Objective: To prepare perillyl alcohol ointment (PAO) and to investigate its properties and transdermal absorption behavior. Methods: The emulsion method was used to prepare PAO. The morphology, stability, and in vitro release were examined, respectively. The transdermal absorption of PAO was evaluated using Franz diffusion cells and the perillyl alcohol content was determined by HPLC. Results: The optimal prescription of PAO was perillyl alcohol, stearic acid, glyceryl monostearate, white vaseline, lanolin, liquid paraffin, triethanolamine, glycerine, and ethylparaben. The product was a pale yellow semi-solid oil-in-water emulsion with a uniform appearance. The content of perillyl alcohol in ointment was (2.89 ± 0.17)%, the release accumulation in vitro achieved 61.25% in 12 h, and the percutaneous penetration rate was 9.42 μg/(cm2·h). The ointment was not stratified after the centrifugation at 3500 r/min for 30 min, and the product was fairly stable under the condition of storing at 0 and 40°C for 30 d. Conclusion: The prepared PAO with increased skin retention amount could be developed into a novel preparation of perillyl alcohol for focal administration.

Background Laser peripheral iridotomy(LPI) is used as the primary therapy for the eyes at risk of angle closure.But there are still 28% eyes with primary angle closure suspect occur angle closure within 2 years after LPI.It is necessary to explore the associated factors of the efficacy of LPI.Objective The aim of this study was to explore the changes of intraocular pressure(IOP) and anterior chamber angle in the fellow eyes of patients with unilateral acute attack of primary angle closure glaucoma (PACG) and analyze the relevant factors influencing the successful rate of LPI.Methods Eighty-seven fellow eyes received LPI from 87 patients with unilateral acute attack of PACG were included in this study and retrospectively analyzed.The IOP and gonioscopy were performed before and 1 week,3,6,9,12 months after LPI.Successful signs of LPI were defined as an IOP 6-21mmHg without any anti-glaucoma medication,none of glaucomatous neuropathy and the coincident visual field loss,and no need of additional glaucomatous medication or surgery.This study was approved by Ethic Committee of the First Hospital of Xinxiang Medical College,and written informed consent was obtained from each patient.Results Seventy-nine eyes of 79 cases finished the medical visit throughout the follow-up duration with the age 61.4±0.4 years and 33(41.8%) males and 46(58.2%) females.The mean IOP was lowed in various time points after LPI in comparison with before operation with the general difference among different time visiting groups(F=4.056,P＜0.01).Shaffer grade was increased in superior,temporal and nasal quadrants and significant differences were found between 1 week group,3 months group or 6 months group and before operation group (P＜0.05).LPI lessened the range of appositional angle closure (AAC) in postoperative 1 week group and 3 months group compared with pre-operative group (P＜0.05),but no statistically significant reduce was seen in range of AAC from 6 months through 12 months after LPI in comparison with pre-operation (P＞0.05).LPI was determined as successful in 61 cases (77.2%) during one-year fellow-up period.Several variables,such as preoperative IOP,Shaffer grade of each quadrant,mean Shaffer grade and the extent of AAC,were significantly different between LPI success and failure group(P＜0.01).Cox stepwise regression analysis found that the success rate was significantly associated with the extent of AAC (Wald=48.150,RR=1.963,P＜0.01) rather than pre-IOP,Shaffer grade of each quadrant,mean Shaffer grade,age and gender (P＞0.05).Conclusion LPI can widen the anterior chamber angle and low IOP in the fellow eyes of PACG attack eyes.The success rate of LPI is associated with the extent of pre-AAC,suggesting that it is necessary for LPI in consideration of the extent of pre-AAC.

0.05).Conclusions Serum NT-proBNP level is sensitive and specific for the diagnosis of pneumonia complicated with CHF and CHD complicated with CHF. There is an increasing tendency of NT-proBNP level companied increasing pulmonary pressure.

OBJECTIVETo investigate the effects of serotonin (5-HTIA) receptors in the hippocampal dentate gyrus (DG) on active avoidance learning in rats.

METHODSTotally 36 SD rats were randomly divided into control group, antagonist group and agonist group(n = 12). Active avoidance learning ability of rats was assessed by the shuttle box. The extracellular concentrations of 5-HT in the DG during active avoidance conditioned reflex were measured by microdialysis and high performance liquid chromatography (HPLC) techniques. Then the antagonist (WAY-100635) or agonist (8-OH-DPAT) of the 5-HT1A receptors were microinjected into the DG region, and the active avoidance learning was measured.

RESULTS(1) During the active avoidance learning, the concentration of 5-HT in the hippocampal DG was significantly increased in the extinction but not establishment in the conditioned reflex, which reached 164.90% ± 26.07% (P <0.05) of basal level. (2) The microinjection of WAY-100635 (an antagonist of 5-HT1A receptor) into the DG did not significantly affect the active avoidance learning. (3) The microinjection of 8-OH-DPAT(an agonist of 5-HT1A receptor) into the DG significantly facilitated the establishment process and inhibited the extinction process during active avoidance conditioned reflex.

CONCLUSIONThe data suggest that activation of 5-HT1A receptors in hipocampal DG may facilitate active avoidance learning and memory in rats.

8-Hydroxy-2-(di-n-propylamino)tetralin ; pharmacology ; Animals ; Avoidance Learning ; Dentate Gyrus ; physiology ; Piperazines ; pharmacology ; Pyridines ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptor, Serotonin, 5-HT1A ; physiology ; Serotonin ; physiology ; Serotonin Receptor Agonists ; pharmacology

In this study, cardiotonic and cardiotoxic effects of Buthus martensi Karsch (BmK) I, a modulator of voltage-gated sodium channels, were investigated on the isolated rat hearts. The results showed that BmK I evoked complex effects characterized by a change in both cardiac mechanical and electrical activity. Langendorff perfusion showed that: (1) maximal left ventricular developed pressure (LVDP(max)) and dp/dt(max) were markedly increased by BmK I (0.5-10 micromol/L) in a dose-dependent manner (n=6, P<0.05), positive chronotropic effects were also induced by BmK I (n=6, P<0.05); (2) negative inotropic action and bradycardia could be elicited at a larger dose of BmK I (20 micromol/L); (3) the coronary flow varied inversely with the positive inotropic effects, coronary flow reduced during positive inotropic effects from 14.5 to 8.6 ml/min after administration of 500 nmol/L BmK I (n=6, P<0.05). In addition, tachycardia and complex cardiac arrhythmias were induced by BmK I (0.5-10 micromol/L). The modulating of BmK I on the heart mechanical, electrical activity could be partially recovered after washing. As propranolol was applied to block the release of catecholamines before administration of BmK I, suggesting that the changes in cardiac mechanical and electrical activity induced by BmK I might not due to catecholamine release from the nerve terminal and subsequent stimulation of the beta-adrenoceptor but attributable to the modulation of BmK I on cardiac voltage-gated sodium channels.
Action Potentials ; drug effects ; Animals ; Electrophysiology ; In Vitro Techniques ; Insect Proteins ; Male ; Myocardial Contraction ; drug effects ; NAV1.5 Voltage-Gated Sodium Channel ; Neurotoxins ; pharmacology ; Patch-Clamp Techniques ; Rats ; Rats, Sprague-Dawley ; Scorpion Venoms ; pharmacology ; Sodium Channel Blockers ; pharmacology ; Sodium Channels ; drug effects

In the present study, the specifically knockdown models of P-gp or MRP2 were constructed by using a series of chemically synthesized small interfering RNA (siRNA) in vitro. The expression of P-gp and MRP2 was measured by real-time PCR and Western blot, and the function was evaluated by applying P-gp and MRP2 substrate, rhodamine and methotrexate. The results showed that MRP2 siRNA-3 or P-gp siRNA-2 significantly decreased the mRNA expression of MRP2 or P-gp, the inhibition ratio was 68% or 84%; MRP2 siRNA-3 or P-gp siRNA-2 at a dose of 80 nmol x L(-1) significantly reduced the protein expression of MRP2 or P-gp at 48 h after treatment, the inhibition ratio was 62% or 70%. Meanwhile, other transporters were not influenced by siRNA. When pretreatment with MRP2 siRNA-3 or P-gp siRNA-2, the efflux of methotrexate or rhodamine decreased significantly and the intra-cellular concentration increased. The results suggested that chemically synthesized siRNA could significantly inhibit the expression and function of MRP2 and P-gp, and the model of RNAi in vitro could be used to evaluate the role of efflux transporters in transportation of drugs.
ATP-Binding Cassette, Sub-Family B, Member 1 ; genetics ; Gene Knockdown Techniques ; Multidrug Resistance-Associated Proteins ; genetics ; RNA Interference ; RNA, Small Interfering ; Real-Time Polymerase Chain Reaction

Objective To explore the relationship between IL-1?-511C/T and IL-1?+3953C/T site polymorphisms and the susceptibility of pediatric epilepsy.Methods Under the case-control study,IL-1?-511C/T and IL-1?+3953C/T site polymorphisms in 117 patients with pediatric epilepsy and 95 healthy individuals controls(healthy control group) were analyzed with polymerase chain reaction restriction and fragment length polymorphism(PCR-RFLP),the relationship between IL-1?-511C/T,IL-1?+3953 C/T site polymorphisms and the risk of pediatric epilepsy were analyzed.SAS 8.0 software was used to analyze the data.Results Multiple variate logistic regression analysis revealed that compared with healthy control group,there was no relationship between the IL-1?-511C/T site polymorphisms and the susceptibility of pediatric epilepsy individuals,carrying at least one +3953T variant allele(CT and TT genotypes) had a significantly increased risk for pediatric epilepsy(adjusted OR=2.46,95%CI 1.03-5.87),compared with the wild-type genotype(+3953CC).Furthermore,individuals with epilepsy or febrile seizures family history had a significantly higher risk(adjusted OR=4.12,95%CI 1.28-29.34),compared with those with both CC genotypes.Conclusions These findings support the hypothesis that IL-1?-511C/T site polymorphisms have no relationship with epilepsy,but the IL-1?+3953C/T polymorphism may contribute to the risk of developing pediatric epilepsy.

Cell Transformation, Neoplastic ; drug effects ; genetics ; Dimethyl Sulfoxide ; pharmacology ; Electroporation ; methods ; HL-60 Cells ; Humans ; Membrane Proteins ; genetics ; Neoplasm Proteins ; genetics ; RNA Interference ; RNA, Small Interfering ; genetics ; Stromal Interaction Molecule 1 ; Transfection

Objective To investigate the expression and significance of Smad 7,Smurf 1 and Smurf 2 in basal cell carcinoma and squamous cell carcinoma.Methods Biopsy specimens were resected from 14 patients with basal cell carcinoma,19 patients with squamous cell carcinoma and 30 normal controls.Quanti- tative real-time PCR and immunohistochemical techniques were utilized to assess the expression of Smad 7, Smurf 1 and Smurf 2 in these specimens.Results The gray scale for staining of Smad 7,Smurf 1 and Smurf 2 was 166.61?7.11,166.08?8.71,and 166.25?8.15 respectively in basal cell carcinoma,161.66?5.52,166.84?9.27,and 169.98?9.48 respectively in squamous cell carcinoma.The expression levels of Smad 7,Smurf 1 and Smurf 2 were all significantly increased in basal cell carcinoma and squamous cell car- cinoma in comparison with normal controls.Conclusions The over-expression of Smad 7,Smurf 1 and Smurf 2 may interfere with transforming growth factor?signaling transduction pathway through several links,therefore prevent the inhibitory effect of transforming growth factor?on epidermal proliferation,and accelerate the abnormal proliferation in above epidermal tumors.

Adult ; Eye Injuries ; surgery ; Female ; Humans ; Male ; Middle Aged ; Occupational Diseases ; surgery ; Vitrectomy