AIMTo study the synthesis and antibacterial activity of ciprofloxacin derivatives.

METHODSCiprofloxacin derivatives were synthesized primarily from 2-methyl-5-nitroimidazol and ciprofloxacin through nucleophilic substitution. The antibacterial activity of the synthesized compounds were tested.

RESULTSNine new compounds were synthesized. The structure of the title compounds were confirmed by 1H NMR, MS and element analysis.

CONCLUSIONCompounds II, IVC and IVD showed appreciable antibacterial activity, and were worth further studying.

Animals ; Anti-Infective Agents ; chemical synthesis ; chemistry ; pharmacology ; Ciprofloxacin ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Escherichia coli ; drug effects ; Female ; Mice ; Molecular Structure ; Nitroimidazoles

OBJECTIVETo evaluate the impact of menarche age (MA) on obese status in late puberty (LP) and mid-life (ML) females.

METHODS2035 girls aged 16 to 18 years were selected from a Beijing Child and Adolescent Metabolic Syndrome (BCAMS) study, which was performed from April to October in 2004, as the LP study population. 479 women aged 41 to 52 years were from the Fetal Origin of Adult Disease (FOAD) cohort, which established in 1995 to 2001, as the ML study population. Based on the 25 and 75 percentile of MA of each population, all subjects of LP and ML were divided into early, middle, and late matured groups, respectively. Overweight and obesity were defined by Chinese age-, gender-specific BMI criteria for LP girls, and Chinese BMI criteria for ML women while central obesity was defined by the waist-to-height ratio (WHtR) cutoff of 0.5. Multiple linear regression was used to explore the associations between MA and BMI, waist circumference (WC) and WHtR. The impact of early menarche on obese status in late life was estimated by odds ratio (OR) using logistic regression analyses.

RESULTSThe prevalence of overweight and obesity increased with the decrease of MA in both LP and ML population. When MA had a one-year advance, a 0.58 kg/m2 increase in BMI and a 1.1 cm increase in WC during LP, and a 0.35 kg/m2 increase in BMI and a 0.6 cm increase in WC during ML were observed. After adjustment for age, residence area and life style related variables, those who experienced earlier menarche were at higher risk of suffering from obesity in LP (OR :8.740, 95% CI: 3.653-20.911) and during ML (2.498, 1.145-5.453) when compared to those with later menarche. We also noticed that the risk increased for central obesity [LP: 14.280 (3.223-63. 267), ML: 15.604 (1.821-133.679)].

CONCLUSIONMenarche age appeared to be an independent predictor for obese status in LP and ML among women.

Adiposity ; physiology ; Adolescent ; Adult ; Female ; Humans ; Linear Models ; Menarche ; physiology ; Middle Aged ; Obesity ; epidemiology ; Prevalence ; Puberty ; physiology ; Risk Factors

OBJECTIVETo explore the mechanisms of muscovite gastric mucosal protective effect.

METHODRat model of chronic gastritis were used. After gastric mucosal injury was induced, the rats were divided into 6 groups and were treated with different drugs. 2 weeks later, the tissue and blood samples were obtained and measured.

RESULTThe general conditions, the observations under macroscopy, microscope and electron microscope of the middle and high dose of muscovite groups resembled those of the normal group. Their PH levels were higher than those of the model group, and the rates of intestinal metaplasia were lower, but the PGE2 level of the middle dose of muscovite group was the highest.

CONCLUSIONMuscovite can be adsorbed on the surface of the gastric mucosa. It has gastric mucosal protective effect by improving excretion of mucus and synthesis of PGE2 in gastric mucosa, restraining gastric acid, reversing of intestinal metaplasia and decreasing inflammation cells.

Aluminum Compounds ; pharmacology ; Animals ; Dinoprostone ; blood ; Gastric Juice ; chemistry ; Gastric Mucosa ; pathology ; ultrastructure ; Gastritis ; blood ; chemically induced ; pathology ; Hydrogen-Ion Concentration ; Materia Medica ; pharmacology ; Microscopy, Electron, Scanning ; Potassium Compounds ; pharmacology ; Protective Agents ; pharmacology ; Rats ; Rats, Wistar ; Silicates ; pharmacology ; Sodium Salicylate

The effect of Rhizoma curcumae oil on the learning and memory in rats exposed to chronic hypoxia and the possible mechanisms were investigated. The rats were divided randomly into 5 groups (14 animals in each group): control, chronic hypoxia, chronic hypoxia with low (5 mg/kg body weight), middle (10 mg/kg body weight) and high (20 mg/kg body weight) concentrations of Rhizoma curcumae oil injection. The animals undergoing chronic hypoxia were exposed to hypoxia in a hypoxic chamber containing 10% O(2) and 5% CO(2) for 10 h/d, lasting 28 d. Morris water maze (MWM) test was used to obtain the scores of leaning and memory. The superoxide dismutase (SOD) activity and malonaldehyde (MDA) content were determined in the serum and hippocampus as well as [Ca(2+)](i) in the hippocampus. The expression of phosphorylated Ca(2+)/calmodulin-dependent protein kinase II (p-CaMKII) in the hippocampus was evaluated by using immunohistochemistry and Western blot. Compared with the control group, the chronic hypoxia group showed the following changes: (1) The escape latency to the hidden platform was remarkably prolonged (P<0.05); (2) The content of MDA and [Ca(2+)](i) were obviously higher, but the activity of SOD and the expression of p-CaMKII were significantly lower (P<0.05, P<0.01). Compared with the chronic hypoxia group, groups with Rhizoma curcumae oil injection had the following changes: (1) The escape latency to the hidden platform was remarkably shorter in 10, 20 mg/kg body weight groups (P<0.05); (2) The content of MDA and [Ca(2+)](i) were markedly decreased in 5, 10, 20 mg/kg body weight groups (P<0.05, P<0.01), but the activity of SOD in the serum and the expression of p-CaMKII were significantly higher in 10, 20 mg/kg body weight groups (P<0.05, P<0.01). The results showed that the capacity of learning and memory was degraded following chronic hypoxia. The decrease in MDA content and [Ca(2+)](i) and (or) the increase in SOD activity and p-CaMKII expression might participate in the enhancing effect on learning and memory induced by Rhizoma curcumae oil.
Animals ; Calcium ; metabolism ; Calcium-Calmodulin-Dependent Protein Kinase Type 2 ; metabolism ; Curcuma ; chemistry ; Hippocampus ; metabolism ; Hypoxia ; physiopathology ; Learning ; drug effects ; Malondialdehyde ; metabolism ; Memory ; drug effects ; Plant Oils ; pharmacology ; Rats ; Rhizome ; chemistry ; Superoxide Dismutase ; metabolism

OBJECTIVETo provide an appropriate angle and depth of needle insertion in acupuncture at Zusanli (ST 36) and avoid injuring the nerve and blood vessel and exert the most effect.

METHODSEighty adult lower-limb samples were used to dissect and observe the relative layered structures and adjoining important nerves and blood vessels in needling Zusanli (ST 36) according to the national standard.

RESULTSThe needling depth from the skin to the interosseous membrane and from the skin to posterior border of tibialis posterior is (2.22 +/- 0.31) cm and (4.42 +/- 0.53) cm, respectively. There are flabellate branches of anterior tibial arteries and deep peroneal nerves around the needle in the superficial layer of interosseous membrane. The vessel and nerve bundles containing tibial nerve and posterior tibial vessels can be touched when the needle body past through tibialis posterior.

CONCLUSIONIt is recommended that ideal average depth of acupuncture is 2.22 cm and the maximum depth is 4.42 cm for oblique needling Zusanli (ST 36). When it is injected, the needle should be perpendicularly inserted or deviated slightly to the direction of tibia and paralleled to medial surface of tibia. And the safe needling depth is generally less than 5 cm. The point of the body surface between tibialis anterior and extensor digitorum longus at 3 cun below Dubi (ST 35) is also an effectively stimulating point.

Acupuncture Points ; Female ; Humans ; Male ; Needles ; Tibia ; anatomy & histology

OBJECTIVETo investigate whether apollon immunoexpression in breast cancer tissues helps to predict pathological complete response (pCR) after neoadjuvant chemotherapy (NAC).

METHODSThe expressions of Apollon, Her-2, estrogen receptor (ER) and progesterone receptor (PR) were detected immunohistochemically in biopsy tissues from 124 breast cancer patients. The clinical responses to NAC were evaluated in line with the response evaluation criteria in solid tumors (RECIST). The pCR rate was analyzed for different types of breast cancer. The correlations between Apollon status with Her-2, ER, PR, lymph node status and tumor size were analyzed. Immunohistochemistry was used to compared the changes in Apollon expression in the breast cancer tissues before and after NAC.

RESULTSThe pCR rate was 18.5% (23/124) in these patients. Negative expressions of apollon, ER and PR were all associated with a higher pCR rate after NAC. Apollon was significantly correlated with Her-2, ER, PR and lymph node involvement. Chemotherapy significantly down-regulated apollon expression in the tumor cells.

CONCLUSIONA negative apollon expression might be a predictor of pCR in patients with breast cancer.

Biopsy ; Breast Neoplasms ; drug therapy ; metabolism ; Female ; Gene Expression Regulation, Neoplastic ; Humans ; Immunohistochemistry ; Inhibitor of Apoptosis Proteins ; metabolism ; Neoadjuvant Therapy ; Receptor, ErbB-2 ; metabolism ; Receptors, Estrogen ; metabolism ; Receptors, Progesterone ; metabolism

Objective To explore the clinical effect of the transurethral ureteroscopic holmiumlaser lithotripsy in the treatment of ureteral calculi.Methods This study conducted a retrospective analysis of 205 patients with ureteral calculi from September 2015 to June 2017 in the affiliated hospital of Panzhihua university.According to the surgical method,all the patients were divided into control group (102 cases) who were treated with conventional pneumatic lithotripsy and observation group(103cases) who received transurethral ureteroscopic holmiumlaser lithotripsy.The surgical efficacy,renal function indexes and surgical indexes of the two groups were compared and analyzed respectively.Results The total effective rate of observation group was 97.06％,the control group was 85.00％,the difference between two groups was significantly(P ＜ 0.05).There was no significant difference in Cr and BUN level before surgery between two groups (P ＞ 0.05);after treatment,the Cr and BUN levels of two groups were improved significantly (P ＜ 0.05);while the renal function improved index of observation group was significantly better than that of control group,the difference was significant(P ＜ 0.05).The intraoperative blood loss,operative time and postoperative hospital stay of the observation group were significantly lower than those of control group (P ＜ 0.05).Conclusion The transurethral ureteroscopic holmiumlaser lithotripsy and normal air pressure ballistic were both well treatment for ureteral calculi,but patients with the holmium laser lithotripsy have better renal function indexes and operation index.

Objective To explore the influence of Mac-1 deficiency on tumor growth of melanoma. Methods The population of Mac-1 gene knock-out ( Mac-1 -/ -) mice was expanded. B16-F10 cells were subcutaneously injected into the C57BL/6J mice (control group) and Mac-1 -/ -mice (experiment group), respectively. Subsequently,the survival rate, tumor volume and body weight were recorded. The proliferation and infiltration of macrophages were detected by immunohistochemistry. Results The survival rate of Mac-1 -/ - mice was significantly improved compared with the C57BL/6J mice (P ﹤0. 001). The tumor volume and body weight were remarkably decreased in the Mac-1 -/ - mice compared with the control group (P﹤0. 001). Meanwhile, the tumor cell proliferation index was decreased in the Mac-1 -/ - mice compared with the control group (P﹤0. 01). Furthermore, the infiltration of macrophages in the tumor tissues was also decreased in Mac-1 -/ - tumor mice compared with control group. Conclusions Mac-1 gene deletion can significantly suppress melanoma growth.

OBJECTIVE: To explore one of evidence for pathologic diagnosis of early myocardial ischaemia. METHODS: Rats were ligated of the left coronary artery according to a previously documented technique, and heart tissue was sampled at different ischaemia time. The expression of CX43 in myocardial cell was detected by Immunohistochemistry. RESULTS: It is showed that the distribution and amount of CX43 positive staining in each group of the myocardial ischaemia was different from that of the control group. CONCLUSION The changes of CX43 detected by Immunohistochemical methods may be helpful for the diagnosis of early myocardial ischaemia, but further pathologic investigation and research is necessary.
Animals ; Connexin 43/metabolism* ; Disease Models, Animal ; Female ; Forensic Pathology ; Immunohistochemistry ; Male ; Myocardial Ischemia/pathology* ; Myocytes, Cardiac/metabolism* ; Myometrium/pathology* ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Staining and Labeling ; Time Factors ; Tissue Distribution

The type I interferon and IFNAR play an important role in hepatitis B virus (HBV) infection and anti-HBV therapy. However, its mechanism of action is still poorly understood. To gain more insights into the role of type I interferon and type I interferon receptor (IFNAR) in HBV infection, we established an HBV persistent replication IFNAR knockout (IFNAR(-/-)) mouse model and preliminarily applied this model. At first, the progeny of IFNAR(-/-) mouse was reproduced. Then hydrodynamic injection with pAAV/HBV1.2 plasmid was conducted to establish the persistent HBV replication IFNAR(-/-) mouse model. At last, we applied this model to evaluate the effect of nucleoside analogues entecavir (ETV) on HBV replication. It was found that there was no difference in the serum HBsAg and HBeAg levels and HBcAg expression in the liver tissue between the ETV treated groups and normal saline (NS) treated group, but the serum HBV DNA levels were significantly suppressed 10, 25, 40 and 55 days after the ETV treatment [P=0.035, P=0.00, P=0.149 and P=0.084, IFNAR knockout (KO) control group vs. C57BL/6 ETV groups, respectively; P=0.081, P=0.001, P=0.243 and P=0.147, IFNAR KO control group vs. IFNAR KO ETV groups, respectively]. Interestingly, there was no difference in serum HBV DNA levels between the ETV treated IFNAR(-/-) and C57BL/6 mice. This result suggests that HBV suppression during ETV treatments doesn't depend on type I interferon and IFNAR. Collectively, persistent HBV replication IFNAR(-/-) mouse model that we established is a useful and convenient tool to detect the function of the type I interferon and IFNAR in HBV infection and anti-HBV treatments.
Animals ; Chronic Disease ; Disease Models, Animal ; Female ; Hepatitis B ; genetics ; virology ; Hepatitis B virus ; physiology ; Humans ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Receptor, Interferon alpha-beta ; genetics ; metabolism ; Virus Replication ; genetics