Premature ejaculation (PE) is a common male sexual disorder with an incidence rate of 20-30%. Recent clinical trials have demonstrated that phosphodiesterase type 5 inhibitors (PDE5i), as the first-line drug for erectile dysfunction (ED), can improve ejaculatory function probably by acting on the peripheral and central adrenergic nerves. The possible action mechanisms of PDE5i may involve lessening of the central sympathetic output, modulation of the contractile responses from the vas deferens, seminal vesicles, prostate and urethra, induction of peripheral analgesia, and prolonging of the total erectile duration, increasing the confidence of ejaculation control, and reducing the post-ejaculation refractory time. This review discusses the possible mechanisms and clinical application of PDE5i in the treatment of PE.
Ejaculation ; drug effects ; Erectile Dysfunction ; drug therapy ; Humans ; Male ; Muscle Contraction ; Phosphodiesterase 5 Inhibitors ; therapeutic use ; Premature Ejaculation ; drug therapy ; Seminal Vesicles ; physiology ; Vas Deferens ; physiology

In this paper, we described basic connotations of comparative effectiveness research (CER), expounded the application of CER in chronic obstructive pulmonary disease (COPD). In addition, on the basis of research practice of Chinese medical treatment for COPD in recent years, we put forward the thought of the junction point of Chinese medicine in CER on COPD from the perspective in screening effective Chinese herbs, establishing treatment program/methods/technologies, and outcomes evaluation.
Comparative Effectiveness Research ; Humans ; Medicine, Chinese Traditional ; Outcome Assessment (Health Care) ; Pulmonary Disease, Chronic Obstructive ; therapy

Objective To investigate the protective effect of sevoflurane on the brain against focal ischemia-reperfusion(I/R)injury and its mechanism.Methods Twenty-four male SD rats weighing 250-300 g were randomly allocated into 3 groups(n=8 each):group Ⅰ sham operation;grouop Ⅱ I/R and group Ⅲ I/R + sevoflurane.The rats were anesthetized with intraperitoneal chloral hydrate 300 mg?kg~(-1).Middle cerebral artery occlusion(MCAO)was produced by insertion of a 4-0 mono-filament nylon thread with rounded tip at bifurcation of right common carotid artery into internal carotid artery.The nylon thread was advanced cranially until resistance was felt.The depth of insertion was 18-20 mm.After 3 h MCAO the thread was withdrawn to allow reperfusion.In group Ⅲ the animals inhaled 1.0 MAC sevoflurane for 30 min at 30 min before reperfusion.The rectal temperature of the animals was kept at 36.5-37.5℃.At the end of 24 h reperfusion the animals were weighed again.The animals'neurological deficit was evaluated using Zea Longa score(0=no defcit,4=unable to walk and unconscious).The animals were then killed.The neuronal apoptosis in striatum was assessed(TUNEL)and the PKC protein expression in striatum was determined by immunocyto-chemistry.Results The body weight of the animals in I/R group was significantly reduced after 24h reperfusion as compared to the body weight before ischemia (P＜0.01),while in control group and sevoflurane group there was no significant difference in the body weight before and after sham operation or I/R.The neurological deficit scores were significantly higher in I/R group than in sevoflurane group.The number of apoptotic neurons in striatum was significantly higher in I/R group than in sevoflurane group.The PKC expression in striatum was significantly higher in sevoflurane group than in I/R group (P＜0.01).Conclusion 1.0 MAC sevoflurane inhalation has protective effect on the brain against I/R injury. Upregulation of PKC expression in striatum decreased by I/R is involved in the mechanism.

To optimize the Scutellaria baicalensis extraction process, the filter paper method and the bacteriostatic ratio method were adopted to determine the in vitro bacteriostatic efficacy of water extracts and 60% alcohol extracts from S. baicalensis. The quantitative analysis of multi-components by single-marker (QAMS) was used to determined the contents of four active components, baicalin, wogonoside, baicalein and wogonin. In addition, with the bacteriostatic ratio and the overall desirability of the contents of four active components as indexes, the orthogonal experiment was adopted to detect the effect of water addition, extraction frequency and extraction time. The optimal extraction process was to add 12 times of water for the first time, 10 times of water for the second time, extract for 2 time, 2 h for each time. This optimization process is stable and feasible, with a higher bacteriostatic ratio in extracts.
Alcohols ; chemistry ; Anti-Bacterial Agents ; chemistry ; isolation & purification ; pharmacology ; Chemical Fractionation ; methods ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Scutellaria baicalensis ; chemistry ; Water ; chemistry

To offer the reference and method for salt damage in the cultivation of Marsdenia tenacissima, the seeds of M. tenacissima collected from Maguan city ( Yunnan province) were taken as the test materials to study the effects of different priming materials on improving germination and growth under high-level salt stress condition. Four different treatments, which were GA3, KNO3-KH2PO4, PEG-6000, NaCl, combined with ANOVA were applied to test the performance of germination energy, germination percentage, germination index, MDA, SOD, and CAT. The results showed that the seed germination was obviously inhibited under salt stress and the soaked seeds with different priming materials could alleviate the damage of salt stress. Under these treatments, the activities of SOD, CAT the content of soluble protein significantly increased. While the content of MDA significantly decreased. The maximum index was obtained when treated with 1.20% KNO3-KH2PO4, the germination percentage increased from 52.67% to 87.33% and the activity of SOD increased from 138.01 to 219.44 respectively. Comparing with the treatment of 1.20% KNO3-KH2PO4, the germination percentage of treating with 300 mg x L(-1) GA3 increased from 52.67% to 80.67%, while the activity of SOD increased from 138.01 to 444.61.
Germination ; drug effects ; physiology ; Marsdenia ; drug effects ; growth & development ; Nitrates ; pharmacology ; Polyethylene Glycols ; pharmacology ; Potassium Compounds ; pharmacology ; Seeds ; drug effects ; growth & development ; Sodium Chloride ; pharmacology ; Stress, Physiological ; Xanthones ; pharmacology

Objective To explore the best time point for the ipsilateral hepatocellular apoptosis and the contralateraI hepatic hypertrophy after selective portal vein embolization(SPVE)in rabbit.Methods In a randomized study design,forty rabbits were divided into 5 groups with 8 rabbits per-group,including one as the control and the other 4 were treated with SPVE during open surgery.The rabbits were killed postoperatively,in 3,7,14,21 days respectively after the embolization.The hepatic lobes volume,the ipsilateral hepatocellular necrosis rates and apoptosis index,and liver functions were determined as well. Results In the treatment groups,the average amount of the right liver volumes decreased from 46.4 cm~3 preoperatively to 46.0,44.4,42.0,39.7 cm~3 in groups of 3,7,14,21 days postoperatively;meanwhile,the left liver volumes increased from 54.0 cm~3 preoperatively to 54.5,56.3,61.7,63.9 cm~3 respectively during 3, 7,14,21 days after the procedures.The rates of future remaining live volumes(FRLV)increased from 53.8% preoperatively to 54.2%,55.9%,59.0%,61.0% at 3,7,14,21 days postoperatively.The apoptosis indexes of hepatocells from group A to E were 8.1%,12.2%,19.4%,20.1%,14.2% respectively.Conclusions SPVE leads to atrophy of the ipsilateral hepatic lobe and hypertrophy of contralateral lobe,indicating that hepatocytes undergone apoptosis,rather than necrosis.The time point is 7 to 14 days.

Objective:A fingerprint of raw material, extract ed and injections of radix notoginseng has been studied and provides the quality information.Method:Polaris C18-A column was used, with mixtu res of acetonitrile and water as mobile phase in a gradient mode. The wavelength of measurement was 203nm.Result:According to the selected chr omatographic conditions, a good fingerprint of radix notoginseng and its extract , preparation has been described.Conclusion:The method is simp le, accurate with good reproducibility. It may be practical value for the qualit y control of sample for radix notoginseng and its preparation.

Bicyclol with benzyl alcohol structure, is a poorly water-soluble drug, used for the treatment of chronic hepatitis B. To increase the drug solubility and oral bioavailability, a Bicyclol-phospholipid complex was studied on its preparation, formation mechanism, and the influence on drug physicochemical properties and oral absorption. The complex was prepared by a solvent evaporation method. The optimal formulation was selected by orthogonal experimental design, and a reasonable evaluating method of the complexation rate was established. Various methods, such as differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and 31P nuclear magnetic resonance (31P-NMR), were used to explore the phase state and formation mechanism of the complex. The solubility of drug in complex was investigated in water/n-octanol. Preliminary study of its absorption and liver tissue distribution in rats was also carried out. The results showed that Bicyclol and phosphatidylcholine can be complexed entirely in the molar ratio 1 : 2. Bicyclol was dispersed in phospholipids as amorphous state. They were combined by intermolecular hydrogen bond due to charge transfer effect which occurred between the two polarities of the double bond between phosphorus and oxygen (P=O) of phosphatidylcholine and benzalcohol group of Bicyclol. The solubility of the complex compared to the active pharmaceutical ingredient (API) was effectively enhanced 5.75 times in water and 7.72 times in n-octanol, separately. In addition, drug concentrations were also enhanced 43 times in plasma and 13 times in liver with one hour after administering the complex to rats via oral gavage. All of these indicated that Bicyclol with benzalcohol group can interact with phospholipids to form complex, improving drug's physicochemical properties, thus further increasing its absorption and target tissue distribution. This study also provided theoretical reference for the research of other benzalcohol derivatives complexed with phospholipids.
1-Octanol ; Animals ; Biological Availability ; Biphenyl Compounds ; pharmacokinetics ; Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Phospholipids ; pharmacokinetics ; Rats ; Solubility ; Spectroscopy, Fourier Transform Infrared ; Tissue Distribution ; X-Ray Diffraction

Astragalus membranaceus var. mongholicus and Hedysarum polybotrys belong to different genera, but have similar drug efficacy in traditional Chinese medicine theory, and H. polybotrys was used as the legal A. membranaceus var. mongholicus previously. In this study, similarities and differences between them were analyzed via their ITS/ITS2 fragments information. The ITS (internal transcribed spacer) regions were amplified using polymerase chain reaction and then sequenced in two-way. The alignment lengths of ITS regions were 616 bp, in which 508 loci were consistent, and 103 loci were different, accounting for 82.47% and 16.72% of the total ITS nucleotides in length, respectively. As genotype determines phenotype, 1HNMR-based metabolomic approach was further used to reveal the chemical similarities and differences between them. Thirty-four metabolites were identified in the 1H NMR spectra, and twenty-seven metabolites were the common components. Amino acids, carbohydrates and other primary metabolites were similar, while a large difference existed in the flavonoids and astragalosides. This study suggests that A. membranaceus var. mongholicus and H. polybotrys show similarities and differences from molecular and chemical perspectives, which has laid a foundation for elucidating the effective material basis of drug with similar efficacy and resources utilization.
Astragalus membranaceus ; chemistry ; genetics ; DNA, Plant ; genetics ; DNA, Ribosomal Spacer ; genetics ; Drugs, Chinese Herbal ; chemistry ; Fabaceae ; chemistry ; genetics ; Flavonoids ; chemistry ; Metabolome ; Metabolomics

The present study aims to predict the action targets of antidepressant active ingredients of Xiaoyaosan to understand the "multi-components, multi-targets and multi-pathways" mechanism. Using network pharmacology, the reported antidepressant active ingredients in Xiaoyaosan (saikosaponin A, saikosaponin C, saikosaponin D, ferulic acid, Z-ligustilide, atractylenolide I, atractylenolide II, atractylenolide III, paeoniflorin, albiflorin, liquiritin, glycyrrhizic acid and pachymic acid), were used to predict the targets of main active ingredients of Xiaoyaosan according to reversed pharmacophore matching method. The prediction was made via screening of the antidepressive drug targets approved by FDA in the DrugBank database and annotating the information of targets with the aid of MAS 3.0 biological molecular function software. The Cytoscape software was used to construct the Xiaoyaosan ingredients-targets-pathways network. The network analysis indicates that the active ingredients in Xiaoyaosan involve 25 targets in the energy metabolism-immune-signal transmutation relevant biological processes. The antidepressant effect of Xiaoyaosan reflects the features of traditional Chinese medicine in multi-components, multi-targets and multi-pathways. This research provides a scientific basis for elucidation of the antidepressant pharmacological mechanism of Xiaoyaosan.
Antidepressive Agents ; pharmacology ; Benzoates ; Bridged-Ring Compounds ; Coumaric Acids ; Drug Evaluation, Preclinical ; Drugs, Chinese Herbal ; pharmacology ; Flavanones ; Glucosides ; Glycyrrhizic Acid ; Lactones ; Medicine, Chinese Traditional ; Monoterpenes ; Sesquiterpenes ; Software