Herba Hedyotis Diffusae has many kinds of pharmacological activities such as anti-tumor, antioxidant, immune regulation and so on. This article collected and reported the related literature at home and abroad in recent years, found that pharmacological active ingredients of Herba Hedyotis Diffusae show consistency of polysaccharides and flavonoids to varying degrees, and summarized the pharmacological effects and extraction and purification process. The author believed that, the study about Herba Hedyotis Diffusae has made relatively great achievements, but the research mainly focused on polysaccharides or flavonoids, and efficacy of Herba Hedyotis Diffusae was not in enough in-depth exploration. The indicator of extraction and purification process is relatively single. This study estimated the mechanism of Herba Hedyotis Diffusae from the aspects of absorption and metabolism of intestinal flora and relationship between medicine structure and exert efficacy, hoping to optimize the extracting processes by multiple indexes, and provided references for further exploitation and utilization of Herba Hedyotis Diffusae.

Objective:To explore the main economic and social factors influencing human health. Methods:By using the partial least squares(PLS) method and the panel data from areas of China in 2011, regression model related with economic social factors and human life expectancy was built. Results: Per capital GDP, the proportion of the tertiary industry, the number of people beyond college diploma per million people and the number of health technical personnel per 1 000 people has inverse relationshop with life expectancy;the proportion of medical costs accounted for fiscal expenditure, the ratio of fiscal deficit, rate of unemployment and Gini coefficient have reverse relationshop with life expectancy. Conclusion: To improve the level of human health, it needs to take comprehensive measures.

Objective: To explore the impact of regional economy on structure of total health expenditure. Methods: According to the panel data of China from 2002 to 2011, the partial least-squares regression method was used to build the relationship model of regional economy and total health expenditure construction. Results: Per capital GDP, the proportion of the tertiary industry, financial revenue per capita and urban residents disposable income have negative correlation with resident individual health expenditure, while the Engel coefficient has positive relationship with them. Conclusion: Optimizing industrial structure and raising the income of residents are the key factors of optimizing the structure of total health expenditure.

Objective:To investigate the influence of Prunus tomentosa thunb total flavonoids (PTTTF) in the inflammatory factors in the lipopolysaccharide(LPS)-induced cellular inflammation model, and to clarify its mechanism. Methods:The cellular inflammation models of the RAW264.7 cells and human neutrophils (PMN) induced by LPS were established. The cells were divided into control group, model group, dexamethasone group (DXM), and different doses (0.4,4.0, and 40.0 mg·L-1) of PTTTF groups. The expression levels of inflammatory factors including interleukin-1β(IL-1β), interleukin-6(IL-6), inducible nitric oxide synthase(iNOS),tumor necrosis factor-α(TNF-α) and high mobility group protein B1(HMGB1)mRNA in the RAW264.7 cells were detected by RT-PCR. The expression levels of NF-κB, and signal pathway key molecules ERK1/2 and p-JNK proteins in the RAW264.7 cells were determined by Western blotting method. Flow cytometry was used to detect the percentages of RAW264.7 cells in different cell cycles and the apoptotic rates of PMN. Results:Compared with control group, the expression levels of IL-1β, IL-6, iNOS, TNF-α, and HMGB1 mRNA in the RAW264.7 cells in model group were significantly increased (P<0.05 or P<0.01),and the expression levels of NF-κB,ERK1/2, and p-JNK proteins were also significantly increased (P<0.01);the percentage of RAW264.7 cells in S phase was increased (P<0.05);the apoptotic rate of PMN was significantly decreased (P<0.05). Compared with model group,the expression levels of IL-1β, iNOS, TNF-α, and HMGB1 mRNA in the RAW264.7 cells in 4.0 and 40.0 mg·L-1 PTTTF groups and DXM group were significantly decreased(P<0.05 or P<0.01), the expression levels of NF-κB,ERK1/2, and p-JNK proteins were significantly decreased(P<0.05), and the percentages of RAW264.7 cells in S phase were significantly decreased (P<0.05 or P<0.01); the apoptotic rates of PMN were increased(P<0.05 or P<0.01). Conclusion:PTTTF can down-regulate the expression levels of inflammatory factors in the RAW264.7 cell inflammation models induced by LPS. This effect may be related to decreasing the percentage of inflammatory cells in S phase, promoting the apoptosis, and down-regulating the expressions of NF-κB, ERK1/2, and p-JNK proteins.

Career Mobility ; China ; Humans ; Occupational Health Services ; statistics & numerical data ; Sampling Studies

Objective To optimize the synthesis process of iloperidone 1 for industrial production.Methods Piperi-dine-4-carboxylic acid, acetic acid and acetic anhydride were used as starting materials to generate 2 via amidation, Friedel-Crafts acylation, hydration, oximation, intramolecular cyclization and salification.Compound 2 was treated with 4-(3-chloropropoxy)-3-methoxyphenylethanone through condensation to afford iloperidone.The target compound 1 was prepared with an overall yield of 34.9%.Results and Conclusion Such factors as the ratio of the raw materials, the catalyst, reactive time were investigated and optimized to make the reaction conditions mild and easy to control with less side effects.The structure has been confirmed by IR, 1 H-NMR and MS.

This study was aimed to observe the clinical effect of nerve root cervical spondylosis treatment by muscle meridian manipulation with small-angle sagittal localized rotational pulling of the neck . A total of 60 cases of nerve root cervical spondylosis were randomly divided into two groups , which are the treatment group (by muscle meridian manipulation with small-angle sagittal localized rotational pulling of the neck) and the control group ( by tendon-soothing manipulation ) . The results showed that there were significant differences ( P< 0 . 01 ) in the comparison of cure rate after treatment . The total efficiency of the treatment group was 93 . 33%, and the control group was 70 . 00%. The treatment group showed better clinical effect with significant difference ( P < 0 . 05 ) . It was concluded that the application of muscle meridian manipulation with small-angle sagittal localized rotational pulling of the neck is maneuverable and time-saving in the treatment of cervical spondylosis . It has a remarkable therapeutic effect and is suitable for clinical application .

CB2-selective agonists have drawn attention in drug discovery, since CB2 becomes a promising target for the treatment of neuropathic pain without psychoactive or other CNS-related side effects. However, the lack of experimental data of the 3D structures of human cannabinoid receptors hampers the understanding of the binding modes between ligands and CB2 by traditional methods. In the present work, combinational molecular modeling studies including flexible docking, MD simulations and free energy calculations were performed to investigate the interaction modes and mechanism of CB2-unselective agonist CP55940 and CB2-selective agonist GW842166X, separately binding with the homology model of CB2 in a DPPC/TIP3P simulated membrane environment. The binding free energies calculated by MM-PBSA method give an explanation for the activity differences of the studied ligands. Binding free energies decomposition by MM-GBSA method shows that the van der Waals interaction is the dominant driving force during the binding process. Our MD simulations demonstrate that Phe197 could be a critical residue for the binding of CB2-selective agonists. Furthermore, by using the MD simulated binding conformer as a template, the 3D-QSAR studies were performed with the comparative molecular field analysis (CoMFA) approach on a set of GW842166X analogues. A combinational exploration of both CoMFA steric and potential contour maps for CB2 affinities and the MD studied interaction modes sheds light on the structural requirements for CB2 agonists and serves as a basis for the design of novel CB2 agonists.

Objective To study and compare the metabolism of Hedyotis diffusa flavonoid extract in intestinal flora from human, normal rats and pseudo germ-free rats in vitro. Methods Intestinal flora of human, normal rats and pseudo germ-free rats were incubated with Hedyotis diffusa extract, rutosid, isoquercitrin and quercitrin under anaerobic conditions at 37℃.High-performance liquid chromatography with diode-array detection ( HPLC-DAD ) was used for the analysis of components and metabolic products.The trends of metabolic transformation of the various components were analyzed according to the changes in chromatographic peak areas at different incubation time points. Results The components of Hedyotis diffusa extract and its monomer were quickly metabolized by human and normal rat intestinal flora and the main metabolite was quercetin.However, they were hardly metabolized by intestinal flora from pseudo germ-free rats. The metabolism effect of intestinal flora was weaker on components than on the corresponding monomers. Conclusion By comparing flavonoids metabolism in intestinal flora from human, normal rats and pseudo germ-free rats, the important role of intestinal microflora in the metabolism of flavonoids is further confirmed.

Objective To synthesize Wye-125132,an inhibitor of mTOR,and to establish a synthetic route for industrial production.Methods Barbituric acid was used as the raw material to synthesize the intermediate 2, 4, 6-trichrolo-pyrimidine-5-carbaldehyde 2 via Vilsmeier-Haack and chlorination reaction, while intermediate 5 was prepared via 3-step reaction from 1,4-dioxaspiro-[4,5]decan-8-one.The condensation of 2 and 5 was followed by substitution reaction to obtain the key intermediate 7.The side chain 9 was prepared by 3-step reaction from bromine aniline.Then the title product 1 was obtained with the reaction of Suzuki cross-coupling of 7 and 9.The structures of intermediate and target compounds were confirmed by MS and 1 H-NMR.Results and Conclusion Compared with the method reported in the literature,this new synthesis method possesses some advantages, such as ready availablity of raw materials, simple operation, mild reaction conditions and easy disposal of products.The total yield is 13.2%,and the purity of the target compound is 99.77%.