This study is aimed to make a comprehensive introduction to the anti-MRSA drugs,and also to compare the safety and efficacy among a variety of anti-MRSA drugs.Finally,it is pointed that we should select the anti-MRSA drugs precisely according to different situation of disease when treating the infection with MRSA.Then we can make the individualized treatment for patients and provide a basis for the disease when treatment of patients as well.

Objective To study the antibacterial mechanisms of berberine and try to understand the reasons why bacteria cells difficultly resisted to it. Methods Detecting the minimal inhibitory concentration (MIC) of bacterial cultures incubated under sub-MIC concentration of berberine, Huanglian, and Neomycin for more than 200 generations, in order to analyze the bacteria resistance. Detecting the binding kinetics of berberine to DNA, RNA, and proteins. Observing the changes in bacterial cell surface structure with scanning electron microscopy. Detecting the Ca2+ and K.+ released from berberine-treated bacterial cells with atomic absorption spectrum. Detection the absorption of methyl-3H-thymine (3H-dT), 3H-uridine (3H-U), and 3H-tyrosine (3H-Tyr) into berberine-treated bacterial cells. Results MICs of bacterial cultures, growing more than 200 generations in MH medium with 1/2 MIC of berberine (BA200) or Huanglian (HA200), did not increase compared to the control, while remarkably increased in MH medium with 1/2 MIC of Neomycin (NA200). In addition, from the culture NA200 it was easy to isolate resistant mutant strains which could grow in MH medium with more than four times MIC Neomycin, but from the culture BA200 and HA200 it was difficult to isolate berberine or Huanglian mutant strains could grow in MH medium with more than four times MIC berberine or Huanglian. The binding kinetics of berberine to DNA, RNA, and proteins illustrated that berberine could easily and tightly bind to DNA and RNA, and hardly dis-bind from DNA- and RNA-berberine complexes. Berberine could easily bind to protein too, but also easily dis-bind from berberine-protein complex. The bacterial cells treated with berberine sharply decreased the absorption of 3H-dT, 3H-U, and 3H-Tyr, as the radioactive precursors of DNA, RNA, and protein biosynthesis. Berberine could damage bacterial cell surface structure, especially for Gram-negative bacteria. Ca2+ and K+ released from berberine-treated cells increased significantly compared to the control. Conclusion All of above results indicate that bacterial cells could not easily become resistant mutants to berberine. The mechanisms for the bactericidal effect of berberine include: inhibiting DNA duplication, RNA transcription, and protein biosynthesis; influencing or inhibiting enzyme activities; destructing the bacterial cell surface structure and resulting in Ca2+ and K+ released from cells. All of the berberine bactericidal mechanisms are the most essential physiological functions for a live cell, if influenced any one such function, the mutation would be lethal mutation, so that it is difficult to get berberine resistant cells. The results in this paper also prefigure that berberine and its related Chinese medicines would provide a feasible way to control antibiotic resistance problem.

The pathogenesy of diabetic peripheral neuropathy(DPN) is approached according to collaterals diseases theory in this study,indicated that defi ciency of both vital energy and yin is the chief pathologic foundation and obstruction of collaterals by blood stasis and phlegm is the critical element in DPN.Furthermore,highlight of differentiation of symptoms and signs,therapeutic principle and diagnosis and treatment based on differentiation are illuminated.This study has supplied a new idea for precaution and treatment of DPN.

Objective To explore the effect of application of continue performance test (CPT) in screening of attention deficit hyperactivity disorder( ADHD ). Methods Thirty-five children with ADHD and65 normal children had been applied with CPT and Conner questionnaire test. Used rank sum test to examine the outcome, established receiver operating characteristic (ROC) curve, analyzed the most valuable index among various data, formulated abnormal critical value, and carried on a consistency check between CPT screening outcome and clinical diagnosis outcome. Results Each CPT index of 35 children with ADHD was obviously higher than those of normal children(P＜ 0.05 ). Most indexes' area under the ROC curve exceeded 0.7, reactive time of VST was the highest among each index which achieved 0.915. It was high conformity between CPT screening outcome and clinical diagnosis outcome (Kappa = 0.935 ). Conclusion CPT can be applied in ADHD screening.

To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.

To explore an efficient strategy for the conversion of antibacterial fluoroquinolones into antitumor fluoroquinolones, an azole heterocyclic ring of oxadiazole instead of the C-3 carboxylic acid group with a functionalized hydrazone group as a modified side-chain, fifteen novel 2-(fluoroquinolon-3-yl)-oxadiazole-5- sulfanylacetylhydrazone derivatives 7a-7o were designed and synthesized on the basis of the pharmacophore hybridization principle from pefloxacin, separately. The structures for fifteen title compounds were characterized by elemental analysis, 1H NMR and MS, and their in vitro antitumor activity against Hep-3B cell line was evaluated by a MTT assay. The results showed that the title compounds exhibited more significantly inhibitory activity than that of the parent pefloxacin, in which compounds with electron-withdrawing group attached on aryl ring had more potency than that of compounds with electron donating group, especially compounds with a carboxylic substituent were comparable to comparison doxorubicin. It suggests that it is favorable for an improvement of antitumor activity to remain a carboxylic acid unit at the aromatic ring.

AIM: To investigate the effect of dexmedetomidine (DEX) on renal injury induced by lung ischemia/reperfusion (I/R) in mice and its relationship with endoplasmic reticulum stress response.METHODS: Healthy SPF male C57BL/6J mice, weighing 20~24 g, aged 8~10 weeks, were randomly divided into 5 groups (n=10 each): sham operation group (sham group), I/R group, atipamezole (Atip) group, DEX group, and DEX+Atip group.In vivo lung I/R model was established by occlusion of the left pulmonary artery for 30 min followed by 180 min of reperfusion in the mice.The Atip (250 μg/kg), DEX (20 μg/kg) and DEX+Atip were intraperitoneally infused into the mice before left pulmonary hilus was blocked in Atip group, DEX group and DEX+Atip group, and other operations were the same as I/R group.After experiment, the mice were killed, and the renal tissues were harvested to observe the morphological changes.The enzymatic activity of caspase-3, serum creatinine and blood urea nitrogen, and cell apoptotic index of the renal cells were also analyzed.The expression of c-Jun N-terminal kinase (JNK), caspase-12, CCAAT/enhancer-binding protein homdogous protein (CHOP) and glucose-regulated protein 78 (GRP78) at mRNA and protein levels in the renal tissues was determined by RT-PCR and Western blot.RESULTS: Compared with sham group, the enzymatic activity of caspase-3, serum creatinine and blood urea nitrogen, renal cell apoptotic index, and the mRNA and protein levels of JNK, caspase-12, CHOP and GRP78 in I/R group were significantly increased (P<0.01), and the renal tissues had obvious damage under light microscope.Compared with I/R group, Atip group and DEX+Atip group, the enzymatic activity of caspase-3, serum creatinine and blood urea nitrogen, renal cell apoptotic index, and the mRNA and protein levels of JNK, caspase-12 and CHOP in DEX group were significantly decreased, and the expression level of GRP78 significantly increased (P<0.01).Furthermore, the renal tissue damage was obvious reduced.CONCLUSION: DEX effectively relieves the renal injury induced by lung I/R in mice, which may be associated with exciting α2-adrenergic receptor and inhibiting endoplasmic reticulum stress response.

Objectives To systematically evaluate the effect of music given to pregnant rats on the development of brain functions in the offspring rats and to provide scientific evidence for the application of antenatal musical training and the promotion of welfare for laboratory animals.Methods We comprehensively retrieved and collected the research literatures related to the effect of music on brain function development in offsprings of the pregnant rats from Pubmed,Web of Science,Cochrane Library,Wanfang,Weipu,CNKI and CBMdisc.The retrieval time was set from the foundation date of databases to 2 April,2016.We selected literatures according to the inclusion and exclusion criteria,evaluated their utilities,then extracted and qualitatively described the data.Results Seven experimental studies were selected in this study including 4 published in Chinese and 3 in English.The object laboratory animals of those studies were Wistar or SD rats.Music materials involved comfort music,classic music,violin concerto(Liangzhu/The butterfly lovers).Intervention were given to the pregnant rats roundly from the gestation until parturition.These results showed that,to some extent,music stimulations during gestation may promote the development of brain function and improve spatial memory of the offspring rats.However,expressions of some functional receptors were not significantly altered.Conclusions Appropriate music provided to the pregnant rats promote the development of brain functions in their offspring.

Objective To study the effect of Punica granatum( pomegranate) see d oil( PSO) on proliferation and apop-tosis behaviors of breast cancer cells.Methods Fatty acid composition was detected by gas chromatography,breast cancer cells, MCF-7 and MDA-MB-231 were treated with PSO, cell proliferation was observed by MMT, cell apoptosis was analyzed by flow cytometry,and expression levels of proliferation and apoptosis-related proteins were detected by Western blot.Results Punicic acid (PA) was the major fatty acid in PSO(74.41%).PSO could inhibit the proliferation while in-ducing apoptosis in both cell lines in a dose-and time-dependent manner, significantly decrease the expression level of Cox-2 and Bcl-2, increase the expression level of Bax and caspase-3 (cleaved),remarkably upregulate the expression of P53 in MCF-7, and downregulate p53 expression in MDA-MB-231.Conclusion PA may be one of the functional ingredients of PSO which can inhibit proliferation and induce apoptosis in breast cancer cells.These effects are probably mediated by regu-lating the expression of Cox-2, Bcl-2, Bax, caspase-3 (cleaved) and p53.

Objective To evaluate the effects of intrathecal low-dose naloxone,morphine and fentanyl on the expression of motillin (MTL) in the hippocampus of rats with incisional pain.Methods Seventy-two healthy male Sprague-Dawley rats,weighing 180-220 g,aged 6-8 weeks,in which intrathecal catheters were successfully implanted,were randomly divided into 6 groups (n =12 each) using a random number table:normal saline group (NS group),incisional pain group (P group),morphine + fentanyl + incisional pain group (MFP group),and naloxone (0.2,1.0 and 5.0 ng/kg) + morphine + fentanyl groups (MFPN1,MFPN2 and MFPN3 groups).Incisional pain was induced by an incision made into the plantar surface of the right hindpaw.At 20 min before induction of incisional pain,the mixture of morphine 5 μg/kg and fentanyl 0.25 mg/kg was injected intrathecally in group MFP,and the mixture of naloxone 0.2,1.0 and 5.0 ng/kg,morphine and fentanyl were injected intrathecally in MFPN1,MFPN2 and MF-PN3 groups,respectively.Six rats in each group were selected,and the mechanical paw withdrawal threshold (MWT) and thermal paw withdrawal latency (TWL) were measured at 24 h before intrathecal catheterization (T0,baseline),at 24 h before induction of incisional pain (T1),and at 1,3 and 6 h after operation (T2-4).The left 6 rats in each group were selected and sacrificed at 6 h after operation,and the hippocampi,body of the stomach and duodenum were removed for detection of MTL content by enzyme-linked immunosorbent assay.Results Compared with group NS,the MWT was significantly decreased,and the TWL was shortened at T2-4 in P and MFPN3 groups,the MWT was significantly decreased,and the TWL was shortened at T4 in group MFPN1,and the TWL was prolonged at T2 in group MFPN2,the MTL contents in hippocampus and body of the stomach were significantly decreased in P,MFP,MFPN1 and MF-PN3 groups,the MTL contents in duodenum were increased in P and MFPN3 groups,and the MTL contents in duodenum were decreased in MFP and MFPN1 groups (P＜0.05),and no significant change was found in the parameters mentioned above in group MFPN2 (P＞0.05).Conclusion Intrathecal naloxone 1.0 ng/kg combined with morphine and fentanyl can inhibit up-regulation of the expression of MTL in the hippocampus of rats with incisional pain,and then is involved in the maintenance of stable gastrointestinal motility.