3.Competitiveα-amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid receptor antagonists:research advances
Dian XIAO ; Lingxiao WANG ; Xinbo ZHOU ; Song LI
Journal of International Pharmaceutical Research 2014;(4):407-412
α-Amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) receptor, a subtype of ionotropic glutamate receptors widely distributed in the central nervous system, mediates the fast excitatory neurotransmission. Meanwhile more and more evidence indicates that AMPA receptor plays an important role in synaptic plasticity as well as central sensitization, and it also has close relationships with nervous system diseases. Over stimulation of AMPA receptor would produce excitotoxicity, leading to neuronal damage and finally resulting in a multitude of nervous system diseases, such as epilepsy, amyotrophic lateral scelerosis,Parkinson′s dis-ease. Competitive AMPA receptor antagonists that downregulate AMPA receptor′s function are of great importance in the prevention and treatment of nervous system diseases. This article reviews the research advances of competitive AMPA receptor antagonists.
4. Competitive α-amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid receptor antagonists: Research advances
Journal of International Pharmaceutical Research 2014;41(4):407-412
α-Amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) receptor, a subtype of ionotropie glutamate receptors widely distributed in the central nervous system,mediates the fast excitatory neurotransmission. Meanwhile more and more evidence indicates that AMPA receptor plays an important role in synaptic plasticity as well as central sensitization, and it also has close relationships with nervous system diseases. Over stimulation of AMPA receptor would produce excitotoxicity, leading to neuronal damage and finally resulting in a multitude of nervous system diseases,such as epilepsy, amyotrophic lateral scelerosis, Parkinson's dis-ease. Competitive AMPA receptor antagonists that downregulate AMPA receptor's function are of great importance in the prevention and treatment of nervous system diseases. This article reviews the research advances of competitive AMPA receptor antagonists.
5.Observation on effect of danxiaoling in supplementary treatment of intrahepatic cholestasis in pregnancy.
Dian-yun SHI ; Hua CHEN ; Mei XIAO
Chinese Journal of Integrated Traditional and Western Medicine 2002;22(2):116-118
OBJECTIVETo evaluate the curative effect of Danxiaoling Pill (DXLP), a Chinese herbal preparation, in treating intrahepatic cholestasis in pregnancy (ICP).
METHODSFifty-eight cases of ICP were divided randomly into two groups and treated by DXLP and Composite Yiganling as control respectively with the other identical conventional treatment. The changes of clinical symptoms, related laboratory parameters after treatment and the condition of labor were observed.
RESULTSThe total effective rate in both groups was 100%, but the markedly effective rate in the DXLP treated group was higher than that in control group (P < 0.01). Levels of blood cholyglycine acid (CGA), alanine transaminase (ALT), aspartate transaminase (AST), total bilirubin, total cholesterol and low density lipoprotein were all decreased in both groups after treatment, but DXL showed a better efficacy in decreasing CGA, ALT and AST than that of Yiganling. Moreover, the amniotic fluid meconium contaminated rate, premature delivery occurrence in the DXLP group were lower than those in the control group, while the weight of newborn baby was higher in the former than in the latter.
CONCLUSIONDXLP could effectively lower the serum bile acid and improve liver function in treating ICP.
Adult ; Alanine Transaminase ; blood ; Aspartate Aminotransferases ; blood ; Cholestasis, Intrahepatic ; blood ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Glycocholic Acid ; blood ; Humans ; Phytotherapy ; Pregnancy ; Pregnancy Complications ; blood ; drug therapy
6.Role of heat shock protein 47 on experimental diabetic nephropathy of rats.
Dian-ge LIU ; Qing-juan ZHANG ; Zhuang GONG ; Xiao-chun WU ; Yu-feng LÜ
Chinese Journal of Pathology 2007;36(9):627-628
Actins
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metabolism
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Animals
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Collagen Type III
;
metabolism
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Collagen Type IV
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metabolism
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Desmin
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metabolism
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Diabetes Mellitus, Experimental
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complications
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Diabetic Nephropathies
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metabolism
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pathology
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HSP47 Heat-Shock Proteins
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metabolism
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Kidney Glomerulus
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metabolism
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pathology
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Male
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Random Allocation
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Rats
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Rats, Sprague-Dawley
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Vimentin
;
metabolism
7.Study on effect of pH on rectum permeability of active ingredients in Reduning suppositories in vitro.
Ming YAN ; Ying-chun WEI ; Jin MENG ; Dian-hong XU ; Yun WU ; Wei XIAO
China Journal of Chinese Materia Medica 2015;40(8):1493-1496
OBJECTIVETo investigate the effect of different pH on rectum permeability of chlorogenic acid and geniposide.
METHODFour kinds of Reduning suppositories of different pH were separated and put into the rectum to study the suppositories in vitro and the content of chlorogenic acid and geniposide samples was determined by HPLC to calculate the permeation in 24 hours.
RESULTWith increase of pH within 2.5-7.4, the steady state flux of chlorogenic acid was increased, but the steady state flux of geniposidesamples was steady.
CONCLUSIONAdjusted the pH can increase the rectum permeability of active ingredients in Reduning auppositories.
Animals ; Chlorogenic Acid ; pharmacokinetics ; Drugs, Chinese Herbal ; pharmacokinetics ; Hydrogen-Ion Concentration ; Iridoids ; pharmacokinetics ; Male ; Permeability ; Rats ; Rats, Sprague-Dawley ; Rectum ; metabolism ; Suppositories ; pharmacokinetics
8.Effect of Buddleia flavonoids drug-containing plasma on the expression of STAT1 phosphoprotein in lacrimal gland epithelial cells in vitro
Fang, WANG ; Qing-Hua, PENG ; Xiao-Lei, YAO ; Quan-Long, WU ; Dian, LI
International Eye Science 2010;10(1):5-8
AIM: To explore the effect of Buddleia flavonoids drug-containing plasma and androgen receptor(AR) blocker on the expression of STAT1 phosphoprotein.METHODS: In vitro lacrimal gland epithelial cells were cultivated with H2O2 to establish the dry eye apoptosis state. Blank plasma group, Buddleia officinalis plasma total flavonoids interfere with drug-containing group, and the intervention group of testosterone propionate were set. The expressions of STAT1 phosphoprotein of each group were observed by Western blot and AR blocker flutamide was used to explore the intended androgen effect of Buddleia flavonoids.RESULTS: After the intervention of drug-containing plasma, the expression of STAT1 Phosphoprotein in Buddleja officinalis drug-containing plasma intervention group(0.353±0.494) and testosterone propionate intervention group(0.502±0.036) were enhanced and the differences between the two groups were significant (P<0.01). After using the AR blocker in all groups, the expression of STAT1 phosphoprotein in each group (0.268±0.061,0.283±0.106,0.213±0.071) had no difference.CONCLUSION: Buddleja officinalis drug-containing plasma total flavonoids can promote the expression of STAT1 phosphorylation.
9.Research expression of Slit3 and Robo4 in corneal neovascularization of rats
Shi-Yi, XIAO ; Li, WANG ; Ren-Dian, CHEN ; Jin, WU ; Yue-Li, ZHANG ; Li, HE
International Eye Science 2014;(7):1190-1192
AlM: To explore the roles of neuronal axon-guidance molecules Slit3 and Robo4 receptor in corneal neovascularization ( CNV ) by study their expression in neovascularized cornea of rats.
METHODS: CNV models were established by implantation pellets containing basic fibroblast growth factor ( bFGF ) into corneal stroma. CNV models were measured by biomicroscopy photography. lmmunohistochemical staining and imaging analysis system were used to detect the expression of Slit3 and Robo4 in the models after 1, 4, 7, 10 and 14d.
RESULTS:The area of CNV and the expression of Slit3, Robo4 were increased in CNV models compared to that in normal cornea and reached highest level on 7d. And the expression level of Slit3 and Robo4 were significantly correlated with the size of CNV on every time point except 1d (r=0. 84-0. 91, all P<0. 05).
CONCLUSlON: The expression of Slit3 and Robo4 may be related to the CNV development. They are potential therapeutical target for CNV.
10.A continuous-monitoring procedure of alkaline phosphatase activity with p-acetylphenylphosphace as substrate
Ling WANG ; Zhong-Xin LI ; Dian-Jun WEI ; Xiao-Qin DING ; Zong-Hua HU ; Hui JIN ;
Chinese Journal of Laboratory Medicine 2001;0(03):-
Objective To establish a new determination method for the measuring of alkaline phosphatase activity (ALP) with p-acetyl phenyl phosphace (PAP-PNa_2) as substrate.Methods With the help of Vital semiautomatic analyzer,researched a continuous-monitoring procedure and set up experimental parameters.Results When using this assay,the wavelength of PAP's absorption was 325 nm and the Km of ALP was 0.376 mmol/L.The molecular extinction coefficient of PAP at 340 nm was 23 390 L?mol~(-1)? cm~(-1) and the concentration of citrate buffer was 0.438 mol/L.During the process,we found that the optimum pH of enzyme was 10.4,and the concentration of substrate was 5.0 mmol/L.The time of linear reaction was 900 seconds,and the linear range was 0-1 110 U/L.Serum total ALP were 63.1-118.3 U/ L(male) and 52.5-89.0 U/L(female),based on results from 60 heath adults.Conclusions The method is practical in its repetition and convenience,saves time and is not liable to be affected by bilirubin in serum.It is especially suited to the use of automatic analyzers.