the first time. The chemical structures of the isolated compounds were identified by NMR, UV, and MS analyses. Their anti-inflammatory activities were investigated by measuring nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 macrophages. Among all the isolates, compounds 6, 7 and 10 showed potent inhibitory activity against LPS-stimulated NO production in RAW264.7 cells (IC50: 31.9, 25.2 and 6.3 µM, respectively). Furthermore, APTH and S-(−)-trolline (10) inhibited induction of inflammatory cytokines or mediators such as interleukin-1ß (IL-1ß) and inducible nitric oxide synthase (iNOS) via suppression of nuclear factor κB (NF-κB) translocation into the nucleus. In addition, 10 suppressed extracellular signal-regulated protein kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAPK) phosphorylation in a dose-dependent manner. These results conclusively demonstrated that compound 10 displays anti-inflammatory activity via suppression of NF-κB activation and the ERK-MAPK signaling pathway in LPS-stimulated RAW264.7 cells.


Assuntos
Alcaloides/farmacologia , Anti-Inflamatórios/farmacologia , Lipopolissacarídeos/efeitos adversos , Macrófagos/metabolismo , Vitaceae/química , Alcaloides/química , Animais , Anti-Inflamatórios/química , Citocinas/metabolismo , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Fosforilação/efeitos dos fármacos , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Células RAW 264.7
19.
Chem Biodivers ; 15(8): e1800070, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29806965

RESUMO

Tetrastigma hemsleyanum Diels & Gilg, a well-known traditional Chinese medicine, possesses antitumor and anti-inflammatory activity, etc. However, the anti-diabetic effect has not been determined. In our present study, a water-soluble polysaccharide, named THP with molecular weight of 93 307 Da, was isolated from T. hemsleyanum by DEAE-52 ion-exchange and Sephadex G-100 chromatography. It contains rhamnose, arabinose, mannose, glucose, and galactose in the molar ratio of 0.07:0.14:0.38:0.21:0.31. Then anti-diabetic effects of THP were examined by treating alloxan-induced diabetic mice with different doses (100, 200, and 300 mg/kg) of THP orally. The results showed that THP could decrease the blood glucose, TC, TG, LDL-C levels, increase the body weight, HDL-C, insulin levels, and enhance the activities of antioxidant enzyme system in alloxan-induced diabetic mice. Furthermore, the histopathological examination of pancreas, liver, and kidney indicated that THP could protect and reverse ß-cells in diabetic mice with low damage to liver and kidney, which suggests that THP may stimulate pancreatic release of insulin and can be an effectively potential candidate for diabetes mellitus.


Assuntos
Antioxidantes/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Polissacarídeos/farmacologia , Vitaceae/química , Aloxano , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/patologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Masculino , Medicina Tradicional Chinesa , Camundongos , Camundongos Endogâmicos ICR , Tamanho do Órgão/efeitos dos fármacos , Polissacarídeos/química , Polissacarídeos/isolamento & purificação
20.
J Plant Physiol ; 218: 258-264, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28915504

RESUMO

Flavonoids are a ubiquitous multifunctional group of phenolics of paramount importance for the terrestrial plants involved in protection from biotic and abiotic stresses, color and chemical signaling and other functions. Deciphering of in situ absorption of foliar Flv is important but was thought to be impossible due to a strong overlap with other pigments, complex in situ chemistry of Flv and sophisticated leaf optics. We deduced in situ absorbance of foliar Flv and introduced a concept of specific absorbance spectrum indicative of each pigment group contribution to light absorption and provided a rationale for the choice of spectral bands for non-destructive assessment of Flv in leaves with variable content of other pigments including anthocyanins. Only a narrow band 400-430nm was suitable for Flv assessment, however the effect of other pigments remained substantial, so subtraction of their contribution was necessary. The devised leaf absorbance-based algorithm allowed estimating Flv with error below 21%. Absorption by Flv in plant tissues might extend into the blue and can be commensurate to that of chlorophylls and carotenoids. The potential capacity of Flv to shield the cell in situ from the visible light might be essential for assessments of high light stress tolerance of plants.


Assuntos
Botânica/métodos , Flavonoides/análise , Folhas de Planta/química , Espectrofotometria/métodos , Fenômenos Ópticos , Rosaceae/química , Vitaceae/química
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