1.Characteristics of Phthalate Esters Pollution in Indoor Settled Dust
Xingtao LIN ; Ting SHEN ; Xiaolei YU
Journal of Environment and Health 2007;0(12):-
Objective To investigate the pollution of phthalate ester in indoor environment. Methods Settled dust samples from 10 households, 10 offices and 10 student dormitories in Beijing were collected. Seven kinds of phthalate esters in these samples were determined with solid phase extraction-high performance liquid chromatography (SPE-HPLC) .Dates were analyzed statistically by nonparametric tests. Results The main phthalate esters in dust were di (2-ethylhexyl) phthalate (DEHP), dibutyl phthalate (DBP) and dicyclohexyl phthalate (DCHP). Of phthalate esters, DEHP with the range of 28-6 073 mg/kg had the highest concentration in indoor dust. The total level of phthalate esters in households was the highest, offices followed, student dormitories was the last. The Kurskal-Wallis H test showed that the concentrations of BBP, DEHP and DCHP in dust were significantly different in 3 types of rooms (P
2.Design of acetylcholinesterase inhibitor for Alzheimer's disease therapy: from multi-binding site inhibitors to multi-target directed ligands.
Wenchao YANG ; Qi SUN ; Ningxi YU ; Xiaolei ZHU ; Guangfu YANG
Acta Pharmaceutica Sinica 2012;47(3):313-21
Alzheimer's disease (AD) is a complex neurodegenerative disorder which seriously causes the dementia in elderly people and afflicts millions of people worldwide. Drug discovery for Alzheimer's disease therapy has been a hot research area and a big challenge, in which development of acetylcholinesterase (AChE) inhibitors design was the most active and some AChE inhibitors are commercially available for AD medication already. However, practical using of commercial AChE inhibitors showed their limited usefulness and related adverse effects. Thus, it is extremely urgent to find novel AChE inhibitors with higher potency and less adverse effects. Based on the accurate crystallographic studies about AChE, strategies for multi-binding site AChE inhibitors have been formed, followed by design of the multi-target directed ligands. In this review, the structures and binding modes of commercial AChE inhibitors were briefly discussed, together with the development of AChE inhibitor design for AD therapy: from multi-binding site inhibitors to multi-target directed ligands.
3.Study on MR tracking of magnetically labeled swine mesenchymal stem cells after autologous transplantation into acute injured liver in vivo
Xiaolei SHI ; Liang FANG ; Zhengyang ZHOU ; Weiping YU ; Yitao DING
Chinese Journal of Hepatobiliary Surgery 2010;16(2):125-129
Objective To evaluate in vivo tracking of swine mesenchymal stem cells (MSCs) la-beled with super paramagnetic iron oxide (SPIO) in intraportal transplantation by a clinical 1.5T MR.Methods MSCs were isolated from swine and cultured as well as expanded, which were then incuba-ted with SPIO (Feridex I. V.). Prussian blue staining was performed for showing intracelluar irons.To establish a swine model of acute liver necrosis, 0.5 g/kg of D-galactosamine was administrated to 10 pigs. MSCs(labeled cells in six, unlabeled cells in four)were injected into liver via portal veins. MR imaging was performed with a clinical 1.5T MR immediately before and at 6 h, 3 d, 7 d, 14 d after transplantation, respectively. Results Prussian blue staining of SPIO labeled MSCs could be effec-tively labeled and the labeling efficiency was almost 100%. Signal intensity loss in liver by SPIO labe-ling on FFE sequence persisted until 14 days after transplantation. Histological analysis by Prussian blue staining showed homing of labeled MSCs in liver after 14 days, primarily distributing in hepatic sinusoids and liver parenchyma. Conclusion MSCs can be labeled with SPIO in vitro successfully.MRI can monitor magnetically labeled MSCs transplanted into liver.
4.Effect of humic acid and soil on the dissolution performance of depleted uranium in water
Xiaolei CUI ; Zhiying GUO ; Yueqin LIANG ; Shui YU
Chinese Journal of Radiological Medicine and Protection 2013;(1):76-79
Objective To study the effect of humic acid (HA) and soil on dissolution performance of depleted uranium (DU).Methods Using the static dissolve-adsorption experiment and inductively coupled plasma-mass spectrometry(ICP-MS) to determine uranium concentration and 235U/238U isotope ratios of the samples at different time and study the dissolution of DU in water.Results The solubility of DU in water was reduced by 90% by adding HA.Soil could increase the solubility of DU in water by nearly 25%,adding an appropriate amount of HA could play a supporting role on the dissolution of DU,in this experiment adding 5% of HA was best.Conclusions Soil and HA could produce positive and negative impact on the solubility of DU in water,and the combined effect of the two relied on the complex absorption and complexation reactions of soil,HA and dissolved uranium ions.
5.Development in New Dosage Forms of Active Components from Ginkgo Biloba Extracts
Xiaolei SHI ; Yuan ZHU ; Jiangnan YU ; Ximing XU
China Pharmacist 2014;(11):1943-1946
The main active components in Ginkgo biloba extracts were Ginkgo biloba flavonoids and lactone compounds. This pa-per reviewed on the kinds and pharmacological effects of the active ingredients in Ginkgo biloba extracts, and focused on four aspects including controlled-release preparations, solubilized solid preparations, nanoparticle formulations and time- and site-specific formula-tions to introduce the development in the new dosage forms of Ginkgo biloba flavonoids and lactone compounds.
6.Effects of EPO on expression of TGF-β1 and ColⅠin myocardium of liver cirrhosis rats
Weiping ZHANG ; Ying YU ; Qin GAO ; Xiaolei GUO ; Sudong GUAN
Chinese Pharmacological Bulletin 2015;(10):1398-1402
Aim To observe the effects of liver cirrho-sis on the expression of transforming growth factor-β1 ( TGF-β1 ) and ColⅠin rat myocardium and interven-tion of erythropoietin ( EPO ) . Methods Thirty-six male Sprague-Dasley rats were randomly divided into three groups:control group, liver cirrhosis group and EPO group, then the cardic hemodynamic parameters in vivo and levels of serum lactate dehydrogenase ( LDH ) as well as creatine kinase isoenzyme ( CK-MB) were measured. With Masson′s trichrome stain, changes of collagen formation of myocardial tissue in different groups were observed. Also the mRNA ex-pressions of TGF-β1 and ColⅠin myocardium were de-tected by RT-PCR. Results In contrast to control group, rats in liver cirrhosis group showed a decline in systolic and diastolic function of left ventricule, rising myocardial enzyme, a distinct increase of cardiac colla-gen deposition, as well as an elevation of TGF-β1 and ColⅠmRNA expressions. In contrast to liver cirrhosis group, rats in EPO group demonstrated an improve-ment in systolic and diastolic function of left ventricule as well as in cardiac collagen deposition, and a de-crease in both myocardial enzyme and TGF-β1 and ColⅠmRNA expressions. Conclusion Liver cirrhosis can lead to the changes of myocardial structure and function in rats,and it can accelerate myocardial inter-stitial fibrosis; EPO can protect the myocardial injury in liver cirrhosis rats.
7.Inhibition effect of curcumin on proliferation and invasion of breast cancer cell by decreasing expression of MT1-MMP
Junqing YU ; Guangyu YAO ; Xiaolei HU ; Lujia CHEN ; Changsheng YE
The Journal of Practical Medicine 2017;33(9):1394-1396
Objective To investigate whether MT1-MMP is involved in the inhibition effect of curcumin on the proliferation and invasion of breast cancer cell and the mechanism . Methods Firstly, MCF-7 cell lines transfected by MT1-MMP eukaryotic expression vector was established. We divided all cells into 3 groups,including null vector transfection group, non-transfected and transfected group with different concentrations of curcumin. The expression of MT1-MMP protein, the proliferation and invasion ability were respectively analyzed by western blot, transwell method, and cell counting kit-8 (CCK-8). Results The expression of MT1-MMP was inhibited by curcumin. Transwell and CCK-8 experiment indicated the proliferation and invasion abilities of MT1-MMP transfected MCF-7 cells were inhibited by curcumin in a concentration dependent manner. Conclusion The inhibition value of curcumin on proliferation and invasion is probably due to its ability to inhibit the expression of MT1-MMP.
8.Medical and non-medical factors influencing termination of pregnancy in Chinese women with fetal malformation
Xiaolei ZHANG ; Xiaowei HUANG ; Yu XIONG ; Xiaotian LI
Chinese Journal of Perinatal Medicine 2017;20(6):420-426
Objective To investigate the rate of termination of pregnancy (TOP) in gravidas with prenatally diagnosed fetal malformation and to analyze the influences of medical and non-medical factors on decision making.Methods This was a prospective cohort study. Gravidas who took part in a multidisciplinary consultation due to fetal malformation and finished a questionnaire after consulting from September 12, 2012 to May 2, 2013 were recruited. Exclusion criteria were chromosomal disorders and isolated abnormal ultrasound soft markers. The questionnaire survey was conducted to understand the patient's backgrounds and to collect their feedbacks on the consultation. Decisions of the gravidas on TOP were followed up by phone in 2014 and 2016. If a gravida chose to continue her pregnancy, her baby's outcome was also recorded.T test,Chi-square test or Fisher's exact test, or rank-sum tests (Mann-Whitney or Wilcoxon) or Logistic regression was used for statistical analysis.Results (1) Altogether 229 gravidas were recruited and 10 of them were lost to follow-up, so 219 cases were finally analyzed. Among the 219 cases, 35.6% (78/219) chose to terminate their pregnancies. (2) Neonatal prognosis was predicted based on the type and severity of the disease and was divided into four levels including good prognosis (122 cases, 55.7%), medium prognosis (20 cases, 9.1%), poor prognosis (17 cases, 7.8%) and unsure prognosis (60 cases, 27.4%). (3) Gravidas who chose to terminate their pregnancies were younger than their counterparts choosing to continue to term (average age: 27.8±4.1 vs 29.0±3.9,t=2.257,P<0.05). Gravidas who went to the consultation before the 24th gestational week carried double risk of TOP than those after the 24th gestational week [termination rate: 52.5% (31/59) vs 29.4% (47/160),χ2=10.089,P<0.01). (4) Gravidas with fetal growth restriction (FGR) were at triple risk of TOP than those without (OR=2.850, 95%CI: 1.323-6.140) after adjusting for maternal age, gestational age at consultation and prognostic evaluation. Comparing with the good prognosis group, in which the rate of TOP was 19%, the unsure (OR=2.354, 95%CI: 1.108-5.004), medium (OR=16.188, 95%CI: 4.732-55.372) and poor (OR=14.515, 95%CI: 3.61-58.359) prognosis groups had higher risk of TOP. (5) There were 63 women informed us their reasons for TOP (multiple choices), among which 57 (90.5%) were due to unsure neonatal outcomes, and 10 (15.9%) were due to emotional factors. (6) Maternal satisfaction with neonatal prognosis was 2 to 5 points (medium score, ten-point system) lower in gravidas choosing to TOP than in those choosing to continue pregnancy regardless of good, unsure, or medium neonatal prognosis. No significant difference in maternal satisfaction was found among gravidas with poor neonatal prognosis.Conclusions The rate of TOP in gravidas with prenatally diagnosed fetal malformation remains high in China. Factors that can negatively influence the rate of TOP are consultation after the 24th gestational week, better perceived neonatal prognosis and higher maternal satisfaction with neonatal prognosis. Uncertainty of the neonatal prognosis is the leading cause of maternal dissatisfaction.
9.Absorption, distribution and excretion of 2-fluorine-6-trifl-uoromethylpyridine in rats by radioactivity isotope tracing method
Lihong LIN ; Yang YU ; Xiaolei LI ; Na LI ; Yanan PANG
Chinese Journal of Pharmacology and Toxicology 2017;31(6):670-674
OBJECTIVE To study the absorption,distribution and excretion of 2-fluorine-6-trifluoromethylpyridine (JJBD) in rats.METHODS [14C] Radioactivity isotope tracing method was used.Male SD rats were ig given a single dose of JJBD 10 and 100 mg·kg-1 (radioactivity:3.7 GBq·kg-1).Concentrations of rat plasma,tissue,feces,urine and bile were determined with a liquid scintillation counting (LSC) analyzer.Toxicokinetics (TK) parameters were fitted using WinNonlin.RESULTS TK parameters of JJBD 10 and 100 mg · kg-1 in male SD rats were as follows:area under the curve (AUC(0-t)) was 22 548±1579 and (203 395±27 586) h·iμg Eq.·L-1,half time (t1/2) was 15.8±1.0 and (14.1±0.9) h,peak time (Tmax) was 4.0±3.0 and (6.0±5.0) h,peak concentration (Cmax) was 1450±355 and (7776±1703) μg Eq.·L-1.JJBD was mainly distributed in fat,livers,kidneys,stomachs and intestinal walls.The concentration of JJBD in most of the tissues reached peak values after 4 h.However,JJBD couldn't be detected in the muscle,thymus gland,brain,gonad or spleen.Excretion rate of JJBD was 43.1% in urine,29.7% in feces and 9.97% in cleaning solution within 0-168 h.JJBD could be excreted through bile at a rate of 28.1% within 0-72 h.CONCLUSION JJBD can be absorbed immediately and excreted slowly in SD rat.There is no accumulation risk.The distribution of JJBD in vivo is very extensive,but cannot go through the blood-brain barrier.JJBD is mostly excreted through feces and urine.
10.Protective effects of theaflavins on radiation injury of thymus
Xiaodan HAN ; Junling ZHANG ; Xiaolei XUE ; Yu ZHAO ; Saijun FAN
Tianjin Medical Journal 2017;45(7):699-703
Objective To investigate the protective effect of theaflavins on thymus injury caused by total body irradiation (TBI).Methods Twenty-five C57BL/6 mice were randomly divided into 5 groups:control group,4 Gy TBI group,4 Gy TBI + 25 mg/kg theaflavins group,4 Gy TBI + 50 mg/kg theaflavins group and 4 Gy TBI + 100 mg/kg theaflavins group.Thymus index and total number of thymocytes were detected at the 14th d post-irradiation to determine the optimal dose of theaflavins.According to this optimal dose,32 C57BL/6 mice were randomly divided into 4 groups:control group,theaflavins group,4 Gy TBI group and 4 Gy TBI + theaflavins group.Thymus histomorphology,CD4CD8 T cell subsets,and reactive oxygen species (ROS) in thymocytes were examined at the 14th d post-irradiation.Results The irradiated thymus exhibited decreased thymus index and total number of thymocytes (P < 0.05),aberrant histomorphology and T cell subsets (P < 0.05),and increased ROS level in thymocytes (P < 0.05).Compared with 4 Gy TBI group,the thymus index and total number of thymocytes were significantly increased in 4 Gy TBI + 50 mg/kg theaflavins group (P < 0.05).The total number of thymocytes was significantly higher in 4 Gy TBI + 50 mg/kg theaflavins group than that in 4 Gy TBI + 25 mg/kg theaflavins group (P < 0.05).Therefore,50 mg/kg theaflavins was chosen as the optimal dose for subsequent experiments.Moreover,the aberrant histomorphology of irradiated thymus was alleviated by theaflavins.A decline in the percentage of CD4-CD8-T cells and an elevation of CD4+CD8-and CD4+CD8+ T cells were found in irradiated mice administered with theaflavins (P < 0.05).Compared with 4 Gy TBI group,the ROS level was significantly decreased in 4 Gy TBI + theaflavins group (P < 0.05).Conclusion Theaflavins exhibits a protective effect on radiation-induced thymus injury.