Adipates ; analysis ; Air Pollutants, Occupational ; analysis ; Esters ; analysis ; Gas Chromatography-Mass Spectrometry ; methods ; Phthalic Acids ; analysis ; Workplace

By using the pharmacophore model of mineralocorticoid receptor antagonists as a starting point, the experiment stud- ies the method of traditional Chinese medicine formula design for anti-hypertensive. Pharmacophore models were generated by 3D-QSAR pharmacophore (Hypogen) program of the DS3.5, based on the training set composed of 33 mineralocorticoid receptor antagonists. The best pharmacophore model consisted of two Hydrogen-bond acceptors, three Hydrophobic and four excluded volumes. Its correlation coefficient of training set and test set, N, and CAI value were 0.9534, 0.6748, 2.878, and 1.119. According to the database screening, 1700 active compounds from 86 source plant were obtained. Because of lacking of available anti-hypertensive medi cation strategy in traditional theory, this article takes advantage of patent retrieval in world traditional medicine patent database, in order to design drug formula. Finally, two formulae was obtained for antihypertensive.
Antihypertensive Agents ; chemistry ; pharmacology ; Databases, Factual ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Medicine, Chinese Traditional ; methods ; Mineralocorticoid Receptor Antagonists ; chemistry ; pharmacology ; Models, Molecular

Administration, Inhalation ; Bronchiolitis ; drug therapy ; Bronchodilator Agents ; administration & dosage ; therapeutic use ; Budesonide ; administration & dosage ; therapeutic use ; Female ; Humans ; Infant ; Male ; Poly I-C ; administration & dosage ; therapeutic use

BackgroundIt has been well-known that integrin linked kinase(ILK) plays an important role in the pathogenesis of neorascularization.But there are few researches to elucidate the relationship between ILK and retinal nevascularization. Objective This study was to explore the expression and significance of ILK on retinal neovascularization and new vessels regression in the oxygen-induced retinopathy(OIR) mouse model. Methods One hundred and twenty-eight 7-day-old C57BL/6J mice were randomly divided into the normal group and model group.The mice were rose in(75±2)％O2 environment with mother mice together for 5 days and then in normal environment for 5 days to establish the OIR models.The mice in normal group were rose in the normal environment for 21 days.The 17-day-old mice were sacrificed and retinal sections were prepared for histopathological examination and the numbers of the cellular nuclei of vascular endotheliumbreaking retinalinternal limiting membranewere calculated.Retinal sections and sheeting were prepared in 12,14,17 and 21 -day-old mice to examine the formation and regression of new blood vessel using ADP histochemistry staining,and then immunochemistry,real-time PCR and Western-blotting were used to detect the expressions of ILK and its mRNA in retina. ResultsThe numbers of the cellular nuclei of vascular endothelium breaking retinal internal limiting membrane were (45.64 ± 12.17 )in OIR group,and those of the normal group were( 0.35±0.14 )with a significant difference between two groups (t =22.85,P＜0.05).Retinal new blood vessel appeared in 14-day mice,and peaked in 17-day mice and then regression in 21-day mice.ILK protein was expressed mainly in retinal ganglion cell layer,inner nuclear layer,inner plexiform layer and photoreceptor layer.Real-time PCR showed that ILK mRNA expressing levels in retina in model group were( 1.00±0.22),(1.85±0.17),(1.58±0.43) and(1.53±0.36) respectively in 12-,14-,17- and 21-day mice.Westernblotting determined that the A value of the ILK/β-actin was increased in 12-,14-,17-day mice and decreased in 21-day mice,and the A values were significantly higher in model group than the control group in various aged mice ( t =2.97,P＜0.05 ;t =11.88,P＜0.01 ;t =16.84,P＜0.01 ;t =13.00,P＜0.01 ). ConclusionsThese results indicate a space-time corresponding relation between the expression of ILK and retinal neovascularization.The obvious positive expression of ILK may be highly correlated with retinal neovascularization.

Objective To study the variation of the pancreatic head arteries and its value in pan- creas transplantation.Methods The DSA data of 300 cases were studied retrospectively:192 cases of celiac trunk angiography,102 cases of superior mesenteric artery angiography,and 6 cases of the com- bined.The distribution and variation of the arteries on the pancreatic head were observed.Results In the celiac angiography cases,typical gastroduodenal artery,superior pancreaticoduodenal artery and its branches were visualized in 73 cases(38%).The posterior superior panereaticoduodenal artery was not anastomosed with the posterior inferior pancraticoduodenal artery in 3 cases.The posterior pancre- aticoduodenal arcade was discontinued in 1 case.The anterior superior pancreaticoduodenal artery, posterior superior pancreaticodoodenal artery,and dorsal pancreatic artery were only distributed across the upper head of the pancreas separately but were not anastomosed each other in 1 case.The variation rate of pancreaticoduodenal arterial arcades was 6.8%(5/73).In 102 cases of the superior mesenteric artery angiography,the inferior pancreaticoduodenal artery was visualized in 42 cases(41%)while its branches were not visualized.In 6 cases of the combined angiography,superior panereaticoduodenal artery was visualized in all of the cases,of which anterior and posterior arcades were visualized in 4 cases(66.7%).The gastroduodenal artery reconstruction was performed in 3 cases of clinical pancre- as transplantation,all of the receivers maintained a normal blood glucose level after transplantation and no surgical complications were found.Conclusions The superior pancreaticoduodenal artery might of- fer more blood supply than inferior pancreaticoduodenal artery in the pancreatic head.The arterial re- construction of the transplanted pancreas should include the gastroduodenal artery because of the pos- sibility of arterial variation on the pancreatic head.

Objective To observe the influence of coal burning fluorosis on learning and memory ability in rats and reveal its possible mechanisms. Methods Healthy 48 SD rats were divided into control, low-fluoride and high-fluoride group. All rats in fluoride exposed groups were fed with the eom polluted by drying processes with burning coal containing high level of fluoride obtained from the endemic fluorosis area to produce the animal model of fluorosis. The experiment period were 3,6 mouths, respectively. The ability of leaning and memory was measured by Morris test and cholinesterase activity detected by photometric method at 3 or 6 month after experiment, respectively. Results Fluoride contents signifieantlly influenced the escape latency, the numbers of crossing the platforms and the time of staying the platforms(the value of F was 29.29,6.47,6.50, respectively, P<0.01).In addition, the numbers of crossing the platforms and the time of staying the platforms were influenced by the exposed time(the value of F was 16.11,45.59, P<0.01). Furthermore, the fluoride contents and the exposed time had an interaction between the numbers of crossing the platforms and the time of staying the platforms (the value of F was 4.67,5.68, P<0.05 or<0.01). Three months after the experiment, the mean values of escape latency [(14.71± 4.85)s] of rats in highly fluoride exposed group were significantly prolonged as compared with controls [(9.28±4.22)s]; 6 month after the experiment, the mean values of escape latency[(12.42±8.03)s, (17.48± 8.05)s] of rats in both groups exposed to fluoride were significantly prolonged as compared to controls [(7.04± 3.29)s, P<0.05]. The decreased numbers of crossing the platforms[(1.62±0.87)number] and the declined time of staying the platforms[(16.70±5.02)s] were found in the rats exposed to high fluoride as compared to controls [(3.53±1.67 )number, (23.33±5.35)s, P<0.05]. The fluoride contents obviously influenced the activities of acetylcholinesterase and butylcolinesterase (the value of F was 12.83,13.27, P<0.01). On the other hand, the times of breeding also influnced the activities of butylcolinesterase (the value of F was 16.26, P<0.01). In 3 months of the experiment, the activities of butylcolinesterase [(0.55±0.12)kU/g] in low fluoride exposed group were significantly decreased in comparison with controls[(0.73±0.10)kU/g, P<0.05]. The activities of acetylcholinesterase[(0.62±0.42)kU/g] and butylcolioesterase[(0.58±0.10)kU/g] in high fluoride group were significantly decreased as compared to eontrois[(1.41±0.52), (0.73±0.10)kU/g, P<0.05]. The correlation analysis showed that there was a negative correlation between the cholinesterase and the escape latency(r=-0.68, P< 0.01), and a positive correlation between the cholinesterase and the time of staying the platforms(r=0.57, P< 0.01). Conclusions The ability of learning and memory in rats with coal buring fluorosis was decreased, which might be connected to the decreased activity of cholinesterase in a dose-effect correlation.

Humans ; Lead ; toxicity ; Male ; Reproduction ; drug effects ; Sperm Count ; Sperm Motility ; drug effects

OBJECTIVETo provide inspiration and ideas for clinical treatment of coronary heart disease (CHD) by data mining technology based frequency analysis and cluster analysis of medical records, prescriptions and herbs in treating CHD by distinguished veteran doctors of traditional Chinese Dedicine (TCM).

METHODSTotally 386 medical cases were retrieved from Wanfang Data, Chinese Scientific Journals Database (VIP medical information resources system, China National Knowledge Infrastructure (CNKI), and Typical Collections of Medical Cases by Contemporary Distinguished Veteran Doctors of Traditional Chinese Medicine. They input into database trimmed after unified standard. Medication laws of CHD by distinguished veteran doctors of TCM were analyzed using frequency analysis and cluster analysis, and so on.

RESULTSDistinguished veteran doctors of TCM frequently used top ten herbs in treatment of C D as Salvia miltiorrhiz , Ligusticum wallichii, Trichosanthes kirilowi, Pinellia ternat, Angelica sinensis, Poria coco stragalu , Panax ginseng, Allium macrostemon, and Radix Ophiopogonis. Cluster analysis summarized that there were 16 herb pairs commonly used, 7drug assemblies consisting of 3 herbs and 5 drug assemblies consisting of multiple herbs.

CONCLUSIONSDistinguished veteran doctors of TCM mainly used herbs assemblies capable for invigorating Pi to resolve phlegm, and promoting qi and activating blood circulation in treating CHD. Meanwhile, they concurrently used herbs combination of nourishing Xin and tranquilization, and regulating yin and yang.

China ; Cluster Analysis ; Coronary Artery Disease ; therapy ; Data Mining ; Databases, Factual ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Medicine, Chinese Traditional

Adult ; Female ; Fungi ; Humans ; Laryngitis ; microbiology ; Mycoses ; Vocal Cords ; microbiology

The combined application of statins that inhibit HMG-CoA reductase and fibrates that activate PPAR-α can produce a better lipid-lowering effect than the simple application, but with stronger adverse reactions at the same time. In the treatment of hyperlipidemia, the combined administration of TCMs and HMG-CoA reductase inhibitor in treating hyperlipidemia shows stable efficacy and less adverse reactions, and provides a new option for the combined application of drugs. In this article, the pharmacophore technology was used to search chemical components of TCMs, trace their source herbs, and determine the potential common TCMs that could activate PPAR-α. Because there is no hyperlipidemia-related medication reference in modern TCM classics, to ensure the high safety and efficacy of all selected TCMs, we selected TCMs that are proved to be combined with statins in the World Traditional/Natural Medicine Patent Database, analyzed corresponding drugs in pharmacophore results based on that, and finally obtained common TCMs that can be applied in PPAR-α and combined with statins. Specifically, the pharmacophore model was based on eight receptor-ligand complexes of PPAR-α. The Receptor-Ligand Pharmacophore Generation module in the DS program was used to build the model, optimize with the Screen Library module, and get the best sub-pharmacophore, which consisted of two hydrogen bond acceptor, three hydrophobic groups and 19 excluded volumes, with the identification effectiveness index value N of 2. 82 and the comprehensive evaluation index CAI value of 1. 84. The model was used to screen the TCMD database, hit 5,235 kinds of chemical components and 1 193 natural animals and plants, and finally determine 62 TCMs. Through patent retrieval, we found 38 TCMs; After comparing with the virtual screening results, we finally got seven TCMs.
Acyl Coenzyme A ; metabolism ; Animals ; Databases, Factual ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Hydrophobic and Hydrophilic Interactions ; Hydroxymethylglutaryl-CoA Reductase Inhibitors ; chemistry ; pharmacology ; Lipid Metabolism ; drug effects ; Lipids ; blood ; Medicine, Chinese Traditional ; Models, Molecular ; Quantitative Structure-Activity Relationship ; Technology