Fifteen known compounds were isolated from Swertia delavayi by silica gel, Sephadex LH-20 and Rp-18 column chromatographies. Based on extensive spectroscopic analysis (MS, 1H, 13C-NMR), their structures were identified aserythrocentaurin (1), erythrocentaurindimethylacetal (2), sweroside (3), swertiamarin (4), gentiopicroside (5), swertiakoside A (6), 2'-O-acetylswertiamarin (7), 4'-O-[(Z) -coumaroyl] swertiamarin (8), 1,5,8-trihydroxy-3-methoxyxanthone (9), 8-O-β-D-glucopyranosyl-1-hydroxy-2,3, 5-trimethoxyxanthone (10), 8-O-[β-D-xyl- opyranosyl-(1 --> 6)-β-D-glucopyranosyl]-7,8-dihydroxy-3-methoxyxanthone (11), isovitexin (12), β-sitosterol (13), daucosterol (14), and oleanolic acid (15). Among them, ten ones (14, 7-11, 13) were obtained from S. delavayi for the first time. The isolates were evaluated for their anti-HBV activities in HepG 2. 2. 15 cell line in vitro. The results showed that compound 1, 2, 6, 7, 9 and 12 exhibited significant inhibitory activity on HBV DNA replication with IC50 values from 0.05 to 1.46 mmol x L(-1).
Antiviral Agents ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Hepatitis B virus ; drug effects ; genetics ; Magnetic Resonance Imaging ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Swertia ; chemistry

Objective To study the effects of ribosomal protein L41 (RPL41) on the proliferation and apoptosis of human retinoblastoma Y79 cells and its underlying mechanisms.Methods Y79 cells were seeded in RPMI 1640 medium containing 10％ fetal bovine serum for passage culture.Then the cells were divided into control group,with cells left untreatment,(40 μmol · L-1,80 μmol · L 1 and 120 μmol · L-1) RPL41 treatment group according to the concentration.Next CellTiter-Glo fluorescence cell viability testing system was used to observe the viability of Y79 cells in all groups,and flow cytometry was applied to measure the cell apoptotic rate in 100 μmol · L 1 RPL41 treatment group,with Hoechst staining for the observation of nuclear morphometry of apoptotic cells,and finally,Western blot was used to determine the expression of activating transcription factor 4 (ATF4) of each group.Results Compared with the control group,the viability of Y79 cells in the 40 μmol · L-1 RPL41 treatment group was (97.9 ± 1.5) ％,with no significant difference (P =0.055);and the viability in the 80 μmol · L-1 and 120 μmol · L-1 RPL41 treatment group was (87.6 ± 1.8)％ and (63.9 ± 2.0) ％,respectively,both of which were significantly different from the control group (both P ＜ 0.05),so RPL41 inhibited the viability of Y79 cells,and 100 μmol · L-1 RPL41 promoted the apoptosis of Y79 cells,with the apoptotic rate of (17.33 ± 2.47)％.Compared with normal cells,the apoptotic cells in the 100 μmol · L 1 RPL41 treatment group showed bright color and smaller cell volume by Hoechst staining.Western blot showed that PRL41 significantly decreased the expression of ATF4 protein and the expression of ATF4 protein in the 40 μmol · L 1,80 μmol · L-1 and 120 μmol · L 1 treatment group were 0.76 ± 0.04,0.29 ± 0.04,0.29 ± 0.05,respectively,all of which were significantly different from the control group (all P ＜ 0.01).Conclusion RPL41 can inhibit the proliferation and promote the apoptosis of human retinoblastoma Y79 cell,and its mechanism may be related to the expression of ATF4.

Neurodegenerative disease is common and frequently occurs in elderly patients. Previous studies have shown that ginsenoside Rg1 was able to inhibit senescent of brain, but the mechanism on the brain during the treatment remains elucidated. To study the mechanism of ginsenoside Rg1 in the process of anti-aging of brain, forty male SD rats were randomly divided into normal group, Rg1 normal group, brain aging model group and Rg1 brain aging model group, each group with 10 rats (brain aging model group: subcutaneous injection of D-galactose (120 mg kg(-1)), qd for 42 consecutive days; Rg1 brain aging model group: while copying the same test as that of brain aging model group, begin intraperitoneal injection of ginsenosides Rg1 (20 mg x kg(-1)) qd for 27 d from 16 d. Rg1 normal group: subcutaneous injection of the same amount of saline; begin intraperitoneal injection of ginsenosides Rg1 (20 mg x kg(-1)) qd for 27 d from 16 d. Normal: injected with an equal volume of saline within the same time. Perform the related experiment on the second day after finishing copying the model or the completion of the first two days of drug injections). Learning and memory abilities were measured by Morris water maze. The number of senescent cells was detected by SA-beta-Gal staining while the level of IL-1 and IL-6 proinflammatory cytokines in hippocampus were detected by ELISA. The activities of SOD, contents of GSH in hippo- campus were quantified by chromatometry. The change of telomerase activities and telomerase length were performed by TRAP-PCR and southern blotting assay, respectively. It is pointed that, in brain aging model group, the spatial learning and memory capacities were weaken, SA-beta-Gal positive granules increased in section of brain tissue, the activity of antioxidant enzyme SOD and the contents of GSH decreased in hippocampus, the level of IL-1 and IL-6 increased in hippocampus, while the length of telomere and the activity of telomerase decreased in hippocampus. Rats of Rg1 brain aging group had their spatial learning and memory capacities enhanced, SA-beta-Gal positive granules in section of brain tissue decreased, the activity of antioxidant enzyme SOD and the contents of GSH increased in hippocampus, the level of IL-1 and IL-6 in hippocampus decreased, the length contraction of telomere suppressed while the change of telomerase activity increased in hippocampus. Compared with that of normal group, the spatial learning and memory capacities were enhanced in Rg1 normal group, SA-beta-Gal positive granules in section of brain tissue decreased in Rg1 normal group, the level of IL-1 and IL-6 in hippocampus decreased in Rg1 normal group. The results indicated that improvement of antioxidant ability, regulating the level of proinflammatory cytokines and regulation of telomerase system may be the underlying anti-aging mechanism of Ginsenoside Rg1.
Aging ; drug effects ; Animals ; Brain ; drug effects ; Ginsenosides ; pharmacology ; Male ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo evaluate the effect of comprehensive control strategy of schistosomiasis with emphasis on infection source control in Anhui province.

METHODSForty endemic villages in Guichi district, Chizhou city, Anhui province were selected as national pilot villages in the years from 2006 to 2008, and another 10 provincial pilot villages were respectively selected from 10 highly endemic villages in 7 cities in 2007. The comprehensive infection source control measures, including "replace cattle with machines", "raise livestock in pens", "improve the sanitary toilets", "supply safe water " and so on were carried out among the above pilot villages. At the end of 2008, 13 national pilot villages and 6 provincial pilot villages were selected to investigate the popularity of schistosomiasis, and the effect of the comprehensive control strategy in those villages were compared.

RESULTSAfter implementing the comprehensive control strategy, the infectious rate of schistosomiasis in national pilot villages decreased from 4.57% (487/10 659) to 1.76% (147/8370), with the reduction rate at 61.49%, whose difference showed statistical significance (χ(2) = 115.16, P < 0.01); and the density of infected snails decreased from 0.0067/0.1 m(2) to 0.0008/0.1 m(2), the infectious rate of snails decreased from 0.28% to 0.04%, whose reduction rates were 88.06% and 85.71% respectively. While as to the provincial pilot villages, the infectious rate of schistosomiasis decreased from 1.27% (54/4254) to 0.21% (14/6592), with the reduction rate at 83.46%, whose difference showed statistical significance (χ(2) = 94.57, P < 0.01); and the density of infected snails decreased from 0.0025/0.1 m(2) to 0.0003/0.1 m(2), the infection rate of snails decreased from 0.13% to 0.05%, whose reduction rates were 88.00% and 61.54% respectively.

CONCLUSIONThe comprehensive control strategy with emphasis on infection source control implemented in marshland and lake regions can effectively control the transmission of schistosomiasis.

Animals ; China ; epidemiology ; Disease Reservoirs ; parasitology ; Humans ; Infection Control ; methods ; Livestock ; Pilot Projects ; Rural Health ; Schistosomiasis ; epidemiology ; parasitology ; prevention & control ; Snails ; parasitology

Objective To explore the correlation between the level of serum homocysteine (Hcy) and the thickness of retinal ganglion cell layer (GCL) on optical coherence tomography (OCT) in patients with type 2 diabetes.Methods Totally 60 diabetic patients were collected from October 2016 to October 2017 in the Shengjing Hospital of China Medical University,and they were divided into two groups:diabetic patients without retinopathy (NDR group,n =30) and non-proliferative diabetic retinopathy group (NPDR group,n =30) according to the ETDRS classification,and meanwhile additional 30 healthy subjects were enrolled as control group.The level of serum Hcy was detected,and the retinal GCL thickness was measure using OCT in all patients for the analysis of the correlation of serum Hcy level with the thickness of GCL.Results The serum Hcy level was (11.87 ± 2.19) nmol · L-1 in the control group,(14.87 ± 0.42)nmol · L-1 in the NDR group and (20.77 ± 2.40) nmol · L-1 in the NPDR group,which was significantly increased gradually,and the difference was statistically significant (P =0.000),but the thickness of GCL was (88.33 ± 6.36) μm,(81.73 ± 1.41) μm and (64.00 ± 12.73) μm in the three groups,accordingly,which was decreased significantly gradually,with statistically significant difference (P =0.000).Along with the progress of fundus lesions,the level of serum Hcy increased,but the thickness of GCL decreased,and there was a significant negative correlation of the serum Hcy level with the thickness of GCL in the retina by Pearson (r =-0.908,P =0.000).Conclusion The increase of serum Hcy level in diabetic patients is associated with the decrease of retinal GCL thickness,and Hcy is involved in neurodegenerative changes in patients with diabetic retinopathy.

OBJECTIVETo analyze the distribution of trimethylamine N-oxide (TMAO) in healthy adults with different risk factors and explore its association with gut microbiota.

METHODSWe collected fasting blood samples and fresh fecal samples from 181 subjects without atherogenesis in the carotid arteries. Plasma TMAO levels of the subjects were determined using stable isotope dilution liquid chromatography-tandem mass spectrometry (LC-MS). The fecal DNA was extracted, and the 16S rRNA V4 tags were amplified and sequenced by Illumina HiSeq 2000. The association between TMAO and classical cardiovascular risk factors were analyzed. Gut microbial community structure was analyzed with QIIME, and LEfSe was used to identify the biomarkers.

RESULTSThe median (IQR) TMAO level was 2.66 (1.96-4.91) µmol/L in the subjects. TMAO level was significantly correlated with body mass index and operational taxonomic units (OTU). Individuals with high TMAO levels were found to have abundant Clostridiales, Phascolarctobacterium, Oscillibacter, and Alistipes but less abundant Anaerosprobacter.

CONCLUSIONChinese subjects have in general low levels of TMAO. TMAO levels are not significantly correlated with the classical cardiovascular risk factors or the gut microbial structures.

Adult ; Atherosclerosis ; Bacteria ; isolation & purification ; Biomarkers ; blood ; Cardiovascular Diseases ; blood ; Chromatography, Liquid ; Gastrointestinal Microbiome ; Humans ; Methylamines ; blood ; RNA, Ribosomal, 16S ; isolation & purification ; Risk Factors ; Tandem Mass Spectrometry

OBJECTIVETo provide scientific basis data for revising the national hygiene criteria of "Classification of hazard conditions of productive dust" (GB5817-86).

METHODSThe data of the retrospective study and the field survey data were analyzed with correlation and regression analysis. The product of total dust concentration of respiratory exposure (mg/m(3)), total ventilation during exposure (m(3)/d per psrson), and level of free SiO(2) in dust (%) was the respiratory exposure dose of free SiO(2) (mg per day per person) which was used as dose criteria value of classification of hazard degree of dust.

RESULTSUsing free SiO(2) exposure dose and the dose-effect relationship, the hazard degrees of the dust were divided into 5 grades: 0, I, II, III, IV (0 - 8.0, 8.1 - 12.0, 12.1 - 16.0, > 24.1 mg per day per person).

CONCLUSIONThe exposure dose of free SiO(2) is closely related to the pathogenesis of silicosis. Using the exposure dose of free SiO(2) as the classification indicator of hazard degree of dust is reliable, simple and easy to execute.

China ; Dust ; analysis ; Hazardous Substances ; analysis ; Humans ; Lung ; diagnostic imaging ; pathology ; Occupational Exposure ; standards ; Radiography ; Retrospective Studies ; Safety Management ; standards

OBJECTIVETo assess the efficacy and safety of three different Chinese medical principles in treating patients with male infertility (oligospermia/asthenozoospermia).

METHODSTotally 128 patients with male infertility were classified into 3 groups, i.e., Shen-essence deficiency syndrome, Pi-Shen deficiency syndrome, Shen-deficiency blood-stasis syndrome. They were assigned to the Chinese medical treatment group (96 cases) and the Western medical treatment group (32 cases) by stratified randomization in the ratio of 3: 1. Those in the Chinese medical treatment group were treated with Chinese drugs for Shen invigorating and blood activating, Shen invigorating and Pi supplementing, Shen-qi benefiting. Those in the Western medical treatment group were treated with Clomifene (at the daily dose of 25 mg per day, once daily). Three months consisted of one therapeutic course. The parameters of semen, the pregnancy rate, and adverse reactions were observed.

RESULTSTotally 24 patients dropped out in the two group, 17 in the Chinese medical treatment group (9 patients of Shen deficiency blood stasis syndrome, 5 of Shen-Pi deficiency syndrome, and 3 of Shen-essence deficiency syndrome) and 7 in the Western medical treatment group. Compared with before treatment, there was no statistical difference in the improvement of semen amount at 3 months after treatment between the two groups (P > 0.05). There was statistical difference in the improvement of semen density, class A semen, class A +B semen, and 1-h activity ratio (P < 0.05). The improvement was most obvious in Shen deficiency blood stasis syndrome, followed by Shen-Pi deficiency syndrome and Shen-essence deficiency syndrome. The improvement was the weakest in the Western medical treatment group. There was no statistical difference in the improvement of semen amount, semen density, class A semen, or 1-h activity ratio at 3 months after treatment between the two groups (P > 0.05). Best effect was obtained in improving class A + B semen quality in patients of Shen deficiency blood stasis syndrome, showing statistical difference when compared with the other two syndrome types and the Western medical treatment group (P < 0.05, P < 0.01). No obvious adverse reaction occurred in the two groups during the treatment course.

CONCLUSIONShen invigorating and blood activating method could improve the semen density and semen activities, and it was superior to other therapeutic methods.

Adult ; Asthenozoospermia ; classification ; therapy ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Male ; Medicine, Chinese Traditional ; methods ; Oligospermia ; classification ; therapy ; Phytotherapy ; methods ; Semen Analysis ; Young Adult

OBJECTIVETo evaluate the safety and reliability of cyclosporine microemulsion (CsA-ME) C(2) monitoring and to determine the target level of C(2) in Chinese adult liver transplant recipients.

METHODS53 Chinese adult liver transplant recipients were randomly divided into three groups (group C(0), n = 17; group high level C(2), n = 18; group low level C(2), n = 18). Blood chemistry reflecting heart, liver and renal function and CsA level were examined at certain interval during follow-up. The change of immune status and episodes of rejection were also observed closely.

RESULTSThe group low level C(2) had the lowest CsA oral dose (2.51 +/- 0.37 mg/kg/d), and had significant difference compared with the other groups (P < 0.01). The best liver, heart and renal function was observed in group low level C(2). The CD(4)(+)/CD(8)(+) ratio of group low level C(2) was 1.04 +/- 0.68, which had no significant difference with C(0) group. The rejection incidence of the three groups had no significant difference. group low level C(2) had highest clinical benefit ratio (72.22%), while the clinical benefit of group high level C(2) is the lowest (11.11%).

CONCLUSIONSWith rational target level, C(2) monitoring can show us the proper oral dose of CsA which can decrease the side effects remarkably without rejection episodes increasing. The target level of C(2) in Chinese adult liver transplant recipients might be: 600-800 ng/ml 1 to 6 months posttransplant, 400-600 ng/ml 7-12 months posttransplant.

Administration, Oral ; Adolescent ; Adult ; Cyclosporine ; administration & dosage ; pharmacokinetics ; Drug Monitoring ; Emulsions ; Female ; Follow-Up Studies ; Graft Rejection ; prevention & control ; Humans ; Immunosuppressive Agents ; administration & dosage ; pharmacokinetics ; Liver Transplantation ; immunology ; Male ; Middle Aged ; Postoperative Period ; Transplantation, Homologous

OBJECTIVETo analyze the correlation between drug exposure (AUC0-4) and blood concentration of different sample points during Neoral absorption phase in Chinese adult liver transplant recipients, and to evaluate the possibility of using post-dose 2 hour level (C2) as a surrogate marker of AUC0-4 for the therapeutic drug monitoring (TDM) of Neoral.

METHODSNeoral levels at 0, 1, 2, 3, and 4 hours (C1, C2, C3, C4) after morning dose of 22 de novo Chinese adult liver transplant recipients were monitored during different posttransplant periods. Liner regression was used to analyze the correlation between CsA concentration at different time points and the AUC0-4.

RESULTSThe best correlation was found at C2, while the correlation of C0 was the lowest. During following-up, the correlation between C2 and AUC0-4 was very stable.

CONCLUSIONC2 had the best correlation with drug exposure. This correlation is very stable. C2 may be used as a good surrogate marker of AUC0-4 for the TDM of Neoral.

Adult ; Area Under Curve ; Asian Continental Ancestry Group ; Cyclosporine ; blood ; pharmacokinetics ; Drug Monitoring ; methods ; Emulsions ; Female ; Graft Rejection ; prevention & control ; Humans ; Immunosuppressive Agents ; blood ; pharmacokinetics ; Intestinal Absorption ; physiology ; Liver Transplantation ; immunology ; Male ; Middle Aged ; Monitoring, Immunologic ; methods ; Postoperative Period