[Evaluation of the Normal Structures of Parotid Duct Using Magnetic Resonance Hydrography].

Objective To investigate the normal structures of parotid duct by using magnetic resonance(MR)hydrography. Methods MR three-dimensional heavy T2-weighted imaging was performed in 21 normal subjects.After taking 200 mg of vitamin C orally for 3 minutes,the subjects underwent parotid duct coronal hydro-magnetic resonance imaging.The images were transferred to the GE AW4.5 workstation,on which multi-planner reformation was performed using Functool software.The numbers of the parotid duct,accessory parotid duct,segments,and its branches was counted and the length and diameter of the intra-and extra-parotid ducts were measured. Results Accessory ducts were found in 24 parotid glands(57.1%,24/42),with the average length being(9.54±9.98)mm and the average diameter being(0.87±0.88)mm.The intra-parotid ducts were found to be with 3 segments were in 3 cases(7.14%,3/42),with 2 segments in 19 cases(45.23%,19/42),and with 1 segment in 20 cases(47.62%,20/42).The average number of the branches of the first,second and third segment was 2.38,0.88,and 0.1,respectively.The average length of the intra-parotid duct was(36.97±7.97)mm,with its average diameter being(2.01±0.76)mm.The average length of extra-parotid duct was(34.98±10.25)mm,with its average diameter being(2.13±0.79)mm.The average length of the whole parotid duct was(71.95±11.47)mm,with its average diameter being(2.07±0.68)mm. Conclusion The parotid duct,the accessory parotid duct,and the segments and their branches of the intra-parotid duct can be accurately displayed by MR hydrography.

Novel naftopidil derivatives containing methyl phenylacetate and their blocking effects on α1D/1A-adrenoreceptor subtypes.

α1-Adrenoceptor (α1-AR) antagonists are considered to be the most effective monotherapy agents for lower urinary tract symptoms associated with benign prostatic hyperplasia (LUTS/BPH). In this study, we synthesized compounds 2-17, which are novel piperazine derivatives that contain methyl phenylacetate. We then evaluated the vasodilatory activities of these compounds. Among them, we found that compounds 2, 7, 12, which contain 2-OCH3, 2-CH3 or 2, 5-CH3, respectively, exhibited potent α1-blocking activity similar to protype drug naftopidil (1). The antagonistic effects of 2, 7, and 12 on the (-)-noradrenaline-induced contractile response of isolated rat prostatic vas deferens (α1A), spleen (α1B) and thoracic aorta (α1D) were further characterized to assess the sub receptor selectivity. Compared with naftopidil (1) and terazosin, compound 12 showed the most desirable α1D/1A subtype selectivity, especially improved α1A subtype selectivity, and the ratios pA2 (α1D)/pA2 (α1B) and pA2 (α1A)/pA2 (α1B) were 17.0- and 19.5-fold, respectively, indicating less cardiovascular side effects when used to treat LUTS/BPH. Finally, we investigated the chiral pharmacology of 12. We found, however, that the activity of enantiomers (R)-12 and (S)-12 are not significantly different from that of rac-12.

[Research on the Source Identification of Mine Water Inrush Based on LIF Technology and PLS-DA Algorithm].

Rapid source identification of mine water inrush has great significance for early warning and rescuing after the mine water inrush. Conventional method taking the concentration of ions as the discriminant factor takes such a long time that a method of rapid source identification of mine water inrush is in urgent need. This method is combined with Laser induced fluorescence (LIF) technology and Partial Least Squares-Discriminant Analysis (PLS-DA) algorithm. In the experiment, 405 nm laser was used to excite the water and 100 groups of fluorescence spectrum from 5 different aquifer of the mine were obtained. According to the spectra curve features, the data was compressed to obtain proper spectral data. 15 groups of spectrum of each water inrush samples were applied, with a total of 75 groups of spectrum as the prediction set while the rest of 25 groups of spectrum as the test set. To verify the experimental result, an experimental model was built with soft independent modeling of class analogy (SIMCA) to compare with PLS-DA. The result shows that the fluorescence spectra of different aquifer water samples is of great difference, without any pre-treatment, the PLS-DA algorithm based on the PLS model has higher modeling accuracy compared with SIMCA algorithm, which reaches to 100%, the validation results and the correlation of separation of variables are both more than 0.951, the RMSECV and RMSEP are both less than 0.123, using the model to identify the 5 water samples of test set, the accuracy are up to 100%.

[Research on the Source Identification of Mine Water Inrush Based on LIF Technology and SIMCA Algorithm].

Rapid source identification of mine water inrush is of great significance for early warning and prevention in mine water hazard. According to the problem that traditional chemical methods to identify source takes a long time, put forward a method for rapid source identification of mine water inrush with laser induced fluorescence (LIF) technology and soft independent modeling of class analogy (SIMCA) algorithm. Laser induced fluorescence technology has the characteristics of fast analysis, high sensitivity and so on. With the laser assisted, fluorescence spectrums can be collected real-time by the fluorescence spectrometer. According to the fluorescence spectrums, the type of water samples can be identified. If the database is completed, it takes a few seconds for coal mine water source identification, so it is of great significance for early warning and post-disaster relief in coal mine water disaster. The experiment uses 405 nm laser emission laser into the 5 kinds of water inrush samples and get 100 groups of fluorescence spectrum, and then put all fluorescence spectrums into preprocessing. Use 15 group spectrums of each water inrush samples, a total of 75 group spectrums, as the prediction set, the rest of 25 groups spectrums as the test set. Using principal component analysis (PCA) to modeling the 5 kinds of water samples respectively, and then classify the water samples with SIMCA on the basis of the PCA model. It was found that the fluorescence spectrum are obvious different of different water inrush samples. The fluorescence spectrums after preprocessing of Gaussian-Filter, under the condition of the principal component number is 2 and the significant level α = 5%, the accuracy of prediction set and testing set are all 100% with the SIMCA to classify the water inrush samples.

Piperazine-Derived α1D/1A Antagonist 1- Benzyl-N- (3-(4- (2-Methoxyphenyl) Piperazine-1-yl) Propyl) -1H- Indole-2- Carboxamide Induces Apoptosis in Benign Prostatic Hyperplasia Independently of α1-Adrenoceptor Blocking.

Previous studies have indicated that α1D/1A antagonist naftopidil (NAF) suppresses prostate growth by decreasing cell proliferation without affecting apoptosis and prostate volume in benign prostatic hyperplasia (BPH). A NAF-derived α1D/1A antagonist 1- benzyl-N-(3-(4-(2-methoxyphenyl) piperazine-1-yl) propyl)-1H-indole-2- carboxamide (HJZ-12) has been reported from our laboratory, which exhibits high subtype-selectivity to both α1D- and α1A- AR (47.9- and 19.1- fold, respectively) with respect to a1B-AR in vitro. However, no further study was conducted. In the present study, a pharmacological evaluation of HJZ-12 in BPH was performed on an estrogen/androgen-induced rat BPH model and human BPH-1 cell line. In vivo, HJZ-12 exhibited better performance than NAF in preventing the progression of rat prostatic hyperplasia by not only decreasing prostate weight and proliferation (similar to NAF) but also, shrinking prostate volume and inducing prostate apoptosis (different from NAF). In vitro, HJZ-12 exhibited significant cell viability inhibition and apoptotic induction in BPH-1 cell line, without presenting cell anti-proliferation properties. Intriguingly, the role of HJZ-12 on cell viability and apoptosis was an α1-independent action. Furthermore, RNA-Seq analysis was applied to screen out six anti-apoptotic genes (Bcl-3, B-lymphoma Mo-MLV insertion region 1 [Bmi-1], ITGA2, FGFR3, RRS1, and SGK1). Amongst them, Bmi-1 was involved in the apoptotic induction of HJZ-12 in BPH-1. Overall, HJZ-12 played a remarkable role in preventing the progression of prostatic hyperplasia through α1-independent apoptotic induction, indicating that it will be a multi-target effective candidate for BPH treatment.

Inhibitory effect of α1D/1A antagonist 2-(1H-indol-3-yl)-N-[3-(4-(2-methoxyphenyl) piperazinyl) propyl] acetamide on estrogen/androgen-induced rat benign prostatic hyperplasia model in vivo.

Benign prostatic hyperplasia (BPH) is a common disorder of the urinary system in aging men. 2-(1H-indol-3-yl)-N-[3-(4-(2-methoxyphenyl) piperazinyl) propyl] acetamide (HJZ-3), which is derived from naftopidil, exhibited 97.7- and 64.6-fold greater inhibitory effects for a1D adrenoceptor than for a1B- and a1A-adrenoceptors in vitro, respectively. To investigate the therapeutic potential for treating BPH, we evaluated the pharmacological activity of HJZ-3. Specifically, we evaluated through estrogen/androgen-induced rat benign prostatic hyperplasia model in vivo. HJZ-3 effectively prevented the progression of rat prostatic hyperplasia by suppressing the increase in prostate index and reducing the quantitative analysis of the relative acinus volume, relative stroma, epithelial volume and epithelial thickness and expression of proliferating cell nuclear antigen and α-smooth muscle actin. HJZ-3 decreased α1A- and α1D-adrenoceptor protein expressions in prostate tissue. HJZ-3 is a good alternative for α1A- and α1D-adrenoceptor blocker. It may relax smooth muscle tone and relieve symptoms of BPH.