AIMTo synthesize oxazolindinone derivatives and test their antibacterial activities.

METHODS3-Halo-4-methylaniline was acylated with benzyl chloroformate, followed by cyclization with (R)-glycidyl butyrate, acylation with methanesulfonyl chloride, substitution with NaN3, reduction with H2 + Pd/C or P(OMe)3 + HCl, acylation with Ac2O, and bromination with NBS to form bromides VIIIa and VIIIb, Substitution of the bromides with various amines including aliphatic amine and aromatic amine provided the target compounds IXa and IXb. The in vitro antibacterial activity of the target compounds was tested.

RESULTSFifty one new compounds were designed and synthesized. And their structures were confirmed by 1H NMR and elemental analyses or MS. Some physical constants such as [alpha]D25 were reported also. Compounds VIIb, IXa1, IXa2, IXa7, IXb1, IXb3, IXb10, IXb16 and IXb23 had moderate in vitro antibacterial activity against G+ bacteria but they were less active than linezolid or norfloxacin.

CONCLUSIONInsertion of methylene group between 4-position of phenyl and morpholinyl group in linezolid derivatives can not increase the antibacterial activity.

Acetamides ; pharmacology ; Anti-Bacterial Agents ; chemical synthesis ; chemistry ; pharmacology ; Linezolid ; Microbial Sensitivity Tests ; Molecular Structure ; Oxazolidinones ; chemical synthesis ; chemistry ; pharmacology ; Staphylococcus ; drug effects ; Streptococcus ; drug effects

OBJECTIVETo observe changes in the expression of autophagy-related proteins, Beclin-1 and LC3, in the hippocampal tissue of neonatal rats with hypoxic-ischemic brain damage (HIBD) at different time points, and to investigate the effect of rapamycin (Ra) on the expression of the above two proteins.

METHODSA total of 108 7-day-old Sprague-Dawley rats were randomly divided into sham, HIBD, and Ra groups (n=36 each). The HIBD model was established using the modified Rice method. For sham rats, only the left common carotid artery was separated without ligation or hypoxic treatment. For Ra-treated rats, 0.5 mg/kg Ra was administered by an intraperitoneal injection 1 hour before model establishment. The rats were anesthetized and sacrificed to collect brain tissues at 0, 6, 12, 24, 48, and 72 hours after model establishment. Changes in the expression of Beclin-1 and LC3 proteins in rat hippocampus were examined by Western blot.

RESULTSThe expression level of Beclin-1 in HIBD rats began to increase at 0 hour, peaked at 24 hours, and then declined thereafter, similar as those of Beclin-1 and LC3-II in Ra-treated rats. The expression level of LC3-II in HIBD rats began to increase at 0 hour, peaked at 12 hours, and then declined thereafter. At all time points, both Beclin-1 and LC3-II expression levels were significantly higher in HIBD and Ra-treated rats than in sham rats (P<0.05); except LC3-II at 12 hours, Beclin-1 and LC3-II expression levels were significantly higher in Ra-treated rats than in HIBD rats (P<0.05).

CONCLUSIONSHypoxia-ischemia activates autophagy in rat hippocampal cells, while Ra enhances the expression process of autophagy.

Animals ; Apoptosis Regulatory Proteins ; analysis ; Autophagy ; Beclin-1 ; Female ; Hippocampus ; chemistry ; Hypoxia-Ischemia, Brain ; metabolism ; Male ; Microtubule-Associated Proteins ; analysis ; Rats ; Rats, Sprague-Dawley ; Sirolimus ; pharmacology

OBJECTIVETo explore the possible correlation between the driver's occupation and male semen quality.

METHODSSemen samples were collected from 1,223 infertile men (78 drivers and 1,145 non-drivers) and 100 normal men, and their liquefaction, sperm density, sperm vitality, sperm motility and sperm shape were analysed.

RESULTSThe abnormal rates of semen quality in sterile male drivers were significantly higher than in non-drivers(P < 0.05) and in normal men(P < 0.01). The semen abnormal rates in drivers with more than 8 years' driving experience were higher than in those with less than 8 years' driving experience(P < 0.05).

CONCLUSIONDriving occupation can result in abnormal semen quality.

Adult ; Automobile Driving ; Humans ; Infertility, Male ; etiology ; Male ; Middle Aged ; Occupational Diseases ; etiology ; Semen ; cytology ; Sperm Count ; Sperm Motility

OBJECTIVETo detect absorbed bioactive compounds of the water extract whose pharmacodynamic effect was craniocerebral protection for quality control assessment.

METHODSAnthraquinones in water extract of rhubarb (WER), in cerebrospinal fluid (CSF) of patients with traumatic brain injury (TBI) and in ipsilateral cortex of TBI rats following oral WER were respectively explored by ultra performance liquid chromatography with photodiode array detector (UPLC-PDA) method developed in the present study. The effects of anthraquinones absorbed into injured cortex on superoxidase dismutase (SOD) activity in TBI rats were detected. The antioxidative anthraquinones absorbed into target organ were evaluated for quality control of WER.

RESULTSAnthraquinones in WER were aloe-emodin, rhein, emodin, chrysophanol, and physcion. Only the last anthraquinone was found in CSF and in ipsilateral cortex under this chromatographic condition. Physcion increased SOD activity in TBI rats significantly.

CONCLUSIONSPhyscion was the main active compound of rhubarb against craniocerebral injury via antioxidant pathway. According to our strategy, the exploration of physcion suggested the possibility of a novel quality control of WER in treating TBI injury.

Absorption ; drug effects ; Animals ; Anthraquinones ; cerebrospinal fluid ; chemistry ; Biological Products ; analysis ; cerebrospinal fluid ; chemistry ; Brain Injuries ; drug therapy ; pathology ; Chromatography, Liquid ; instrumentation ; methods ; Emodin ; administration & dosage ; analogs & derivatives ; pharmacology ; therapeutic use ; Humans ; Limit of Detection ; Linear Models ; Male ; Plant Extracts ; chemistry ; Quality Control ; Rats ; Rats, Sprague-Dawley ; Reference Standards ; Reproducibility of Results ; Rheum ; chemistry ; Water ; chemistry

Objective::To study the protective effect and mechanism of Qidong Yixin oral liquid on doxorubicin-induced myocardial toxicity in mice. Method::Ninety male ICR mice were randomly divided into normal group, model(DOX) group, DOX+ Qidong Yixin oral liquid group (9.55, 23.88, 47.75 g·kg^-1) and high dose group (47.75 g·kg^-1) with 15 mice in each group. The normal group and model group were given pure water by gavage, and each dose group of Qidong Yixin oral liquid was given different doses of Qidong Yixin oral liquid once a day for 21 days. On the seventh day, normal saline was injected into the abdominal cavity of the normal group and the high dose group of Qidong Yixin oral liquid. Doxorubicin was injected into the abdominal cavity of the other groups (15 mg·kg^-1). After 21 days, the weight and heart weight of mice were weighed and cardiac index was calculated. Serum was taken for the detection of lactate dehydrogenase (LDH), creatine kinase (CK), aspartate aminotransferase (AST). Heart was taken for hematoxylin-eosin (HE) staining, superoxide dismutase (SOD), glutathione peroxidase (GSH-PX), catalase (CAT) in myocardial tissue were detected. The expression of nuclear factor NF-E2 related factor (Nrf2) and heme oxygenase-1 (HO-1) were detected by Western blot. Result::Compared with normal group, adriamycin could significantly reduce the body weight of mice (P<0.01), increase the activities of LDH, CK and AST in serum(P<0.01), and decrease the activities of antioxidant enzymes (P<0.01). Compared with DOX group, high dose Qidong Yixin oral liquid could significantly increase the weight of mice (P<0.05, P<0.01), decrease the level of myocardial three enzymes(P<0.01), increase the activity of antioxidant enzymes(P<0.05, P<0.01), and increase the expression of Nrf2 and HO-1(P<0.01). Conclusion::Qidong Yixin oral liquid has a good protective effect on doxorubicin myocardial toxicity. Its mechanism may be related to activating Nrf2/HO-1 signaling pathway and alleviating oxidative stress injury.