Clinical Medicine ; Humans ; Neoplasms ; prevention & control ; Periodicals as Topic ; Research

Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.
2-Hydroxypropyl-beta-cyclodextrin ; Alkaloids ; chemistry ; Chemistry, Pharmaceutical ; methods ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Rutaceae ; chemistry ; Solubility ; beta-Cyclodextrins ; chemistry

BACKGROUND: Edaravone can alleviate brain injury and improve neurological functions and symptoms. This study aimed to investigate the effect of edaravone on the p38Mitogen-activated protein kinases/Caspase-3 (p38MAPK /Caspase-3) pathway after diffuse brain injury (DBI) in rats. METHODS: DBI models were established according to the description of Marmarou's method. A total of 250 rats were divided (random number) into four groups: control group (CG, n=45), model group (MG, n=77), low-dose edaravone group (n=67, dosage 5 mg/kg) and high-dose edaravone group (n=61, dosage 10 mg/kg). After 1, 6, 24, 48, and 72 hours after injury, brain tissues were collected. The changes of neuron morphous in the hippocampal region were observed through Nissl staining. The expression levels of phosphorylated p38MAPK and caspase-3 were detected by immunohistochemistry and Western blotting respectively. Learning and memory function were tested with Morris water maze from the 3rd to 7th day after injury. RESULTS: Some neurons had histopathologic changes of necrosis and apoptosis in the model group compared with the control group. The phosphorylated p38MAPK expressions increased at 1, 6, 4, and 48 hours (P<0.05), but no significant difference was observed at 72 hours (0.54±0.19 vs. 0.40±0.14, P>0.05). Caspase-3 expressions increased at 6, 24, 48, and 72 hours respectively (P<0.05), but there was no significant difference at 1 hour (0.59±0.29 vs. 0.40±0.17, P>0.05). From the 3rd to 6th day during the Morris water maze test, the latency to find the platform was significantly prolonged (P<0.05) and times of rats crossing the platform was decreased on the 7th day (2.28±1.18 vs. 8.20±1.52, P<0.05). The phosphorylated p38MAPK expressions decreased at 6, 24 and 48 hours respectively in the low dose edaravone group compared with the model group (P<0.05), whereas no significant difference was seen at 1 hour (1.66±0.80 vs. 1.85±0.86, P>0.05). Caspase-3 expression decreased at 6, 24, 48, and 72 hours (P<0.05). The latency to find the platform was significantly shortened (P<0.05), and times of rats crossing the platform increased (4.17±1.15 vs. 2.28±1.18, P<0.05). The above mentioned parameters changed more significantly in the high-dose edaravone group than in the low-dose edaravone group. CONCLUSION: Edaravone can alleviate brain tissue damage after DBI, inhibit p38MAP signal activation after early injury, reduce the expression of caspase-3, and promote the recovery of neurological function in the late period.

OBJECTIVETo examine the expression of recombinant cytolethal distending toxin (CDT) produced by Actinobacillus actinomycetemcomitans (Aa).

METHODSCDT encoding gene cdtABC was amplified by PCR. Through TA clone and restriction endonuclease digestion, gene cdtABC and vector pQE60 were ligated to form pQE60-cdtABC expression system which transformed into competent cells. Protein expression was induced by IPTG and examined by SDS-PAGE and Western-blotting.

RESULTSRandom colony PCR of pQE60-cdtABC transformed cells demonstrated that all strains contained cdtABC gene. The DNA sequence was blast with cdtABC gene from GenBank and 99% homology was obtained. SDS-PAGE and Western-blotting confirmed that recombinant CDT was obtained.

CONCLUSIONSCDT protein expression system was reconstructed and recombinant protein was obtained. Actinobacillus actinomycetemcomitans;

Aggregatibacter actinomycetemcomitans ; genetics ; metabolism ; Bacterial Toxins ; genetics ; metabolism ; Genetic Vectors ; Recombinant Proteins ; genetics ; metabolism

OBJECTIVETo measure the utility value of different skeletal malocclusion for patients receiving orthodontic treatment.

METHODSUtility value of different skeletal malocclusion for patients was measured by rating scale and time trade-off.

RESULTSThe youth group had higher utility values than adult group for skeletal malocclusion Class II (protruding facial type) with median mandibular angle. The utility value of skeletal malocclusion Class III (concave facial type) with low mandibular angle was the lowest, and the utility value of skeletal malocclusion Class II (protruding facial type) with median mandibular angle was the highest. There was no difference in the utility values by rating scale and by time trade-off.

CONCLUSIONFor some skeletal malocclusion, the youth had different utility values with the adult.

Adolescent ; Adult ; Cephalometry ; Face ; Female ; Humans ; Male ; Malocclusion ; Malocclusion, Angle Class III ; Mandible

OBJECTIVESTo evaluate the effects of varicocele (VC) on IL-1 and NO levels in testes of rats with VC.

METHODSMale adult Wistar rats were divided into two groups randomly, VC group (n = 30) and pseudo-operation group (n = 20), and the levels of IL-1 and NO in the testes were determined and compared.

RESULTSThe levels of IL-1 and No of left tests in VC group were higher than those in pseudo-operation group, respectively(P < 0.01). While the levels of IL-1 and NO of right testes between two groups were not significantly different (P > 0.05). More over, the level of IL-1 correlated significantly with that of NO(r = 0.572, P < 0.01).

CONCLUSIONSThe results revealed that the changes of IL-1 and NO levels in the testes of rats with VC might be the reason which caused testes damage, disturbance of spermatogenesis and even infertility.

Animals ; Disease Models, Animal ; Interleukin-1 ; metabolism ; Male ; Nitric Oxide ; metabolism ; Rats ; Rats, Wistar ; Testis ; metabolism ; ultrastructure ; Varicocele ; metabolism

OBJECTIVETo investigate the effects of exposure to decabrominated diphenyl ether (PBDE-209) on learning and memory of BALB/c mice.

METHODSEighteen female BALB/c mice were randomized divided into 3 groups and gavaged with peanut oil in the control groups and 300, 1500 mg x kg(-1)xd(-1) PBDE-209 in peanut oil daily in two exposed groups respectively for 4 weeks. The learning and memory ability of mice were tested by the Morris water maze and the shuttling box respectively. The body weight and organs index were measured and the acetylcholinesterase and butyrylcholinesterase activity in brain were determined. The liver histopathological examination was performed.

RESULTSThe heart index in high dose PBDE-209 group was higher than that of the low dose PBDE-209 group (P < 0.05). The results of Morris water maze showed that escape latency period was significantly shorter than the control group (F = 3.134, P < 0.05). The swimming time in the second quadrant of low dose PBDE-209 group was (15.78 +/- 10.92) s, significantly shorter compared with the swimming time in the second quadrant of the control group's [(28.80 +/- 8.67) s] (P < 0.05). There was no significant difference in the times of active avoidance in the shuttling between three groups (F = 3.423, P = 0.06). There were no significant differences in acetylcholinesterase and butyrylcholinesterase activity in brain of PBDE-209 groups compared with the control group (P > 0.05). Histologically liver damages in structure such as adipose degeneration and swelling were observed in PBDE groups.

CONCLUSIONExposure to PBDE-209 slightly impairs the space learning and memory ability of BALB/c mice, and it has some hepatotoxicity.

Animals ; Behavior, Animal ; Dose-Response Relationship, Drug ; Female ; Halogenated Diphenyl Ethers ; toxicity ; Maze Learning ; drug effects ; Memory ; drug effects ; Mice ; Mice, Inbred BALB C ; Toxicity Tests

OBJECTIVETo compare the number of the Tannerella forsythensis (T. forsythensis), total bacteria, and proportion of T. forsythensis in subgingival specimens in diseased sites of chronic periodontitis patients and in healthy sites of periodontally healthy subjects, and clarify the relationship between bacterial load and periodontal status.

METHODSSubgingival plaque samples from 61 chronic periodontitis patients and 12 healthy controls (positive for T. forsythensis by conventional PCR) were analyzed with TaqMan real-time polymerase chain reaction assay for T. forsythensis and total bacteria. Quantification was performed with species-specific primer/probe, universal primer/ probe and serial dilution of plasmid standards.

RESULTSNumbers of T. forsythensis and total bacteria(P<0.001) , the proportion of T. forsythensis in subgingival specimens (P<0.05) were significant higher in diseased sites of chronic periodontitis patients than in healthy sites of healthy subjects. In addition, a significant correlation was found between the number of bacteria and various probing depth (P<0.001). There was no significantly difference between the proportion of T. forsythensis in subgingival plaque and probing depth.

CONCLUSIONNumber of T. forsythensis are closely associated with periodontal status, and demonstrate the broad potential of real-time polymerase chain reaction application on periodontology.

Adult ; Bacteroides ; Chronic Periodontitis ; Dental Plaque ; Female ; Humans ; Male ; Middle Aged ; Periodontitis ; Polymerase Chain Reaction ; Porphyromonas gingivalis

OBJECTIVETo investigate the expression of MMP-2 and MMP-3 in periodontal tissues of rat periodontitis model at different stages of inflammation of varied severity.

METHODSThe periodontal tissues were immunohistochemically stained by antibody of MMP-2 and MMP-3.

RESULTSMMP-2 and MMP-3 were both strongly positive in gingival epithelia and fibroblasts in periodontal ligament in rat periodontitis model. And chronic periodontitis showed lower expression of MMP-2 and MMP-3 than that of acute gingivitis and acute peridontitis.

CONCLUSIONThe expression of MMP-2 and MMP-3 varies in different stage of periodontitis. MMP-2 and MMP-3 may play an important role in development of periodontitis.

Animals ; Chronic Periodontitis ; Fibroblasts ; Gingivitis ; Male ; Matrix Metalloproteinase 2 ; Periodontal Ligament ; Periodontitis ; Rats

Adolescent ; Brain Injuries ; blood ; complications ; Cerebral Infarction ; blood ; etiology ; Child ; Child, Preschool ; Female ; Fibrin Fibrinogen Degradation Products ; analysis ; Humans ; Male