1.Influence of AKT on survival and apoptosis of gastric adenocarcinoma cells.
Yong LIU ; Ming-zhi LU ; Si-si FAN ; Sheng YUAN
Chinese Journal of Pathology 2009;38(5):340-341
Adenocarcinoma
;
pathology
;
Apoptosis
;
drug effects
;
Cell Line, Tumor
;
Cell Survival
;
drug effects
;
Dose-Response Relationship, Drug
;
Humans
;
Nucleosides
;
administration & dosage
;
pharmacology
;
Proto-Oncogene Proteins c-akt
;
antagonists & inhibitors
;
Pyridazines
;
administration & dosage
;
pharmacology
;
Stomach Neoplasms
;
pathology
2.Gender-related differences of cytochrome P450 3A4 activity
Yuan GU ; Duanyun SI ; Changxiao LIU
Chinese Pharmacological Bulletin 2003;0(09):-
Gender-related differences in drug pharmacokinetics have frequently been considered as potentially important determinants for the clinical effectiveness of drug therapy. Major molecular factors involved in drug disposition include drug-metabolising enzymes and drug transporters. Oxidative drug metabolism by cytochrome P450 (CYP) enzymes is a major pathway for drug elimination. CYP3A4,the major human drug-metabolizing CYP enzymes,has repeatedly been suggested higher metabolic activity in women than that in men,which sex-dependent secretory patterns of growth hormone that may be responsible for.
3.Consistency of CT Perfusion Measurement in Basal Ganglia:An Experimental Study in the Mode of Volume Helical Shuttle
Guanmin QUAN ; Si QI ; Tao YUAN ; Yang LIU
Chinese Journal of Medical Imaging 2015;(9):649-653
PurposeIt is important to keep the consistency of CT perfusion imaging (CTP) measurement in the evaluation of intracranial disorders. The purpose of this paper is to probe into the consistency of basal ganglia hemodynamic characteristics in normal rabbits with CTP measurement in the mode of volume helical shuttle (VHS).Materials and Methods Brain CTP scans of 10 healthy rabbits were carried out in the VHS mode. The images derived from CTP were separately analyzed by two radiologists (A and B) with different experiences. ROIs were placed in the bilateral basal ganglia of the subjects and parameters such as cerebral blood volume (CBV), cerebral blood flow (CBF) and mean transit time (MTT) were measured three times in each rabbit. Thirty days later, radiologist A analyzed the CTP images again with the same method. Differences of parameters in bilateral basal ganglia measured by different radiologists at different periods were compared respectively and consistency of the measurements was further assessed.Results There was no significant difference among the three measurements of CBV, CBF and MTT in bilateral basal ganglia (F=0.162, 0.050 and 0.488,P>0.05). TheICC of CBV, CBF and MTT measured by the two radiologists for the first time were 0.84, 0.81 and 0.79; while theICC of CBV, CBF and MTT measured by radiologist A twice were 0.80, 0.89 and 0.84, which showed that the results had good consistency measured by different radiologists at different times.Conclusion With the same post-processing software, the consistency of CTP of basal ganglia in the VHS mode is satisfactory in healthy rabbits, which suggests this technique may be a suitable means in the evaluation of basal ganglia hemodynamics in animal models.
4.Simultaneous determination of clevidipine butyrate and its metabolite clevidipine acid in dog blood by liquid chromatography-tandem mass spectrometry.
Huihui WEI ; Yuan GU ; Yanping LIU ; Guangli WEI ; Yong CHEN ; Changxiao LIU ; Duanyun SI
Acta Pharmaceutica Sinica 2015;50(10):1290-6
A rapid, sensitive and simple liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of clevidipine butyrate and its primary metabolite clevidipine acid in dog blood. After one-step protein precipitation with methanol, the chromatographic separation was carried out on an Ecosil C18 column (150 mm x 4.6 mm, 5 µm) with a gradient mobile phase consisting of methanol and 5 mmol · L(-1) ammonium formate. A chromatographic total run time of 13.0 min was achieved. The quantitation analysis was performed using multiple reaction monitoring (MRM) at the specific ion transitions of m/z 454.1 [M-H]- --> m/z 234.1 for clevidipine butyrate, m/z 354.0 [M-H]- --> m/z 208.0 for clevidipine acid and m/z 256.1 [M-H]- --> m/z 227.1 for elofesalamide (internal standard, IS) in the negative ion mode with electrospray ionization (ESI) source. The linear calibration curves for clevidipine butyrate and clevidipine acid were obtained in the concentration ranges of 0.5-100 ng · mL and 1-200 ng · mL(-1), separately. The lower limit of quantification of clevidipine butyrate and clevidipine acid were 0.5 ng · mL(-1) and 1 ng · mL(-1). The intra and inter-assay precisions were all below 12.9%, the accuracies were all in standard ranges. Stability testing indicated that clevidipine butyrate and clevidipine acid in dog blood with the addition of denaturant methanol was stable under various processing and/or handling conditions. The validated method has been successfully applied to a pharmacokinetic study of clevidipine butyrate injection to 8 healthy Beagle dogs following intravenous infusion at a flow rate of 5 mg · h(-1) for 0.5 h.
5.Rules for acupoint selection in treatment of perimenopausal syndrome based on data mining technology.
Ling-yun LU ; Si-yuan ZHOU ; Ting LIU ; Er-qi QIN ; Yu-lan REN ; Ying LI
Chinese Acupuncture & Moxibustion 2014;34(10):1017-1022
OBJECTIVETo analyze the rules for acupoint selection of acupuncture and moxibustion in domestic clinical treatment of perimenopausal syndrome based on data mining technology in modern times.
METHODSThe relevant literature were retrieved from Chinese Biomedical Literature Database (CBM), China National Knowledge Infrastructure (CNKI) and Wanfang database on this disease treated with clinical acupuncture and moxibustion in China from 1978 to 2013. The database of acupuncture-moxibustion prescription was set up. The relevant regulations of data mining technology were used to analyze the rules for acupoint selection.
RESULTSTotally, 211 papers, 254 acupuncture-moxibustion prescriptions and 130 acupoints were included. The total frequency of acupoints application was 2193 times, with 14 meridians involved. The utilization of the acupoints in the lower limbs and on the back were 33.0% (723/2193) and 23.8% (521/2193) and those of yin and yang meridians were 51.8% (1136/2193) and 44.0% (965/2193), respectively. The utilization of the specific acupoints accounted for 88.7% (1946/2193).
CONCLUSIONIn clinical treatment of perimenopausal syndrome with acupuncture and moxibustion in modern times, the acupoint selection from involved meridians is the basis, associated with multiple methods of acupoint combination; yin and yang meridians are equally important and the specific acupoints are considered particularly critical in application.
Acupuncture Points ; Acupuncture Therapy ; China ; Clinical Trials as Topic ; Female ; Humans ; Perimenopause ; physiology
6.Biofeedback therapy for chronic prostatitis: Application and consideration.
Si-da CHEN ; Jing LI ; Shen-qing LI ; Li-huan QIAN ; Yuan HE ; Bu-ping LIU
National Journal of Andrology 2016;22(1):57-62
Studies of biological feedback (BF) for the treatment of chronic prostatitis (CP) are occasionally reported have exhibited some related problems. This article presents an evaluation of the published literature on the BF treatment of CP at home and abroad in the aspects of instrument, method, application, effect, function, and mechanism. UROSTYMTM and MyoTrac are often employed and their operating paths are basically the same. NIH prostate symptom scores, urinary function, pain, sexual function, immune function, prostate fluid, and other indicators are generally used for the analysis of the effects of BF alone or in combination with other therapies on CP and its related symptoms. Either BF alone or BF combined with other therapies can promote urination, reduce pain, improve the quality of life, attenuate inflammation, improve sexual function, adjust immunity, and lessen physical and chemical stimulation. However, the relevant literature is of low quantity and quality, the reported studies are not standardized, and exploration of the action mechanisms is neglected.
Biofeedback, Psychology
;
Humans
;
Male
;
Prostatitis
;
therapy
;
Quality of Life
7.Research Progress in Drug Interactions of Haloperidol
Kai LEI ; Yuan HUANG ; Si ZHANG ; Guofang HE ; Dong LIU ; Xiuhua REN
China Pharmacist 2017;20(2):334-337
Objective:To summarize the drug interactions of haloperidol used in combination with the other drugs to provide refer-ence for safe, reasonable and effective use of haloperidol in clinics. Methods:By retrieving Micromedex? , Pubmed, CNKI and so on, the interactions between haloperidol and the other drugs were summarized and analyzed. Results:The effect of haloperidol was on do-pamine receptors, and haloperidol was mainly metabolized by hepatic cytochrome P450 ( CYP) enzymes. When haloperidol was com-bined with the other drugs, significant interactions of pharmacokinetics and pharmacodynamics were induced by affecting CYP enzymes or dopamine receptor. Conclusion:In clinical practice, the other drugs combined with haloperidol should be reasonable and careful to ensure safe, effective and rational drug use.
8.Effect of dexmedetomidine on expression of OGG1 mRNA in rat hippocampal neurons subjected to oxygenglucose deprivation/reoxygenation and restoration
Yanna SI ; Hongguang BAO ; Liu HAN ; Yuan ZHANG ; Mengmeng CAI ; Xinyi XIE
Chinese Journal of Anesthesiology 2013;33(8):1003-1006
Objective To evaluate the effect of dexmedetomidine on the expression of 8-Oxoguanine DNA glycosylase 1 (OGG1) mRNA in rat hippocampal neurons subjected to oxygen-glucose deprivation/reoxygenation and restoration (OGD/R).Methods Hippocampal neurons isolated from pathogen-free neonatal Sprague-Dawley rats born within 3 days,were cultured primarily and seeded in 96-well plates (100 μl/well) or 6-well plates (2 ml/well) at the density of 1 × 106 cells/ml.The cells were randomly divided into 5 groups (n=30 each):control group (group C),group OGD/R,and different concentrations of dexmedetomidine groups (DEX1-3 groups).The cells were cultured in normal culture medium in group C and the cells were subjected to OGD/R in the other groups.In DEX1-3 groups,dexmedetomidine with the final concentrations of 0.1,1.0 and 10.0μmol/L were added,respetively,at 2h before OGD.At 24h of restoration,hippocampal neurons were stained with haematoxylin and eosin (H.E) for examination of pathological changes,the cell survival rate was detected by MTT method,the activity of superoxide dismutase (SOD) and content of malondialdehyde (MDA) were detected by colorimetric method,and the expression of OGG1 mRNA was detected by RT-PCR.Results The pathological changes of neurons were obvious in group OGD/R,and the pathological changes of neurons were significantly mitigated in DEX1,DEX2 and DEX3 groups.Compared with group C,the cell survival rate and SOD activity were significantly decreased,MDA content was increased,and the expression of OGG1 mRNA was down-regulated in OGD/R,DEX1,DEX2 and DEX3 groups (P < 0.05).Compared with group OGD/R,the cell survival rate and SOD activity were significantly increased,MDA content was decreased,and the expression of OGG1 mRNA was up-regulated in DEX1,DEX2 and DEX3 groups (P < 0.05).There was no significant difference in the indices mentioned above between DEX1,DEX2 and DEX3 groups (P > 0.05).Conclusion Dexmedetomidine may protect hippocampal neurons against oxidative stress injury by up-regulating the expression of OGG1 mRNA in rat hippocampal neurons subjected to OGD/R.
9.Determination of halometasone and its pharmacokinetics study in rabbit plasma by LC-MS/MS
Jingyuan LIU ; Linan WU ; Yuanhui YANG ; Yuan GU ; Guangli WEI ; Duanyun SI
Chinese Pharmacological Bulletin 2017;33(3):411-416
Aim TodevelopandvalidateaLC-MS/MS assay to quantify halometasone in rabbit plasma and study pharmacokinetics of halometasone after dermal topical administration of Halometasone Cream.Meth-ods Theplasmasamplewassubmittedtoliquid-liquid extraction using methyl tertiary butyl ether,with dexa-methasone as the internal standard (IS ).Chromato-graphic separations were performed on a Diamonsil C18 column(100 mm ×4. 6 mm,5 μm)with a linear gra-dient of methanol and 2 mmol · L-1 ammonium ace-tate.Halometasone and dexamethasone(IS)were ion-ized with an ESI source operated in negative ion mode, and the detected ions were m/z 503. 1→413. 0 (halo-metasone),m/z 391. 0→361. 0 (dexamethasone ). The test article could be monitored in rabbit plasma when following single dermal topical administration of Halometasone Cream at 1 g/100 cm2 to rabbits by u-singavalidatedLC-MS/MSassay.Results Calibra-tion curve was linear over the concentration range of0. 02~20 μg·L-1 in rabbit plasma.For low,medi-um,high concentration of QC solutions,the intra-and inter-day precision was in the range of 3. 72% ~7. 87%, and the accuracy was within 99. 1% to 103%. The pharmacokinetic parameters in rabbits were as follows:Tmax,Cmax,AUC0-t,T1/2 was (7. 38 ± 1. 06)h,(1. 16 ±0. 527)μg·L-1,(18. 8 ±7. 23)h·μg·L-1 ,(13. 8 ±3. 70)h,respectively.Conclusions ThisLC-MS/MSanalysismethodhashighsensitivi-ty,and sample processing method is simple,which has been rigorously validated.The method could be suc-cessfully applied to the pharmacokinetic study of halo-metasone after skin administration of Halometasone Cream to rabbits.
10.Effect of Qingguang'an on elastic fiber, MMP- 7, TlMP - 1 in scarring area of filtration canal after glaucoma surgery
Yuan-Bi, LI ; Qing-Hua, PENG ; Xue-Si, HUANG ; Xiao-Liu, CHEN ; Han-Yu, TAN
International Eye Science 2015;(1):20-25
?AlM: To observe the effect of Qingguang'an on elastic fiber, MMP-7, TlMP-1 in scarring area of filtration canal after glaucoma surgery through the four Qingguang'an effective groups and Qingguang'an granules, to discuss and compare their mechanism of action on scarring area of filtration canal.?METHODS:Four effective components of Qingguang'an were used in groups D, E, F, G and H after glaucoma surgery, compared with group A ( blank ) , group B (model) and group C ( MMC) to observe the effect of elastic fiber, MMP-7, TlMP-1 in scarring filtration canal.?RESULTS:Compared with the preoperative basic lOP and 2d , 1, 2, 4wk postoperative lOP of groups C, E and H, the lOP of three group rose up slower than other groups, and kept the lowest data at 28d. There was significant difference compared with the rest of A, B, D, F, G groups (P<0. 05). The area and density of elastic fiber in surgery group were significantly different with that of black control group ( P<0. 05 ), but there were no statistical differences between groups C and H, groups C and F, groups H and E (P>0. 05). The difference was statistically significant among other groups (P<0. 01).?CONCLUSlON:The scarring area of filtration canal after glaucoma surgery is the major reason which lead to the failure of surgery. Qingguang'an effective group 2, Qingguang'an granules and MMC could reduced the scar tissue by restrained the elastic fiber, TlMP - 1 and increased the MMP-7. By observing the experimental results that both Qingguang'an effective group 2 and Qingguang'an granules could restrained the scarring area of filtration canal, the effects were unbiased, Qingguang'an granules group is better than effective group 2.