1.Preparation and preliminary pharmacodynamic study of rectal suppository of low molecular weight heparin
Guangxi ZHAI ; Hengchang ZANG ; Yuanjun ZHONG
Chinese Journal of Biochemical Pharmaceutics 2001;22(3):119-120
Purpose The aim is to investigate the rectal suppository of low molecular weight heparin(LMWH).Methods The suppository was prepared by way of heating and fusion,the drug release property was studied with the release test in vitro and the absorption of LMWH into blood was tested by the changes of rabbits blood coagulation time. Results The drug release property in vitro followed Fick′s diffusion equation and LMWH could enter the blood through rectal medication. Conclusion The absorption from the rectum was another route of LMWH into the blood.
2.Virtual Screening of Histone Deacetylase Receptor Inhibitor among Lignanoid Compounds
Ke DI ; Huanhuan YU ; Yuanjun ZOU ; Rui DING ; Meng ZHONG ; Xiuying XU ; Yimin ZHENG
China Pharmacy 2016;(4):494-497
OBJECTIVE:To virtually screen lignanoid compounds with inhibitory effect of histone deacetylase(HDAC)by vir-tual screening method. METHODS:Using“lignanoid”as keyword,requiring CNKI,VIP,PubMed and other database,lignanoid compounds were collected as ligand to establish ligand base, histone deacetylase receptor HDAC2 (PDB code:4LXZ) and HDAC8 (PDB code:1T69) were selected from PDB database,and then ligands and 3D active site of receptors were docked by SYBYL-X 2.0 software. The affinity of receptors to ligand was reflected by total score. RESULTS:345 lignanoid compounds, 4LXZ and 1T69 primary ligand were used to establish ligand base which included 347 ligands. Ligands No.275,271,110,200, 056,258,181,129,037,270,187 were demonstrated good affinity with receptors HDAC2 and HDAC8. Ligands and receptors residue were docked via hydrogen bond. CONCLUSIONS:Lignanoid compounds have inhibitory effect on HDAC;virtual screen-ing method is effective in natural product activity prediction,which can provide quick access to and theoretical guidance for new pharmacological studies of lignanoid compounds.
3.The effect of chlamydiaphage phiCPG1 capsid protein Vp1 on the Chlamydia trachomatis
Yuanjun LIU ; Shu-ping HOU ; Jiu-rong WEI ; Yan LI ; Man-li QI ; Hui-ping WANG ; Quan-zhong LIU
Chinese Journal of Microbiology and Immunology 2012;32(5):403-407
Objective To investigate the effect of recombinant chlamydiaphage phiCPG1 capsid protein Vp1 on Chlamydia trachomatis(Ct) after Vp1 was co-cultured with Ct (reference strains and clinical strains).Methods The recombinant chlamydiaphage phiCPG1 capsid protein Vp1 was expressed and purified.Equal amount of Ct standard strains (E/UW-5/Cx and D/UW-3/Cx) or clinical strains,which had been incubated with Vp1 protein at the concentration of 53 μg/ml for 3 h at room temperature,were inoculated into McCoy.After cell culture,idione stain and transmission electron microscope were used to observe the effect of Vp1 on the Ct.The effect of Vp1 protein on the cell line McCoy was determined by MTT assay,the responses of Escherichia coli BL21 and DH5α toward Vp1 protein were determined using broth microdilution assays.Results Vp1 had obviously inhibitive effect on Ct,the inhibition ratios were about 40%-70%in clinical strains,72% in reference strain D and 78% in E,respectively.Abnormally enlarged RBs were observed after Vp1-treatment and Vp1 could arrest chlamydial developmental cycle using electron microscope.There was no effect of Vp1 on McCoy cells or bacteria BL21 or DH5α.Conclusion The recombinant Vp1 from phiCPG1 has obviously inhibitive effect on the growth of Ct,it will be helpful for the treatment of Ct infection in clinic.
4.Effect of cyclic RNA hsa-circ-0001360 on homocysteine-induced apoptosis of human umbilical vein endothelial cells
Yuanjun KUANG ; Sumei YU ; Yingyi ZHONG ; Xuhong ZHANG ; Shengchao MA ; Anning YANG ; Yinju HAO ; Jiantuan XIONG ; Yun JIAO ; Yideng JIANG
Chinese Journal of Tissue Engineering Research 2024;28(25):4060-4064
BACKGROUND:Increased homocysteine level induces apoptosis of human umbilical vein endothelial cells,but the mechanism remains unclear. OBJECTIVE:To investigate the role of hsa-circ-0001360 in human umbilical vein endothelial cell apoptosis induced by homocysteine. METHODS:In vitro cultured human umbilical vein endothelial cells were divided into control group,homocysteine group,interference control group,interference control + homocysteine group,hsa-circ-0001360 interference group,hsa-circ-0001360 + homocysteine interference group,overexpression control group,overexpression control + homocysteine group,hsa-circ-0001360 overexpression group and hsa-circ-0001360 + homocysteine overexpression group.All groups were treated with 100 μmol/L homocysteine.After 72 hours of intervention,the expressions of apoptosis-related proteins Bax,Bcl-2,and Caspase-3 were detected by western blot assay.The apoptotic rate was detected by flow cytometry.Quantitative real-time PCR was used to detect the expression of hsa-circ-0001360. RESULTS AND CONCLUSION:(1)Compared with the control group,the expression of Caspase-3 and Bax was significantly increased(P<0.01),and the expression of Bcl-2 was significantly decreased(P<0.01),and the apoptotic rate was significantly increased(P<0.01)in the homocysteine group.(2)Compared with control group,the expression of hsa-circ-0001360 was significantly increased in the homocysteine group(P<0.01).(3)The expression of hsa-circ-0001360 was significantly higher in the cytoplasm than that in the nucleus(P<0.01).(4)Compared with the interference control C group and interference control + homocysteine group,the expressions of Caspase-3 and Bax were significantly decreased(P<0.01),while the expression of Bcl-2 was significantly increased(P<0.01);the apoptotic rate was significantly decreased(P<0.01)in sh-hsa-circ-0001360 interference group and sh-hsa-circ-0001360 + homocysteine interference group.(5)Compared with overexpression control group and overexpression control + homocysteine group,the expressions of Caspase-3 and Bax were significantly increased(P<0.01),while the expression of Bcl-2 was significantly decreased(P<0.01);the apoptotic rate was significantly increased(P<0.01)in the hsa-circ-0001360 overexpression group and the hsa-circ-0001360 + homocysteine overexpression group.(6)In conclusion,hsa-circ-0001360 can promote the apoptosis of human umbilical vein endothelial cells induced by homocysteine.