Adult ; Connective Tissue Cells ; Female ; Humans ; Male ; Middle Aged ; Myofibroblasts ; cytology ; Nasal Polyps ; pathology ; Young Adult

In this study, we designed and synthesized 12 novel aloperine derivatives with different core structures. Among them, compound 3 with a ten-membered ring core was obtained through a special ring expansion reaction after γ-H Huffman elimination of quaternary ammonium salt, and the structure was verified by X-single crystal diffraction. Furthermore, their antiviral activity against human β-coronavirus HCoV-OC43 was evaluated by CCK-8 assay. Quaternary ammonium salt 2a and 3 had a good inhibitory effect against HCoV-OC43, and 2a had the highest anti-HCoV-OC43 activity with an EC₅₀ values of 3.77 μmol·L^-1 and a SI value of over 53.1. Schrӧdinger molecular docking results showed that both 2a and 3 might display their anti-HCoV-OC43 activity by directly acting on host TMPRSS2 and SR-B1. The results expanded the structural types of endocyclic aloperine and the function against coronavirus, and provided useful scientific data for the development of pharmaceutical applications of these compounds.

Endoscopy ; instrumentation ; Frontal Sinus ; surgery ; Humans ; Retrospective Studies ; Surgical Instruments

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

OBJECTIVETo study possible mechanisms of Shangjuxu (ST37) and the large intestine.

METHODSTotally 40 SD rats were selected. The distension of end colon was used as injured afferent stimulus. Activities of locus coeruleus (LC) neurons were recorded by extracellular microelectrode technique. Shangjuxu (ST37) and Hegu (L14) were needled to observe general features of discharge reactions, distention of colon induced discharge reactions of LC, and its effects on distention of colon induced discharge reactions of LC.

RESULTSDistention of colon could induce incrased discharge of LC neurons by 127.33% ± 45.48%. But needling at Shangjuxu (ST37) and Hegu (L14) could inhibit this injured response by 38.24% ± 7.69% and 21.29% ± 13.16% respectively (all P < 0.01).

CONCLUSIONSNeedling at Shangjuxu (ST37) and afferent signals of colon distension converged and interacted with each other. Needling at Shangjuxu (ST37) could significantly inhibit colon distension induced discharge of LC neurons, which might be one of mechanisms for Shangjuxu (ST37) and the large intestine relationship.

Acupuncture Therapy ; Animals ; Colon ; Intestine, Large ; Locus Coeruleus ; physiology ; Neurons ; Rats ; Rats, Sprague-Dawley

The index system of comparative advantages was constructed for the pharmaceutical manufacturing in-dustry in different provinces , municipalities directly under the Central Government , and autonomous regions ac-cording to the integrated comparative advantage theory .The integrated comparative advantages in different provinces , municipalities directly under the Central Government , and autonomous regions were scored by principal component analysis and qualitatively analyzed by clustering analysis to reveal their spatial distribution , thus providing the deci-sion-making support for the policy makers, manufacturers, investors and staff of pharmaceutical manufacturing in-dustry.

Objective To explore the clinical,radiological findings and pathogenic factor of spondylometaphyseal dysplasia.Methods Five cases were reported and the relevant documents were studied retrospectively.Plain X-ray film was performed in all patients.Results There were 4 male and 1 female,age ranged from 4 to 15 years with average of 9 years.The main features of 5 cases included delayed bone age,stature short,short trunk,waddling gait noted,scoliosis in 2 cases,kyphoscoliosis in 1 case,severe genu valgum in 2 cases.The main X-ray appearance of 5 cases is multiple irregularities of long bones metaphyses associated with platyspondylia,epiphysis is normal.Type Ⅰ SMD in 2 cases,Type Ⅱ SMD in 1 case,Type Ⅲ SMD in 2 cases.Conclusion When we meet children with delayed bone age and stature short,and muhiple irregularities of long bones metaphyses associated with platyspondylia were seen in X-ray plain film.we should think about spondylometaphyseal dysplasia.

Objective To observe the clinical efficacy of acupuncture at the three nasal acupoints plus bloodletting at Suliao (GV 25) in treating rosacea.Method Sixty rosacea patients were randomized into a treatment group and a control group, 30 cases each. The treatment group was intervened by acupuncture at the three nasal acupoints plus bloodletting at Suliao (GV 25), while the control group was intervened by ordinary medication. The skin lesion scores of the two groups were observed before and after 4-week treatment, and the clinical efficacies were also compared. Result The skin lesion scores were significantly changed after respectively 2, 3 and 4 weeks of treatment in both groups (P<0.05). The skin lesion scores in the treatment group were significantly different from those in the control group respectively after 2, 3 and 4 weeks of treatment (P<0.05). The total effective rate was 93.3％ in the treatment group versus 73.3％ in the control group, and the between-group difference was statistically significant (P<0.05). Conclusion Acupuncture at the three nasal acupoints plus bloodletting at Suliao (GV 25) is an effective approach in treating rosacea.

Objective:To investigate the effect on the phenotype and function of CIK cells induced from splenic lymphocyte in mice treated with carboxylated single-walled carbon nanotubes.Methods:CIK cells were treated with carboxylated single-walled carbon nanotubes at different concentrations.Cell growth status was observed using inverted fluorescence microscopy.The killing effect was de-termined by MTS method.Immunophenotype was analyzed by flow cytometry.Results: With the increase of the effect target ratio,the killer rate of CIK was gradually enhanced and the optimal effect target ratio was 20:1.With the increase of the dose of carboxylated single-walled carbon nanotubes,the proportion of Treg cells decreased.When CIK cells were treated with 0.5 μg/ml carboxylated single-walled carbon nanotubes(CNTs),the proportion of CD3+CD4+and CD3+CD8+was significantly higher than that of the control group(P<0.05),and the killing effects of CIK anchieved best results to B16 cells,H22 cells and RM-1cells.Conclusion: The carboxylated single-walled carbon nanotubes enhanced the ability of CIK cells to kill tumor cells,significantly which provide has potential value in tumor drug development.

Osteoarthritis (Osteoarthritis, OA) is a common clinical degenerative joint disease with increased incidence rate in recent years. Animal experiment is one of the important ways to explore pathogenesis and treatment of OA, while induced animal model is the most important part in animal experiment. Intra-articular injection of drugs is a classical method for establishing animal model of OA. Choose of animal should follows the principle of correlation, appropriateness and practicability, injections should perform in accordance with experimental purposes and subject, detections means and evaluation methods also should corresponding to experimental reality. The gold standard of OA animal model and intra-articular injections has not build, need further study.
Animals ; Cytokines ; analysis ; Disease Models, Animal ; Injections, Intra-Articular ; Mice ; Osteoarthritis ; diagnosis ; etiology ; immunology ; Rabbits ; Rats