Identification and characterization of three new flavonoids from Rhododendron dauricum / 中国天然药物

The present study was designed to determine the major chemical constituents of the leaves of Rhododendron dauricum L. Compounds were isolated and purified by various chromatographic methods, and their structures were elucidated by physicochemical properties and spectral data. The present study identified two new C-methyl flavanones, 5, 7, 3', 5'-tetrahydroxy-6, 8-di-C-methyl flavanone (1) and 5, 4'-dihydroxy-8-C-methylflavanone-7-O-β-D-glucopyranoside (2), and one new flavonoid glycoside, quercetin-3-O-β-D-(6"-O-cinnamoyl)-galactoside (3), along with seven known compounds, including syzalterin (4), poriolin (5), farrerol-7-O-β-D-glucopyranoside (6), myrciacetin (7), quercetin-3-O-β-D-(6-p-hydroxy-benzoyl)-galactoside (8), quercetin-3-O-β-D-(6-p-coumaroyl)-galactoside (9), and 5, 7, 3', 5'-tetrahydroxyl flavanone (10). Compounds 1-3 were determined to be new flavonoids; compounds 4-6 were isolated from this species for the first time; and compounds 7-10 were reported for the first time from this genus.

Snake venom galactoside-binding lectins: a structural and functional overview

Snake venom galactoside-binding lectins (SVgalLs) comprise a class of toxins capable of recognizing and interacting with terminal galactoside residues of glycans. In the past 35 years, since the first report on the purification of thrombolectin from Bothrops atrox snake venom, several SVgalLs from Viperidae and Elapidae snake families have been described, as has progressive improvement in the investigation of structural/functional aspects of these lectins. Moreover, the advances of techniques applied in protein-carbohydrate recognition have provided important approaches in order to screen for possible biological targets. The present review describes the efforts over the past 35 years to elucidate SVgalLs, highlighting their structure and carbohydrate recognition function involved in envenomation pathophysiology and potential biomedical applications.

Snake venom galactoside-binding lectins: a structural and functional overview

Snake venom galactoside-binding lectins (SVgalLs) comprise a class of toxins capable of recognizing and interacting with terminal galactoside residues of glycans. In the past 35 years, since the first report on the purification of thrombolectin from Bothrops atrox snake venom, several SVgalLs from Viperidae and Elapidae snake families have been described, as has progressive improvement in the investigation of structural/functional aspects of these lectins. Moreover, the advances of techniques applied in protein-carbohydrate recognition have provided important approaches in order to screen for possible biological targets. The present review describes the efforts over the past 35 years to elucidate SVgalLs, highlighting their structure and carbohydrate recognition function involved in envenomation pathophysiology and potential biomedical applications.(AU)

Cyanidin-3-O-galactoside and blueberry extracts supplementation improves spatial memory and regulates hippocampal ERK expression in senescence-accelerated mice / 生物医学与环境科学（英文）

<p><b>OBJECTIVE</b>To investigate whether the antioxidation and the regulation on the Extracellular Regulated Protein Kinases (ERK) signaling pathway are involved in the protective effects of blueberry on central nervous system.</p><p><b>METHODS</b>30 Senescence-accelerated mice prone 8 (SAMP8) mice were divided into three groups and treated with normal diet, blueberry extracts (200 mg/kg•bw/day) and cyaniding-3-O-galactoside (Cy-3-GAL) (50 mg/kg•bw/day) from blueberry for 8 weeks. 10 SAMR1 mice were set as control group. The capacity of spatial memory was assessed by Passive avoidance task and Morris water maze. Histological analyses on hippocampus were completed. Malondialdehyde (MDA) levels, Superoxide Dismutase (SOD) activity and the expression of ERK were detected.</p><p><b>RESULTS</b>Both Cy-3-GAL and blueberry extracts were shown effective functions to relieve cellular injury, improve hippocampal neurons survival and inhibit the pyramidal cell layer damage. Cy-3-GAL and blueberry extracts also increased SOD activity and reduced MDA content in brain tissues and plasma, and increased hippocampal phosphorylated ERK (p-ERK) expression in SAMP8 mice. Further more, the passive avoidance task test showed that both the latency time and the number of errors were improved by Cy-3-GAL treatment, and the Morris Water Maze test showed significant decreases of latency were detected by Cy-3-GAL and blueberry extracts treatment on day 4.</p><p><b>CONCLUSION</b>Blueberry extracts may reverse the declines of cognitive and behavioral function in the ageing process through several pathways, including enhancing the capacity of antioxidation, altering stress signaling. Cy-3-GAL may be an important active ingredient for these biological effects.</p>

Double-mutated oncolytic adenovirus combined with gemcitabine for treating an orthotopic nude mouse model of bladder cancer / 中华肿瘤杂志

<p><b>OBJECTIVE</b>To investigate the therapeutic efficacy of double-mutated oncolytic adenovirus AxdAdB-3 in combination with gemcitabine for treating bladder cancer in an orthotopic nude mouse model.</p><p><b>METHODS</b>The susceptibility to the adenovirus was evaluated in bladder cancer cell lines YTS-1, T24, 5637 and KK47, and normal cell lines HCV29 and WI38. The cells were infected with AxCAlacZ and stained with 5-bromo-4-chloro-3-indolyl-β-galactoside (X-Gal). Immunostaining against adenoviral hexon protein was performed to determine the selective replication of AxdAdB-3 in the cancer cells. Flow cytometry was used to determine the YTS-1 cells in S phase of cell cycle after adenovirus infection. Cell viability after AxdAdB-3 and/or gemcitabine was measured by CCK-8 assay. Orthotopic bladder cancer model was established in nude mice, and the inhibitory efficacy of intravesical instillation therapy with AxdAdB-3 or/and gemcitabine was assessed.</p><p><b>RESULTS</b>Gene transduction efficiency was different among the cell lines, and correlated with expression of CAR. 5637 and KK47 cells with high expression of CAR were more susceptible to the adenovirus, whereas YTS-1 and T24 cells with little CAR expression were resistant to adenoviral infection. Immunostaining showed that the expression levels of hexon protein varied among the cell lines. Normal cells infected with AxdAdB-3 expressed little hexon protein. The proportion of S-phase cells was (39 ± 3) % and (49 ± 5) % in the AxCAlacZ- and AxdAdB-3-infected bladder cancer cells, respectively. AxdAdB-3 effectively induced S-phase entry of cell cycle (P < 0.05). AxdAdB-3 combined with gemcitabine significantly inhibited the growth of bladder cancer cell lines. In vivo, the mean weight of the bladder tumors in mice treated with intravesical instillation of AxCAlacZ, gemcitabine, AxdAdB-3, and AxdAdB-3 + gemcitabine were 400.6, 126.4, 82. 0, 40.4 mg, respectively. Either AxdAdB-3 (P < 0.0001) and gemcitabine (P < 0.0001) suppressed the tumor growth in nude mice, and the combination therapy reduced tumors more effectively than either AxdAdB-3 (P < 0.0001) or gemcitabine (P < 0.0001) alone.</p><p><b>CONCLUSIONS</b>Intravesical instillation therapy with AxdAdB-3 in combination with gemcitabine can effectively inhibit the orthotopic bladder cancer in nude mouse, and further relevant clinical studies are guaranteed.</p>

One new galloyl glycoside from fresh leaves of Psidium guajava L / 药学学报

To investigate the chemical constituents of Psidium Guajava L, the EtOH/H2O extract of the fresh leaves was subjected to various chromatography. Five constituents with galloyl moiety were isolated and elucidated as 1-O-(1, 2-propanediol)-6-O-galloyl-beta-D-glucopyranoside (1), gallic acid (2), ellagic acid (3), ellagic acid-4-O-beta-D-glucopyranoside (4) and quercetin-3-O-(6"-galloyl) beta-D-galactopyranoside (5) by spectroscopic methods, including 2D NMR and HR-ESI-MS spectrometry as well as by comparison with published data. Compounds 4 and 5 were obtained from P. guajava for the first time, and compound 1 is a new polyhydroxyl compound.

A new C-glycosylflavone from Peperomia dindygulensis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Peperomia dindygulensis.</p><p><b>METHOD</b>Several column chromatographic methods were used to isolated compounds from P. dindygulensis and spectroscopic methods (1H-NMR, 13C-NMR, HMQC, HMBC, 1D- HOHAHA, NOE) were used to identify the structures of isolated compounds.</p><p><b>RESULT</b>Compound 1 was isolated and identified as 2"-O-beta-D-galactosylisoswertisin.</p><p><b>CONCLUSION</b>Compound 1 was a new compound.</p>

Preparation and liver targeting of floxuridinyl dibutyrate solid lipid nanoparticles / 药学学报

This paper described the preparation and liver targeting traits of new solid lipid nanoparticles (SLN) containing floxuridinyl dibutyrate (FUDRB) modified with beta-D-galactosides (G2). FUDRB-SLN and FUDRB-G2SLN were prepared by thin layer ultrasonic technique. Transmission electron microscopy micrograph analysis demonstrated that the particle sizes of FUDRB-SLN and FUDRB-G2SLN were (137.5 +/- 11.1) nm and (95.0 +/- 10.7) nm. Drug loading were 9.64% and 8.56%, and entrapment efficiency were 99.81% and 96.23%, respectively. The concentrations of floxuridine (FUDR) in serum and some organs (liver, kidney and lung) were determined by RP-HPLC after iv administration of SLN. FUDR release was confirmed, and a significant enrichment of SLN modified with G2 was observed in liver with G2 complex (targeting rates of SLN-G2 was 8.28 for liver) in comparison with FUDR-sol (targeting rate was 2.56). FUDR could be detected in liver in mice at 480 min after iv administration of FUDRB-G2SLN. These results suggested that incorporation of G2 (4%-5%, g/g) into SLN enhanced the liver targeting-ability of FUDRB. SLN containing G2 could be a useful drug carrier system for liver targeting.

Studies on chemical constituents from stellaria media. I / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Stellaria media.</p><p><b>METHOD</b>The compounds were isolated with various column chromatography and semi-preparative HPLC. The structures were determined by modem spectroscopic methods (IR, UV, 1H-NMR, 13C-NMR, HMBC, ESI-MS).</p><p><b>RESULT</b>Five compounds were isolated and identified as apigenin 6-C-beta-D-galactopyranosyl-8-C-alpha-L-arabinopyranoside (1), apigenin 6-C-alpha-L-arabinopyranosyl-8-C-beta-D-galactopyranoside (2), apigenin 6-C-beta-D-galactopyranosyl-8-C-beta-L-arabinopyranoside (3), apigenin 6-C-beta-D-glucopyranosyl-8-C-beta-D-galactopyranoside (4), apigenin 6, 8-di-C-alpha-L-arabinopyranoside (5).</p><p><b>CONCLUSION</b>Compounds 1-5 were obtained from Stellaria genus for the first time.</p>

The effect of gum Arabic oral treatment on the iron and protein status in chronic renal failure patients under regular hemodialysis in Central Sudan

Objective To assess the effect of gum arabic (Acacia Senegal) oral treatment on the iron and protein status in chronic renal failure patients. Material and Methods Thirty-six chronic renal failure (CRF) patients (under regular hemodialysis); and 10 normal subjects participated in this study. The patients were randomly allocated into the following groups: Group A (n=12): CRF patients under low protein diet (LPD) (less than 40 gram/day); and gum arabic (50 g/day) treatment; Group B (n=14): CRF patients under LPD; gum arabic; iron (ferrous sulphate 200 mg/day) and folic acid (5 mg/day) treatment; Group C (control group; n=10): CRF patients under LPD; iron and folic acid treatment; Group D (n=10): normal volunteers who were kept on normal diet beside a daily dose of 50 gm gum arabic. Each of the above treatments was continued for three consecutive months. Predialysis blood samples were collected from each subject before treatment; and twice per month for three months. Hemoglobin (Hb); hematocrit; total protein; albumin; globulin and 24-hour urine volume as well as serum iron; total iron-binding capacity (TIBC);transferrin saturation; packed cell volume (PCV) and; mean corpuscular hemoglobin concentration (MCHC) were determined. Results Following administration of gum arabic oral treatment for three months; serum iron increased by 5.85and 4.81for groups A and B; respectively. These increases were significantly different from the baseline (P0.05); and control group C (P0.01). TIBC was significantly decreased in group A (4.44) and in group B (4.31) as compared with the baseline and control group C (P0.05). Transferrin saturation was significantly increased by 7.77; and 9.59for groups A and B; respectively; compared with the baseline (P0.05) and control group C (P0.01). Hb; PCV; MCHC; serum total protein; albumin and globulin; and 24-hour urine volume showed no statistically significant differences from the baseline and control groups. Conclusion The improvement in iron status due to oral administration of gum arabic could reduce the need for oral iron prescription

Preliminary proteome analysis of mouse embryonic fibroblast conditioned medium / 中南大学学报(医学版)

OBJECTIVE@#To perform the proteome analysis of conditioned medium prepared from mouse embryonic fibroblast feeder layers by 2-dimensional (2D) electrophoresis and mass spectrometry and to find out the possible differentiation-inhibitory factor in conditioned medium.@*METHODS@#Feeder layers were prepared by 60Co gamma-irradiation on mouse embryonic fibroblast. Insulin-transferrin-sodium selenite supplemented medium was used to culture the feeder layers for 24 hours. The condioned medium prepared from mouse embryonic fibroblast feeder layers were made into powder by lyophilization, the redissolved solution was applied to Sephadex G-50 gel filtration chromatography, and then cold acetone was used to precipitate the proteins in the eluted solution. The protein samples were applied to 2D electrophoresis. The 2D images were analyzed by 2D image analysis software. Selected protein spots were digested by trypsin, analyzed by mass spectrometry, and then searched against the NCBInr batabase using Mascot MS/MS Ions Search.@*RESULTS@#The protein samples extracted from mouse embryonic fibroblast feeder layers conditioned medium could be used for 2D electrophoresis. On 2D images, there were (221+/-67) spots. Most of the proteins were located in the region of MW 20 approximately 70 kD, pI 4 approximately 8. Using mass spectrometry, we preliminarily identified 13 spots: 3 keratins, 3 transferrins, 1 trypsin precursor, 2 unknown proteins (3 spots), 1 connexin 46, 1 beta-galactoside binding protein, and 1 secreted protein, acidic and rich in cysteine.@*CONCLUSION@#Conditioned medium prepared from mouse embryonic fibroblast feeder layers contain beta-galactoside binding protein and secreted protein, acidic and rich in cysteine.

Chemical constituents of the rhizome of Matteuccia struthiopteris / 药学学报

<p><b>AIM</b>To study the chemical constituents of the rhizome of Matteuccia struthiopteris (L.) The constituents were separated and purified by column chromatography with normal Todaro.</p><p><b>METHODS</b>phase silica gel and Sephadex LH-20. Their structures were identified on the basis of physical and spectral data (MS, NMR, HMBC and HMQC).</p><p><b>RESULTS</b>Four compounds were isolated and identified as 1-O-beta-D-gl ucopyranosyl-(2S,3R,4E, 8Z) -2-N-(2'-hydroxydocosanoyl) eicosasphinga-4,8-dienine (1), 1-O-beta-D-galactosyl-(6-->1)-alpha-D-galactosyl-2,3-O-dihexadecanoyl-glycerol (2), succinic acid (3), D-mannitol (4).</p><p><b>CONCLUSION</b>Compounds 1 and 2 are new compounds. Compounds 3 and 4 were isolated from this plant for the first time.</p>

Studies on chemical constituents in herbs of Dracocephalum moldavica II / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Dracocephalum moldavica.</p><p><b>METHOD</b>The compounds were isolated by using RA polystyrene resin, polyamide and silica gel column chromatography, The structures of the compounds were elucidated on the basis of physic-chemical properties and spectra data.</p><p><b>RESULT</b>Six compounds were identified as syringaresinol4-O-beta-D-monoglucoside (I), sy-ringaresinol-4,4'-O-bis-beta-D-glucoside (II), kaempferol-3-O-beta-D-(6"-O-p-coumaroyl)-galactopyranoside (III), 2"-p-coumarylastragalin (IV), takakin-8-O-beta-D-glucopyranoside (V), beta-daucosterol (VI).</p><p><b>CONCLUSION</b>Compounds I-V were obtained from genus Dracocephalum for the first time.</p>

Studies on the flavonoids in stem of Rhododendron anthopogonoide II / 中国中药杂志

<p><b>OBJECTIVE</b>To further investigate the flavonoids of Rhododendron anthopogonoide.</p><p><b>METHOD</b>The compounds were isolated and purified by Sephadex LH-20, polyamide and silica gel column chromatography. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.</p><p><b>RESULT</b>Six compounds were isolated and identified as: taxifolin (I), guaijaverin (II), reynoutrin (III), quercitrin (IV), polystachoside (V) and quercetin-4'-O-beta-D-galactoside (VI).</p><p><b>CONCLUSION</b>For the first time, compound VI was separated from Ericaceae plant, compounds II and V were isolated from Rhododendron plant, and compounds I and II were obtained from this plant.</p>

Studies on the new triterpenoid saponin of the aerial part of Cimicifuga foetida / 中国中药杂志

<p><b>OBJECTIVE</b>To find new active constituents from the aerial part of Cimicifuga foetida.</p><p><b>METHOD</b>Various column chromatographic techniques were used for the isolation and purification of the principles. The structures were elucidated on the basis of spectral data and chemical evidences.</p><p><b>RESULT</b>Four 9,19-cycloartane triterpenoid saponins were obtained and identified as Cimifoetiside III (25-anhydrocimigenol-3-O-beta-D-galactopyranoside, 1), 25-O-acetyl-cimigenol xylopyranoside (2), 25-O-acetyl-cimigenol galactopyranoside (3), 7 beta-hydrocimigenol xylopyranoside (4).</p><p><b>CONCLUSION</b>Compound 1 is new and compound 4 was isolated from this plant for the first time.</p>

Two flavonoids from Lagopsis supina / 药学学报

<p><b>AIM</b>To study the chemical constituents of Lagopsis supina.</p><p><b>METHODS</b>Compounds were isolated by column chromatography of silica gel and Sephadex LH-20, and the structures were determined by spectral analysis.</p><p><b>RESULTS</b>Two compounds were isolated and elucidated as apigenin-7-O-(6"-(E)-p-coumaroyl)-beta-D-galactopyranoside (I) and apigenin-7-O-(3",6"-di-(E)-p-coumaroyl)-beta-D-galactopyranoside (II).</p><p><b>CONCLUSION</b>I and II are new compounds.</p>

Enhanced Expressions and Histological Characteristics of Intravenously Administered Plasmid DNA in Rat Lung

Cationic liposome-mediated gene transfection is a promising method for gene therapy. In this study, the transfection efficiency and histological patterns were evaluated in rat lung after intravenous administration via femoral vein of naked plasmid DNA, naked plasmid DNA with pretreatment of DOTAP, and DOTAP-cholesterol-plasmid DNA complex. Plasmid DNA encoding bacterial LacZ gene was used. For quantification of LacZ gene expression, -galactosidase assay was performed. For histologic examination, X-gal staining and immunohistochemical staining for transfected gene products were performed. Pretreatment of DOTAP prior to the infusion of naked plasmid DNA increased transfection efficiency up to a level comparable to DOTAP-cholesterol-plasmid DNA complex injection. Transfected genes were mainly expressed in type II pneumocytes and alveolar macrophages in all animals. We conclude that the high transfection efficiency is achievable by intravenous administration of naked plasmid DNA with pretreatment of DOTAP, to a level comparable to DOTAP-cholesterol-plasmid DNA complex. In this regard, naked plasmid DNA administration with pretreatment of DOTAP could be a more feasible option for intravenous gene transfer than DOTAP-cholesterol-plasmid DNA complex, in that the former is technically easier and more cost-effective than the latter with a comparable efficacy, in terms of intravenous gene delivery to the lung.

Lectinas solubles beta-galactosídicas / Beta-galactoside solubles lectins

Sobre la base de estudios estructurales y funcionales, las lectinas animales se han clasificado en dos tipos: el Tipo C, caracterizado por su dependencia de los iones de calcio y el Tipo S que no es calciodependiente, sino tioldependiente. Entre estas últimas, se ha estudiado ampliamente el grupo de lectinas S-Lac, que son extraídas con buffers salinos con lactosa, en presencia de tioles. Contituyen una familia de proteínas realcionadas estructuralmente, que contienen una serie de aminoácidos conservados. Se unen específicamente a glicoconjugados complementarios y su biosíntesis y localización son reguladas por el desarrolo. Su rol puede relacionarse con diversas actividades biológicas que poderían variar según el órgano.

An improved method for chemical devitellinization of X-gal stained Drosophila embryos.

In Drosophila developmental biological studies, X-gal staining is commonly employed to study the spatio-temporal expression of the lacZ reporter gene in the transformed flies or their embryos. Study of the lacZ pattern in embryos often suffers from the lack of an efficient and high yielding technique for devitellinization of X-gal stained embryos. Devitellinization techniques employed during antibody staining, in situ hybridization or embryonic cuticular preparations generally do not give satisfactory results when used for similar purpose in X-gal stained embryos. This results in the flaky appearance of the blue stain. We present here an improved chemical devitellinization technique which gives a high yield of devitellinized embryos and a better resolution of the X-gal staining pattern.

Identification of endogenous soluble glycoprotein receptors of bovine brain grey matter 14 kDa beta-galactoside-binding lectin.

The 14 kDa beta-galactoside-binding lectin from bovine brain grey matter (BBL) covalently attached to caproic acid-Sepharose by the N-hydroxy succinimide procedure was used to isolate endogenous glycoprotein receptors of this lectin. BBL-Sepharose could sugar-specifically retain several endogenous soluble glycoproteins with subunit molecular mass (in kDA) 44, 51, 60, 123 and 186. BBL, conjugated with horse radish peroxidase, could sugar-specifically recognize several glycoprotein subunits with molecular mass (in kDA) 58, 87, and 117 and 186 on Western blots. The only protein from an extract of bovine brain grey matter, that retained on Sepharose-immobilized endogenous N-linked glycoproteins and subsequently eluted with beta-galactosides was BBL as confirmed by electrophoresis and agglutination inhibition measurement. N-linked glycoproteins from bovine heart and even from human placenta were also efficient receptors of BBL. These results suggest that 14 kDa beta-galactoside-binding lectin is the major protein, if not the only one, that sugar-specifically interacts with endogenous soluble glycoproteins in bovine brain grey matter.