Scavenger receptor CD36 could bind and endocytose oxLDL into macrophages which were then differentiated into foam cells that constitute the atherosclerotic lesion core, and was considered to be a potential target to treat atherosclerosis. In the establishment of the compound library of berberine (BBR, 1) analogues, we discovered that 13-hexylberberine (2) showed an antagonistic activity against CD36. Taking 2 as the lead compound, 21 derivatives were synthesized and their antagonistic activities were evaluated via an ELISA-like high-throughput screening (HTS) model. The primary structure-activity relationships were studied. It was indicated that the introduction of suitable groups at the 2- and 3-position of the aromatic ring A or at the 9-position of the aromatic ring D could enhance the activity. Among the 21 studied compounds, 7g bearing a benzyloxyl group at the 9-position provided a highest CD36 antagonistic activity with the IC50 value of 7.7 micromol L(-1). Besides, its antagonistic activity was further verified with Sf9 insect cell HTS model. So berberine analogues are a new family of CD36 receptor antagonists and worthy to be studied further.

Objective To explore the protective effects of dipeptidyl peptidase-4 inhibitor (DPP-4I) on AD-like neurodegenerative changes and its mechanism. Methods The human neuroblastoma cell line SH-SY5Y on the logarithmic phase was divided into six groups:control group (CON group, treated with PBS contained 1‰DMSO for 12 h), wortmannin intervention group (W group, treated with 0.03 μmol/L wortmannin for 12 h), DPP-4I intervention group (DPP-4I group, treated with 10μmol/L DPP-4I for 12 h), both DPP-4I and wortmannin intervention group (DPP-4I+W group, pre-treated with 10 μmol/L DPP-4I for 2 h, then 0.03 μmol/L wortmannin for 12 h), DPP-4I, wortmannin and Ex9-39 intervention group (DPP-4I+W+Ex9-39 group, pre-treated with 10μmol/L Ex9-39 for 2 h, then 10μmol/L DPP-4I for 2 h followed by 0.03μmol/L wortmannin for 12 h), and Ex9-39 intervention group (Ex9-39 group, treated with 10μmol/L Ex9-39 for 12 h). MTT assay was used to detect the cell vitality. Western blot assay was used to detect the level of total tau protein (tau-5) and phosphorylated tau at different sites (pSpS199/202, pT231 and pS396), the level of phosphorylated neurofilaments (NF-H, NF-M) and phosphorylation of critical enzyme in PI3K/Akt/GSK-3β signaling pathway. Results (1) The cell vitality decreased, the levels of pSpS199/202, pT231, pS396 and NF-H/M increased significantly in W group than those in CON group. However, comparing with CON group, the above mentioned parameters reversed in DPP-4I group. Comparing with W group, the cell vitality increased and phosphorylated levels of above mentioned indices were decreased in DPP-4I+W group. (2) The cell vitality showed a decline trend while the levels of phosphorylation tau at three different sites and NF-H/M were higher in Ex9-39 group than those in CON group. Comparing with DPP-4I+W group, the results of the phosphorylated levels showed the same changes in DPP-4I+W+Ex9-39 group. (3) Comparing with CON group, the expression levels of phosphorylated PI3K, Akt and GSK3β increased significantly in DPP-4I group, while those decreased in W group. Additionally, the expression levels of phosphorylated PI3K, Akt and GSK3β were significantly increased in DPP-4I+W group than those in W group. Conclusion DPP-4I can enhance the level of GLP-1 and activate PI3K/Akt/GSK-3βinsulin signaling pathway to improve the hyperphosphorylated tau and NFs induced by wortmannin, and to protect AD-like neurodegeneration.

Objective To investigate the staphylococcal chromosomal cassette mec (SCCmec)genotypes and molecular epidemi-ology of hospital-acquired MRSA.Methods A total of 26 non-duplicate MRSA isolates with the same resistant pattern were studied.SCCmec genotyping was analyzed by multiplex PCR.Repetitive element polymerase chain reaction (Rep-PCR)tech-nique was used to analyze the homology between these strains based on the DiversiLab system.Results The most common geno-type of these MRSA strains was SCCmec-III (84.6%).Two strains belonged to SCCmec-II and 1 SCCmec-IV.SCCmec-I strain was not identified.Based on the results of DiversiLab analysis,these MRSA strains were classified into 10 groups.The genetic similarity ranged from 40% to 100% among these SCCmec types.The two strains of SCCmec-II belonged to the same subtype.The similarity coefficient was higher than 90% for one strain of SCCmec-III subtype 1.The 4 strains of SCCmec-III subtype 3 were grouped into the same set with a similarity coefficient of > 95%.The MRSA strains of SCCmec-III subtype 2 was divided into 5 groups (similarity co-efficient > 90%).Conclusions SCCmec-III is the major genotype of MRSA isolates in our hospital.MRSA strains may spread in some wards.Clinicians and infection control department should pay close attention to this issue.

OBJECTIVETo study the relation between the content of 5-hydroxymethyl-furfural (5-HMF) and the degree of floating sugar in root of Achyranthes bidentata.

METHODAn HPLC method was applied with a Waters Symmetry C18 3.9 mm x 150 mm (5 microm) column by using methanol-water (12:88) as the mobile phase at a flow rate of 1.0 mL x min(-1) and a UV detection of 280 nm.

RESULTAlong with the degree's deepening of floating sugar, the content of 5-HMF varied with the different shades of the sample. The content was 10 times higher in the black sample (highest degree of flowing suger) than that in the yellowish sample (normal). The concentrations of 5-HMT in five yellowish samples of roots of A. bidentata were 0.162 mg x g(-1) to 0.332 mg x g(-1).

CONCLUSIONThe content increasing of 5-HMF in the root of A. bidentata was related to the degree of flowing sugar.

Achyranthes ; chemistry ; Carbohydrates ; analysis ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; analysis ; Furaldehyde ; analysis ; Plant Roots ; chemistry

Objective To comprehensively characterize the diterpene alkaloids in Radix Aconiti Kusnezoffii.Methods The diterpene alkaloids were isolated and purified by strong acid cation exchange resin solid phase extraction column(SCX-SPE),and identified by ultra high performance liquid chromatography-Q-Exactive Orbitrap mass spectrometry(UHPLC-Q-Exactive Orbitrap MS).Results A total of 99 diterpene alkaloids were identified from Radix Aconiti Kusnezoffii,including 27 diester diterpene alkaloids(DDA),29 monoester diterpene alkaloids(MDA),40 amide diterpene alkaloids(ADA),2 polyester diterpene alkaloids(PDA)and 1 long-chain ester diterpene alkaloid(LDA).Conclusion The SCX-SPE combined with UHPLC-Q-Exactive Orbitrap MS method,established in this paper,can rapidly identify a large number of diterpene alkaloids in Radix Aconiti Kusnezoffii,which provides scientific proof for the study of pharmacodynamic substance basis and quality control of Radix Aconiti Kusnezoffii.

OBJECTIVETo evaluate the restoration of function after spinal cord injury (SCI) in patients of different ages who have underwent intraspinal transplantation of olfactory ensheathing cells (OECs).

METHODSOne hundred and seventy-one SCI patients were included in this study. Of them, 139 were male and 32 were female, with age ranging from 2 to 64 years (mean, 34.9 years). In all SCI patients the lesions were injected at the time of operation with OECs. According to their ages, the patients were divided into 5 groups: 51 years group (n = 14). The spinal cord function was assessed based on the American Spinal Injury Association (ASIA) Classification System before and 2 - 8 weeks after OECs transplantation. One-way ANOVA and q test were used for statistical analysis, and the data were expressed as mean +/- SD.

RESULTSAfter surgery, the motor scores increased by 5.2 +/- 4.8, 8.6 +/- 8.0, 8.3 +/- 8.8, 5.7 +/- 7.3 and 8.2 +/- 7.6 in 5 age groups respectively (F = 1.009, P = 0.404); light touch scores increased by 13.9 +/- 8.1, 15.5 +/- 14.3, 12.0 +/- 14.4, 14.1 +/- 18.5 and 24.8 +/- 25.3 respectively (F = 1.837, P = 0.124); and pin prick scores increased by 11.1 +/- 7.9, 17.2 +/- 14.3, 13.2 +/- 11.8, 13.6 +/- 13.9 and 25.4 +/- 24.3 respectively (F = 2.651, P = 0.035). Restoration of pin prick in > 51 years group was better than other age groups except 21 - 30 years group.

CONCLUSIONOECs transplantation can improve the neurological function of spinal cord of SCI patients regardless of their ages. Further research into the long-term outcomes of the treatment will be required.

Adolescent ; Adult ; Age Factors ; Child ; Child, Preschool ; Female ; Humans ; Male ; Middle Aged ; Olfactory Bulb ; cytology ; transplantation ; Spinal Cord ; physiology ; Spinal Cord Injuries ; surgery ; Treatment Outcome