1.Solubilization Effect of Surfactant on Amphotericin B
Hong LIU ; Zaijun YU ; Ming LIU ; Yi ZHANG
China Pharmacy 1991;0(05):-
OBJECTIVE:To study the solubilization effect of different surfactant on amphotericin B.METHODS:Surfaceactive solution with series of concentrations were prepared by several agents including span-20,tween-40,tween-60,tween-80 and poloxamer 188 as non-ionic surfactant,hexadecyltrimethylammonium chloride (HTMAC) as cationic surfaceactive agent,sodium dodecyl benzene sulfonate (SDBS) and sodium deoxycholate as anionic surfaceactive agent,lecithin as bi-ionactiveagent.The solubilization effect of surfactant on amphotericin B was determined by UV spectrophotometry with maximum solubilization percentage as index.RESULTS:Maximum solubilization ratio in the range of 0.2~4.0 mg?mL-1 were as follows:1 365.44% for span-20 (4 mg?mL-1),353.46% for tween-40 (0.8 mg?mL-1),1 165.30% for tween-60 (4 mg?mL-1),973.46% for tween-80 (0.4 mg?mL-1),1 527.95% for poloxamer 188 (4 mg?mL-1),1 199.16% for sodium dodecyl benzene sulfonat (4 mg?mL-1),1 671.68% for hexadecyltrimethylammonium chloride (4 mg?mL-1),88.62% for sodium deoxycholate (4 mg?mL-1) and 314.36% for lecithin (4 mg?mL-1).CONCLUSIONS:Surfactant span-20,tween-60,tween-80,poloxamer 188,sodium dodecyl benzene sulfonat and hexadecyltrimethylammonium chloride have remarkable solubilization effect on amphotericin B.But tween-40,sodium deoxycholate and lecithin have unapparent solubilization effect on amphotericin B.
2.Effects and mechanisms of chloro-oxime derivatives on spatial learning and memory dysfunction in two dementia animal models
Xiaobing YU ; Qin WANG ; Kefan YANG ; Lixia FAN ; Zaijun ZHANG ; Yuqiang WANG ; Liang TAO
Chinese Pharmacological Bulletin 2014;(5):662-667
Aim To explore the effects and mecha-nisms of choro-oxime derivatives on spatial learning and memory impairment in Kunming mice and SD rats induced by scopolamine and Aβ1-42 , respectively. Methods 40 Kunming mice were randomly divided into 5 groups: control group, model group, donepezil treatment group, arimoclomol treatment group and TCO-2 treatment group. There were 8 mice in each group. Mice of control group were established by intra-peritoneal injection of saline, and mice of other groups were injected with scopolamine and caused memory im-pairment. Both control group and model group were treated with solvent by intraperitoneal administration;donepezil treatment group received donepezil by intra-gastric administration; arimoclomol treatment group and TCO-2 treatment group were given the correspond-ing drugs by abdominal injection, respectively. The solvent and drugs were given at the same time every morning for 8 days. Spatial learning and memory abili-ty were tested by Morris water maze from the fifth day of the drugs administration. 40 SD rats were divided into 5 groups the same as the dementia model men-tioned above. Mice of control group were established by intracerebroventricular injection of saline, and mice of other groups were injected with insoluble Aβ1-42 to be induced of memory impairment. Solvent and drugs were also delivered as mentioned above. Morris water maze was carried out from the fifth day of the drug de-livery. After that, acetyl cholinesterase activity of hip-pocampus was tested with acetyl cholinesterase reagent kit; the content of Aβ1-42 in hippocampus was meas-ured by ELISA assay kit;the expression of phosphoryl-ated tau proteins was detected by Western Blot. Re-sults In both two dementia models, choro-oxime de-rivatives could improve the spatial learning and memory ability, shorten the escape latency and increase the times of crossing the former platform. Choro-oxime de-rivatives could also inhibit the acetyl cholinesterase ac-tivity in animal brain, decrease the concentration of Aβ1-42 and the expression of phosphorylated tau pro-teins in the dementia rats’ hippocampus. Conclusions Spatial learning and memory deficits induced by sco-polamine and Aβ1-42 could be reversed by choro-oxime derivatives. It may be concerned with enhancement of the cholinergic system functions and reduction of the levels of Aβ1-42 and phosphorylated tau proteins in the brain.
3.Effects of new drug T-006 on improving learning and memory abilities in scopolamine-induced dementia Kunming mice
Qi SONG ; Qin WANG ; Weili WU ; Min SHAO ; Yu ZHANG ; Zaijun ZHANG ; Yuqiang WANG ; Liang TAO
Chinese Pharmacological Bulletin 2016;32(6):812-817
Aim ToexploretheeffectsofnewdrugT-006 on improving learning and memory abilities in scopolamine-induced dementia mice and its possible mechanism.Methods 72maleKunmingmicewere randomly divided into six groups:normal control group,model group,donepezil treatment group,T -006 treatment group with different doses(1,3 and 10 mg·kg-1 ).All mice were treated by intragastric ad-ministration for 14 consecutive days. Learning and memory abilities were tested by a five-day Morris water maze trial from the 1 1 th day.the first 4 days of the five-day Morris water maze,the navigation test was performed,the last day of Morris water maze is the spatial probe test.During the navigation test, mice were intraperitoneally given 2 mg · kg-1 scopolamine 20 minutes before entering the water,while normal control group mice administrated with sterile saline in-stead.Mice were not given T-006 nor scopolamine in spatial probe test.After Morris water maze,all mice were sacrificed for hippocampus and cortex.The activi-ties of AchE and SOD and the levels of GSH and MDA in hippocampus and cortex were measured after tissue harvesting.Results Comparedwithmodelgroup,T-006 could obviously improve learning and memory abil-ities in scopolamine-induced mice, significantly in-crease the levels of SOD and GSH and decrease the levelsofMDAandAchE.Conclusion T-006can significantly improve cognitive abilities in scopolamine-induced dementia mice,and its relevant mechanism may be closely related to its antioxidative effect and the ability to decrease AchE level.
4.Effect of rasagiline on neuroprotection and behavior improvement in MPTP-induced acute mouse model of Parkinson′s disease
Ruizuo YAN ; Baojian GUO ; Pei YU ; Zaijun ZHANG
Journal of China Pharmaceutical University 2016;47(5):603-608
This study aimed at investigating the neuroprotective effect and behavior improvement of rasagiline on 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine(MPTP)model mice of Parkinson′s disease. The tyrosine hydroxylase(TH)-positive dopaminergic neurons in substantia nigra were observed by immunocytochemistry. HPLC-ECD was used to detect the dopamine and its metabolite levels. Western blot was used to examine the protein expression of TH. The results showed that the mice appeared a series of acute behavior change after the injection of MPTP. Rasagiline(20 mg/kg)exerted significant protection against MPTP-induced loss of TH-positive dopaminergic neurons. The TH-positive neurons in rasagiline-treated mice brain increased significantly compared with those of MPTP-treated group. Rasagiline also enhanced dopamine and its metabolite levels in striatum significantly. In conclusion, rasagiline has protective effect on the acute mouse model of MPTP-induced Parkinsonism.
5.The clinical application of balloon dilation Eustachian tuboplasty in patients with Eustachian tube dysfunction
Ying ZHANG ; Ying SHI ; JinCheng ZHAO ; Xin MA ; ZhanHong JIA ; JingQiu ZHANG ; ZaiJun WU ; Yu WANG
Journal of Clinical Otorhinolaryngology Head and Neck Surgery 2016;30(8):649-652
Objective:To evaluate the clinical application of balloon dilation Eustachian tuboplasty (BET) in patients with Eustachian tube dysfunction (ETD). Method:Twenty-five patients who were diagnosed as ETD and reserved BET surgery were retrospectively analyzed in this study. Result:After 1-year's follow-up, among 25 ETD patients, the total cure rate was 55.9% and the effective rate was 85.3%. The cure rate and effective rate was 52.9% and 76.5% in the delayed opening of the ET group; 58.8% and 94.1% in the unopened group, which was higher than the other one. Conclusion:BET surgery is safe and effective in the treatment of BET patients.