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1.
Braz. J. Pharm. Sci. (Online) ; 55: e18201, 2019. tab, graf
Article in English | LILACS | ID: biblio-1011651

ABSTRACT

Oxidative stress plays the central role in the pathogenesis and progression of diabetic complications. The present study aims to investigate the beneficial effect of oral administration of flavone baicalein in streptozotocin-nicotinamide (STZ-NA) induced diabetic rats by measuring oxidative stress markers, antioxidant enzyme activities and expression analysis of antioxidant genes. Experimental diabetes was induced by a single intraperitoneal (i.p.) injection of STZ (55 mg /kg b.wt), 15 min after the i.p. administration of NA. At the end of the experimental period, thiobarbituric acid reactive substances (TBARS), activities of antioxidant enzymes and expression levels of superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and glutathione peroxidase (GPx) were measured in diabetic rats along with serum biochemical parameters namely total cholesterol (TC), total triglyceride (TG), aspartate transaminase (AST) alanine transaminase (ALT) and glycosylated hemoglobin (HbA1c). Oral administration of baicalein (40 mg/kg b.wt/day) demonstrated a significant ameliorative effect on all studied biochemical and oxidative stress parameters. Biochemical findings were corroborated by qPCR expression analysis which showed significant upregulation of antioxidant genes in diabetic rats. These results suggest that baicalein supplementation may reduce diabetes and its complications by suppressing oxidative stress and enhancing gene expression and antioxidant enzyme activities in diabetic rats.


Subject(s)
Animals , Male , Child, Preschool , Rats , Gene Expression , Niacinamide/pharmacology , Flavones/analysis , Diabetes Mellitus, Experimental/prevention & control , Gene Expression/drug effects , Glyburide/pharmacology , Oxidative Stress , Antioxidants/pharmacology
2.
Article in Chinese | WPRIM | ID: wpr-774541

ABSTRACT

This research aims to develop an UHPLC method, based on core-shell column(i.e. superficially porous particles), for simultaneous determination of eight isoflavonoids including formononetin,(6αR,11αR)-3-hydroxy-9,10-dimethoxypterocarpan, calycosin-7-O-β-D-glucopyranoside,(3R)-7,2-dihydroxy-3,4-dimethoxyisoflavone, calycosin, ononin,(6αR,11αR)-9,10-dimethoxypterocarpan-3-O-β-D-glucopyranoside, and(3R)-7,2-dihydroxy-3,4-dimethoxyisoflavan-7-O-β-D-glucopyranoside in Astragali Radix. The analysis was performed on an Agilent Poroshell EC-C_(18 )column(2.1 mm×100 mm, 2.7 μm) with 0.2% formic acid solution(A)-acetonitrile(B) as mobile phase for gradient elution. The flow rate was 0.5 mL·min~(-1), with column temperature of 40 ℃ and the wavelengths were set at 260 and 280 nm. According to the results, all calibration curves showed good linearity(R~2>0.999 8) within the tested concentration ranges. Both the intra-and inter-day precisions for 8 isoflavonoids were less than 0.80%, with the mean recovery at the range of 94.71%-104.6%. Thus, the newly developed UHPLC method using core-shell column owned the advantages in terms of rapid analysis, low column pressure and less solvent consumption, thus enabling the usage of conventional HPLC systems. Meanwhile, quantitative evaluation was carried out for 22 batches of commercial Astragali Radix. It has been found that great variations occurred for the content of the individual isoflavonoids among different batches; in contrast, the total content of total 8 isoflavonoids(>0.1%) was stable in most samples, indicating that it was reasonable to involve all isoflavonoids as the chemical markers for the quality control of Astragali Radix.


Subject(s)
Astragalus Plant , Chemistry , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Reference Standards , Flavones , Phytochemicals , Plant Roots , Chemistry , Quality Control
3.
Article in English | WPRIM | ID: wpr-776881

ABSTRACT

The anti-inflammatory active ingredients of Zhi-Shi-Zhi-Zi-Chi-Tang (ZSZZCT), a traditional Chinese medicine formula, were predicted and identified using an approach based on activity index, LC-MS, semi-preparative LC and NMR. Firstly, the whole extract of ZSZZCT was analyzed using liquid chromatography-quadrupole time of flight-mass spectrometry (LC-Q-TOF-MS) and liquid chromatography - ion trap mass spectrometry (LC-IT-MS), 79 constituents were detected and 39 constituents were identified unambiguously or tentatively. Subsequently, the whole extract of the formula was separated into multiple components and the activity index method was used to calculate index values of the 79 constituents by integrating the chemical and pharmacological information of multiple components. Four polymethoxyl flavones were predicted as the major active constituents according to the activity index values. Furthermore, three polymethoxyl flavones were prepared using the strategy with semi-preparative LC guided by LC-MS, and their anti-inflammatory activities were validated. The results show that three polymethoxyl flavones with higher positive index values, i.e., 3, 5, 6, 7, 8, 3', 4'-heptamethoxyflavone, 3-hydroxynobiletein and tangeretin had significant anti-inflammatory effects. In conclusion, the predicted results indicated that the activity index method is feasible for the accurate prediction of active constituents in TCM formulae.


Subject(s)
Animals , Anti-Inflammatory Agents , Chemistry , Pharmacology , Drugs, Chinese Herbal , Chemistry , Pharmacology , Flavones , Chemistry , Pharmacology , Lipopolysaccharides , Toxicity , Macrophages , Metabolism , Medicine, Chinese Traditional , Mice , Molecular Structure , Nitric Oxide , Metabolism , Plant Extracts , Chemistry , Pharmacology , Plants, Medicinal , Chemistry
4.
Rev. peru. med. integr ; 4(3): 90-95, 2019. ilus, tab
Article in Spanish | LILACS, MTYCI | ID: biblio-1145708

ABSTRACT

Objetivo. Determinar la estructura química de flavonas aisladas del extracto metanólico de hojas de Marrubium vulgare L. "Cordón", mediante comparación con lo publicado por TJ Mabry. Materiales y métodos. Se elaboró extracto metanólico de hojas de Marrubium vulgare L. "Cordón" . Se determinó su solubilidad en solventes de polaridad creciente. Se detectaron los componentes químicos utilizando tricloruro férrico, reactivo de Shinoda, gelatina, entre otros reactivos cromogénicos. Se realizó cromatografía en capa fina y por espectroscopía UV/VIS se propusieron estructuras químicas para los metabolitos tipo flavonas presentes en el extracto metanólico de hojas de Marrubium vulgare L. "Cordón" . Resultados. El extracto metanólico de hojas de Marrubium vulgare L. "Cordón" fue soluble en solventes de mediana polaridad. Los metabolitos secundarios encontrados fueron flavonoides, taninos y alcaloides. Se propusieron estructuras químicas de flavonas a través del análisis de los espectros UV/Vis, y por comparación con tablas publicadas en la literatura. Conclusiones. Se determinaron nueve estructuras químicas de metabolitos secundarios tipo flavonas del extracto metanólico de hojas de Marrubium vulgare L. "Cordón" mediante comparación con lo publicado por TJ Mabry.


Objective. Determine the chemical structure of flavones isolated from the methanolic extract of Marrubium vulgare L. "Cordón" leaves by comparison with that published by TJ Mabry. Materials and methods. Methanolic leaf extract of Marrubium vulgare L. "Cordón" was prepared. Its solubility in solvents of increasing polarity was determined. The chemical components were detected using ferric trichloride, Shinoda reagent, gelatin, among other chromogenic reagents. Thin layer chromatography was performed and by UV / VIS spectroscopy chemical structures were proposed for flavone metabolites present in the methanolic leaf extract of Marrubium vulgare L. "Cordón". Results. The methanolic extract of Marrubium vulgare L. "Cordón" leaves was soluble in medium polarity solvents. The secondary metabolites found were flavonoids, tannins and alkaloids. Chemical structures of flavones were proposed through the analysis of the UV / Vis spectra, and by comparison with tables published in the literature. Conclusion. Nine chemical structures of flavone secondary metabolites of the methanolic leaf extract of Marrubium vulgare L. "Cordón" were determined by comparison with that published by TJ Mabry.


Subject(s)
Marrubium/chemistry , Flavones , Plants, Medicinal , Spectrum Analysis , Plant Extracts , Chromatography , Phytochemicals , Medicine, Traditional
5.
Braz. J. Pharm. Sci. (Online) ; 54(1): e17178, 2018. tab, graf
Article in English | LILACS | ID: biblio-951912

ABSTRACT

ABSTRACT Antioxidants from natural sources hold high values regarding their indispensible roles in the development of nutraceuticals, pharmaceuticals and cosmetic products. Oroxylum indicum L. is a common medicinal plant with a wide range of therapeutic properties, including a notable antioxidant potency that was reported, yet has not been subjected to more detailed studies. The present study evaluated the potency of Oroxylum indicum methanol stem bark extract, along with its hexane, ethyl acetate, methanol fractions, three flavones including baicalein, oroxylin A and chrysin using DPPH assay. In terms of IC50 values, the crude extract (65,48 µg/mL) exhibited moderate inhibitory activity which was as half potent as that of its ethyl acetate fraction (32,94 µg/mL). This fraction was also superior to the methanol and hexane fractions, as their IC50 were 57,19 and 137,95 µg/mL respectively. Remarkably, a yellow powdery sub-fraction consisted of isolated compounds showed powerful activity (32,89 µg/mL) compared to those of its components, revealing the intriguing effect of synergism while giving evidence for the theory of structure-activity relationship between some flavones and their antioxidant capability. Perpetual search for new radical scavenging agents in Oroxylum indicum is emboldened considering its partially exploited potential in this study


Subject(s)
Plant Extracts/analysis , Bignoniaceae/classification , Methanol/analysis , Antioxidants/adverse effects , In Vitro Techniques , Plant Stems/adverse effects , Inhibitory Concentration 50 , Plant Bark/adverse effects , Flavones
6.
Article in English | WPRIM | ID: wpr-691396

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of total flavone of haw leaves (TFHL) on the expression of nuclear factor erythroid-2 related factor (Nrf2) and other related factors in nonalcoholic steatohepatitis (NASH) rats induced by high-fat diet and then to further discuss the mechanism of TFHL's prevention against NASH.</p><p><b>METHODS</b>High-fat diet was fed to 40 rats to establish the NASH model. Then model rats were intragastrically administrated with 40, 80, 160 mg/(kg•day) TFHL, respectively. The pathological changes of liver tissues in NASH rats were detected by oil red O and hematoxylin-eosin (HE) stainings. The expression of Nrf2 in rat liver was examined through immunohistochemistry. The level of 8-iso-prostaglandin F2α in serum was detected through enzyme linked immunosorbent assay (ELISA). The mRNA and protein levels of Nrf2 and other related factors in liver tissue were measured by real-time reverse transcriptionpolymerase chain reaction and western blot.</p><p><b>RESULTS</b>Lipid deposition, hepatic steatosis, focal necrosis in lobular inflammation and ballooning degeneration were emerged in livers of NASH rats. The 8-iso-prostaglandin F2α in the serum of NASH rats increased significantly compared with the control group (P<0.05). The mRNA of Nrf2, hemeoxyenase1 (HO-1) and the mRNA and protein levels of quinine oxidoreductase (NQO1) in NASH rats liver tissue showed a striking increase, while the mRNA levels of Keap1, r-glutamylcysteine synthethase (rGCS) and glutathione S-transferase (GST) were significantly decreased compared with the control group (P<0.05). After TFHL treatment, 8-iso-prostaglandin F2α level in serum significantly decreased, and Nrf2 mRNA and protein levels in hepatocytes nucleus enhanced compared with the model group (P<0.05 or 0.01). Meanwhile the Keap1 mRNA, the mRNA and protein levels of HO-1, NQO1 antibody, rGCS antibody, GST increased after TFHL treatment (P<0.05 or 0.01).</p><p><b>CONCLUSIONS</b>Nrf2 and other related factors were involved in development of NASH, and they also served as an important part in its occurrence. By regulating expression of Nrf2 and other related factors, TFHL may play a role in antioxidative stress and prevention of NASH.</p>


Subject(s)
Animals , Cell Nucleus , Metabolism , Crataegus , Chemistry , Dinoprost , Metabolism , Flavones , Pharmacology , Therapeutic Uses , Lipids , Chemistry , Liver , Metabolism , Pathology , NF-E2-Related Factor 2 , Genetics , Metabolism , Non-alcoholic Fatty Liver Disease , Drug Therapy , Genetics , Pathology , Phytotherapy , Plant Leaves , Chemistry , RNA, Messenger , Genetics , Metabolism , Rats, Sprague-Dawley
7.
Article in Chinese | WPRIM | ID: wpr-690005

ABSTRACT

<p><b>OBJECTIVE</b>To explore function and related molecular mechanism of osteopractic total flavone (OTF) on tendon healing in rats.</p><p><b>METHODS</b>Ten male rats aged for 8 weeks were collected and weighted from 180 to 220 g. Tendon stem cells were cultivated, the third tendon stem cells were used for experiment. OTP treated with 0, 0.1, 1, 10 ng/ml were added into tendon stem cells, and expression change of ALP, Runx2, OCN, VEGF, P-S6, P-4E/BP1 were detected after 14 days. Forty male rats aged for 8 weeks (weighted 180 to 220 g) were established extra-articular tendon-bone transplanting healing model, and divided into experimental group and control group. Experimental group were treated with OTF(100 mg·kg⁻¹·d⁻¹), while control group was treated by normal saline with the same volume. Tendon-bone healing degree were detected by biomechanical testing at 3 and 6 weeks after surgery, histological detection were applied to detect tendon-bone healing and number of new vessles.</p><p><b>RESULTS</b>After treated by OTP, ALP staining and active index detection showed there were statistical differences among 0, 0.1, 1, 10 ng/ml group. After 14 days' cultivation, western blotting results showed mTOR downstream marker protein P-S6 protein expression were gradually increased with increase of density of OTP, expression of P-4E/BP1 was reduced, while expression of Runx2, OCN, VEGF were increased. Biological detection results showed that there was no significant difference in mechanical strength between experimental group(0.78±0.05) N/mm and control group (0.51±0.02) N/mm at 3 weeks after surgery, while mechanical strength in experimental group (1.36±0.09) N/mm was higher than control group (1.01±0.08) N/mm at 6 weeks after surgery. Histological results showed maturity of tendon-bone surface cell were higher at 3 and 6 weeks in experimental group, sharpey fiber growth more density, calcification extent of mesenchyme was high, and new bone, vessels were increased.</p><p><b>CONCLUSIONS</b>OTF could promote osteogenic differentiation of tendon stem cells through mTOR signaling in vitro, and stimulate tendon-bone healing in bone tunnel and enhance connection quality between tendon and bone.</p>


Subject(s)
Animals , Biomechanical Phenomena , Bone Transplantation , Cell Differentiation , Cells, Cultured , Flavones , Pharmacology , Male , Osteogenesis , Rats , Stem Cells , Cell Biology , TOR Serine-Threonine Kinases , Metabolism , Tendons , Cell Biology , Transplantation , Wound Healing
8.
Article in English | WPRIM | ID: wpr-739679

ABSTRACT

Cirsium japonicum belongs to the Asteraceae or Compositae family and is a medicinal plant in Asia that has a variety of effects, including tumour inhibition, improved immunity with flavones, and antidiabetic and hepatoprotective effects. Silymarin is synthesized by 4-coumaroyl-CoA via both the flavonoid and phenylpropanoid pathways to produce the immediate precursors taxifolin and coniferyl alcohol. Then, the oxidative radicalization of taxifolin and coniferyl alcohol produces silymarin. We identified the expression of genes related to the synthesis of silymarin in C. japonicum in three different tissues, namely, flowers, leaves, and roots, through RNA sequencing. We obtained 51,133 unigenes from transcriptome sequencing by de novo assembly using Trinity v2.1.1, TransDecoder v2.0.1, and CD-HIT v4.6 software. The differentially expressed gene analysis revealed that the expression of genes related to the flavonoid pathway was higher in the flowers, whereas the phenylpropanoid pathway was more highly expressed in the roots. In this study, we established a global transcriptome dataset for C. japonicum. The data shall not only be useful to focus more deeply on the genes related to product medicinal metabolite including flavolignan but also to study the functional genomics for genetic engineering of C. japonicum.


Subject(s)
Asia , Asteraceae , Cirsium , Dataset , Estrone , Flavones , Flowers , Gene Expression Profiling , Genetic Engineering , Genomics , Humans , Plants, Medicinal , Sequence Analysis, RNA , Silymarin , Transcriptome
9.
Article in Chinese | WPRIM | ID: wpr-771531

ABSTRACT

The aim of this paper was to study the effect of total flavones of Clematis filamentosa Dunn(TFCD) post-conditioning against myocardial ischemia-reperfusion injury (MIRI) and the role of PI3K/Akt-eNOS signaling pathway. Forty male SD rats were divided randomly into five groups: Sham group, model group (I/R), TFCD post-conditioning group (TFCD), TFCD post-condition-ing+LY294002 (a PI3K/Akt signaling pathway inhibitor) group (TFCD+LY), and LY294002 group (LY). At the end of reperfusion, hemodynamic parameters were recorded, morphology changes of myocardial tissue were evaluated by using HE staining, and myocardial infarct size were observed, blood samples were obtained to determine plasma activation of lactate dehydrogenase (LDH), creatine kinase (CK) nitric oxide (NO), endothelial nitric oxide synthase (eNOS), superoxide dismutase (SOD), maleic dialdehyde (MDA) and glutathione peroxidase (GSH-Px). The expressions of Akt, p-Akt, eNOS and p-eNOS proteins were assessed by using Western blot, and eNOS and inducible nitric oxide synthase (iNOS) mRNA was measured by RT-PCR. The results showed that, compared with the model group, TFCD post-conditioning remarkably improved hemodynamics function and myocardial structure, reduced myocardial infarct size and enhanced the contents of NO, eNOS, SOD and GSH-Px, and decreased the contents of LDH, CK and MDA, increased the levels of phosphorylation of Akt and eNOS protein expression, eNOS and iNOS mRNA expression significantly(P<0.05 or P<0.01). These effects were inhibited by LY294002, a blocker of PI3K/Akt signaling pathway. The above experiments indicated that TFCD post-conditioning could significantly reduce MIRI in rats, the mechanism of which may be associated with increasing antioxidation, scavenging oxygen free radicals, regulating NO generation and activating PI3K/Akt-eNOS signaling pathway.


Subject(s)
Animals , Clematis , Flavones , Male , Myocardial Reperfusion Injury , Nitric Oxide Synthase Type III , Phosphatidylinositol 3-Kinases , Proto-Oncogene Proteins c-akt , Rats , Rats, Sprague-Dawley , Signal Transduction
10.
Braz. j. med. biol. res ; 50(8): e5991, 2017. graf
Article in English | LILACS | ID: biblio-888980

ABSTRACT

Asthma is a chronic allergic disease characterized by airway inflammation, airway hyper-responsiveness (AHR), and mucus hypersecretion. T-lymphocytes are involved in the pathogenesis of asthma, mediating airway inflammatory reactions by secreting cytokines. The phosphoinositide 3-kinase (PI3K) and Notch signaling pathways are associated with T cell signaling, proliferation, and differentiation, and are important in the progression of asthma. Thus, compounds that can modulate T cell proliferation and function may be of clinical value. Here, we assessed the effects of tangeretin, a plant-derived flavonoid, in experimental asthma. BALB/c mice at postnatal day (P) 12 were challenged with ovalbumin (OVA). Separate groups of mice (n=18/group) were administered tangeretin at 25 or 50 mg/kg body weight by oral gavage. Dexamethasone was used as a positive control. Tangeretin treatment reduced inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF) and also restored the normal histology of lung tissues. OVA-specific IgE levels in serum and BALF were reduced. AHR, as determined by airway resistance and lung compliance, was normalized. Flow cytometry analyses revealed a reduced Th17 cell population. Tangeretin reduced the levels of Th2 and Th17 cytokines and raised IFN-γ levels. PI3K signaling was inhibited. The expressions of the Notch 1 receptor and its ligands Jagged 1 and 2 were downregulated by tangeretin. Our findings support the possible use of tangeretin for treating allergic asthma.


Subject(s)
Animals , Mice , Asthma/drug therapy , Signal Transduction/drug effects , Anti-Asthmatic Agents/therapeutic use , Flavones/therapeutic use , Asthma/immunology , Cytokines/drug effects , Cytokines/immunology , Th2 Cells/drug effects , Th2 Cells/immunology , Th1 Cells/drug effects , Th1 Cells/immunology , Disease Models, Animal , Proto-Oncogene Proteins c-akt/drug effects , Proto-Oncogene Proteins c-akt/immunology , Th17 Cells/drug effects , Th17 Cells/immunology , Animals, Newborn , Mice, Inbred BALB C
11.
Pakistan Journal of Pharmaceutical Sciences. 2017; 30 (6): 2085-2089
in English | IMEMR | ID: emr-189718

ABSTRACT

A novel flavone derivative has been synthesized in good yield from ketone and aldehyde. The structure has been established by different spectroscopic techniques like H NMR, C NMR, IR and elemental analysis. The compound was then screened for its acute toxicity and antinociceptive activity studies on animal model. The novel compound was safe upto a maximum dose of 500mg/kg body weight oral dose in mice and showed 65.92 and 82.18% pheriperal analgesic activity at 15 and 30mg/kg body weight doses. Central antinociceptive activity of the compound was 53.13 and 64.44% at 15 and 30mg/kg body weight respectively


Subject(s)
Animals, Laboratory , Flavones , Analgesics , Mice , Toxicity Tests, Acute , Chalcone
12.
Article in Korean | WPRIM | ID: wpr-31813

ABSTRACT

PURPOSE: The purpose of this study was to estimate the dietary flavonoid intakes of Korean adults according to socioeconomic status. METHODS: Using data from the 2007~2012 Korea National Health and Nutrition Examination Survey, a total of 31,112 subjects aged over 19 years were included in this study. We estimated individuals' daily intakes of total flavonoids and seven flavonoid subclasses, including flavonols, flavones, flavanones, flavan-3-ols, anthocyanins, proanthocyanidin, and isoflavones,by linking food consumption data with the flavonoids database for commonly consumed Korean foods. We compared intakes of flavonoids according to the levels of household income and education. RESULTS: Average dietary flavonoid intakes of the study subjects were 321.8 mg/d in men and 308.3 mg/d in women. Daily flavonoid intakes were positively associated with household income level (p < 0.0001) and education level (p < 0.0001). The subjects in the highest household income and highest education level group (OR 0.37, 95% CI 0.30~0.45, p < 0.0001 in men, OR 0.50, 95% CI 0.41~0.60, p < 0.0001 in women) had a lower likelihood of having low total flavonoid intake (less than 25 percentile) compared to the lowest household income and lowest education level group. The food group that contributed to total flavonoid intake with the biggest difference between the lowest and highest groups for both household income level and education level was beverages. CONCLUSION: This study shows that socioeconomic status was positively associated with flavonoid intake in a representative Korean population. Further research is needed to analyze the association of flavonoid intake with health outcomes according to socioeconomic status such as household income and education level.


Subject(s)
Adult , Anthocyanins , Beverages , Education , Family Characteristics , Female , Flavanones , Flavones , Flavonoids , Flavonols , Humans , Korea , Male , Nutrition Surveys , Social Class
13.
Rev. peru. med. integr ; 2(3): 803-809, 2017. tab, graf, ilus
Article in Spanish | LILACS, MTYCI | ID: biblio-876804

ABSTRACT

Objetivos: Proponer la estructura química de componentes fenólicos aislados del extracto etanólico de hojas de Satureja pulchella "panisara", quien en la actualidad presenta el nombre de Clinopodium pulchellum (Kunth) Govaerts y evaluar preliminarmente el posible efecto antioxidante de los compuestos fenólicos. Materiales y métodos: Se realizó una identificación fitoquímica mediante ensayos de solubilidad, tamizaje fitoquímico, cromatografía en capa fina y espectroscopía UV/VIS. Por otro lado, se realizó un ensayo preliminar de la actividad antioxidante usando la prueba de 1,1-difenil-2-picrilhidracilo (DPPH). Resultados: Se determinó que el extracto etanólico de hojas de Clinopodium pulchellum (Kunth) Govaerts "panisara" es soluble en solventes polares. Los metabolitos secundarios encontrados son compuestos fenólicos tipo flavonoides, alcaloides, quinonas y glicosidos. Se propone siete estructuras químicas de flavonoides a través del análisis de los espectros UV/Vis, y mediante comparación con lo publicado por TJ Mabry y Olga Lock. Al realizar el ensayo preliminar de la actividad antioxidante usando la prueba de 1,1-difenil-2-picrilhidracilo (DPPH) se observó disminución de absorbancia, al aplicar el extracto frente al control. Conclusiones: Se propone la estructura química de 7 metabolitos secundarios tipo flavonas que podrían explicar una posible acción antioxidante del extracto etanólico de hojas de Clinopodium pulchellum (Kunth) Govaerts "panisara".


Subject(s)
Humans , Phenolic Compounds , Plant Extracts/chemistry , Spectrum Analysis , Antioxidants , Flavones
14.
Einstein (Säo Paulo) ; 14(1): 56-63, Jan.-Mar. 2016. tab, graf
Article in English | LILACS | ID: lil-778496

ABSTRACT

ABSTRACT Objective To evaluate the phytochemical composition of hydroethanolic extracts from powdered aerial parts of Turnera diffusa Willd (Turneraceae; T. diffusa), as well as its toxicity in astrocytes. Methods Chemical analyses of hydroethanolic extract from powdered aerial parts ofT. diffusa were carried out using HPLC-DAD-ESI-MS/MS.In vitro assays using astrocytes culture were performed to evaluate cell death. Results Flavone-C, O-diglycosides, such as, luteolin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside, apigenin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside and apigenin-7-O-6”-p-coumaroylglucoside were the main compounds found in this hydroethanolic extract. Concentration time-effect demonstrated the toxicity of this extract at a concentration of 1,000µg/mL in astrocyte culture, after 6 and 24 hours of incubation. Conclusion In phytochemical analyses, important antioxidants (mainly flavonoids) were observed. T. diffusa extracts presented cytotoxic effect in high concentrations, leading to increased cell death in astrocyte culture.


RESUMO Objetivo Avaliar a composição fitoquímica do extrato hidroetanólico das partes aéreas de Turnera diffusa Willd (Turneraceae; T. diffusa) e sua toxicidade em astrócitos. Métodos Análises químicas do extrato hidroetanólico de partes aéreas de T. diffusa foram feitas por HPLC-DAD-ESI-MS/MS. Os ensaiosin vitro utilizaram culturas de astrócitos para avaliar morte celular. Resultados Flavonas-C, O-diglicosídeos, como, luteolina-8-C-[6-deoxi-2-O-raminosil]-xilo-hexos-3-ulosideo, apigenina-8-C-[6-deoxi-2-O-raminosil]-xilo-hexos-3-ulosideo e apigenina-7-O-6”-p-cumaroilglucosídeo foram os principais constituintes encontrados neste extrato hidroetanólico. Uma curva tempo-concentração demonstrou toxicidade desse extrato na concentração de 1.000µg/mL, na cultura de astrócitos após 6 e 24 horas de incubação. Conclusão Nas análises fitoquímicas, importantes antioxidantes, sobretudo flavonoides, foram observados. Extratos de T. diffusa apresentaram efeitos citotóxicos em altas concentrações, ocasionando aumento de morte celular em cultura de astrócitos.


Subject(s)
Animals , Rats , Plant Extracts/chemistry , Astrocytes/drug effects , Turnera/chemistry , Antioxidants/chemistry , Plant Extracts/toxicity , Astrocytes/chemistry , Chromatography, High Pressure Liquid/methods , Cell Death/drug effects , Spectrometry, Mass, Electrospray Ionization/methods , Flavones/analysis , Flavones/toxicity
15.
Bol. latinoam. Caribe plantas med. aromát ; 15(1): 29-40, ene. 2016. ilus, graf, tab
Article in English | LILACS | ID: biblio-907515

ABSTRACT

Pedalitin, isolated from the aerial part of Rabdosia japonica (Labiatae), inhibited soybean lipoxygenase-1 (EC 1.13.11.12, Type I) with an IC50 of 152.5 uM. The progress curves for an enzyme reaction, pedalitin inactivate the lipoxygenase-1 in a time dependent, irreversible manner, exhibiting kinetics with a kinact/KI of 59.6 +/- 10 mM-1min-1. In the pseudoperoxidase activity, pedalitin is very slowly oxidized by the soybean lipoxygenase-1 catalyzed decomposition of lipid hydroperoxides.


Pedalitina, aislada de las partes aereas de Rabdosia japonica inhibió a la lipooxigenasa-1 (EC 1.13.11.12 tipo I) con un IC50 de 152.5 uM. La curva de progreso para una acción enzimática, pedalitina inactivó a la lipooxigenasa-1 de una manera dependiente del tiempo, de una manera irreversible, exhibiendo una cinética con una kinact/KI de 59.6 +/- mM-1min-1. En la actividad pseudoperoxidasa, pedalitina es oxidada lentamente por la descomposición de la lípido hidroperóxido de la lipooxigenasa-1 de poroto de soya.


Subject(s)
Flavones/isolation & purification , Flavones/pharmacology , Isodon/chemistry , Lipoxygenase Inhibitors/pharmacology , Soybeans/enzymology , Kinetics , Lipoxygenase Inhibitors/isolation & purification , Time Factors
16.
Article in Chinese | WPRIM | ID: wpr-286313

ABSTRACT

<p><b>OBJECTIVE</b>To explore the protective effect and mechanism of total flavones of Bidens pilosa L. (TFB) on IgA1 induced injury of venous endothelial cells in Henoch-Schönlein purpura (HSP) children patients. METHODS Human umbilical venous endothelial cells (HUVECs) were taken as subject. They were intervened by normal IgA1 and HSP children patients' serum IgA1, and added with different concentrations TFB at the same time. Then they were divided into the blank control group, the normal control group, the HSP IgA1 group, and HSP IgA1 plus TFB (1.0, 0.5, 0.25 mg/mL) groups. Levels of TNF-α and IL-8 in supernate were detected by ELISA. The NO level was detected by nitrate reductase method. mRNA and protein expressions of NF-κB and ICAM-1 in HUVECs were detected by fluorescent quantitative PCR and Western blot respectively.</p><p><b>RESULTS</b>Compared with the normal control group and the blank control group, levels of IL-8, TNF-α, and NO all significantly increased in the HSP group (P < 0.05). Compared with the HSP group, levels of IL-8, TNF-α, and NO significantly decreased after intervention of TFB (1.0 and 0.5 mg/mL; P < 0.05, P < 0.01). Results of fluorescent quantitative PCR and Western blot showed, as compared with the blank control group and the normal control group, mRNA and protein expressions of NF-κB and ICAM-1 in HSP children patients' serum IgA1 induced venous endothelial cells significantly increased with statistical difference (P < 0.05, P < 0.01). Compared with the HSP group, mRNA and protein expressions of NF-KB and ICAM-1 were obviously down-regulated after intervention of TFB (1.0, 0.5, 0.25 mg/mL), with statistical difference (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>TFB could protect vascular damage by inhibiting in vivo high expression of NF-κB, reducing the production of IL-8, TNF-α, and NO in vascular endothelial cells of HSP children patients.</p>


Subject(s)
Bidens , Chemistry , Child , Flavones , Pharmacology , Human Umbilical Vein Endothelial Cells , Humans , Immunoglobulin A , Blood , Intercellular Adhesion Molecule-1 , Metabolism , Interleukin-8 , Metabolism , NF-kappa B , Metabolism , Nitric Oxide , Metabolism , Purpura, Schoenlein-Henoch , Blood , RNA, Messenger , Metabolism , Tumor Necrosis Factor-alpha , Metabolism
17.
Article in English | WPRIM | ID: wpr-812481

ABSTRACT

The present study was designed to isolate and characterize the analgesic compounds of Artemisa sacrorum Ledeb. The EtOAc crude extracts from the aerial parts of Artemisa sacrorum Ledeb were separated by chromatography and the structures of new compounds were elucidated based on spectral analyses. Analgesic activities of the isolated compounds were assessed in rats with hot plate test and paw pressure assay. Two new flavone C-glycosides, named as Sacroroside A and B (Compounds 1 and 2) were isolated from the EtOAc crude extract of the aerial parts ofArtemisa sacrorum Ledeb. They showed significant analgesic effects. In conclusion, Compounds 1 and 2 are new natural products, which show significant analgesic effects in a dose-dependent manner.


Subject(s)
Analgesics , Chemistry , Pharmacology , Therapeutic Uses , Animals , Artemisia , Chemistry , Disaccharides , Chemistry , Pharmacology , Therapeutic Uses , Flavanones , Chemistry , Pharmacology , Therapeutic Uses , Flavones , Chemistry , Pharmacology , Therapeutic Uses , Hot Temperature , Male , Molecular Structure , Pain , Drug Therapy , Phytotherapy , Plant Components, Aerial , Plant Extracts , Chemistry , Pharmacology , Therapeutic Uses , Pressure , Rats, Wistar
18.
Article in Chinese | WPRIM | ID: wpr-337928

ABSTRACT

The current study to separate and identify constituents from Millettia nitida var. hirsutissima. The compounds from Millettia nitida var. hirsutissima were isolated by means of various chromatographic techniques such as column chromatography over ODS and Sephadex LH-20, preparative HPLC, and the structures of these isolated compounds were identified through spectroscopic analyses. Nine isoflavonoids and two flavans were isolated and identified as 5-O-methy genistein (1), 7-hydroxy-3',4'-dimethoxyisoflavone (2), ononin (3), catechin (4), formononetin (5), genistein (6), calycosin (7), (-)-gallocatechin (8), sissotrin (9), wistin (10), daidzin (11). Compounds 1, 2, 9 are obtained from the genus Millettia for the first time,and compounds 4, 8 are isolated from this plant for the first time.


Subject(s)
Drugs, Chinese Herbal , Chemistry , Flavones , Chemistry , Isoflavones , Chemistry , Mass Spectrometry , Millettia , Chemistry , Molecular Structure
19.
Article in Chinese | WPRIM | ID: wpr-351311

ABSTRACT

This research established an HPLC method for determination of six C-Glycoside flavones of warer-soluble total flavonoids from Isodon lophanthoides var. gerardianus (Benth.) H. Hara, and studied the antitumor activity of the warer-soluble total flavonoids. The HPLC system consisted of Kromasil 100-5 C18 (4.6 mm x 250 mm, 5 microm) column and a solution system of methanol, acetonitrile and 0.5% formic acid gradient elution at a flow rate of 0. 8 mL x min(-1) and the wavelength of detector was at 334 nm. The column temperature was 25 degrees C. The antitumor activity of water-soluble flavonoids was assayed using HepG2 cell as the tested cell. The linear ranges of vicenin II, vicenin III, isoschaftoside, schaftoside, vitexin, 6, 8-di-C-a-L-arabinosylapigenin were 0.25-2.53, 0.12-1.20, 0.37-3.69, 0.16-1.63, 0.19-1.92, 0.14-1.42 microg, respectively. The average recoveries (n = 6) were 99.6% (RSD 0.87%), 100.2% (RSD 2.0%), 99.6% (RSD 1.8%), 97.9% (RSD 1.5%), 98.8% (RSD 1.2%), 98.6% (RSD 1.2%), respectively. After exposure in 24, 48, 72 h, the total flavonoids showed inhibitory effect on the proliferation of HepG2 cells with IC50 as the evaluation index, the IC50 values of 1.89, 1.71, 1.51 g x L(-1), respectively. The method is quick, simple and accurate with good re- producibility, and can be used for determination of vicenin II, vicenin III, isoschaftoside, schaftoside, vitexin, 6, 8-di-C-a-L-arabino- sylapigenin in the warer-soluble total flavonoids from L lophanthoides var. gerardianus. The warer-soluble total flavonoids from L lophanthoides have inhibitory effect on the proliferation of HepG2 cells.


Subject(s)
Antineoplastic Agents, Phytogenic , Pharmacology , Cell Line, Tumor , Cell Proliferation , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Pharmacology , Flavones , Pharmacology , Humans , Isodon , Chemistry , Monosaccharides , Pharmacology
20.
Article in Chinese | WPRIM | ID: wpr-279261

ABSTRACT

A phytochemical investigation on the stems of Garcinia bracteata collected from Xishuangbanna resulted in the isolation of a new flavone. By analysis of the HRESIMS, IR, UV, 1D and 2D NMR spectra, the structure of the new compound was determined as 7-methoxy-4',6-dihydroxy-8-isobutyryl-flavone(1). Compound 1 was also tested for its anti-tobacco mosaic virus(TMV) activity. Results suggested the 1 possessed remarkable anti-TMV activity, with an inhibition rate of 28.2%.


Subject(s)
Antiviral Agents , Chemistry , Pharmacology , Drugs, Chinese Herbal , Chemistry , Pharmacology , Flavones , Chemistry , Pharmacology , Garcinia , Chemistry , Magnetic Resonance Spectroscopy , Plant Leaves , Chemistry , Tobacco Mosaic Virus
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