Cinobufacino injection is a significant anti-tumor medicine for the treatment of various tumors in clinic, which was made from water extraction of the skin of Bufo bufo gargarizans. In present paper, HPLC-DAD-FT-ICR-MS method was used to identify the major bufadienolides in cinobufacino for the first time. Solid-phase extraction with dichloromethane and silica was used to enrich the total bufadienolides in cinobufacino. Based on the UV and high resolution MS/MS data, 33 bufadienolides were analyzed and characterized. Among them, eight compounds were identified by comparing with standard references unambiguously. This study elucidated the major bufadienolides in cinobufacino, which provided material foundation of cinobufacino and will be benefit for the further pharmacological research.
Amphibian Venoms ; chemistry ; Animals ; Bufanolides ; analysis ; chemistry ; Bufo bufo ; Chromatography, High Pressure Liquid ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

Cinobufacino injection is purified from water extraction of the skin of Bufo bufo gargarizans, which has been widely used for various cancers in clinic with significant anti-tumor effects. Bufadienolides were regarded as the main active constituents of cinobufacino injection in previous reports. In present study, 6 bufadienolides were isolated and purified from Cinobufacino injection. Their structures were identified as 3-epi-ψ-bufarenogin (1), ψ-bufarenogin (2), 3-epi-arenobufagin (3), arenobufagin (4), 3-epi-gamabufotalin (5), and 3-oxo-arenobufagin (6), separately. Among them, 1 and 3 were new compounds, 5 and 6 were new natural products. Compounds 1, 2 and compounds 3, 4 were two pairs configuration isomers at C-3, separately.
Animals ; Bufanolides ; chemistry ; isolation & purification ; Bufo bufo ; Injections ; Skin ; chemistry

Objective To compare maternal and neonatal outcomes after induction,elective cesarean section and spontaneous onset of labor in uncomplicated term nulliparous women.Methods A total of 3751 uncomplicated term nullipara who delivered in Peking Union Medical College Hospital from Sept 2002 to April 2007 were retrospectively analyzed.They were divided into three groups:the induction group, the elective cesarean section group,and the spontaneous onset of labor group.Their general conditions (such as age,weeks of pregnancy,hospital days and cost),postpartum complications(such as postpartum hemorrhage,puerperal morbidity,urinary retention,blood transfusion,delayed healing,and trauma),and Apgar score were compared by statistic methods.Results(1)Among 3751 women,501(13.3%)of them underwent induction(the induction group),1634(43.6%)delivered by cesarean section(cesarean section group),the other 1616(43.1%)women underwent spontaneous onset of labor(the spontaneous onset of labor group).(2)Results of general conditions:the spontaneous onset of labor group had the shortest hospital days,which was longer in the induction group,and the longest in the selective cesarean section group(P

OBJECTIVETo study the accuracy of the application of the intrapartum fetal oxygen saturation (FSO2) monitoring in predicting fetal acidosis and diagnosing intrauterine fetal distress.

METHODSContinuous FSO2 monitoring as well as internal and external fetal heart rate monitoring were applied respectively in 60 women in labor during active phase of the first stage and the second stage. All the monitoring methods were validated with standard sensitivity, specificity, positive predictive value, negative predictive value, and accuracy on the bases of Apgar score and cord artery blood analysis.

RESULTSThe mean FSO2 in the active phase of the first stage were significantly higher than in the second stage of labor. FSO2 correlated with pH, PO2, PCO2, and base excess (BE) of cord blood to a significant degree. There was linear correlation between FSO2 and cord artery blood pH. Using 30% cutoff diagnosing intrauterine fetal distress, the sensitivity, specificity, and accuracy were 80%, 100% and 98.3%, respectively.

CONCLUSIONFSO2 monitoring is an effective method diagnosing intrauterine fetal distress.

Acidosis ; diagnosis ; Apgar Score ; Female ; Fetal Blood ; chemistry ; Fetal Distress ; blood ; diagnosis ; Fetal Monitoring ; methods ; Heart Rate, Fetal ; Humans ; Monitoring, Physiologic ; Oximetry ; methods ; Oxygen ; blood ; Partial Pressure ; Pregnancy ; Prenatal Diagnosis

This study is to investigate if madecassoside can protect against myocardial reperfusion injury in rabbit heart in vivo. The ischemia reperfusion model was established. Left ventricular function and ECG were monitored at the ischemia and reperfusion period. The infarct areas were expressed as percentage. The levels of LDH, CK, MDA and SOD were measured and C-reactive protein (CRP) in serum was measured by ELISA kit. Cardiomyocyte apoptosis were measured by TUNEL staining. A monoclonal rabbit anti-goat Bcl-2 proteins as primary antibody was used for Bcl-2 immunohistochemical staining. Treatment with madecassoside (3.2, 1.6 and 0.8 mg x kg(-1)) i.v. during ischemia reperfusion injury attenuated myocardial damage, that is, characteristic of decreasing infarct size, decreasing LDH and CK release. Activities of SOD were diminished and MDA level increased obviously in control group whereas pretreatment with madecassoside significantly blunted the decrease of SOD activity, markedly reduced the levels of MDA, CRP and cardiomyocyte apoptosis, and upregulated the expression of Bcl-2. Madecassoside has the protective effect against myocardial ischemia reperfusion injury, and effects of anti-lipid peroxidation, enhancement of SOD activity, anti-inflammation and anti-apoptosis.
Animals ; Apoptosis ; drug effects ; C-Reactive Protein ; metabolism ; Cardiotonic Agents ; isolation & purification ; pharmacology ; Centella ; chemistry ; Creatine Kinase ; blood ; Electrocardiography ; L-Lactate Dehydrogenase ; blood ; Lipid Peroxidation ; drug effects ; Male ; Malondialdehyde ; blood ; Myocardial Reperfusion Injury ; metabolism ; pathology ; Myocardium ; metabolism ; pathology ; Myocytes, Cardiac ; pathology ; Plants, Medicinal ; chemistry ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; Rabbits ; Random Allocation ; Superoxide Dismutase ; blood ; Triterpenes ; isolation & purification ; pharmacology

0.05). The RBC folate level of birth defect group except the urinary defect was significantly lower compared with the control group(233-547 vs 689 nmol/L,P

Objective To understand the current status of the prevention and control of endemic fluorosis in the southwestern area of Shandong province. Methods In 2007, the progress of water-improving defluoridation, the operating state and water fluoride content of the water-improving project, which was determined by fluorosis selective ion electrode, and the inhabitant related indexes of endemic fluorosis were extensively surveyed in the three main fluorosis counties-Jiaxiang, Yuncbeng and Liangshan of the southwestern area of Shandong province. Results Among 1371 fluorosis villages in the 3 counties, 53.61%(735/1371) of which had undergone water-improving defluoridation, the rate in Jiaxiang, Yuncheng and Liangshan being 38.0% (220/579),65.51% (378/577) and 63.72% ( 137/215 ) respectively; the normally functioning rate of this project was 76.73% (564/735), projects out of order accounted for 23.27% (171/735). Among 263 well-functioning projects from the three counties, the rate with water fluoride higher than 1.0 mg/L was 35.36%(93/263), the maximum value being 4.17 mg/L. The urine fluoride content of 440 children aged 8 - 12 years and 484 adults over 30 years old were examined in 13 fluorosis villages of the three counties, the geometric mean was 2.98,3.06 mg/L respectively; the individual maximum was 12.83,14.49 mg/L respectively; the detectable rate of dental fluorosis among children aged 8 - 12 was 84.28% (649/770) ,17.66%(136/770) had defect and the index of dental fluorosis was 1.89; the rates of the clinical and X-ray skeletal fluorosis of the adults aged more than 30 were 44.40%(234/527) and 24.67%(130/527) respectively, and the abnormal electrocardiography rate was 32.43% (168/518) in the adult, mostly T-wave abnormality. Conclusions The progress of the water-improving defluoridation in the southwestern area of Shandong province was relatively slow, the water fluoride content of the water-improving projects seriously exceeded standard, and the condition of the fluorosis had not been effectively controlled.

Objective To understand the fulfillment of control measures of endemic fluorosis and find out the prevalent trend of this disease in Shandong Province from 1992 to 2006 in order to provide a scientific basis for the set up of control strategies. Methods According to "the National Survey Scheme of Endemic fluorosis", Huantai County in 1992-1996 and Liaagshan County in 1997-2006 were selected, where water-improving defluoridation and the contents of water fluoride were searched in two counties; dental fluorosis and urine fluoride in children aged 8-12 years old, clinical and X-ray skeletal fluorosis in adult over 16 years old were searched respectively in Lijia Village of Huantai County and Dongxu Village of Liangshan County. Results One hundred percent(304/304) high-fluoride villages of Huantai County in 1992 and 63.72% (137/215) villages of Liangshan County in 2006 had finished the project of water-improving defluoridation; the rate of high-fluorine water(>1.0 mg/L) in normal operation projects was 5.00%(5/100)-17.14%(18/105) in Huantai County from 1992 to 1996, and 18.97%(11/58)-45.61%(26/57) in Liangshan County from 1997 to 2006. The water fluoride of Lijia Village was<1.0 mg/L from 1992 to 1996, the water fluoride of Dongxu Village was<0.5 mg/L from 1997 to 2006. The detection rate of dental fluorosis of children aged 8-12 years at Lijia Village dropped from 30.86%(25/81) in 1992 to 10.13%(8/79) in 1996(χ2=12.41, P<0.05), and the Dongxu Village dropped from 68.95%(151/219) in 1997 to 0(0/38) in 2006(χ2=222.04, P<0.01). In the Lijia and Dongxu Villages, urine fluoride in children aged 8-12 years old was lower than 1.40 mg/L. In the adults over 16 years of the two villages, the positive rate of X-ray skeletal fluorosis of Lijia Village dropped from 30.0%(15/50) in 1992 to 13.95%(6/43) in 1996(χ2=3.41, P>0.05), and all the cases were in degree I, the rate of Dongxu Village dropped from 64.58%(31/48) in 1997 to 16.67% (4/24) in 2006(χ2=14.71, P<0.01), and no eases of degrees Ⅲ was detected. Conclusions The progress of water defluoridation was uneven in 2 counties, slow in Liangshan County; and the water fluoride in part of the project exceeded standard; the water fluorid of 2 surveyed villages was normal and the endemic fluorosis was under control. More financial input is requested to accelerate the process of water defluoridation and to reinforce the management of the projects and illness monitoring, thus to reduce the harm of fluorosis to the limit.

Objective To explore the effect of patent foramen ovale(PFO)on white matter lesions(WMLs) in migraine without aura(MwoA).Methods Thirty-five patients with MwoA were examined by contrast transcranial Doppler(cTCD)and magnetic resonance imaging(MRI).According to the results of PFO and MRI Flair data,the patients' age,sex and headache characteristics were matched,and the WMLs were compared between the PFO positive group and negative group.Results Seven cases of WMLs were recruited in PFO positive group(19 cases)and the WMLs were distributed in the frontal lobe and/or the parietal lobe.The score ranged from 1 to 7 points.Five cases of WMLs were enrolled in PFO negative group(16 cases)and the WMLs also were distributed in the frontal lobe and/or the parietal lobe.The score ranged from 1 to 3 points.There was no significant difference in WMLs between the groups(P＞ 0.05).Conclusion White matter lesions in migraine without aura are distributed in the frontal lobe and the parietal lobe,and these findings do not support a relationship between PFO and WMLs.

OBJECTIVEThis study was designed to examine the in vitro effects of fenvalerate on steroid production and steroidogenic enzymes mRNA expression level in rat granulosa cells.

METHODSUsing primary cultured rat granulosa cells (rGCs) as model, fenvalerate of various concentrations (0, 1, 5, 25, 125, 625 micromol/L) was added to the medium for 24 h. In some cases, optimal concentrations of 22(R)-hydroxycholesterol (25 micromol/L), Follicle stimulating hormone (FSH, 2 mg/L), or 8-Bromo-cAMP (1 mmol/L) were provided. Concentrations of 17 beta-estradiol(E2) and progesterone (P4) in the medium from the same culture wells were measured by RIA and the steroidogenic enzyme mRNA level was quantified by semi-quantitative RT-PCR.

RESULTSFenvalerate decreased both P4 and E2 production in a dose-dependent manner while it could significantly stimulate rGCs proliferation. This inhibition was stronger in the presence of FSH. Furthermore, it could not be reversed by 22(R)-hydroxycholesterol or 8-Bromo-cAMP. RT-PCR revealed that fenvalerate had no significant effect on 3 beta-HSD, but could increase the P450scc mRNA level. In addition, 17 beta-HSD mRNA level was dramatically reduced with the increase of fenvalerate dose after 24 h treatment.

CONCLUSIONFenvalerate inhibits both P4 and E2 production in rGCs. These results support the view that fenvalerate is considered as a kind of endocrine-disrupting chemicals. The mechanism of its disruption may involve the effects on steroidogenesis signaling cascades and/or steroidogenic enzyme's activity.

3-Hydroxysteroid Dehydrogenases ; analysis ; metabolism ; 8-Bromo Cyclic Adenosine Monophosphate ; pharmacology ; Animals ; Base Sequence ; Cells, Cultured ; Dose-Response Relationship, Drug ; Estradiol ; analysis ; metabolism ; Female ; Follicle Stimulating Hormone ; pharmacology ; Granulosa Cells ; cytology ; drug effects ; metabolism ; Hydroxycholesterols ; pharmacology ; Nitriles ; pharmacology ; Progesterone ; analysis ; metabolism ; Pyrethrins ; pharmacology ; RNA, Messenger ; analysis ; metabolism ; Rats ; Steroids ; metabolism