Transient receptor potential vanilloid 1 (TRPV1) is a non-selective positive ion channel that is mainly expressed in sensory neurons and a member of transient receptor potential (TRP) family. The receptor could be activated by mechanical irritation, chemical irritation or endogenous ligand to mediate pains and cause injury to body functions. Traditional Chinese medicine believes that the mechanism of pain is that "stagnation leads to pain". Specifically, both of the contracture and tautness caused by cold and the blood stasis could result in blood impassability and pain. Most of traditional Chinese medicines for clearing heat and removing toxicity have the anti-inflammatory effect, while those for warming interior, and promoting blood circulation to remove blood stasis have the effect in smoothening blood vessels. Therefore, either with the anti-inflammatory effect or the effect in smoothening blood vessels, traditional Chinese medicines for clearing heat and removing toxicity, warming interior, and promoting blood circulation have the analgesic effect In this paper, the authors summarize the analgesic effect of the above three traditional Chinese medicines, with TRPV1 as the target.
Analgesics ; administration & dosage ; Animals ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Pain ; drug therapy ; genetics ; metabolism ; TRPV Cation Channels ; antagonists & inhibitors ; genetics ; metabolism

Brain Neoplasms ; metabolism ; Cell Line, Tumor ; Glioma ; metabolism ; Humans ; Neoplastic Stem Cells ; drug effects ; metabolism ; Reactive Oxygen Species ; metabolism ; Sodium Selenite ; pharmacology

Obesity is an established risk factor for endometrial cancer. Leptin, a secreted protein of the ob gene by white adipose tissue, plays an important role in the regulation of food intake and energy consumption in the brain and acts as a potential growth stimulator in normal and neoplastic cancer cells. However, a direct role for leptin in endometrial cancer has not been demonstrated. In the present study, the effect of leptin on the proliferation of Ishikawa endometrial cancer cells was investigated as well as the possible mechanism(s) underlying this action in endometrial cancers which express both short and long isoforms of leptin receptors. The expression of leptin receptor (ObRb) in Ishikawa cells was detected by RT-PCR and Western blotting. The cells after serum starvation, were treated by leptin with various concentrations (0, 10, 50, 100, 150 ng/mL) for different durations (6, 12, 24 h). The effect of leptin treatment on cell proliferation was examined by MTT assay. Meanwhile, inhibitory effect of Janus tyrosine kinase 2 (JAK2)/signal transducer and activator of transcription 3 (STAT3) inhibitor AG490 or extracellular signal-regulated kinase 1/2 (ERK1/2) inhibitor PD98059 on the proliferation of Ishikawa cells induced by leptin was also studied. Ishikawa cells were treated with 100 ng/mL leptin for various periods (0, 20, 40, 60 min), and the levels of STAT3 phosphorylation and ERK1/2 phosphorylation were examined by Western blotting. The results showed that leptin induced the phosphorylation of STAT3 and the activation of ERK1/2 in a time- and dose-dependent manner in the Ishikawa endometrial cancer cells. Blocking STAT3 phosphorylation with the inhibitor AG490, or blocking ERK1/2 activation by the specific ERK1/2 kinase inhibitor, PD98059, abolished leptin-induced proliferation of Ishikawa cells. In addition, leptin was found to potently induce the invasion of endometrial cancer cells in a Matrigel invasion assay. Leptin-stimulated invasion was effectively blocked by pharmacological inhibitors of STAT3 (AG490) and ERK1/2 kinase (PD98059). These results suggested that leptin promotes endometrial cancer growth and invasiveness by activating STAT3 and ERK1/2 signaling pathways and therefore blocking its action at the receptor level can be a rational therapeutic strategy.

?AlM: To investigate the outcome and safety of Ahmed glaucoma valve implantation treatment in uncontrolled primary congenital glaucoma ( PCG) .
? METHODS: Twenty - two eyes in 22 children with uncontrolled PCG were reviewed retrospectively and underwent Ahmed glaucoma valve implantation treatment from January 2011 to December 2014. Main checking index included intraocular pressure ( lOP ) before and after operation, corneal diameter and complications.
?RESULTS: Preoperative mean age was 3. 74±2. 24y, and 2. 59 ± 1. 78y apart from the last operation. Postoperative average lOP was 35. 22 ± 6. 36mmHg. Average corneal diameter was 12. 79 ± 0. 75mm. Mitomycin C ( 0. 3 - 0. 5mg/mL ) was used in all operations for 3-5min. Glaucoma valves were implanted in the temporal or nose above the equator sclera. Postoperative lOP was 11. 4±4. 45mmHg at 1wk, and 16. 73± 7. 23mmHg after 12mo. As lOP< 21mmHg for success criteria, lOP of 16 eyes ( 73%) were controlled after 12mo. Preoperative 6 cases had shallow anterior chamber, recovered spontaneously. No serious complication was recorded, such as rejection of glaucoma valve, endoophthalmitis and corneal decompensation.
?CONCLUSlON:Ahmed glaucoma valve implantation in uncontrolled PCG is a safe and viable treatment.

OBJECTIVETo construct eukaryotic expression vector of ribosomal protein sl5(RPs15) gene and study its effect on mouse skin fibroblasts in vitro.

METHODSThe RPs15 cDNA encoding region of fetal mouse skin was amplified by reverse transcription-polymerase chain reaction (RT-PCR) method and cloned into eukaryotic expression vector pcDNA3.1(-). The recombinant plasmid was transfected into adult mouse skin fibroblasts by FuGENE6 transfection reagents. Then the expression of RPs15 gene, was detected and its biological effect on fibroblasts was measured.

RESULTSThe DNA sequencing result of pcDNA3.1/RPs15 was identical with the reported. The RPs15 gene was expressed in transfected fibroblasts. The growth density of fibroblasts decreased with the conformation changing accordingly.

CONCLUSIONSThe eukaryotic expression vector pcDNA3.1/RPs15 is successively constructed and can be expressed in mouse skin fibroblasts. The results set up a basis for further study of the effect of RPs15 gene on skin fibroblasts.

Animals ; Cells, Cultured ; DNA Repair ; DNA, Complementary ; genetics ; Epithelial Cells ; metabolism ; Fibroblasts ; metabolism ; Genetic Vectors ; Mice ; Nuclear Proteins ; genetics ; Plasmids ; Ribosomal Proteins ; Skin ; cytology ; Transfection

OBJECTIVETo investigate the relationship between serotonin (5-HT) and epilepsy and the mechanism of learning-memory in pilocarpine (PILO)-induced epileptic rats after 5,7-dihydroxytryptamine (5,7-DHT) microinjection in median raphe nucleus.

METHODSAdult S D rats were randomly divided into 3 groups: PILO group, PILO+ 5,7-DHT group, vehicle control group; PILO group was divided into two groups by status epilepticus (SE): PILO + SE group and PILO - SE group. The rats' seizures and cortex electroencephalography (EEG) were observed by video EEG. The rats' spatial learning-memory was evaluated by Morris water maze. Finally, serotonergic neuron in raphe nuclei was observed by immunohistochemistry.

RESULTSAfter treatment of 5,7-DHT (PILO + 5,7-DHT group), the success rate, the mortality and the frequency of chronic spontaneous seizures in pilocarpine-induced epilepsy model were all improved. Compared with the control group, the number of serotonergic neuron in raphe nuclei was decrease in PILO + SE group (P < 0.05). Moreover, it's extremely decrease in PILO + 5,7-DHT group (P < 0.01). Compared with control group, the mean escape latency was prolonged, the times of crossing target was decreased and the retention time in target zone was shortened in PILO + SE group (P < 0.05), but there was no significant difference between PILO + SE group and PILO + 5,7-DHT group.

CONCLUSIONDepletion of serotonin may facility the rats' epileptic seizures, but we could not interpret which may cause epileptic rats' cognitive deficit.

5,7-Dihydroxytryptamine ; toxicity ; Animals ; Epilepsy ; chemically induced ; metabolism ; psychology ; Male ; Maze Learning ; Memory ; Pilocarpine ; adverse effects ; Raphe Nuclei ; Rats ; Rats, Sprague-Dawley ; Serotonin ; metabolism

OBJECTIVETo evaluate the estrogenic activity of several kinds of Chinese herbal medicines.

METHODUse zoopery and reporter gene technique to study the estrogenic activity of five Chinese herbal medicines. Zoopery: weanling female Kunming mice weight 9-12 g were administrated botanical extracts of Selaginella tamariscina, Pinus Massoniana, Corallodiscus flabellate, Dryopteris sublaeta and Leonurus heterophyllus, the positive control group with Nilestriol tablets and control group with water, respectiely. On the eighth day, the animals were sacrificed and the uteri were separated solely and weighed. Reporter gene technique: Induce the expression of reporter gene controlled by ERE and measure the activity of luciferase on cell's clear supernatant.

RESULTThe botanical extracts of S. tamariscina can increase weights of mice (P < 0.01); In the expression of reporter gene controlled by ERE, Either ERalpha or ERbeta's has estrogenic activity (P < 0.01). Follow in the zoopery we find the water part and the n-butanol part of S. tamariscina are the two active parts.

CONCLUSIONS. tamariscina and it's water part and n-butanol part have estrogenic activities, effect on ERbeta is greater than ERalpha.

Animals ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Estrogen Receptor alpha ; metabolism ; Estrogen Receptor beta ; metabolism ; Female ; Leonurus ; chemistry ; Mice ; Organ Size ; drug effects ; Phytoestrogens ; isolation & purification ; pharmacology ; Pinus ; chemistry ; Plants, Medicinal ; chemistry ; Selaginellaceae ; chemistry ; Uterus ; anatomy & histology

Cardiac Catheterization ; Catheterization ; methods ; Female ; Humans ; Lutembacher Syndrome ; diagnostic imaging ; therapy ; Middle Aged ; Ultrasonography

OBJECTIVETo study the changes of pharmacokinetics of 6,7-dimethoxycoumarin in a rat model of alpha-naphthylisothiocyanate (ANIT)-induced experimental hepatic injury after oral administration of Yinchenhao Decoction (, YCHD) using an ultra pressure liquid chromatography (UPLC) method.

METHODSRats were divided into a normal group and a model group, after modeled by 4% ANIT (75 mg/kg) for 48 h, they were orally administrated with YCHD extract at the dose of 0.324 g/kg, and then blood was collected from their orbital sinus after different intervals. Changes in liver function were monitored by the levels of liver enzymes [alanine aminotransferase (ALT), aspartate aminotransferase (AST)] and bilirubins [total bilirubin (TBIL), direct bilirubin (DBIL)], the concentration of 6,7-dimethoxycoumarin in plasma were measured by UPLC, and the pharmaceutical parameters were calculated with DAS2.1.1 software.

RESULTSThe concentration-time curve of both normal and modeled rats after oral administration of YCHD was obtained. Their time to maximum plasma concentration (t(max)) were both 0.25 h, the maximum concentration (C(max)) were 4.533 μg/mL and 6.885 μg/mL, and their area under concentration-time curve (AUC)(0→24h) were 16.272 and 32.981, respectively. There was a 51.88% and 100.46% increase in C(max) and AUC(0-t) (P<0.05), but there showed a 45.52% and 92.93% reduction in clearance of drug and volum of distribution (P<0.05), respectively.

CONCLUSIONSHepatic injury could significantly influence the pharmacokinetics of 6,7-dimethoxycoumarin after oral administration of YCHD, the absorption and distribution process was accelerated in liver injured rats, but the metabolism and elimination process was slowed. And this may lead to a significant accumulation of 6,7-dimethoxycoumarin in the body.

1-Naphthylisothiocyanate ; Administration, Oral ; Animals ; Chemical and Drug Induced Liver Injury ; blood ; drug therapy ; metabolism ; physiopathology ; Coumarins ; blood ; pharmacokinetics ; Disease Models, Animal ; Drug Evaluation, Preclinical ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; therapeutic use ; Liver ; drug effects ; physiopathology ; Models, Biological ; Rats ; Rats, Sprague-Dawley ; Validation Studies as Topic

OBJECTIVETo observe the effect of environmental risk factors in occupational noise exposure on hearing loss and find out the susceptible population of noise induced hearing loss (NIHL).

METHODSA case-control study was designed to study the effect of environmental risk factors on NIHL. 2400 workers exposed to 75 approximately 120 dB noises from an air conditioning factory in southern China served as the subjects. 202 workers were selected from 10% of population with the maximum hearing shift of the left ear to 3000 Hz noises as the NIHL susceptible group while 204 workers from 10% of population with the least hearing shift as the NIHL tolerant group. A questionnaire was designed to carry out an investigation, and an occupational health survey was used to identify the occupational risk factors which might affect the hearing system. The univariate analysis and multivariate analysis were used to observe the effect of environmental risk factors on NIHL.

RESULTSThe results of univariate analysis showed that smoking, alcohol drinking, organic solvent, heavy metal, heat, dust were significantly was associated with NIHL (P < 0.05). Multivariate analysis showed that only heat was associated with NIHL (P < 0.05), and OR value was 1.804 (95% CI: 1.101 approximately 2.958).

CONCLUSIONExposure to heat may be a high risk factor of NIHL.

Case-Control Studies ; Female ; Hearing Loss, Noise-Induced ; etiology ; Humans ; Male ; Occupational Diseases ; etiology ; Occupational Exposure ; adverse effects ; Risk Factors ; Surveys and Questionnaires