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 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.
3.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.
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.