Objective: To study the synthesis and antibacterial activity of 7 substituted 1 (2 fluoroethyl) 6,8 difluoro 1, 4 dihydro 4 oxo 3 quinolone carboxylic acid compounds. Methods: The title compounds were synthesized by condensation,cyclization, nucleophilic substitution. Antibacterial activity in vitro was determined with 6 kinds of common pathogenic bacteria. Results: Eleven compounds of 7 substituted 1 (2 fluoroethyl) 6,8 difluoro 1,4 dihydro 4 oxo 3 quinolone carboxylic acid were designed and synthesized. These compounds were firstly reported. The chemical structures of all compounds were determined by IR, 1HNMR and elementary analysis. CompoundⅠ 1,Ⅰ 2,Ⅱ 4 showed better antibacterial activities than that of fleroxacin. Conclusion: Some of the title compounds show potent antibacterial activities and should be further studied. [

In this research,we chiefly explored a new fast test method--microtox technology to evaluate the comprehensive toxicity of Shen Mai injection.We investigated characteristic parameters of vibrio fischeri (CS234) under different conditions in the pursuit of the optimum test parameters of the reliable method;and then locked the best parameters for Shen Mai injection assay with the products from different manufacturers by microtox fast test.As a result,the optimum reaction condition included 0.9 mL recovery liquid in each freeze-dried vial and 50 μL bacteria suspension of each sample within 2 mL solution in aggregate with 10-mins detection after adding bacteria suspension which pH value ranging from 5 to 10 and luminous intensity from 0.8 to 1.2 million in 10 mins.The relative standard deviation values of replication experiment and precision test were all below 15％.Under this optimum detection condition,it was found that the EC50 values were 35.60％,92.34％ and 146.57％,differing among the samples from three representative drug manufacturers,respectively (P ＜ 0.01).In conclusion,the concentration-effect relationship of Shen Mai injection existed in the toxicity assessment of vibrio fischeri with various ECs0 values from the three manufacturers.These results suggested that biological detection standards of Shen Mai injection presented great growth potential.Microtox-based fast test in the evaluation of comprehensive toxicity of ShenMai injection showed favorable application prospects over controlling the quality of different sources of products.

Aim To observe effects of Seabuckthorn fatty acids on old rat ovarian granulosa cell apoptosis and expression of bcl-2 and fas,then discuss the adjustive effect of Seabuckthorn fatty acids on ovarian function of menopause.Methods 22 months old rats were randomly divided into 5 groups,estrogen control group,old control group,Seabuckthorn fatty acids group of high dose,middle dose and low dose.In addition,one young control group was made up of 3 months old rats.Rat ovarian granulosa cell apoptosis was detected by TUNEL.The expression of protein bcl-2 and protein fas were detected by immunohistochemistry,and bcl-2 mRNA and fas mRNA by in situ hybridization(ISH).Grey analyse was done using Q550CW image analyse system.Results Compared with the old rats control group,Seabuckthorn fatty acids of high dose,middle dose and low dose can differently restrain rat ovarian granulosa cell apoptosis,enhance the expression of protein bcl-2 and bcl-2 mRNA,weakened the expression of protein fas and fas mRNA.Conclusion Seabuckthorn fatty acids restrains ovarian granulosa cell apoptosis through adjusting the expression of bcl-2 and fas.Sequentially,it adjusts estrogen level and treats menopause syndrome.

Objective To investigate the chemical properties of superficial cardiac neurons. Methods By means of immunohistochemical ABC technique,the study was performed concerning the distribution of calcitonin gene-related peptide(CGRP) and substance P(SP) in the canine main cardiac superficial plexus. Results CGRP-immunoreactive(IR) neurons were found in every plexus,but SP-IR neurons could be observed only in dorsal atria plexus(DAP),inter atria plexus(IAP) and aorta-pulmonary plexus(A-PP).The shape and size of CGRP-IR and SP-IR neurons were similar.The comparative study on atria and ventricles indicated that CGRP-IR and SP-IR neurons in atria were more than those in ventricles.Numerous CGRP-IR,SP-IR nerve fibers could be observed in each fat pats and intermyocardiocytes.These nerve fibers were usually situated near blood vessels,or were attached to vessel wall.Somewhat CGRP-IR and SP-IR nerve fibers were connected with myocardiocytes in some regions.Conclusion The results indicated that actually existed two peptides in canine cardiac superficial plexus.These implied that the regulations of the two kinds of peptidergic neurons to atria and ventricle were different.The two kinds of neurons mentioned above were likely to perform different or similar functions in canine heart.CGRP and SP could possibly modulate the activities of myocardiocytes and vessels of heart directly.

Pyroptosis, a form of cell death associated with inflammation, is known to be involved in diabetic nephropathy (DN), and discoid domain receptor 1 (DDR1), an inflammatory regulatory protein, is reported to be associated with diabetes.However, the mechanism underlying DDR1 regulation and pyroptosis in DN remains unknown. We aimed to investigate the effect of DDR1 on renal tubular epithelial cell pyroptosis and the mechanism underlying DN. In this study, we used high glucose (HG)-treated HK-2 cells and rats with a single intraperitoneal injection of streptozotocin as DN models. Subsequently, the expression of pyroptosis-related proteins (cleaved caspase-1, GSDMD-N, Interleukin-1β [IL-1β], and interleukin-18 [IL-18]), DDR1, phosphorylated NF-κB (p-NF-κB), and NLR family pyrin domain-containing 3 (NLRP3) inflammasomes were determined through Western blotting. IL-1β and IL-18 levels were determined using ELISA. The rate of pyroptosis was assessed by propidium iodide (PI) staining. The results revealed upregulated expression of pyroptosisrelated proteins and increased concentration of IL-1β and IL-18, accompanied by DDR1, p-NF-κB, and NLRP3 upregulation in DN rat kidney tissues and HG-treated HK-2 cells. Moreover, DDR1 knockdown in the background of HG treatment resulted in inhibited expression of pyroptosis-related proteins and attenuation of IL-1β and IL-18 production and PI-positive cell frequency via the NF-κB/NLRP3 pathway in HK-2 cells. However, NLRP3 overexpression reversed the effect of DDR1 knockdown on pyroptosis. In conclusion, we demonstrated that DDR1 may be associated with pyroptosis, and DDR1 knockdown inhibited HG-induced renal tubular epithelial cell pyroptosis. The NF-κB/NLRP3 pathway is probably involved in the underlying mechanism of these findings.

Based on the theory of “manifestation-body and spirit-qi”， it is considered that the pathogenesis of tic disorders （TD） involves three manifestations of “wind， phlegm and fire”， with wind as the leading factor and phlegm and fire as the accompanying factors. It is advocated to identify the abnormality of body and spirit， summarize the evolution of manifestation， and prescribe flexibly based on qi movement of zang-fu organs. Among them， the common symptoms related to tics are mostly belong to wind symptoms， which originated from lung qi failing to purify and liver qi over-ascent. The method of soothing liver wood and purifying lung gold is adopted， and modified Xiaochaihu Decoction （小柴胡汤） and Cangerzi Powder （苍耳子散） are recommended； Patients with prolonged illness and strange symptoms are often mixed with phlegm， which stemmed from the fact that spleen failing to rise clear and stomach failing to downward turbid. The method of raising spleen-earth and lowering stomach-earth is adopted， and modified Yigong Powder （异功散） and Erchen Decoction （二陈汤） are recommended； Patients with severe symptoms are often mixed with fire symptoms， which originated from discordance of water and fire and hyperactivity of heart fire. The method of interacting heart and kidney and coordinating water and fire is adopted， and modified Xiegan Pill （泻肝丸） and Liuwei Dihuang Pill （六味地黄丸） are recommended， in order to regulate qi movement， harmonize body and spirit， and improve the symptoms.