1.Regulation of proliferation and apoptosis of K562 cells by changes of Ras-ERK pathway induced by simvastatin
Qinfang TAN ; Xiaomei LIAO ; Bi CHEN
Journal of International Oncology 2009;36(12):949-953
Objective To investigate the changes in molecule levels of Ras-ERK signal pathway of K562 cells treated with simvastatin in vitro,and to illustrate that simvastatin inducing the changes in molecule levels of Ras- ERK signal pathway is involved in regulation of proliferation and apoptosis of K562 cells. Methods K562 cells,the chronic myelocytic leukemia(CML) cell lines,were cultured and treated with simvastatin in vitro and proliferation activity of K562 cells was detected by MTT. The changes of apoptosis rate and cell cycle of K562 cells were measured by flow cytometry(FCM). The molecular changes of Ras-ERK signal pathway were analyzed by RT- PCR in transcriptional level. Results The proliferation of K562 cells was inhibited by simvastatin,and G_0-G_1 arrested in K562 cells and significant apoptosis rate was observed with FCM. Most molecules of Ras- ERK signal pathway expressed differentially at transctiptional level. Conclusion Simvastatin probablely inhibit proliferation and induces apoptosis of K562 cells,depending on Ras-ERK signal pathway which is involved in cell proliferation and apoptosis.
2.Discussion of indication for selecting ectopic pregnancy treated by trans-uterine artery embolization
Wenjian XU ; Caifang NI ; Xiaomei TAN
Journal of Interventional Radiology 1992;0(01):-
Objective To discuss the selection of indication for using uterine artery perfusion and embolization in tubal pregnancy. Methods Fifty one cases of tubal pregnancy were treated by superselective trans-uterine artery (TUA) catheterization with perfusing Methorexate (MTX) and then embolized the uterine arteries by gelfoam. The comparisons among serum P-HCG concentration, abdominal bleeding and the size of the ectopic mass could state the importance of the indication selection preprocedurally. Results Forty eight of the 51 cases were cured by this method, when the ectopic mass size≥5 cm, the cure rate was low, 33.33% (P
3.Investigation of Environmental Noise Perception of Residents in Lu'an City
Xiaomei WANG ; Lvgui TAN ; Xiaosheng LIU
Journal of Environment and Health 2007;0(11):-
Objective To understand the situation of, mental health and behavior of the residents influenced by the environment noise. Methods From Feb. till Mar. 2005 and from Sep. till Oct. 2006, the residents living in 4 functional districts in Lu'an city, Anhui Province for one year or more were investigated by questionnaire. The investigation involved the general status, noise perception, behavior, adjustability and so on. 952 available questionnaires from 84 sites were attained. Results The significant differences were seen in the environmental noise perception among sex, age, occupation and health status (P
4.Investigation of metabolic kinetics and reaction phenotyping of ligustrazin by using liver microsomes and recombinant human enzymes.
Yan TAN ; Xiaomei ZHUANG ; Guolin SHEN ; Hua LI ; Yue GAO
Acta Pharmaceutica Sinica 2014;49(3):374-9
The metabolic characteristics of ligustrazin (TMPz) in liver microsomes were investigated in the present study. The reaction phenotyping of TMPz metabolism was also identified by in vitro assessment using recombinant human cytochrome P450 enzymes (CYP) and UDP glucuronosyltransferases (UGT). TMPz was incubated at 37 degrees C with human (HLM) and rat liver microsomes (RLM) in the presence of different co-factors. The metabolic stability and enzyme kinetics of TMPz were studied by determining its remaining concentrations with a LC-MS/MS method. TMPz was only metabolically eliminated in the microsomes with NADPH or NADPH+UDPGA. In the HLM and RLM with NADPH+UDPGA, t1/2, K(m) and V(max) of TMPz were 94.24 +/- 4.53 and 105.07 +/- 9.44 min, 22.74 +/- 1.89 and 33.09 +/- 2.74 micromol x L(-1), 253.50 +/- 10.06 and 190.40 +/- 8.35 nmol x min(-1) x mg(-1) (protein), respectively. TMPz showed a slightly higher metabolic rate in HLM than that in RLM. Its primary oxidative metabolites, 2-hydroxymethyl-3, 5, 6-trimethylpyrazine (HTMP), could undergo glucuronide conjugation. The CYP reaction phenotyping of TMPz metabolism was identified using a panel of recombinant CYP isoforms (rCYP) and specific CYP inhibitors in HLM. CYP1A2, 2C9 and 3A4 were found to be the major CYP isoforms involved in TMPz metabolism. Their individual contributions were assessed b) using the method of the total normalized rate to be 19.32%, 27.79% and 52.90%, respectively. It was observed that these CYP isoforms mediated the formation of HTMP in rCYP incubation. The UGT reaction phenotyping of HTMP glucuronidation was also investigated preliminarily by using a panel of 6 UGT isoforms (rUGT). UGT1A1, 1A4 and 1A6 were the predominant isoforms mediated the HTMP glucuronidation. The results above indicate that the metabolism of TMPz involves multiple enzymes mediated phase I and phase II reactions.
5.In vitro investigation on CYP enzyme based interaction of active components from SIWU decoction
Yan TAN ; Guolin SHEM ; Xiaomei ZHUANG ; Hua LI ; Yue GAO
Chinese Pharmacological Bulletin 2014;(10):1456-1461
Aim To investigate the inhibitory and in-duction effects of the active components of SIWU de-coction on cytochrome P450 enzymes ( CYP ) and as-sess the CYP based drug interaction. Methods Ac-tive components fructose, ferulic acid, paeoniflorin, li-gustrazine and their combinations were incubated sepa-rately with human liver microsomes ( HLM) and probe substrates. Metabolites of the CYP probe substrates were determined by LC-MS/MS to assess the inhibitory activities on human CYP1 A2 , 2 B6 , 2 C9 , 2 C19 , 2 D6 and 3 A4 . Sandwich-cultured rat hepatocytes model was used to evaluate the CYP1 A2 and CYP3 A1/2 induc-tion. Results The inhibitory rates on CYP1A2, 2B6, 2 C9 and 2 C9 by the test groups at 100 μmol · L-1 were all < 62%, while the activities of CYP3 A4 and 2D6 were not affected. The CYP1A2 activities in the test groups of peoniflorin and its combinations ( 50μmol·L-1 ) were significantly enhanced, with the in-creasing fold more than 40% of positive control group. No significant induction on rat CYP3 A1/2 was ob-served for four principles and their combinations. Con-clusions The active components of SIWU decoction do not show significant inhibitory effects on six CYP isoforms. Peoniflorin could induce the CYP1A2 activity in rat hepatocytes. The induction activity is enhanced by the concomitant use of peoniflorin with ferulic acid and/or ligustrazine.
6.Effect of Gegen Qinlian Decoction on Rotavirus-inducing Diarrhea in Neonatal Mice
Lijun SONG ; Wenchang ZHAO ; Xiaomei TAN ; Mengmeng YANG ; Jiabo LUO
Chinese Journal of Information on Traditional Chinese Medicine 2013;(7):35-37
Objective To investigate the anti-rotavirus effect of Gegen Qinlian decoction on rotavirus (RV)-inducing diarrhea neonatal mice model, and provide evidences for pharmacological and pharmacodynamic studies. Methods Neonatal diarrhea mice model of Kunming family infected with RV-Wa was developed. Symptom, diarrhea ratio and severity level, histological changes of neonatal mice’s small intestine and lung was assessed after Gegen Qinlian decoction (0.78 g/kg) treatment. Results Diarrhea ratio, diarrhea severity level, histological changes of neonatal mice’s small intestine and lung were obviously decreased after Gegen Qinlian decoction (0.78 g/kg) treatment. Conclusion Gegen Qinlian decoction has anti-rotavirus effect on RV induced diarrhea.
7.Influence of various compatibilities on puerarin content in Gegen Qinlian Decoction
Kaijin DAI ; Jiabo LUO ; Xiaomei TAN ; Zhaohui WU
Chinese Traditional and Herbal Drugs 1994;0(06):-
Object To set up the quantitative method for determining the puerarin in Gegen Qinlian Decoction (GQD) by RP-HPLC and to study the change of puerarin contents in various combinations of GQD. Methods L 8(2 7) orthogonal design and statistic analysis (SPSS 10.0) were used, the puerarin contents in the samples were determined by HPLC. Results Influence of Radix Scutellaria, Rhizoma Coptidis and Radix Glycyrrhizae Preparata on the puerarin content in GQD was insignificant. And interactions between two of three were insignificant too. In this experiment, puperarin in the sedimentation was found in the compatible decoction of Rhizoma Coptidis and Radix Puerariae. Conclusion The puerarin content is not markedly influenced by Radix Scutellaria, Rhizoma Coptidis and Radix Glycyrrhizae Preparata. Maybe, the change of pH is relevant to the sedimentation in the compatible decoction contained Rhizoma Coptidis. and Radix Puerariae
8.Comparison of the Preventive and Therapeutic Effect of Different Dosage Forms of Vinegar Testudinis Car-apax on Mice with Hemopenia or Osteoporosis
Xinyu WANG ; Xiaomei TAN ; Wenxin ZHANG ; Yuanli HU
China Pharmacy 2017;28(19):2661-2665
OBJECTIVE:To compare the preventive and therapeutic effect of Vinegar testudinis carapax (VTC) water decoc-tion and powder on mice with hemopenia or osteoporosis. METHODS:Mice were randomly divided into normal group (1%CMC-Na),model group (1% CMC-Na),positive group (Compound e-jiao slurry 20 mL/kg or Gusongbao capsule 1.98 g/kg), VTC water decoction and powder low-dose,medium-dose,high-dose groups(1.95,3.90,7.80 g/kg),10 in each group. In hemo-penia mice model experiment,except for the normal group,mice in other groups were intraperitoneally injected cyclophosphamide 0.1 g/kg for modeling,and intragastrically given medicines from the first day(positive drug was Compound e-jiao slurry),once a day,for 8 d. After administration,peripheral blood levels of white blood cells (WBC),red blood cells (RBC),hemoglobin (HG),hematocrit(HCT),platelet(PLT)and bone marrow nucleated cells(BMNC)numbers in femur of mice were determined. In osteoporosis mice model experiment,except for the normal group,mice in other groups were intragastrically given retinoic acid 0.105 g/kg for modeling,and intragastrically given relevant medicines from the first day(positive drug was Gusongbao capsule), once a day,for 30 d. After administration,alkaline phosphatase(ALP)level,organ(thymus,liver,spleen,ovary)coefficients, dry masses and degreasing,ash quality of the femur,and contents of femur calcium and phosphorus in serum of mice were detect-ed. RESULTS:In hemopenia mice model experiment,compared with normal group,WBC,RBC,HG,HCT,PLT levels in pe-ripheral blood and BMNC numbers in femur of mice in model group were decreased (P<0.01). Compared with model group, HCT,PLT,BMNC levels in peripheral blood of mice in VTC water decoction low-dose group,and RBC,HG levels in medi-um-dose group and HCT level in high-dose group were significantly increased (P<0.05). And WBC level in peripheral blood of mice in powder low-dose,high-dose groups and HG level in medium-dose group were significantly increased(P<0.05). In osteo-porosis mice model experiment,compared with normal group,ALP level in serum of mice in model group,dry mass and degreas-ing,ash mass,ash mass/dry mass of degreasing of the femur,and the contents of femur calcium and phosphorus were significantly decreased (P<0.01),there was no significant difference in each organ coefficient (P>0.05). Compared with model group,ALP level in serum and dry mass,phosphorus content of femur of mice in VTC water decoction high-dose group were significantly in-creased (P<0.05);ALP level in serum and dry mass,phosphorus content of femur of mice in VTC,powder medium-dose, high-dose group,the ash mass,ash mass/dry mass of degreasing,contents of femur calcium and phosphorus in VTC powder medi-um-dose group were significantly increased(P<0.05). CONCLUSIONS:VTC water decoction shows better preventive and thera-peutic effect on hemopenia mice;while VTC powder shows better preventive and therapeutic effect on osteoporosis mice.
9.Study on the Effective Component Formula of Mahuang Fuzi Xixin Decoction for Anti-allergic Rhinitis
Yao HUANG ; Dazhi SHI ; Xiaomei TAN ; Yinyin HUANG ; Manli XIA
China Pharmacy 2017;28(19):2635-2638
OBJECTIVE:To study the new formula of effective components in TCM for anti-allergic rhinitis (AR),and pro-vide reference for developing TCM preparations for anti-AR. METHODS:Using pseudoephedrine hydrochloride (0-13.5 mg/kg), total alkaloid extracts of Aconitum carmichaelii (0-21.18 mg/kg),volatile oil of asari radix (0-0.0092 mL/kg) in Mahuang Fuzi Xixin decoction as formula objects,uniform design method was used for drug grouping,and multiple regression analysis was con-ducted for the behavioral scores before and after administration,contents of histamine and immunoglobulin E (IgE) in serum of AR guinea pigs to obtain the best formula. Using Xinqin granule,Loratadine tablet,Mahuang Fuzi Xixin decoction respectively as positive control,efficacy of the best formula was verified from aspects of behavioral scores before and after administration,con-tents of histamine and IgE of AR guinea pigs. And the safety of the best formula was preliminarily observed through acute toxicity test in mice. RESULTS:The best formula was as follow as pseudoephedrine hydrochloride 11.25 mg/kg,total alkaloid extracts of A. carmichaelii 21.18 mg/kg,volatile oil of asari radix 0.0045 mL/kg. Compared with each positive drug group,there were no sig-nificant differences in behavioral scores before and after administration in the best formula group(P>0.05). While compared with Xinqin granule group and Mahuang Fuzi Xixin decoction group,histamine content in serum in the best formula group was signifi-cantly reduced (P<0.05);compared with Xinqin granule and Loratadine tablet group,IgE content in serum in the best formula group was significant decreased (P<0.05). Median lethal dose of the best formula was 1822.04 mg/kg. CONCLUSIONS:The screened best formula shows better effect than Xinqin granule and Mahuang Fuzi Xixin decoction in terms of reducing histamine content in serum,better than Loratadine tablet and Xinqin granule in terms of reducing IgE content in serum,with good safety, which indicates the feasibility of TCM effective component formula to a certain degree.