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1.
Chinese journal of integrative medicine ; (12): 683-690, 2023.
Article in English | WPRIM | ID: wpr-982302

ABSTRACT

OBJECTIVE@#To explore the proliferation inhibitory effect of quinones from Blaps rynchopetera defense secretion on colorectal tumor cell lines.@*METHODS@#Human colorectal cancer cell HT-29, human colorectal adenocarcinoma cell Caco-2 and normal human colon epithelial cell CCD841 were chosen for the evaluation of inhibitory activity of the main quinones of B. rynchopetera defense secretion, including methyl p-benzoquinone (MBQ), ethyl p-benzoquinone (EBQ), and methyl hydroquinone (MHQ), through methyl thiazolyl tetrazolium assay. The tumor-related factors, cell cycles, related gene expressions and protein levels were detected by enzyme-linked immunosorbent assy, flow cytometry, RT-polymerase chain reaction and Western blot, respectively.@*RESULTS@#MBQ, EBQ, and MHQ could significantly inhibit the proliferation of Caco-2, with half maximal inhibitory concentration (IC50) values of 7.04 ± 0.88, 10.92 ± 0.32, 9.35 ± 0.83, HT-29, with IC50 values of 14.90 ± 2.71, 20.50 ± 6.37, 13.90 ± 1.30, and CCD841, with IC50 values of 11.40 ± 0.68, 7.02 ± 0.44 and 7.83 ± 0.05 µg/mL, respectively. Tested quinones can reduce the expression of tumor-related factors tumor necrosis factor α, interleukin (IL)-10, and IL-6 in HT-29 cells, selectively promote apoptosis, and regulate the cell cycle which can reduce the proportion of cells in the G1 phase and increase the proportion of the S phase. Meanwhile, tested quinones could up-regulate mRNA and protein expression of GSK-3β and APC, while down-regulate that of β-catenin, Frizzled1, c-Myc, and CyclinD1 in the Wnt/β-catenin pathway of HT-29 cells.@*CONCLUSION@#Quinones from B. rynchopetera defense secretion could inhibit the proliferation of colorectal tumor cells and reduce the expression of related factors, which would be functioned by regulating cell cycle, selectively promoting apoptosis, and affecting Wnt/β-catenin pathway-related mRNA and protein expressions.


Subject(s)
Humans , beta Catenin/metabolism , Caco-2 Cells , Quinones/pharmacology , Glycogen Synthase Kinase 3 beta/metabolism , Cell Proliferation , Colorectal Neoplasms/metabolism , Cell Line, Tumor , Apoptosis , Benzoquinones/pharmacology , RNA, Messenger , Wnt Signaling Pathway
2.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 148-154, 2022.
Article in English | WPRIM | ID: wpr-929245

ABSTRACT

Four new sesquiterpene quinone meroterpenoids, dysideanones F-G (1-2) and dysiherbols D-E (3-4), were isolated from the marine sponge Dysidea avara collected from the South China Sea. The new structures were elucidated by extensive analysis of spectroscopic data including HR-MS and 1D and 2D NMR spectra, and their absolute configurations were assigned by single-crystal X-ray diffraction and ECD calculations. Anti-inflammatory evaluation showed that dysiherbols D-E (3-4) exhibited moderate inhibitory activity on TNF-α-induced NF-κB activation in human HEK-293T cells with IC50 values of 10.2 and 8.6 μmol·L-1, respectively.


Subject(s)
Animals , Dysidea/chemistry , Porifera , Quinones/pharmacology , Sesquiterpenes/pharmacology , Skeleton
3.
Acta cir. bras ; 35(12): e351202, 2020. tab, graf
Article in English | LILACS | ID: biblio-1152683

ABSTRACT

Abstract Purpose: To investigate the therapeutic benefits of Hydroxysafflor yellow A (HSYA) on blood-brain barrier (BBB) vulnerability after traumatic brain injury (TBI) and identify its potential action of mechanisms on TBIinduced injuries. Methods: The rat TBI model was performed by using a controlled cortical impact device. The BBB permeability induced by TBI was measured through Evans Blue dye superflux and western blotting or polymerase chain reaction (PCR) for tight junctional proteins (TJPs). The post-TBI changes in oxidative stress markers, inflammatory response and neuron apoptosis in brain tissue were also tested. Results: Herein, the results showed that HSYA acutely attenuated BBB permeability via increasing the production of the TJPs, including occludin, claudin-1 and zonula occludens protein 24 h after TBI. Additionally, HSYA could suppress the secretion of proinflammatory factors, such as interleukin-1β, interleukin-6, and tumor necrosis factor-α (IL-1β, IL-6, and TNF-α), and also concurrently down-regulate the expression of inflammation-related Toll-like receptor 4/nuclear factor kappa-B (TLR4/NF-kB) protein. These HSYA challenged changes were accompanied by the decreased TBI induced oxidative stress markers and inhibited the expression of apoptosis proteins Bax, caspase-3 and caspase-9. Conclusions: Taken together, all findings suggested that HSYA (30 mg/kg) are against TBI through improving the integrity in BBB, which are associated with the antioxidant, anti-inflammation and antiapoptosis via the probable mechanism of down-regulation of the TLR4/NF-kB pathway, and its in-detail protective mechanisms are under study.


Subject(s)
Animals , Rats , Blood-Brain Barrier , Brain Injuries, Traumatic/drug therapy , Permeability , Quinones , Chalcone/analogs & derivatives , Apoptosis , Oxidative Stress , Inflammation/drug therapy
4.
Journal of Cancer Prevention ; : 112-122, 2019.
Article in English | WPRIM | ID: wpr-764304

ABSTRACT

BACKGROUND: NAD(P)H:quinone oxidoreductase-1 (NQO1) is a widely-distributed flavin adenine dinucleotide-dependent flavoprotein that promotes obligatory 2-electron reductions of quinones, quinoneimines, nitroaromatics, and azo dyes. This reduces quinone levels and thereby minimizes generation of excess reactive oxygen species (ROS) formed by redox cycling, and concurrent depletion of intracellular thiol pools. Ajoene is derived from crushed garlic. It is formed by a reaction involving two allicin molecules, and is composed of allyl sulfide and vinyl disulfide. Ajoene is present in two isomers, E- and Z-form. METHODS: Expression of antioxidant enzymes and nuclear factor E2-related factor-2 (Nrf2) was measured by Western blot analysis. NQO1 promoter activity was assessed by the luciferase reporter gene assay. ROS accumulation was monitored by using the fluorescence-generating probe 2′,7′-dichlorofluorescein diacetate. The intracellular glutathione levels were measured by using a commercially available kit. RESULTS: Z-ajoene significantly up-regulated the expression of representative antioxidant enzyme NQO1 in non-tumorigenic breast epithelial MCF-10A cells at non-toxic concentrations. Z-ajoene enhanced up-regulation and nuclear translocation of Nrf2, which plays a pivotal role in the induction of many genes encoding antioxidant enzymes and other cytoprotective proteins. Z-ajoene treatment also increased the activity of nqo1-promoter harboring antioxidant response element consensus sequences in MCF-10A cells. Silencing of Nrf2 by small interfering RNA abrogated ajoene-induced expression of NQO1. Z-ajoene activated extracellular signal-regulated kinase (ERK). Inhibition of ERK activation by U0126 abrogated ability of Z-ajoene to activate Nrf2 and to induce NQO1 expression. Intracellular ROS accumulation was observed after treatment with Z-ajoene, whereas the E-isoform was not effective. The inhibition of ROS by treatment with N-acetylcysteine, a radical scavenger, abrogated Z-ajoene-induced expression of NQO1 as well as activation of ERK and Nrf2, suggesting that Z-ajoene augments the Nrf2-dependent antioxidant defense via ROS generation and ERK activation. CONCLUSIONS: Z-ajoene induces NQO1 expression in MCF-10A cells through ROS-mediated activation of Nrf2.


Subject(s)
Humans , Acetylcysteine , Adenine , Antioxidant Response Elements , Azo Compounds , Blotting, Western , Breast , Consensus Sequence , Epithelial Cells , Flavoproteins , Garlic , Genes, Reporter , Glutathione , Luciferases , NF-E2-Related Factor 2 , Oxidation-Reduction , Phosphotransferases , Quinones , Reactive Oxygen Species , RNA, Small Interfering , Up-Regulation
5.
Chinese journal of integrative medicine ; (12): 36-41, 2016.
Article in English | WPRIM | ID: wpr-287148

ABSTRACT

<p><b>OBJECTIVE</b>This study observed attenuating effect of hydroxysafflor yellow A (HSYA), an effective ingredient of aqueous extract of Carthamus tinctorius L, on lipopolysaccharide (LPS)-induced endothelium inflammatory injury.</p><p><b>METHODS</b>Eahy926 human endothelium cell (EC) line was used; thiazolyl blue tetrazolium bromide (MTT) test was assayed to observe the viability of EC; Luciferase reporter gene assay was applied to measure nuclear factor-κB (NF-κB) p65 subunit nuclear binding activity in EC; Western blot technology was used to monitor mitogen activated protein kinase (MAPKs) and NF-κB activation. Reverse transcription polymerase chain reaction (RT-PCR) method was applied to observe intercellular cell adhesion molecule-1 (ICAM-1) and E-selectin mRNA level; EC surface ICAM-1 expression was measured with flow cytometry and leukocyte adhesion to EC was assayed with Rose Bengal spectrophotometry technology.</p><p><b>RESULTS</b>HSYA protected EC viability against LPS-induced injury (P <0.05). LPS-induced NF-κB p65 subunit DNA binding (P <0.01) and nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor α (IκBα) phosphorylation was inhibited by HSYA. HSYA attenuated LPS triggered ICAM-1 and E-selectin mRNA levels elevation and phosphorylation of p38 MAPK or c-Jun N-terminal kinase MAPK. HSYA also inhibited LPS-induced cell surface ICAM-1 protein expression P <0.01) and leukocyte adhesion to EC (P <0.05).</p><p><b>CONCLUSION</b>HSYA is effective to protect LPS-induced high expression of endothelium adhesive molecule and inflammatory signal transduction.</p>


Subject(s)
Humans , Cell Adhesion , Cell Nucleus , Metabolism , Cell Survival , Chalcone , Chemistry , Pharmacology , Therapeutic Uses , E-Selectin , Genetics , Metabolism , Endothelium, Vascular , Pathology , Gene Expression Regulation , Human Umbilical Vein Endothelial Cells , Metabolism , Pathology , I-kappa B Proteins , Metabolism , Inflammation , Drug Therapy , Pathology , Intercellular Adhesion Molecule-1 , Genetics , Metabolism , Leukocytes , Cell Biology , Lipopolysaccharides , MAP Kinase Signaling System , NF-KappaB Inhibitor alpha , Phosphorylation , Protective Agents , Pharmacology , Protein Binding , Quinones , Chemistry , Pharmacology , Therapeutic Uses , RNA, Messenger , Genetics , Metabolism
6.
Tuberculosis and Respiratory Diseases ; : 257-266, 2016.
Article in English | WPRIM | ID: wpr-125743

ABSTRACT

BACKGROUND: Idiopathic pulmonary fibrosis is a common interstitial lung disease; it is a chronic, progressive, and fatal lung disease of unknown etiology. Over the last two decades, knowledge about the underlying mechanisms of pulmonary fibrosis has improved markedly and facilitated the identification of potential targets for novel therapies. However, despite the large number of antifibrotic drugs being described in experimental pre-clinical studies, the translation of these findings into clinical practices has not been accomplished yet. NADH:quinone oxidoreductase 1 (NQO1) is a homodimeric enzyme that catalyzes the oxidation of NADH to NAD+ by various quinones and thereby elevates the intracellular NAD⁺ levels. In this study, we examined the effect of increase in cellular NAD⁺ levels on bleomycin-induced lung fibrosis in mice. METHODS: C57BL/6 mice were treated with intratracheal instillation of bleomycin. The mice were orally administered with β-lapachone from 3 days before exposure to bleomycin to 1-3 weeks after exposure to bleomycin. Bronchoalveolar lavage fluid (BALF) was collected for analyzing the infiltration of immune cells. In vitro, A549 cells were treated with transforming growth factor β1 (TGF-β1) and β-lapachone to analyze the extracellular matrix (ECM) and epithelial-mesenchymal transition (EMT). RESULTS: β-Lapachone strongly attenuated bleomycin-induced lung inflammation and fibrosis, characterized by histological staining, infiltrated immune cells in BALF, inflammatory cytokines, fibrotic score, and TGF-β1, α-smooth muscle actin accumulation. In addition, β-lapachone showed a protective role in TGF-β1–induced ECM expression and EMT in A549 cells. CONCLUSION: Our results suggest that β-lapachone can protect against bleomycin-induced lung inflammation and fibrosis in mice and TGF-β1–induced EMT in vitro, by elevating the NAD+/NADH ratio through NQO1 activation.


Subject(s)
Animals , Mice , Actins , Bleomycin , Bronchoalveolar Lavage Fluid , Cytokines , Epithelial-Mesenchymal Transition , Extracellular Matrix , Fibrosis , Idiopathic Pulmonary Fibrosis , In Vitro Techniques , Inflammation , Lung Diseases , Lung Diseases, Interstitial , Lung , NAD , Pneumonia , Pulmonary Fibrosis , Quinones , Transforming Growth Factor beta1 , Transforming Growth Factors
7.
Mycobiology ; : 157-162, 2015.
Article in English | WPRIM | ID: wpr-729847

ABSTRACT

Lichen-forming fungal proteins have been seldom searched due to many difficulties in their extraction. Phenols, quinones, proteases, and other components released during cell disruption have been known to be the greatest challenges related to protein extraction from lichens. To overcome these problems and maintain good electrophoretic resolution and high protein concentration, an extraction buffer containing polyvinylpolypyrrolidone, ascorbic acid, Triton X-100, polyethylene glycol, proteinase, and oxidase inhibitors in sodium phosphate buffer was developed. This extraction buffer showed high efficiency for all lichen species tested in the study.


Subject(s)
Ascorbic Acid , Electrophoresis , Fungal Proteins , Lichens , Octoxynol , Oxidoreductases , Peptide Hydrolases , Phenol , Phenols , Polyethylene Glycols , Quinones , Sodium
8.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 561-577, 2015.
Article in English | WPRIM | ID: wpr-812509

ABSTRACT

The ocean continues to provide a plethora of unique scaffolds capable of remarkable biological applications. A large number of pyrroloiminoquinone alkaloids, including discorhabdins, epinardins, batzellines, makaluvamines, and veiutamine, have been isolated from various marine organisms. A class of pyrroloiminoquinone-related alkaloids, known as bispyrroloquinones, is the focus of this review article. This family of marine alkaloids, which contain an aryl substituted bispyrroloquinone ring system, includes three subclasses of alkaloids namely, wakayin, tsitsikammamines A-B, and zyzzyanones A-D. Both wakayin and the tsitsikammamines contain a tetracyclic fused bispyrroloiminoquinone ring system, while zyzzyanones contain a fused tricyclic bispyrroloquinone ring system. The unique chemical structures of these marine natural products and their diverse biological properties, including antifungal and antimicrobial activity, as well as the potent, albeit generally nonspecific and universal cytotoxicities, have attracted great interest of synthetic chemists over the past three decades. Tsitsikammamines, wakayin, and several of their analogs show inhibition of topoisomerases. One additional possible mechanism of anticancer activity of tsitsikammamines analogs that has been discovered recently is through the inhibition of indoleamine 2, 3-dioxygenase, an enzyme involved in tumoral immune resistance. This review discusses the isolation, synthesis, and evaluation of bioactivities of bispyrroloquinone alkaloids and their analogs.


Subject(s)
Animals , Humans , Alkaloids , Chemistry , Pharmacology , Anti-Infective Agents , Chemistry , Pharmacology , Antineoplastic Agents , Chemistry , Pharmacology , Biological Products , Chemistry , Pharmacology , Indole Alkaloids , Chemistry , Pharmacology , Indoles , Chemistry , Pharmacology , Pyrroles , Chemistry , Pharmacology , Quinolines , Chemistry , Pharmacology , Quinones , Chemistry , Pharmacology
9.
Chinese Journal of Cardiology ; (12): 728-731, 2015.
Article in Chinese | WPRIM | ID: wpr-351613

ABSTRACT

<p><b>OBJECTIVE</b>To elucidate the effect of hydroxysafflor yellow A ( HYSA) on the proliferation of vascular smooth muscle cells (VSMCs) and the related mechanism.</p><p><b>METHODS</b>VSMCs derived from SD rats were treated with DMEC culture medium (Control), 10 ng/ml PDGF (PDGF group), pretreatment with HYSA at different doses (1, 5, 10, 20, 40, 60 µmol/L) for 24 h then cotreatment with PDGF. After 24 h, MTT assay, Western blot and immunohistochemical staining were performed to evaluate the inhibitory effects of HYSA on VSMCs proliferation.</p><p><b>RESULTS</b>HYSA inhibited PDGF induced VSMCs proliferation in a dose-dependent manner, dowregulated proliferating cell nuclear antigen (PCNA) expression and blocked PDGF activated PDGFR-MEK-ERK1/2 signaling pathway.</p><p><b>CONCLUSIONS</b>HYSA inhibits VSMCs proliferation possibly via downregulating the expression of PCNA and blocking MEK-ERK1/2 signal transduction in VSMCs.</p>


Subject(s)
Animals , Rats , Cell Proliferation , Cells, Cultured , Chalcone , MAP Kinase Signaling System , Mitogen-Activated Protein Kinase 1 , Mitogen-Activated Protein Kinase 3 , Mitogen-Activated Protein Kinases , Muscle, Smooth, Vascular , Myocytes, Smooth Muscle , Proliferating Cell Nuclear Antigen , Quinones , Rats, Sprague-Dawley
11.
Bol. latinoam. Caribe plantas med. aromát ; 13(6): 566-574, nov.2014. ilus, tab
Article in English | LILACS | ID: lil-795827

ABSTRACT

The synthesis of new isomeric ellipticine quinones 3a-c and their in vitro antiproliferative activities on cancer cell lines is reported. The designed N-heterocyclic quinones 3a-c were synthesized through a three step sequence which involves: a) one-pot preparation of 4-methoxycarbonyl-3,4-dimethylisoquinoline-5,8-quinone 1 from 2,5-dihydroxyacetophenone, methyl aminocrotonate and silver (II) oxide; b) regioselective amination of 1 with arylamines to give aminoquinones 2a-c and c) palladium-catalyzed intramolecular oxidative coupling of 7-aminoisoquinoline-5,8-quinones 2a-c. The in vitro antiproliferative activity of the new angular quinones was evaluated againts one normal cell line (lung fibroblasts) and gastric, lung and bladder cancer cell lines in 72-h drug exposure assays. The new compounds displayed similar or higher antiproliferative activity with respect to their quinone precursors 2a-c. The isomeric ellipticine quinone 2b appears as the more active member on bladder cancer cell line (IC50: 2.4 uM), comparable to etoposide used as anticancer reference drug...


Se describe la síntesis de las nuevas quinonas 3a-c, isoméricas de elipticina, y sus actividades antiproliferativas in vitro en líneas de células de cáncer. Las quinonas N-heterocíclicas 3a-c se sintetizaron a través de una secuencia que involucra: a) preparación de 4- metoxicarbonil-3,4-dimetlisoquinolin-5,8-quinone 1 a partir de 2,5-dihidroxiacetofenona, aminocrotonato de metilo y óxido de plata (I); b) aminación regioselectiva de 1 con arilaminas para producir las aminoquinonas 2a-c y c) acoplamiento oxidante intramolecular de 7- aminoisoquinolin-5,8-quinonas 2a-c catalizado con paladio. La actividad antiproliferative in vitro de los nuevos compuestos fue evaluada en una línea celular normal (fibroblastos de pulmón) y líneas de células de cáncer gástrico, pulmón y vejiga en ensayos de exposición de 72 horas a la droga. Las quinonas 3a-c exhiben interesantes propiedades antiproliferativas destacando la elipticinquinona isomérica 2b en células de cáncer de vejiga (IC50: 2.4 uM) comparado con etopósido usada como droga anticancer de referencia. Los nuevos compuestos mostraron actividades antiproliferativa similar o mayor respecto de las correspondientes quinonas precursoras 2a-c. La elipticin quinona isomérica 2b corresponde al miembro más activo en células de câncer de vejiga (IC50: 2.4 uM), comparable a la del etopósido, usada como droga anticáncer de referencia...


Subject(s)
Humans , Ellipticines/pharmacology , Ellipticines/chemical synthesis , Cell Proliferation , Quinones/pharmacology , Quinones/chemical synthesis , Cell Line, Tumor , Oxidative Coupling
12.
Braz. j. microbiol ; 45(3): 985-993, July-Sept. 2014. mapas, tab
Article in English | LILACS | ID: lil-727030

ABSTRACT

In the present study, samples of rhizosphere and root nodules were collected from different areas of Pakistan to isolate plant growth promoting rhizobacteria. Identification of bacterial isolates was made by 16S rRNA gene sequence analysis and taxonomical confirmation on EzTaxon Server. The identified bacterial strains were belonged to 5 genera i.e. Ensifer, Bacillus, Pseudomona, Leclercia and Rhizobium. Phylogenetic analysis inferred from 16S rRNA gene sequences showed the evolutionary relationship of bacterial strains with the respective genera. Based on phylogenetic analysis, some candidate novel species were also identified. The bacterial strains were also characterized for morphological, physiological, biochemical tests and glucose dehydrogenase (gdh) gene that involved in the phosphate solublization using cofactor pyrroloquinolone quinone (PQQ). Seven rhizoshperic and 3 root nodulating stains are positive for gdh gene. Furthermore, this study confirms a novel association between microbes and their hosts like field grown crops, leguminous and non-leguminous plants. It was concluded that a diverse group of bacterial population exist in the rhizosphere and root nodules that might be useful in evaluating the mechanisms behind plant microbial interactions and strains QAU-63 and QAU-68 have sequence similarity of 97 and 95% which might be declared as novel after further taxonomic characterization.


Subject(s)
Bacteria/classification , Bacteria/isolation & purification , Plant Roots/microbiology , Soil Microbiology , Bacterial Typing Techniques , Bacteria/genetics , Cluster Analysis , Cytosol/chemistry , DNA, Bacterial/chemistry , DNA, Bacterial/genetics , DNA, Ribosomal/chemistry , DNA, Ribosomal/genetics , Genes , Glucose 1-Dehydrogenase/genetics , Molecular Sequence Data , Pakistan , Phylogeny , Plants , Quinones/analysis , Rhizosphere , /genetics , Sequence Analysis, DNA
13.
Braz. j. microbiol ; 45(2): 603-611, Apr.-June 2014. ilus, tab
Article in English | LILACS | ID: lil-723124

ABSTRACT

Glucose dehydrogenase (GDH; EC 1.1. 5.2) is the member of quinoproteins group that use the redox cofactor pyrroloquinoline quinoine, calcium ions and glucose as substrate for its activity. In present study, Leclercia sp. QAU-66, isolated from rhizosphere of Vigna mungo, was characterized for phosphate solubilization and the role of GDH in plant growth promotion of Phaseolus vulgaris. The strain QAU-66 had ability to solubilize phosphorus and significantly (p < 0.05) promoted the shoot and root lengths of Phaseolus vulgaris. The structural determination of GDH protein was carried out using bioinformatics tools like Pfam, InterProScan, I-TASSER and COFACTOR. These tools predicted the structural based functional homology of pyrroloquinoline quinone domains in GDH. GDH of Leclercia sp. QAU-66 is one of the main factor that involved in plant growth promotion and provides a solid background for further research in plant growth promoting activities.


Subject(s)
Enterobacteriaceae/enzymology , Enterobacteriaceae/physiology , Glucose 1-Dehydrogenase/genetics , Nerve Growth Factors , Phaseolus/growth & development , Phaseolus/microbiology , Cluster Analysis , Computational Biology , Cytosol/chemistry , DNA, Bacterial/chemistry , DNA, Bacterial/genetics , Enterobacteriaceae/genetics , Enterobacteriaceae/isolation & purification , Glucose 1-Dehydrogenase/chemistry , Models, Molecular , Molecular Sequence Data , Phylogeny , Protein Conformation , Protein Structure, Tertiary , Phosphorus/metabolism , Plant Roots/growth & development , Plant Shoots/growth & development , Quinones/analysis , Sequence Analysis, DNA , Sequence Homology
14.
China Journal of Chinese Materia Medica ; (24): 3295-3300, 2014.
Article in Chinese | WPRIM | ID: wpr-244577

ABSTRACT

Bio-active components from Carthamus tinctorius were separated on the basis of antioxidant capacities in vitro. The antioxidant capacity was investigated on the basis of the ability to scavenge DPPH radical, ABTS radical and reduce Fe3+ of different polar fractions. Furthermore, the chemical compounds were isolated from bio-active fraction, and were evaluated for the antioxidative effects. Five major components were isolated and identified from water extract as 6-hydroxykaempferol 3,6,7-tri-O-β-D-glucoside(1), 6-hydroxykaempferol 3-O-β-rutinoside-6-O-β-D-glucoside (2), 6-hydroxykaempferol 3-O-β-D-glucoside (3), hydroxysafflor yellow A (4) and anhydrosafflor yellow B (5). By evaluating and comparing the antioxidative effects of different fractions and obtained compounds, the results showed that water extract displayed significantly high antioxidative activities and 6-hydroxykaempferol glycosides and quinochalcone C-glycosides were found as main contribution for antioxidant property.


Subject(s)
Antioxidants , Metabolism , Pharmacology , Benzothiazoles , Metabolism , Biphenyl Compounds , Metabolism , Carthamus tinctorius , Chemistry , Chalcone , Metabolism , Pharmacology , Ferric Compounds , Metabolism , Free Radicals , Metabolism , Kaempferols , Metabolism , Pharmacology , Oxidation-Reduction , Picrates , Metabolism , Plant Extracts , Metabolism , Pharmacology , Plants, Medicinal , Chemistry , Quinones , Metabolism , Pharmacology , Sulfonic Acids , Metabolism , Water , Chemistry
15.
Acta Pharmaceutica Sinica ; (12): 1136-1142, 2014.
Article in Chinese | WPRIM | ID: wpr-299156

ABSTRACT

The effect of amygdalin joint hydroxysafflor yellow A (HSYA) on the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and the possible mechanism were studied and explored. Chondrocytes were obtained from endplate of one-month SD rat intervertebral discs and cultured primary endplate chondrocytes. After identification, they were divided into normal group, induced group, amygdalin group, HSYA group and combined group. CCK-8 kit was adopted to detect the proliferation of the endplate chondrocytes. FCM was measured to detect the apoptosis. Real-time PCR method was adopted to observe the mRNA expression of Aggrecan, Col 2 alpha1, Col 10 alpha1, MMP-13 and the inflammatory cytokines IL-1beta. The protein expression of Col II, Col X was tested through immunofluorescence. Compared with the normal group, the proliferation of the endplate chondrocytes decreased while the apoptosis increased (P < 0.05). With down regulation of the mRNA expressions of Aggrecan, Col 2 alpha1 and up regulation of the mRNA expressions of Col 10 alpha1, MMP-13, IL-1beta (P < 0.05), the protein expression of Col II decreased while the protein expression of Col X increased. Compared with the induced group, amygdalin group, HSYA group, the combined group could inhibit the apoptosis and promote the proliferation (P < 0.05). They could increase the mRNA expressions of Aggrecan and Col 2 alpha1 while decrease the mRNA expressions of Col 10 alpha1, MMP-13 and IL-1beta (P < 0.05). They could also enhance the protein expression of Col II while reduce the protein expression of Col X. The effect of the combined group was significantly better than that of amygdalin and HSYA. Amygdalin joint HSYA could inhibit the degeneration of the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and better than the single use of amygdalin or HSYA.


Subject(s)
Animals , Rats , Amygdalin , Pharmacology , Apoptosis , Cells, Cultured , Chalcone , Pharmacology , Chondrocytes , Collagen , Metabolism , Drug Synergism , Interleukin-1beta , Intervertebral Disc , Cell Biology , Quinones , Pharmacology
16.
China Journal of Chinese Materia Medica ; (24): 1653-1656, 2013.
Article in Chinese | WPRIM | ID: wpr-294049

ABSTRACT

<p><b>OBJECTIVE</b>To develop an HPLC method to determine the contents of danshensu, hydroxysafflor yellow A, rosmarinic acid, lithospermic acid, salvianolic acid B in the water extract of mixed Salviae Miltiorrhizae Radix et Rhizoma and Carthami Flos simultaneously.</p><p><b>METHOD</b>The separation were carried out at 30 degrees C on a ZORBAX Eclipse Plus C18 column (4.6 mm x 100 mm, 1.8 microm) with formic acid-500 mmol x L(-1) ammonium formate-water solution (0.5:10:90) as mobile phase A and acetonitrile-formic acid solution (100: 0.5) as mobile phase B in gradient mode at a flow rate of 0.5 mL x min(-1). Detection wavelengths were 280 nm for danshensu, rosmarinic acid, lithospermic acid, salvianolic acid B, and 380 nm for hydroxysafflor yellow A.</p><p><b>RESULT</b>The 5 components were separated well with a good linearity (R2 > 0.999 3) in the range of the test concentration. The average recoveries of danshensu, hydroxysafflor yellow A, rosmarinic acid, lithospermic acid, and salvianolic acid B were 99.1%, 102%, 102%, 98.5% and 101%, respectively.</p><p><b>CONCLUSION</b>This method is simple, accurate, and repeatable.</p>


Subject(s)
Benzofurans , Chalcone , Chromatography, High Pressure Liquid , Methods , Cinnamates , Depsides , Lactates , Quinones , Rhizome , Chemistry , Salvia miltiorrhiza , Chemistry
17.
China Journal of Chinese Materia Medica ; (24): 269-272, 2013.
Article in Chinese | WPRIM | ID: wpr-318680

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the pharmacokinetic effect of Sappan Lignum on hydroxysafflor yellow A (HSYA) in Carthami Flos.</p><p><b>METHOD</b>Concentration of HSYA in rat plasma was detected by RP-HPLC after rats were orally administered with extracts of Carthami Flos or Carthami Flos combined with Sappan Lignum. Pharmacokinetic parameters were calculated by DAS 2.0 pharmacokinetic software.</p><p><b>RESULT</b>In vivo pharmacokinetic models of HSYA were two-compartment open models in both of the Carthami Flos group and the Carthami Flos combined with Sappan Lignum group. After compatibility, HSYA showed a significant lower in apparent volumes of distribution of t(1/2Ka), t(1/2alpha) and V1/F, with slight advance in T(max).</p><p><b>CONCLUSION</b>Sappan Lignum can accelerate absorption, distribution and metabolic process of HSYA in vivo and reduce its accumulation in vivo.</p>


Subject(s)
Animals , Female , Male , Rats , Administration, Oral , Caesalpinia , Chemistry , Carthamus tinctorius , Chemistry , Chalcone , Pharmacokinetics , Chromatography, High Pressure Liquid , Drug Synergism , Drugs, Chinese Herbal , Pharmacokinetics , Flowers , Chemistry , Quinones , Pharmacokinetics , Rats, Sprague-Dawley , Specific Pathogen-Free Organisms , Wood , Chemistry
18.
China Journal of Chinese Materia Medica ; (24): 1851-1855, 2013.
Article in Chinese | WPRIM | ID: wpr-346484

ABSTRACT

<p><b>OBJECTIVE</b>To screen out the main components with no significant difference with Salvia miltiorrhiza diterpene quinones pharmacological action, in order to determine the compatible form of representative components that can describe the overall property of S. miltiorrhiza diterpene quinones.</p><p><b>METHOD</b>According to the results of the in vitro pharmacological experiment, the myocardial ischemia model of rats was induced through intraperitoneal injection of isoproterenol. The pharmacologic effects of S. miltiorrhiza diterpene quinones, combination with principal component A and combination with principal component B were compared in electrocardiogram (changes in J point), enzymology indicators (SOD, MDA, CK, LDH) and pathology (myocardial histological changes), so as to screen out the compatible form of representative components that can describe the overall property of S. miltiorrhiza diterpene quinones.</p><p><b>RESULT</b>The S. miltiorrhiza diterpenoid quinone high-dose group and the B high-dose group were similar in all pharmacological effects, with equal efficacy but no significant difference.</p><p><b>CONCLUSION</b>The S. miltiorrhiza diterpenoid quinone high-dose group and the B high-dose group showed a certain therapeutic effect on ISO-induced myocardial ischemia. Therefore, the four components in the B high-dose group can be used as representative components of S. miltiorrhiza diterpene quinones.</p>


Subject(s)
Animals , Male , Rats , Diterpenes , Pharmacology , Drug Evaluation, Preclinical , Isoproterenol , Pharmacology , Myocardial Ischemia , Drug Therapy , Quinones , Pharmacology , Rats, Sprague-Dawley , Salvia miltiorrhiza , Chemistry
19.
China Journal of Chinese Materia Medica ; (24): 2922-2925, 2012.
Article in Chinese | WPRIM | ID: wpr-338061

ABSTRACT

<p><b>OBJECTIVE</b>To establish an UPLC method for simultaneous determination of purpuroxanthine, purpurin, 1,3,6-trihydroxy-2-methylanthraquinone, rubimaillin in carbonized Rubiae Radix et Rhizoma.</p><p><b>METHOD</b>The components were separated on acquity BEHC18 (2.1 mm x 50 mm, 1.7 microm) using methanol and 0.3% formic acid solution as the mobile phase; The flow rate was 0.2 mL x min(-1) and the volume of injection was 2 microL; the column temperature was maintained at 30 degrees C and the detective wavelength was set at 276 nm.</p><p><b>RESULT</b>There were good liner relationships between the peak area and concentration at ranges of 0.68-34.44 mg x L(-1) (r = 0.9999), 0.66-33.2 mg x L(-1) (r = 0.9997), 0.68-34.08 mg x L(-1) (r = 0.9999), 1.07-53.52 mg x L(-1) (r = 0.9999) for purpuroxanthine, purpurin, 1,3,6-trihydroxy-2-methylanthraquinone, rubimaillin, respectively; the average recovery rates of purpuroxanthine, purpurin, 1,3,6-trihydroxy-2-methylanthraquinone, rubimaillin were 96.95%, 95.75%, 102.5%, 96.15%, respectively, with RSD less than 3%.</p><p><b>CONCLUSION</b>The established method was rapid and simple with good accuracy and reproducibility for the determination of carbonized Rubiae Radix et Rhizoma, the method was suitable for the quality control of carbonized Rubiae Radix et Rhizoma.</p>


Subject(s)
Chromatography, High Pressure Liquid , Quinones , Chemistry , Rhizome , Chemistry , Rubia , Chemistry
20.
China Journal of Chinese Materia Medica ; (24): 3673-3675, 2012.
Article in Chinese | WPRIM | ID: wpr-346884

ABSTRACT

<p><b>OBJECTIVE</b>To establish a method for the determination of hydroxysafflor yellow A in Dedu Honghuaqiwei pill.</p><p><b>METHOD</b>The determination was performed by HPLC method on Diamonsil C18 (4.6 mm x 250 mm, 5 microm) column at 403 nm using methanol-acetonitrile-0.7% phosphoric acid-water (26: 2: 72) as mobile phase. The column temperature was 30 degrees C and the flow rate was 1.0 mL x min(-1).</p><p><b>RESULT</b>The linear rang of hydroxysafflor yellow A was 0.068-0.408 microg and the recovery was 97.66%.</p><p><b>CONCLUSION</b>The result is accurate with good resolution, and the established method can be applied to determine the content of hydroxysafflor yellow A in Dedu Honghuaqiwei pill.</p>


Subject(s)
Chalcone , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Medicine, Mongolian Traditional , Quinones
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