The Analgesic Activity of Bestatin as a Potent APN Inhibitor

Bestatin, a small molecular weight dipeptide, is a potent inhibitor of various aminopeptidases as well as LTA4 hydrolase. Various physiological functions of Bestatin have been identified, viz.: (1) an immunomodifier for enhancing the proliferation of normal human bone marrow granulocyte–macrophage progenitor cells to form CFU-GM colonies; Bestatin exerts a direct stimulating effect on lymphocytes via its fixation on the cell surface and an indirect effect on monocytes via aminopeptidase B inhibition of tuftsin catabolism; (2) an immunorestorator and curative or preventive agent for spontaneous tumor; Bestatin alone or its combination with chemicals can prolongate the disease-free interval and survival period in adult acute or chronic leukemia, therefore, it was primarily marketed in 1987 in Japan as an anticancer drug and servers as the only marketed inhibitor of Aminopeptidase N (APN/CD13) to cure leukemia to date; (3) a pan-hematopoietic stimulator and restorator; Bestatin promotes granulocytopoiesis and thrombocytopoiesis in vitro and restores them in myelo-hypoplastic men; (4) an inhibitor of several natural opioid peptides. Based on the knowledge that APN can cleave several bioactive neuropeptides such as Met-enkaphalins, Leu-enkaphalins, β-Endorphin, and so on, the anti-aminopeptidase action of Bestatin also allows it to protect endopeptides against their catabolism, exhibiting analgesic activity. Although many scientific studies and great accomplishments have been achieved in this field, a large amount of problems are unsolved. This article reviews the promising results obtained for future development of the analgesic activity of Bestatin that can be of vital interest in a number of severe and chronic pain syndromes

Diagnosis and Treatment of Comorbidities of Tourette's Syndrome and Bipolar Disorder in A 10-Year-Old Boy

Changes in moods are one of the comorbid psychiatric manifestations that frequently occur in patients with Tourette's syndrome. The assessment of a manic episode in children with Tourette's syndrome is challenging. Furthermore, the treatment of children with comorbid mania and Tourette's syndrome has not been extensively studied. We present a 10-year-old boy who suffered from both Tourette's syndrome and mania, whose symptoms improved after using lithium and risperidone. The child was diagnosed with Tourette's syndrome at 7 years of age when he suffered from tics and experienced his first manic episode. He received monotherapy, including haloperidol, risperidone and aripiprazole, and the response was poor. When the combination of lithium and risperidone was used, the tics and mania subsided. It is important to assess individuals with Tourette's syndrome for associated bipolar disorder. The treatment of children with both disorders is a major clinical issue, and our case may serve as an example for successful treatment strategies

A face annotation framework with partial clustering and interactive labeling

Face annotation technology is important for a photo management system. In this paper, we propose a novel interactive face annotation framework combining unsupervised and interactive learning. There are two main contributions in our framework. In the unsupervised stage, a partial clustering algorithm is proposed to find the most evident clusters instead of grouping all instances into clusters, which leads to a good initial labeling for later user interaction. In the interactive stage, an efficient labeling procedure based on minimization of both global system uncertainty and estimated number of user operations is proposed to reduce user interaction as much as possible. Experimental results show that the proposed annotation framework can significantly reduce the face annotation workload and is superior to existing solutions in the literature. 1

Structural investigation on GexSb10Se90−x glasses using x-ray photoelectron spectra

The structure of GeₓSb₁₀Se₉₀ˍₓ glasses (x = 7.5, 10, 15, 20, 25, 27.5, 30, and 32.5 at. %) has been investigated by x-ray photoelectron spectroscopy (XPS). Different structural units have been extracted and characterized by decomposing XPS core level spectra, the evolution of the relative concentration of each structural unit indicates that, the relative contributions of Se-trimers and Se-Se-Ge(Sb) structure decrease with increasing Ge content until they become zero at chemically stoichiometric glasses of Ge₂₅Sb₁₀Se₆₅, and then the homopolar bonds like Ge-Ge and Sb-Sb begin to appear in the spectra. Increase of homopolar bonds will extend band-tails into the gap and narrow the optical band gap. Thus, the glass with a stoichiometric composition generally has fewer defective bonds and larger optical bandgap

Research on Winding System of Twisting Machine Based on Multi-parameters

Winding movement of twisting machine is closely related to the package build, package density and yarn quality. The requirements are that the package build is good shaped and the winding tension is proper technically. Namely the angle of winding is fine and there is no overlapping and convex, hard edge on the package. The winding density is same and reasonable on the whole package build. And the fluctuation of winding tension is small. It is becoming development trend that driving of multiple-motors is used on twisting machine. There are many parameters to be controlled such as degree of twist, direction of twist, winding angle and spindle speed and so on. Therefore it is essential to set up reasonable mathematical model of yarn for winding movement

Effect of preemptive local injection of ropivocaine with dexmedetomidine on mirror pain in rats and its mechanism

AbstractObjectiveTo observe the effect of preemptive local injection of ropivocaine with dexmedetomidine on activation of glial cells and on the mirror pain in rats and its mechanism.MethodsA total of 48 adult male Sprague-Dawley rats (weighing 180 g–220 g) were included in the study and randomized into 3 groups, Group S, Group R, and Group RD1. A rat model of persistent postoperative pain evoked by skin/muscle incision and retraction was established in the three groups. Before procedures and nerve extraction, Group S (n = 16) was injected 0.9% saline locally; Group R (n = 16) was injected 0.5% ropivocaine locally, and Group RD1 (n = 16) was injected 0.5% ropivocaine in combined with 1 μg dexmedetomidine locally. After the model being established in the three groups, 8 rats were used for behavior test until 28 d, and dorsal root ganglions (DRGs) of the other 8 rats were harvested on the 3rd day after surgery. Immunofluorescent and transmission electron microscopy were used to observe the activation of glial cells in DRG, and the behavior test results in the three groups were compared.ResultsThe results showed that mechanical pain threshold in ipsilateral hind-paws of the Group S, Group R, Group RD1 animals dropped to (3.640 ± 1.963) g, (5.827 ± 1.204) g, (7.482) ± 1.412 g at 3 d respectively; while in contralateral paws dropped to (7.100 ± 1.789) g, (17.687 ± 1.112) g, (16.213 ± 1.345) g on the 3 d respectively. Immunofluorescent showed that the glial cells were activated in bilateral side DRG after surgery in 3 groups, but ipsilateral paws expressed more active glial cells than contralateral paws. Transmission electron microscopy showed that mitochondria swelling/vacuolization and lysosomes were more obvious in ipsilateral paws than contralateral paws, but Group RD1 formula could reduce glial cells activity, mitochondria swelling/vacuolization and the amount of lysosomes.ConclusionsLocal injection of ropivocaine and/or dexmedetomidine can effectively inhibit the activation of glial cells in DRG, mitigate the pathological changes of neuron in DRG and reduce mirror image pain