2.Preparation of Paeonol-HP-β-cyclodextrin Inclusion Compound and Its Prescription Technology Optimiza-tion
Xin ZHENG ; Peihong YANG ; Lin HE ; Xi CHEN ; Mo CHENG ; Bibo YOU
China Pharmacy 2017;28(4):530-532,533
OBJECTIVE:To prepare paeonol-HP-β-cyclodextrin (PAE-HP-β-CD) inclusion compound and to optimize its pre-scription technology. METHODS:PAE-HP-β-CD was prepared by freeze drying method and validated. Using inclusion rate as in-dex,main drug-accessory ratio,inclusion time,inclusion temperature and stirring speed as factors,the preparation technology was optimized by central composite design-response surface methodology. RESULTS:Prepared PAE-HP-β-CD underwent phase transfor-mation. The optimal inclusion technology was as follows as main drug-accessory ratio of 3.39∶1,inclusion temperature of 50 ℃, inclusion time of 3.2 h, stirring speed of 350 r/min. Relative error between measured value (87.46%) and predicted value (89.12%) of inclusion rate was 1.86%(n=6). CONCLUSIONS:PAE-HP-β-CD inclusion compound is prepared successfully, and its prescription technology is stable and feasible.
3.Expression of Potassium Channels in Peripheral Monocyte from Patients with Coronary Artery Disease and the Regulation of Simvastatin
Shaoping WANG ; Li YOU ; Shiying LI ; Jian WANG ; Hong YANG ; Shujuan CHENG
China Pharmacy 2015;(20):2793-2795
OBJECTIVE:To discuss the expression of voltage-gated potassium channel(KV1.3)and calcium activated potassi-um channel(KCa3.1)in peripheral monocyte from patients with coronary artery disease(CAD)and the regulatory effect of simvas-tatin. METHODS:20 patients with CAD and 8 control patients without CAD diagnosed by percutaneous coronary intervention but correlated to risk factor of CAD were enrolled. The expression of KV1.3 mRNA and KCa3.1 mRNA were measured by RT-PCR in 2 groups,and those of CAD group were measured by RT-PCR after 1 month of simvastatin treatment. RESULTS:Compared with control group,mRNA expression of KV1.3 [(1.54±0.08)vs.(0.77±0.06),P<0.01] and KCa3.1 [(1.32±0.08)vs.(1.06±0.06), P<0.05] were significantly increased in CAD group. mRNA expression of KV1.3 was significantly correlated to the concentration of C reactive protein (CRP)(P=0.003)and was decreased by simvastatin for one month [(1.54 ± 0.08)vs.(1.14 ± 0.05),P<0.01]. However,mRNA expression of KCa3.1 was not correlated to the concentration of CRP and simvastatin didn’t affect it’s expression. CONCLUSIONS:KV1.3 and KCa3.1 in peripheral monocytes may be two new markers of CAD. Regulating KV1.3 may be one of mechanisms of statin’s pleiotrophic effect.
4.Reconstruction and measurement of optic nerve sheath imaging in normal population with multi-slice spiral CT
Yong, YOU ; Hongbo, CHENG ; Ning, FAN ; Ningli, WANG ; Jie, YANG ; Lu, LIU ; Xuyang, LIU
Chinese Journal of Experimental Ophthalmology 2015;33(11):1015-1018
Background Optical nerve damage of glaucomatous eyes is associated with intracranial pressure.Conventional method of evaluating intracranial pressure is to measure cerebrospinal pressure by lumber puncture.However,the measurement of intraorbital optical nerve parameters,a novel method of evaluating intracranial pressure,is introduced in this field.Objective This study was to measure and analyze the intraorbital optic nerve sheath diameter (ONSD) and cross sectional area (ONSA) in normal population using multi-slice spiral CT.Methods This study protocol was approved by Clinical Ethic Committee of Shenzhen Chinese Traditional Medical Hospital and followed Hersinki Declaration.Informed consent was obtained from each individual prior to any medical examination.One hundred and five eyes of 105 normal persons with normal cerebral CT image were enrolled in Shenzhen Chinese Traditional Medical Hospital from January 2012 to September 2013.Cerebral volume was scanned in all the individuals by 64 slice spiral CT.The brain images were obtained for the curve planar rebuilding of intraorbital optical nerve on image post-processing workstation.The maximum and minimum of ONSD and the ONSA in axial sections at 3,6,9,12 and 15 mm far away from globe wall were measured using a standardized technique to analyze the change of optical nerve parameters at different point locations.These parameters were compared in different gender or eyes.The correlation among age and the optical nerve parameters at 3 mm far away from globe wall was evaluated by multivariate regression analysis.Results The average maximal ONSDs were (6.24±0.47), (5.56±0.44),(5.18±0.43),(4.82±0.41) and (4.69±0.41) mm;the average minimal ONSDs were (5.56±0.50),(4.97± 0.41) ,(4.55±0.35),(4.26±0.39) and (4.10±0.40) mm;the average ONSAs were (27.68±4.40),(22.02±3.35) , (18.74± 2.75) , (16.34±2.72) , (15.40±2.68) mm2 at 3,6,9,12 and 15 mm far away from posterior eyeball wall,respectively, showing significant differences in the maximal/minimal ONSDs and ONSAs among the different point locations (F =218.329,215.906,246.924, all at P =0.001).No significant differences were found in the maximal/minimal ONSDs and ONSAs between male and female or between the right eyes and left eyes (gender:t=1.805,P=0.074;t=1.930,P=0.056;t=1.329,P=0.187;eyes:t=0.724,P=0.471;t=1.562,P=0.121;t=1.424,P=0.158).No significant correlations were seen between age and maximal/minimal ONSDs or ONSAs with the coefficients of 1.873,7.415 and-0.853 correspondingly (P =0.847,0.460,0.637).Conclusions Intraorbital section of optical nerve can be rebuilt using standardized technique after scanning of 64 slice spiral CT.The cross section of intraorbital optic nerve sheath is oval in shape and the optic nerve is thinning with the increase of distance far away posterior eyeball wall in normal populatuion.
5.Effects of triamcinolone acetonide and Ketorolac tromethamine on the expressions of aquaporin-4 and vascular endothelial growth factor in hypoxic Müller cell
Wei, CAI ; Yang, CHENG ; Li-na, KE ; You-shun, ZHANG ; Guo-bao, LI
Chinese Journal of Experimental Ophthalmology 2013;31(8):744-748
Background Intravitreal injection with triamcinolone acetonide (TA) may cause complications,including increase of intraoculapressure (IOP),cataracand endophthalmitis.Ketorolatromethamine (Ketorolac) inew,lesadverse reactionof non-steroidal anti-inflammatory drug.The action mechanism of Ketorolaisimilato TA.Therefore,Ketorolamay be completely opartly replace Tin the treatmenof retinal edema.Objective The purpose of thistudy wato investigate the effectof Tand Ketorolaon the expressionof aquaporin-4 (AQP4) and vasculaendothelial growth facto(VEGF) in hypoxiretinal Müllecellin vitro and to explore the mechanism of treating retinal edemwith Tand Ketorolac.MethodThe propose of research and use of the animalwere approved by Animal ExperimenResearch Review Committee of Hubei University of Medicine.Twenty eyeof New Zealand albino rabbitwere extracted and the retinal tissue waisolated.The Müllecellwere cultured and passaged using the enzymatidigestion method and Müllecellwere identified using glial fibrillary acidiprotein (GFAP),vimentin and α-smooth muscle actin (α-SMA) by immunofluorescence staining.The hypoxicell modelwere established by culturing the cellin DMEM with 500 μmol/L CoCl2 fo0,6,12,24 hours.The cellof hypoxifo24 hourwere divided into normal control group,hypoxicontrol group,hypoxia+50,100,200 mg/L To50,100,200 mg/L Ketorolagroups.Corresponding drugwere added into the medium in the differengroups.The expressionof AQP4 mRNand VEGF mRNin Müllecellwere detected by semi-quantitative reverse transcription PC(RT-PCR).ResultThe cellgrew well and reached 80% confluence with the irregulashape and ovoid nuclei 14-15 dayaftecultured.More than 95% primary cellshowed positive reaction to GFAP,vimentin and α-SMA.The expressing levelof AQP4 mRNand VEGF mRNin Müllecell(values) were significantly differenin varioutime point(AQP4 mRNA:F=18.70,P<0.01 ; VEGF mRNA:F =53.20,P<0.01),and those of 6,12 and 24 houraftecultured with CoCl2were increased than those withouCoCl2 (P<0.05).The expressing levelof AQP4 mRNand VEGF mRNin Müllecell(values) were significandifferenamong the normal control group,hypoxicontrol group,hypoxia+50,100,200 mg/L ToKetorolagroup(AQP4 mRNA:F =27.98,P < 0.01 ; VEGF mRNA:F =10.03,P <0.01).Compared with the hypoxicontrol group,the expressing levelof AQP4 mRNand VEGF mRNin the Müllecellwere declined in the hypoxia+ 100,200 mg/L Tgroup and the hypoxia+100,200 mg/L Ketorolagroup (P<0.05).The expressing levelof AQP4 mRNand VEGF mRNwere found statistically insignificandifference between hypoxia+ 100 mg/L Tgroup and hypoxia+ 100 mg/L Ketorolagroup,obetween hypoxia+ 200 mg/L Tgroup and hypoxi+200 mg/L Ketorolagroup (P> 0.05).ConclusionTand Ketorolacan downregulate the expressionof AQP4 and VEGF in Müllecellundehypoxiconditions,inferring thathey have similamechanism in the impacon AQP4 function in retinal edematoueye.
6.Percutaneous laser disc decompression for cervical vertigo.
You-Geng YANG ; Xian-Sheng REN ; Chen YANG ; Jie-Ping CHENG
Chinese Journal of Surgery 2007;45(20):1408-1410
OBJECTIVETo investigate the curative effect and mechanism of transcutaneous laser disc decompression for the treatment of cervical vertigo.
METHODSFrom October 2000 to October 2004, 42 patients with cervical vertigo were treated with percutaneous laser disc decompression by applying a Nd: YAG laser (wavelength is 1064 nm). The postoperative follow-up period was more than 2 months, the change of patients' vertigo were observed.
RESULTSAll the patients were followed up. The mean follow-up period was 7.5 months (from 2 to 36 months). After 2 months of postoperative, 28 patients' vertigo disappeared (67%), 6 patients' vertigo improved (14%), 8 patients' vertigo did not improve. The effective rate was 81%, there was no complication (infection and nerve injury).
CONCLUSIONSCervical intervertebral disc protrusion and cervical spine instability irrigate the neck sympathetic nerve, result in the spasm of vertebral artery, which is the main cause of cervical vertigo. Percutaneous laser disc decompression can decrease intradiscal pressure, increase local temperature, remove the spasm of the vertebral artery. The therapeutic effect for the treatment of cervical vertigo was remarkable.
Adult ; Cervical Vertebrae ; surgery ; Decompression, Surgical ; methods ; Diskectomy, Percutaneous ; methods ; Female ; Follow-Up Studies ; Humans ; Intervertebral Disc ; surgery ; Intervertebral Disc Displacement ; complications ; surgery ; Laser Coagulation ; methods ; Male ; Middle Aged ; Treatment Outcome ; Vertigo ; etiology ; surgery
7.Preparation, characterization, and pulmonary delivery of rifapentine liposomes modified by lauric diethanolamide.
Jia-you SHU ; Xiang-yang QUAN ; Yi SHU ; Yi-ping GUANG ; You-cheng LIU
Acta Pharmaceutica Sinica 2006;41(8):761-764
AIMTo prepare rifapentine (RIF) liposomes modified by surfactants for studying their the water-solubility, drug loading effeciency, release rate and pulmonary drug delivery.
METHODSThe film method was used to prepare RIF liposomes. Of verious RIF liposomes morphology by lauric diethanolamide (LDEA), Tween 80 and azone, the properties were studied, envolving morphology, entrapment drug release rate and dissected lung-membrance penetration rate of swine. Pulmonary delivery study was carried out through bronchoscope.
RESULTSThe particle size of RIF-LDEA liposomes was between 15 - 50 nm. The top entrapment efficiency reached 83.0%. The apparent coefficient of membrane penetration (Kp) was 44.29. LD50 was 675 mg x kg(-1) by iv.
CONCLUSIONLDEA increased the water-solubility, loading effeciency and release rate of RIF liposomes. The prepared RIF-LDEA liposomes were suitable for the treatment of pulmonary tubrculosis through bronchoscope.
Animals ; Antibiotics, Antitubercular ; administration & dosage ; chemistry ; pharmacokinetics ; Drug Carriers ; Drug Delivery Systems ; methods ; Ethanolamines ; chemistry ; Lauric Acids ; chemistry ; Liposomes ; Lung ; metabolism ; Particle Size ; Permeability ; Rifampin ; administration & dosage ; analogs & derivatives ; chemistry ; Solubility ; Swine
8.Evaluation of nasal patency in patients with vasomotor rhinitis.
You YANG ; Zhong-yan LIU ; Yuan ZHANG ; Cheng-yao LIU ; Luo ZHANG
Chinese Journal of Otorhinolaryngology Head and Neck Surgery 2010;45(12):988-992
OBJECTIVETo measure the nasal patency in patients with vasomotor rhinitis (VMR) and healthy controls and to assess its correlation with visual analogue scale (VAS).
METHODSA total of 105 patients with VMR and 71 healthy controls were included in this study. By using nasal rhinomanometry, the pressure-flow curve and got total nasal resistances of 75 Pa and 150 Pa were measured. By means of acoustic rhinometry, the area-distance curve before and after using nasal vasoconstrictor substance was obtained, got the nasal minimum cross-sectional area (MCA), then calculated nasal congestion index (NCI). The outcomes of nasal resistance and acoustic rhinometry in two groups were compared. The correlation between VAS and nasal patency of VMR was evaluated.
RESULTSThe correlation between the outcomes with nasal resistance and acoustic rhinometry and VAS of nasal symptom showed no statistical significance in VMR patients (all P > 0.05). MCA before and after decongestion showed no difference (Z value were -1.541 and -0.626, each P > 0.05), NCI had statistic differences in two groups (Z = -2.707, P < 0.05). Nasal resistance of 75 Pa had statistic differences in two groups (Z = -4.334, P < 0.05), 150 Pa showed no difference (Z = -1.314, P > 0.05).
CONCLUSIONSVasomotor rhinitis is one of the most common non-allergic rhinitis. Subjective symptoms has no correlation with objective nasal patency tests. In clinical practice, comprehensive evaluation of subjective symptoms and objective test results of the patient is required.
Adolescent ; Adult ; Case-Control Studies ; Female ; Humans ; Male ; Middle Aged ; Nose ; physiopathology ; Rhinitis, Vasomotor ; physiopathology ; Rhinometry, Acoustic ; Young Adult
9.Effect of yiqi wenyang huoxue recipe on bone marrow stem cells' mobilization and its influence on heart function in patients with myocardial infarction.
Chinese Journal of Integrated Traditional and Western Medicine 2008;28(12):1078-1081
OBJECTIVETo observe the effect of Yiqi Wenyang Huoxue Recipe (YWHR) on bone marrow stem cells' mobilization and heart function of myocardial infarction (MI) patients.
METHODSSixty acute MI patients were equally assigned to the treatment group and the control group randomly according to the numeration table. Standard therapy composed of subcutaneous injection of 0.4 mL low molecular heparin every 12 h for 7 successive days combined with continuously orally taken of enteric-coated aspirin tablets 0.1 g, Perindopril 4 mg and Atorvastatin 10 mg once a day (if there was no contraindication), was given to all patients. But to the treatment group, one dose of YWHR was given every day additionally, which consisted of Panax ginseng 10 g, Radix Astragali 15 g, Radix Aconiti lateralis preparata 5 g, Radix Ilex pubesceus 30 g and Herbal Leonuri 10 g for 10 successive days. The change of CD34+ cells' count was observed. The infarcted area size was estimated with QRS scoring system at the end of the 3rd week after onset, and the heart function parameters, including left ventricular ejection fraction (LVEF), left ventricular end-systolic volume index (LVESVI), left ventricular end-diastolic volume index (LVEDVI) and wall motion score index (WMSI), were measured with ultrasonic cardiogram.
RESULTSOn the fifth and tenth day, the peripheral CD34+ cell count in the treatment group (48.26 +/- 5.74 and 34.18 +/- 6.70) were significantly higher than that on the day of admission (20.33 +/- 6.01), also higher than the corresponding count in the control group (22.45 +/- 5. 31 and 19.89 +/- 5.93), showing statistical difference (P < 0.01). The QRS score (2.68 +/- 0.41) and infarcted area (22.54 +/- 2.49)% in the treatment group were lower than those in the control group (3.96 +/- 0. 34 and 29.38 +/- 2.59) respectively. Comparison of heart function parameters between groups showed that LVEF (0.59 +/- 0.07 vs. 0.50 +/- 0.07) was higher LVEDVI (68.92 +/- 11.52 vs. 78.46 +/- 13.16), LVESVI (27.47 +/- 7.86 vs. 36.71 +/- 8.85), and WMSI (2.10 +/- 0.11 vs. 2.98 +/- 0.12) were lower in the treatment group than those in the control group respectively, also showing statistical difference (all P < 0.01).
CONCLUSIONYWHR has a good effect on bone marrow stem cell mobilization, it can reduce the infarcted area and improve the heart function of patients with acute MI.
Aged ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Heart ; drug effects ; physiopathology ; Hematopoietic Stem Cell Mobilization ; Hematopoietic Stem Cells ; drug effects ; physiology ; Humans ; Injections ; Male ; Middle Aged ; Myocardial Infarction ; drug therapy ; physiopathology
10.Protective effect of paeoniflorin on nerve cells in APP/PS1 mice and its mechanism
Jia-Hao ZENG ; Cheng-You YANG ; Jun WEN ; Mao-Ying ZHANG ; Xiang-Yu WANG
Chinese Journal of Pathophysiology 2018;34(6):1049-1054
AIM:To investigate the therapeutic and preventive effects of paeoniflorin ( PF) on APP/PS1 mice, and to explore the possible mechanism. METHODS:Fifteen male 5-month-old APP/PS1 non-dominant mice were chosen as normal control group, 15 male 5-month-old APP/PS1 double transgenic mice were used as model group, and 15 male 5-month-old APP/PS1 double transgenic mice treated with 5 mg/kg PF by intraperitoneal injection were allocated in administation group. The learning and memory ability of the mice in each group was detected by Morris water maze. The apoptosis was assessed by TUNEL fluorescence staining. The protein expression of PI3K, Akt, p-PI3K, p-Akt, caspase-3, caspase-9, Bcl-2 and Bax in cerebral cortex and hippocampus was detected by Western Blot. The protein expression levels and distribution of caspase-3 and caspase-9 were detected by immunohistochemistry. RESULTS:(1) Compared with nor-mal control group, the learning and memory ability declined in APP/PS1 model group. Compared with APP/PS1 model group, PF obviously improve the ability of learning and memory in mice. (2) Compared with normal control group, the ap-optosis of nerve cells in APP/PS1 model group significantly increased and distributed in wider areas, while that in PF group was reduced (P<0.05). (3) Compared with APP/PS1 model group, PF could significantly lower pro-apoptotic factors, caspase-3, caspase-9 and Bax (P<0.05), and increase the expression of anti-apoptotic factors, p-PI3K, p-Akt and Bcl-2 (P<0.05). CONCLUSION:PF can up-regulate the expression of Bcl-2 and down-regulate the expression levels of caspase-9, caspase-3 and Bax via the activation of PI3K/Akt pathway, thereby inhibiting the nerve cell apoptosis and pro-tecting the nerve cells, so as to treat neurodegenerative diseases.