In this study,liquiritigenin sulfonation was characterized using recombinant human sulfotransferases( SULTs). The chemical structure of liquiritigenin sulfate was determined by ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry( UPLC-Q-TOF-MS/MS). Then model fitting and parameter estimation were performed using the Graphpad Prism V5 software. Various SULT enzymes( SULT1 A1,1 A2,1 A3,1 B1,1 C2,1 C4,1 E1 and 2 A1) were able to catalyze the formation of liquiritigenin-7-O-sulfate. Sulfonation of liquiritigenin-7-hydroxy( 7-OH) by these eight SULT enzymes consistently displayed the classical Michaelis-Menten profile. According to the intrinsic clearance( CLint) value,the sulfonation rates of liquiritigenin-7-OH by expressed SULT enzymes followed the following rank order: SULT1 C4 > SULT1 A3 > SULT1 E1 > SULT1 A1 > SULT1 A2 > SULT1 B1 >SULT1 C2>SULT2 A1. Further,liquiritigenin-7-O-sulfonation was significantly correlated with the SULT1 A3 protein levels( P<0. 05).Then,human embryonic kidney( HEK) 293 cells over expressing SULT1 A3( named as HEK-SULT1 A3 cells) were conducted. As a result,liquiritigenin-7-O-sulfate( L-7-S) was rapidly generated upon incubation of the cells with liquiritigenin. Consistent with SULT1 A3,sulfonation of liquiritigenin-7-OH in HEK-SULT1 A3 cells also followed the Michaelis-Menten kinetics. The derived Vmaxvalues was( 0. 315±0. 009) μmol·min-1·g-1,Kmwas( 7. 04±0. 680) μmol·L^-1,and CLintwas( 0. 045±0. 005) L·min^-1·g^-1. Moreover,the sulfonation characters of liquiritigenin( 7-OH) in SULT1 A3 were strongly correlated with that in HEK-SULT1 A3 cells( P<0. 001).The results indicated that HEK-SULT1 A3 cells have shown the catalytic function of SULT1 A3 enzymes. In conclusion,liquiritigenin was subjected to efficient sulfonation,and SULT1 A3 enzyme plays an important role in the sulfonation of liquiritigenin-7-OH. Significant sulfonation should be the main reason for the low bioavailability of liquiritigenin. In addition,HEK-SULT1 A3 cells were conducted and successfully used to evaluate liquiritigenin sulfonation,which will provide an appropriate tool to accurately depict the sulfonation disposition of liquiritigenin in vivo.
Arylsulfotransferase ; Flavanones/metabolism* ; Humans ; Tandem Mass Spectrometry

OBJECTIVETo study the effect of stigma maydis polysaccharide (SMPS) on gastrointestinal movement.

METHODTaking charcoal as the indicator and taking ratio of charcoal movement, beginning time of black excretion and stool amount as the index to observe the effect of SMPS on intestinal movement in mice. Taking emthylorange as the indicator and taking the ratio of residual rate of methylorange as the index to observe the effect of SMPS on gastric emptying in mice. Taking methylene blue as the indicator and taking the time of gastric emptying and movement speed of intestinal content as the index to observe the effect of SMPS on gastrointestinal movement in rats. Observing the changes of cholecystokinin (CCK) level in plasm in rats.

RESULTCompared with control, the ratio of charcoal movement increased in mice (P <0.01). The beginning time of black excretion shortened and the stool amount increased in mice (P <0.01). The ratio of residual rate of methylorange increased in mice (P <0. 01). The time of gastric emptying prolonged in rats (P <0.01). The movement speed of intestinal content in rats accelerated (P <0.01). CCK level in plasm increased in rats (P < 0.05).

CONCLUSIONEffects of stigma maydis polysaccharide on gastrointestinal movement are probably related to the increasing of CCK level in plasm.

Animals ; Cholecystokinin ; blood ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Female ; Gastric Emptying ; drug effects ; Gastrointestinal Agents ; isolation & purification ; pharmacology ; Gastrointestinal Motility ; drug effects ; Intestine, Small ; physiology ; Male ; Mice ; Plants, Medicinal ; chemistry ; Polysaccharides ; isolation & purification ; pharmacology ; Random Allocation ; Rats ; Rats, Wistar ; Zea mays ; chemistry

The gold hollow nanospheres have been synthesized by sacrificE-template method and the obtained sample has been characterized by TEM, SEM and XRD. The amperometric formaldehyde gas sensor was assembled with gold hollow nanospheres as the active electrode material and 1 mol/L KOH solution as electrolyte. The equation of linear regression(y=16.63x+4.063×10-7, r=0.9989)between the oxidation current(y(A))and the concentration of formaldehyde(x/(mol/L)) was obtained at the formaldehyde concentration in the range of 0 to 2.23×10-6 mol/L. The sensitivity of the sensor with gold hollow nanospheres as active material increased by about 70% compared with the sensor made of nanoparticles which had the same gold-loading in the work electrode, this method exhibits an advantage of decrease in the cost of the noble metal. This kind of sensor shows potential application in formaldehyde gas detection in this range due to its excellent sensitivity, stable response and good linear relationship.

Chelerythrine is a kind of benzo[c] phenanthridine alkaloids, with such pharmacological activities as antitumor, antibiosis and anti-inflammation, which is widely found in plant of Fumariaceae, Papaveraceae, Ranunculaceae and Rutaceae families. This article summarizes the advances in domestic and foreign studies on pharmacological effect of chelerythrine in the recent decade, in the expectation of providing scientific basis for the in-depth studies, development and utilization of chelerythrine.
Animals ; Anti-Inflammatory Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Benzophenanthridines ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Pesticides ; pharmacology ; Plants, Medicinal ; chemistry

The Nrf2-Keap1-ARE pathway is an important signaling axis that functions to protect cells against oxidative stress and harmful chemicals through the induction of cytoprotective genes. The maintenance and protective role of Nrf2 pathway has been recognized as a means for chemoprevention. On the other hand, constitutive activation of Nrf2, due to somatic mutations of genes that control Nrf2 degradation, promotes carcinogenesis and imparts chemoresistance to cancer cells. Autophagy is another tightly regulated complex cellular process that functions as a cellular quality control system to remove damaged proteins or organelles. Recently, these two cellular pathways were shown to intersect through the direct interaction between p62 (an autophagy adaptor protein) and Keap1. Dysregulation of autophagy was shown to result in prolonged activation of Nrf2 in a p62-dependent manner, which is associated with the pathogenesis and therapies of several human diseases including cancer. In this review, we discuss the molecular mechanisms of p62-mediated Nrf2 signaling pathway, with a special emphasis on their impact on nervous system disease, cardiovascular disease and cancer.

OBJECTIVETo investigate the chemical constituents of Acroptilon repens.

METHODThe ethanol extract of A. repens was isolated and purified by means of chromatography. These compounds were identified by their spectral data.

RESULT11 compounds were isolated and identified as 2alpha, 9beta-dihydroxy-dehydrocostus lactone (1) , cynaropicrin (2) , apigenin (3) , stigmasterol (4) , 4' -hydroxywogonin (5) , ethyl caffeate (6) , p-methoxy-cinnamic acid (7) , luteolin (8) , daucosterol (9) , apigenin-7-O-beta-D-glucoside (10) , syringin (11).

CONCLUSIONCompounds 5-11 were isolated from A. repens for the first time. Compound 1 is new compounds.

Apigenin ; chemistry ; isolation & purification ; Asteraceae ; chemistry ; Caffeic Acids ; chemistry ; isolation & purification ; Flavanones ; chemistry ; isolation & purification ; Lactones ; chemistry ; isolation & purification ; Molecular Structure ; Plant Extracts ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Sesquiterpenes ; chemistry ; isolation & purification

OBJECTIVEIn vitro aminophylline release from matrix tablets with konjac glucomannan (KGM) were studied to elevate the feasibility of KGM used as carrier materials to prepare matrix tablets.

METHODKGM hydrophilic matrix tablets were prepared by direct compression method with aminophylline as the model drug. The effects of test methods, pH values, ionic strength of dissolution media and rotation speeds on drug release were studied by in vitro dissolution experiment.

RESULTThe MDT value tested by Paddle method was less than that tested by Basket method (P < 0.05). Among the rate of drug release in different dissolution media, distillded water is the fastest, pH 6. 8 PBS is the second, 0.1 mol x L(-1) HCL is the slowest. MDT increased with increasing the ionic strength of dissolution media (P < 0.05). MDT decreased with increasing the rotation speed, but the rate of drug release did not increase when the rotation speed was more than 100 r x min(-1) (P > 0.1). The mechanism of drug release were diffusion and erosion.

CONCLUSIONKGM can be used in sustained delivery systems as a good candidate of hydrophilic polymer.

Aminophylline ; chemistry ; pharmacokinetics ; Amorphophallus ; chemistry ; Bronchodilator Agents ; chemistry ; pharmacokinetics ; Chemistry, Pharmaceutical ; Delayed-Action Preparations ; chemistry ; pharmacokinetics ; Drug Carriers ; Hydrogen-Ion Concentration ; Mannans ; chemistry ; Plants, Medicinal ; chemistry ; Solubility ; Tablets

This study is to investigate the inhibitory effect and mechanism of prosapogenin A (PSA) on MCF7. MTT assay was performed to determine the inhibitory effect of PSA on MCF7 cells. PI/Hoechst 33342 double staining was used to detect cell apoptosis. RT-PCR was used to test the mRNA levels of STAT3, GLUT1, HK and PFKL. Western blotting was performed to determine the expression of STAT3 and pSTAT3 protein in MCF7 cells. The results showed that PSA could dose-dependently inhibit cell growth of MCF7 followed by IC50 of 9.65 micrmol x L(-1) and promote cell apoptosis of MCF7. Reduced mRNA levels of STAT3, HK and PFKL were observed in MCF7 cells treated with 5 micromol x L(-1) of PSA. PSA also decreased the level of pSTAT3 protein. STAT3 siRNA caused decrease of mRNA of GLUT1, HK and PFKL which indicated STAT3 could regulate the expressions of GLUT1, HK and PFKL. The results suggested that PSA could inhibit cell growth and promote cell apoptosis of MCF7 via inhibition of STAT3 and glycometabolism-related gene.
Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Apoptosis ; drug effects ; Cell Proliferation ; drug effects ; Glucose Transporter Type 1 ; genetics ; metabolism ; Hexokinase ; genetics ; metabolism ; Humans ; MCF-7 Cells ; Phosphofructokinases ; genetics ; metabolism ; Plants, Medicinal ; chemistry ; RNA, Messenger ; metabolism ; STAT3 Transcription Factor ; genetics ; metabolism ; Saponins ; isolation & purification ; pharmacology ; Veratrum ; chemistry

OBJECTIVETo identify the genotypes of the blood sample whose blood grouping showed discrepancies and study the ABO alleles' molecular characteristics of the involved ancestry.

METHODSBlood samples were preliminary genotyped by PCR-SSP. Complete exon 6 and 7 in the ABO genes were amplified by PCR and the PCR products were directly sequenced and cloning sequenced to identify its genotype.

RESULTSSequence analysis indicated that 3 samples of the family had an nt905A>G mutation in the B gene compared with ABO*B101. Combined with the serological results, the propositus could be typed as Bx02/O102.

CONCLUSIONDNA sequencing analysis is able to identify the serological phenotype samples that forward and reverse group methods were incongruous.

ABO Blood-Group System ; Alleles ; Base Sequence ; Blood Grouping and Crossmatching ; Exons ; Genetic Testing ; Genotype ; Humans ; Mutation ; Phenotype ; Polymerase Chain Reaction

This paper is to report the study of resveratrol-induced apoptosis and its mechanisms in MCF-7 cells. MTT assay was performed to assess the cytotoxicity of resveratrol on MCF-7 cells. Hoechst 33258 staining was used to observe cellular morphologic changes in apoptosis. Apoptosis was measured by flow cytometric analysis and the protein expression was examined by Western blotting analysis. The results indicated that resveratrol could inhibit MCF-7 cell growth in a time- and concentration-dependent manner. Remarkable morphologic changes in the cells after 60 micromol L(-1) resveratrol treatment, including cell nuclear shrinkage, DNA condensation and apoptotic bodies, were observed by Hoechst 33258 staining. Resveratrol could induce apoptosis and activate p38 and p53 in a time dependent manner in MCF-7 cells. In addition, the cell growth inhibitory ratio and the apoptotic ratio of resveratrol-treated group decreased markedly by the p38 MAPK inhibitor SB203580 or p53 inhibitor pifithrin-alpha. Further experiments confirmed that resveratrol-induced p53 activation was reduced by SB203580 whereas the activation of p38 was not affected by pifithrin-alpha. In conclusion, resveratrol induced apoptosis in MCF-7 cells could be through activating p38-p53 signal pathway.
Antineoplastic Agents, Phytogenic ; administration & dosage ; pharmacology ; Apoptosis ; drug effects ; Benzothiazoles ; pharmacology ; Cell Proliferation ; drug effects ; Dose-Response Relationship, Drug ; Enzyme Inhibitors ; pharmacology ; Humans ; Imidazoles ; pharmacology ; MCF-7 Cells ; Pyridines ; pharmacology ; Signal Transduction ; Stilbenes ; administration & dosage ; pharmacology ; Toluene ; analogs & derivatives ; pharmacology ; Tumor Suppressor Protein p53 ; antagonists & inhibitors ; metabolism ; p38 Mitogen-Activated Protein Kinases ; antagonists & inhibitors ; metabolism