Synthesis and protein tyrosine kinases inhibitory activity of substituted benzyl piperazine derivatives / 国际药学研究杂志

Objective Using substituted benzyl piperazine as the raw material to design and synthesize new piperazine deriva-tives with protein tyrosine kinase(PTK)inhibitory activity. Methods Benzoic acid was used as starting compound to synthesize a key intermediate,2-chloroethyl benzoate,and the target compounds were synthesized by further reaction of the key intermediate with different substituted benzyl piperazine derivatives.Enzyme-linked immunosorbent assay(ELISA)was used to test the PTK inhibitory activity of the compounds.Results Fifteen new compounds were synthesized and their structures were verified by IR,1H NMR,MS, and elemental analysis.The PTK inhibitory activity of 3h and 3o was stronger than that of the other compounds.Conclusion The syn-thetic method is simple,and the raw materials are cheap and readily available.Compounds 3h and 3o showed relatively higher PTK in-hibitory activities.

Refractive change after mydriasis optometry combined with amblyopia treatment in children with mixed astigmatism and amblyopia / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: To investigate the effect of mydriasis optometry combined with amblyopia treatment on refraction and amblyopia changes in children with mixed astigmatism and amblyopia.METHODS: Totally 163 children (289 eyes) of mixed astigmatism and amblyopia from January 2010 to May 2011 were treated.All of the patients received mydriatic optometry and spectaculars with amblyopia therapy and were followed up for 5a to observe amblyopia efficacy and refractive status changes.RESULTS: With 5a, main diameter diopter at distant vision decreased year by year, average decline in the first year was 0.55DS, 0.56DS in the second year, 0.72DS in the third year, 0.95DS in the fourth year, 1.89DS in the fifth year.The spherical equivalent changed from 1.12DS at distant to 0.78DS at near.The corrected visual acuity of all the patients at first visit was 0.2-0.8 with varying degrees amblyopia.After a 5-year treatment, it was effective in 268 eyes (92.7%), in which 165 eyes (57.1%) improved, 103 eyes (35.6%) cured, the results was better as the period of spectaculars wearing was longer.There was 36 eyes (37.5%) improved and 60 eyes (62.5%) cured in 1.50-2.50DC group;118 eyes (74.2%) improved, 41 eyes (25.8%) cured in 2.50-3.50DC group;11 eyes (32.3%) improved, 2 eyes (5.9%) cured, 21 eyes (61.8%) useless in >3.50DC Group.The differences of efficacy among the groups were significant (all P<0.05).CONCLUSION: Appropriate spectaculars is the basic for amblyopia treatment.It is effective for most children with mixed astigmatism and amblyopia to take mydriasis optometry and amblyopia treatment.

Cycloplegic effects of 0 . 5 g/L tropicamide in various low myopia age groups / 国际眼科杂志(Guoji Yanke Zazhi)

AlM: To investigated the refraction and cycloplegic effects of 0. 5g/L tropicamide eye drops in various low myopia age groups, and provide clinical guidelines for proper usage of cyclopegic agent in different population.METHODS:Three low myopia age groups (n=45) were selected, non-cycloplegic and cycloplegic auto-refraction using “Shin-Nippon” auto-refractor were performed at various time point for refractive error. The subjective accommodation amplitudes were also collected at each time point. RESULTS: The accommodation amplitude showed a similar but significant decline between 20~60min after the first cyclopegic drops in all three age groups. However, the decline of accommodation amplitudes were not statistically correlated with the results of “Shin-Nippon”auto-refraction results at different time points. CONCLUSlON: The refraction time should be arranged according to the cycloplegic effects of tropicamide. Open-field auto-refractor could reduce the usage of cycloglegice drugs in low myopia groups, even for the youngest.

Evolutionary analysis of neuraminidase gene of A/H7N9 influenza virus / 病毒学报

In 2013, the World Health Organization reported the first case of human infection with a new influenza A (H7N9) virus in China. This has caused damage and panic within certain areas in China. Therefore, analysis of this virus with bioinformatics technology is very necessary. Neuraminidase (NA) is one of the most important antigens of the influenza virus and an important target for anti-flu drugs. In this study, the nucleotide and protein sequences of NA gene of A/H7N9 influenza viruses were retrieved from the NCBI database, and MEGA 5.0 software was employed to construct a phylogenetic tree based on the nucleotide coding sequence; BioEdit software was used to align the nucleotide and protein sequences of NA and calculate the homologies of nucleotides and amino acids and then to analyze the important mutation sites of NA gene. The results demonstrated that the spread of influenza virus H7N9 showed certain geographical and temporal relations. The H7N9 virus isolated from China in 2013 belonged to Euroasiatic serotype, and its NA stalk region hadobvious variation, which may be one of the reasons that this virus infects human. These analyses may be very helpful for understanding the evolutionary relationship and mutation trend of A/H7N9 influenza viruses.

Study on DNA protection of polysaccharide and flavonoids in Artemisia annua L. from different areas with fluorescence probe / 中国药学杂志

OBJECTIVE: To investigate the DNA protection of polysaccharide and flavonoids in 14 kinds of Chinese herbs of Artemisia annua L. from different growing places such as Hunan, Chongqing, Beijing etc. METHODS: The fluorescence integration intensity of DNA, EB and extracts containing polysaccharide and flavonoids from 14 kinds of Artemisia annua L. were determined with EB as a sensitive fluorescence probe. Constant D was used to directly denote the degree of interaction between the drug molecules with DNA. According to the size of D, the protective action of polysaccharide and flavonoids on DNA was discussed. RESULTS: The order of interaction degree of polysaccharide in extracts with DNA was as follows; Hunan Huaihua > Beijing > Shanxi Yushe > Hunan (Xinzhou cultivation) > Shanxi Xinzhou cultivation in room > Chongqing (Xinzhou cultivation) > Hebei Fuping > Shanxi Dingxiang Nanzhuang > Chongqing > Shanxi Xinzhou Luye > Shanxi Yuxian > Shanxi Grey artemisia (Yangqu) ; The order of interaction of flavonoids in extracts with DNA through determination was as follows; Shanxi Xinzhou Luye > Hunan(Xinzhou cultivation) > Shanxi Xinzhou cultivation in room > Chongqing(Xinzhou cultivation) > Wild Artemisia(Shanxi Xinzhou) > Grey artemisia (Shanxi Yangqu) > Shanxi Dingxiang Nanzhuang > Chongqing > Hebei Fuping > Beijing > Shanxi Yushe > Iron rod Artemisia(Shanxi Xinzhou) > Shanxi Yuxian > Hunan Huaihua. The interaction of artemisia polysaccharide and flavonoids with DNA showed a definite dose-effect relationship. CONCLUSION: The extracts of Artemisia annua L. could interact with DNA, but the degree of interaction was different. The bigger the D was, the stronger the interaction was. Copyright 2012 by the Chinese Pharmaceutical Association.

Expression and significance of serum ghrelin level and ovarian tissue growth substance in a rat model of polycystic ovary syndrome / 解放军医学杂志

Objectives To investigate the relationship between ghrelin and estrous cycle and the expression and significance of ghrelin in the ovary and endometrium of rat models of polycystic ovary syndrome (PCOS). Methods A total of 44 eight-week-old SD rats were selected for the present study. Insulin and human chorionic gonadotrophin (HCG) were used in 24 rats to reproduce PCOS model, whereas the remaining 20 were given similar amount of normal saline as the control group. The immunohistochemical method was used to detect the ghrelin expression in the ovary and endometrium of these two groups, whereas ELISA was adopted to determine serum ghrelin levels during different estrous cycles, and also before and after fasting. Results Significant differences in the serum ghrelin levels were observed between before and after fasting in the PCOS rat models (P=0.004). The serum ghrelin levels during different estrous cycles showed periodic variations in the control rats, but without significant difference (P=0.084). The serum ghrelin level of the PCOS model group was lower than that in the control group, but without significant statistical difference (P=0.067). Ghrelin expression could be seen in the ovarian tissue during the whole estrous cycle of rats in the control group. In particular, the expression was significantly elevated at metestrus. The ghrelin expression in the model group was significantly reduced compared with the control group during different estrous cycles (P=0.031). No ghrelin expression was found in the endometrium of rats in the two groups. Conclusions Ghrelin expression may fluctuate periodically during the estrous cycle, and its highest level occurs at the metestrus. Ghrelin may be related to the corpus luteum function, and has no evident relation with the endometrial function.