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To analyze the medication rules for oligoasthenozoospermia (OAZ) observed by Wang Qi, an academician, master of Traditional Chinese Medicine (TCM) and initiator of andrology in TCM.We collected the outpatient cases of OAZ treated by Wang Qi and established a database of clinical medical records using the TCM Inheritance Auxiliary Platform. Employing the integrated rule-based system for analysis of the software, we modified the mutual information method, complex system entropy clustering analysis and other data mining methods, and summarized the medication rules Wang Qi followed in the treatment of OAZ.A total of 134 prescriptions made by Wang Qi for the treatment of OAZ were collected, involving 110 TCM drugs, which are mainly neutral and warm in nature and taste sweet and mostly act through the liver and kidney meridians. The core formula ingredients of the prescriptions included Morinda officinalis, Cuscuta chinensis, Lycium barbarum, Mulberry, Angelica sinensis, Astragalus mongholicus and Fish Maw, and most frequently Morinda officinalis, Cuscuta chinensis, Lycium barbarum and Mulberry.Wang Qi holds that kidney deficiency, dampness-heat, blood stasis and toxin are the main pathogenic factors for OAZ. The basic treatment of OAZ is to invigorate the kidney and replenish the essence, and meanwhile activate blood circulation, dissipate stasis and eliminate dampness-heat.

To investigate the effect of Bazi Granules on sperm quality in male rats with oligoasthenozoospermia (OAS) induced by multi-glycosides of tripterygium wilfordii (GTW).Thirty-six SD male rats were randomly divided into six groups of equal number: normal control, OAS model control, Wuziyanzong Pills (WYP), and low-, medium- and high-dose Bazi. The OAS model was established in the rats except those of the normal control group by intragastrical delivery of GTW at 30 mg/kg/d for 40 days. From the 41st day, the animals of the normal and OAS model control groups were fed with distilled water, those of the WYP group treated by gavage with WYP at 1.02 g/kg/d, and those of the low-, medium- and high-dose Bazi groups intragastically given Bazi Granules 3 (5.27 g/kg), 6 (10.54 g/kg) and 12 (21.08 g/kg) times, respectively, that of the human-equivalent dose. Semen parameters and the contents of superoxide dismutase (SOD) and malondialdehyde (MDA) in the testis tissue were determined after 28 days of treatment.After treatment, the rats of the of the high-, medium- and low-dose Bazi groups, compared with the OAS model controls, showed significant increases in sperm concentration (［1 050.71 ± 203.71］, ［1 370.06 ± 166.01］ and ［1 302.53 ± 476.51］ vs ［617.01 ± 237.08］ ×10⁶/ml, P0.05), sperm motility (［0.56 ± 0.24］%, ［0.73 ± 0.14］% and ［0.70 ± 0.23］% vs ［0.07 ± 0.05］%, P0.05), sperm average path velocity (［85.71 ± 30.35］, ［83.83 ± 10.31］ and ［75.06 ± 19.70］ vs ［43.45 ± 38.74］ μm/s, P0.05), sperm curvilinear velocity (［101.76 ± 23.28］, ［119.60 ± 21.22］ and ［102.11 ± 32.89］ vs ［53.63 ± 47.91］ μm/s, P0.05), sperm straight line velocity (［62.75 ± 7.63］, ［67.80 ± 5.05］ and ［64.11 ± 12.03］ vs ［40.18 ± 36.86］ μm/s, P0.05), and the SOD level (［380.23 ± 75.07］, ［349.53 ± 97.48］ and ［415.07 ± 72.01］ vs ［304.62 ± 27.17］ U/mg, P0.05), but a remarkable decrease in the MDA level (［0.33 ± 0.16］, ［0.22 ± 0.05］ and ［0.34 ± 0.22］ vs ［0.73 ± 0.20］ nmol/mg, P0.05).Bazi Granules can significantly improve the sperm quality of OAS rats, which may be related to its abilities of repairing oxidative stress injury and enhancing oxidation resistance.

Amyloid-β (Aβ) and tau protein are two crucial hallmarks in Alzheimer's disease (AD). Their aggregation forms are thought to be toxic to the neurons in the brain. A series of new 1,2,3,4-tetrahydro-1-acridone analogues were designed, synthesized, and evaluated as potential dual inhibitors for Aβ and tau aggregation. In vitro studies showed that compounds 25-30 (20 μM) with N-methylation of the quinolone ring effectively inhibited Aβ1-42 aggregation by 84.7%-99.5% and tau aggregation by 71.2%-101.8%. Their structure-activity relationships are discussed. In particular, 30 could permeate the blood-brain barrier, bind to Aβ1-42 and tau, inhibit Aβ1-42 β-sheets formation, and prevent tau aggregation in living cells.

A series of 2-arylethenyl-N-methylquinolinium derivatives were designed and synthesized based on our previous research of 2-arylethenylquinoline analogues as multifunctional agents for the treatment of Alzheimer's disease (AD) (Eur. J. Med. Chem. 2015, 89, 349–361). The results of in vitro biological activity evaluation, including β-amyloid (Aβ) aggregation inhibition, cholinesterase inhibition, and antioxidant activity, showed that introduction of N-methyl in quinoline ring significantly improved the anti-AD potential of compounds. The optimal compound, compound a12, dramatically attenuated the cell death of glutamate-induced HT22 cells by preventing the generation of ROS and increasing the level of GSH. Most importantly, intragastric administration of a12•HAc was well tolerated at doses up to 2000 mg/kg and could traverse blood-brain barrier.

A series of disubstituted bis(vinylquinolinium)benzene derivatives were designed, which were prepared through a facile three-component one-pot reaction in good yield. FRET results showed that 1,3-disubstituted benzene derivatives had much stronger stabilization effect on G-quadruplex DNA than that of 1,4-disubstituted benzene derivatives. The introduction of substituted amine side chain at quinolinium obviously increased the binding affinity of compounds to G-quadruplex DNA. It was also found that 1,3-disubstituted benzene derivatives and 1,4-disubstituted benzene derivatives had different effects on the conformation of G-quadruplex DNA by CD spectroscopy analysis. The differences for the interactions of these two classes of compounds with G-quadruplex were further studied and elaborated through molecular modeling experiments.

Additive-free bulk Si-B-N-C ceramics were prepared by pyrolysis of preceramic precursor (PBS-Me), which mainly involves cross linking, warm-pressing and pyrolysis. The density of crack-free bulk ceramic attains 1.94 g/cm3 when Calcined at 1300 °C. The shaped workpieces exhibit amorphous structure even be pyrolysised at 1400°C in N2, and there are some pores existing in the green body derived from warm-pressing and the resulting Si-B-N-C ceramic body, and these pores allow the gaseous byproducts be expeled from bodies. The pyrolyzed samples were studied by high temperature thermo gravimetric analysis, it shows that the Si-B-N-C body had an excellent high temperature resistance.

The on-line estimation of some key hard-to-measure process variables by using soft-sensor technique has received extensive concern in industrial production process. The precision of on-line estimation is closely related to the accuracy of soft-sensor model, while the accuracy of soft-sensor model depends strongly on the accuracy of modeling data. Aiming at the special character of the definition for outliers in soft-sensor modeling process, an outlier detection method based on k-nearest neighbor (k-NN) is proposed in this paper. The proposed method can be realized conveniently from data without priori knowledge and assumption of the process. The simulation result and practical application show that the proposed outlier detection method based on k-NN has good detection effect and high application value.

Up-regulation of a disintegrin and metalloproteinase 10 (ADAM10) to prevent the formation of β-amyloid (Aβ) peptides might be a promising strategy to treat Alzheimer's disease (AD). RNA G-quadruplex motif within the 5'-UTR of the ADAM10 mRNA is an inhibitory element for ADAM10 translation. Thus, mitigation of the suppressive effect of this motif using an RNA G-quadruplex-forming G-rich sequence (QGRS) binder might be a new approach for AD therapy. Herein, a series of new methylquinolinium derivatives were synthesized and screened by surface plasmon resonance (SPR) and the dual-luciferase reporter assay. Among them, compound 24 showed selective affinity for the QGRS of ADAM10 and could strongly up-regulate the translation of it. Moreover, treatment with 24 led to a significant increase of the secretion of sAPPα, consequently decreasing the Aβ40 in cellular. These results illustrate that the interaction between the RNA QGRS and a small molecule may be a new molecular strategy to modulate the translation of ADAM10.

To investigate the protective effects of Jiedu Tongluo injection on cerebral edema induced by focal lesion of cerebral ischemia/reperfusion, the hydrous content of brain and the expressions of intercellular adhesion molecule-1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1), E-selectin and MMP-9 in rats.The model of brain middle cerebral artery ischemia/reperfusion was established by the thread approach. After 24 hours of reperfusion, cerebral edema formation was determined by the hydrous content of brain. The permeability of blood brain barrier was evaluated based on the leakage of Evans blue. Enzyme-linked immunoadsordent assay (ELISA)was used to examine the expression of ICAM-1, VCAM-1, E-selectin. The expression of MMP-9 was measured by immunohistochemistry.JDTL, in the dose of 2 mL x kg(-1) and 4 mL x kg(-1), relieved cerebral edema (P0.05, P0.01), reduced the expressions of ICAM-1, VCAM-land E-selectin and decreased MMP-9 activity (P0. 05, P0.01) in model rats.Jiedu Tongluo injection has a protective effect on rat brain from cerebral edema induced by the injury of focal cerebral ischemia/reperfusion. The mechanism is related to that Jiedu Tongluo injection can reduce the expressions of ICAM-1, VCAM-1 and E-selectin and inhibit of MMP-9 activation in rat brain.

A highly reproducible and broad plasma absorption band nano-silver film was prepared by electrostatic self-assembly technology. The size of nano-silver particles on the surface of silver film, in the scanning electron microscopy (SEM) micrograph, is in a wide distribution from 18 to 200 nm. At the same time, the ultraviolet-visible spectrophotometer was employed to detect the nano-silver film. There is a broad plasma absorption band in the UV-Vis spectrum. To test the SERS activity of the nano-silver film, crystal violet and serum of healthy person were used as probe molecules and the high quality SERS spectra were obtained.