AIMTo synthesize four water-soluble metal porphyrins [5, 10, 15, 20-tetra[4-(4'-pyridine-1) butyloxy phenyl] metalloporphyrins bromide, metal = Zn (I), Cu (II), Mn (III) and Co (IV)] as analogous enzyme having two anti-active oxygen functions.

METHODSThe first function, scavenging O2-, has been proved by using riboflavine-methionine photoreduction methods. The second function, scavenging H2O2, has been demonstrated by using the oxidating Vit C. The third function, scavenging HO*, has been demonstrated by using Fenton reaction. The complexes were measured by the mice liver homogenate technique of mice.

RESULTSFour model compounds could scavenge O2- in the concentration range of 1.0 x 10(-5) - 1.0 x 10(-6) mol x L(-1), decompose H2O2 in the concentration of 1.5 x 10(-6) - 1.0 x 10(-6) mol x L(-1), scavenge HO* in the concentration of 2.0 x 10(-8) - 1.0 x 10(-8) mol x L(-1). All showed that they had obvious action of decreasing the lipid peroxidation in the concentration of 1.0 x 10(-7) mol x L(-1).

CONCLUSIONAll above-mentioned complexes were considered to be qualified analogous enzymes of anti-active oxygen.

Animals ; Cobalt ; Copper ; Free Radical Scavengers ; chemical synthesis ; pharmacology ; Hydrogen Peroxide ; metabolism ; Hydroxyl Radical ; metabolism ; In Vitro Techniques ; Lipid Peroxidation ; drug effects ; Liver ; metabolism ; Malondialdehyde ; metabolism ; Manganese ; Metalloporphyrins ; chemical synthesis ; pharmacology ; Mice ; Reactive Oxygen Species ; metabolism ; Zinc

The plasma visfatin,endothelium-dependent artery dilation and intima-media thickness of common carotid arteries were measured in first-degree relatives of type 2 diabetes,obese patients and control subjects.Regional body fat were detected by MRI.The result suggested that plasma visfatin levels were significantly higher in obese subjects than those in non-obese subjects,and hypervisfatinemia is independently associated with fasting blood glucose.

AIMTo improve the biological activity of A-ring modified analogues of camptothecin.

METHODSA-ring modified camptothecins were synthesized from 10-hydroxycamptothecin or 7-ethyl-10-hydroxycamptothecin (SN-38) in three or four steps. Their cytotoxicity was evaluated using MTY assay, and their in vivo antitumnor activity against mouse liver cancer H22 was tested. Results Five hexacyclic camptothecins (6a, 6b, 6c, 7a and 7b) are target compounds, and ten camptothecin derivatives are new compounds.

CONCLUSIONThe modification of a 1,4-oxazine-2-one ring fused with positions 9 and 10 of A-ring will reduce the antitumor activity of camptothecins.

Animals ; Antineoplastic Agents ; chemical synthesis ; pharmacology ; Camptothecin ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Carcinoma, Hepatocellular ; drug therapy ; pathology ; Cell Line, Tumor ; drug effects ; Female ; Humans ; Liver Neoplasms ; drug therapy ; pathology ; Mice ; Neoplasm Transplantation ; Polycyclic Compounds ; chemical synthesis ; pharmacology

OBJECTIVETo investigate the effect of the photodynamic therapy (PDT) with the new water-soluble metalloporphyrin compound on human prostate cancer PC-3 cells in vitro and the anticancer mechanism of PDT.

METHODSThe new water-soluble manganese, 5,10,15, 20-tetra (N-methyl4-pyridyl) porphinato (2-) tetraiodide salt, was synthesized. The PC-3 cells were treated with the compound of serial concentrations(0, 0.1, 1, 1.0 micromol/L) followed by irradiation of different dosages of visible light. The techniques of MTT and Annexin-V/propidium iodide double-labeled flow cytometry (FCM) were applied to measuring the inhibitory effect of the compound on the growth activity and apoptosis of the cells.

RESULTSWhen the metalloporphyrin compound concentration was within 10 micromol/L and the irradiation time was within 30 min, the water-soluble metalloporphyrin compound had a significant inhibitory effect on the proliferation of PC-3 cells and induced PC-3 cell apoptosis, and the effects depended greatly on metalloporphyrin concentration and illumination dosages. Higher concentrations and dosages induced the death of the majority of PC-3 cells.

CONCLUSIONThe PDT of the water-soluble metalloporphyrin compound followed by light irradiation has a distinctive killing effect on PC-3 cells in vitro, and the rates of proliferation inhibition and cell apoptosis are correlated with metalloporphyrin concentration and the dosages of light irradiation. The results suggest that the mechanism of metalloporphyrin PDT may be involved with the induction of apoptosis in human prostate cancer cells.

Apoptosis ; drug effects ; radiation effects ; Cell Line, Tumor ; Dose-Response Relationship, Drug ; Dose-Response Relationship, Radiation ; Humans ; Male ; Metalloporphyrins ; pharmacology ; Photochemotherapy ; Prostatic Neoplasms ; pathology

OBJECTIVETo investigate the relationship between adiponectin and beta-cell function in abdominal visceral obesity women.

METHODSNine abdominal visceral obesity women (VO), 9 normal subjects (C) and 7 patients with type 2 diabetes mellitus (T2DM) were enrolled in the study. Beta-cell function and insulin sensitivity were determined by hyperglycemic clamp, fasting serum adiponectin was assayed by ELISA and regional body fat was measured by MRI.

RESULTThe levels of first phase insulin release (FPIR), glucose disposal rates (GDR), insulin sensitivity index (ISI) and adiponectin were significantly elevated in control group compared with VO group and T2DM group. As compared with T2DM group, the levels of adiponectin, FPIR, second phase insulin release (SPIR) and maximum insulin release (INS(max)) increased significantly in VO group. Multiple stepwise regression analysis showed that age, FPIR and GDR were positively correlated to adiponectin (B=0.145, 0.194, 0.277 respectively, all P<0.05), while waist-hip ratio was negatively correlated with adiponectin (B=-7.424, P<0.05).

CONCLUSIONThe visceral obesity women have lower adiponectin levels, and hyperadiponectinemia may be the link with insulin secretion.

Abdominal Fat ; Adiponectin ; blood ; Adult ; Female ; Glucose Clamp Technique ; Humans ; Insulin-Secreting Cells ; physiology ; Middle Aged ; Obesity ; blood ; physiopathology

OBJECTIVE: To explore the influencing factors of low back pain and the relationship of the influence of bad working posture, weight load and frequency of load and the dose-response relationship among the occupational workers of key industries in China. METHODS: A total of 57 501 employees from 15 key industries in China were selected as research subjects using stratified cluster sampling method. The occurrence of low back pain in the past one year, as well as occupational factors such as job type, labor organization and work posture were investigated by using the Chinese version Musculoskeletal Disorders Questionnaire. RESULTS: The prevalence of low back pain in the occupational population of key industries in China was 16.4%(9 448/57 501). Multivariate Logistic regression analysis showed that the risk of low back pain in females was higher than that in males(P<0.01). Married, obese, occasional and frequent smokers, and a history of lower back disease were associated with increased risk of low back pain(all P<0.05). The risk of low back pain was associated with older age, higher education level, and lower frequency of physical exercise(all P<0.01). The risk of low back pain was higher with longer working time, greater back curvature, and the high frequency of long standing and sitting position work, uncomfortable working posture, repeated operation per minute, and lifting>5 kg weight(all P<0.01). CONCLUSION: The influencing factors of low back pain in the occupational population of key industries in China include bad working posture, high frequency load, weight load and other individual factors. There is a dose-response relationship with low back posture load and frequency of load.

OBJECTIVE: The current outbreak of Zika virus (ZIKV) poses a severe threat to human health. Two ZIKV strains were isolated from mosquitoes collected from the Dejiang prefecture in China in 2016, which was the first isolation of ZIKV in nature in China. METHODS: In this study, serum samples were collected from 366 healthy individuals and 104 animals from Dejiang prefecture in 2017, and the plaque reduction neutralization test (PRNT) was used to evaluate the seroprevalence of ZIKV. RESULTS: None of the 366 residents from whom the samples were collected were seropositive for ZIKV. None of the 11 pigs from whom the samples were collected were seropositive for ZIKV, while 1 of 63 (1.59%) chickens and 2 of 30 (6.67%) sheep were seropositive for ZIKV. CONCLUSION The extremely low seropositivity rate of ZIKV antibodies in animals in the Dejiang prefecture, Guizhou province in this study indicates that ZIKV can infect animals; however, there is a low risk of ZIKV circulating in the local population.