N-Heterocyclic Compounds, In silico Molecular Docking Studies, and In vitro Enzyme Inhibition Effect against Acetylcholinesterase Inhibitors.

BACKGROUND: This work contains the synthesis of seven new N-heterocyclic compounds bearing imidazole, benzimidazole, pyridine, and morpholine moieties. OBJECTIVES: We aimed to synthesize N-heterocyclic compounds for a more effective drug candidate to increase the amount of acetylcholine in synapses in Alzheimer's disease. All compounds were characterized by 1H NMR, 13C NMR, FTIR and elemental analysis. Enzyme inhibition activity of all compounds against acetylcholinesterase was investigated, which is an indirect treatment for Alzheimer's. Molecular docking was applied to estimate the binding energy of these compounds to the acetylcholinesterase. METHODS: All compounds were synthesized from reactions of 2 equivalents of N-heterocyclic starting material and 1 equivalent of 4,4'-bis(chloromethyl)-1,1'-biphenyl. The inhibition parameters of IC50 and Ki were calculated by the spectrophotometric method. AutoDock4 was used to define the binding pose of the compounds. RESULTS: Ki values were found in the range of 80.03 ± 19.64 to 5014.98 ± 1139.60 nM for AChE as an enzyme inhibition strategy, which is an important parameter for the treatment of neurodegenerative such as Alzheimer's disease. In this study, molecular docking is exerted to predict the binding energy of heterocyclic compounds (especially 2, 3, and 5) against acetylcholinesterase enzyme. Their docking binding energies are in good agreement with experimental findings. CONCLUSION: These new syntheses are drugs that can be used as AChE inhibitors in Alzheimer's disease.

Prevalence of Chlamydia trachomatis, Neisseria gonorrhoeae, and Mycoplasma genitalium among Patients with Urogenital Symptoms in Istanbul.

Chlamydia trachomatis, Neisseria gonorrhoeae, and Mycoplasma genitalium are the three most commonly reported sexually transmitted bacteria. The present study aimed to investigate the presence of C. trachomatis, N. gonorrhoeae, and M. genitalium in urogenital samples collected from 18-68-year-old Turkish patients who were admitted to the hospital with various urogenital symptoms. A total of 360 patients with symptoms of STD were included in the study. Following DNA extraction by QIAamp Mini Kit, the presence of C. trachomatis, N. gonorrhoeae, and M. genitalium were investigated using multiplex real-time PCR. Causative organisms were identified in 68 (18.9%) of 360 patients. C. trachomatis, N. gonorrhoeae, and M. genitalium were detected in 40 (11.1%), 14 (3.9%), and 28 (7.8%) of the patients, respectively. Patients 21-30 years of age represented more than one-third (37.8%) of positive patients. Of all patients, dual infections of C. trachomatis-M. genitalium, N. gonorrhoeae-C. trachomatis, N. gonorrhoeae-M. genitalium, and triple infection of C. trachomatis-N. gonorrhoeae-M. genitalium were determined in 1.6% (6/360), 1.3% (5/360), 0.2% (1/360), and 0.2% (1/360) of the patients, respectively. In CT-, NG-, and MG-positive patients, different STI agents were also found such as HIV, HBV, HPV, HSV2, T. pallidum, and T. vaginalis. In conclusion, among C. trachomatis, N. gonorrhoeae, and M. genitalium, CT was the most frequently detected bacterial cause of STDs in our hospital at Istanbul. Co-infections, which comprise more than one-fifth of the cases, should not be underestimated. Regular screening and following up of STD agents using multiplex real-time PCR-based diagnostic methods enabling the immediate detection of co-infections are essential for the treatment and primary prevention of STDs.

Colonic Visualization of 99mTc-DMSA Due to Enterovesical Fistula.

A 60-year-old woman with recurrent urinary tract infection who had several operations for colorectal carcinoma underwent Tc-DMSA renal scintigraphy which showed an unexpected accumulation of radiotracer in the colon. When symptoms were reviewed, we noticed that she was suffering from pneumaturia and fecaluria which raised the suspicion of enterovesical fistula. Rectal contrast-enhanced computer tomography of pelvis demonstrated enterovesical and enterovaginal fistulas. Colonic radioactivity was considered to be related to retrograde peristalsis of Tc-DMSA from bladder activity via enterovesical fistula. In patients with pelvic surgeries and radiotherapy, radioactivity in the colon should raise the suspicion of enterovesical fistula.

Constitutively reduced sensory capacity promotes better recovery after spinal cord-injury (SCI) in blind rats of the dystrophic RCS strain.

BACKGROUND: We compared functional, electrophysiological and morphological parameters after SCI in two groups of rats Sprague Dawley (SD) rats with normal vision and blind rats from a SD-substrain "Royal College of Surgeons" (SD/RCS) who lose their photoreceptor cells after birth due to a genetic defect in the retinal pigment epithelium. For these animals skin-, intramuscular-, and tendon receptors are major available means to resolve spatial information. OBJECTIVE: The purpose of this study was to check whether increased sensitivity in SD/RCS rats would promote an improved recovery after SCI. METHODS: All rats were subjected to severe compression of the spinal cord at vertebra Th8, spinal cord segment Th10. Recovery of locomotion was analyzed at 1, 3, 6, 9, and 12 weeks after SCI using video recordings of beam walking and inclined ladder climbing. Five functional parameters were studied: foot-stepping angle (FSA), rump-height index (RHI) estimating paw placement and body weight support, respectively, number of correct ladder steps (CLS) assessing skilled hindlimb movements, the BBB-locomotor score and an established urinary bladder score (BS). Sensitivity tests were followed by electrophysiological measurement of M- and H-wave amplitudes from contractions of the plantar musculature after stimulation of the tibial nerve. The closing morphological measurements included lesion volume and expression of astro- and microglia below the lesion. RESULTS: Numerical assessments of BBB, FSA, BS, lesion volume and GFAP-expression revealed no significant differences between both strains. However, compared to SD-rats, the blind SD/RCS animals significantly improved RHI and CLS by 6 - 12 weeks after SCI. To our surprise the withdrawal latencies in the blind SD/RCS rats were longer and the amplitudes of M- and H-waves lower. The expression of IBA1-immunoreactivity in the lumbar enlargement was lower than in the SD-animals. CONCLUSION: The longer withdrawal latencies suggest a decreased sensitivity in the blind SD/RCS rats, which promotes better recovery after SCI. In this way our results provide indirect support to earlier work showing, that hypersensitivity and chronic pain after contusive SCI impair the recovery of locomotor function.

Anatomy of the human orbital muscle (OM): Features of its detailed topography, syntopy and morphology.

The human orbital muscle (OM) is not readily accessible during ordinary anatomical teaching because of insufficient time and difficulties encountered in the preparation. Accordingly, its few anatomical descriptions are supported only by drawings, but not by photographs. The aim of this study was to present OM in dissected anatomic specimens in more detail. Following microscope-assisted dissection, its location, syntopy and morphology were analyzed in 88 orbits of 51 cadavers. Together with the periorbital connective tissue OM filled the infraorbital fissure (IOF) and extended back to the cavernous sinus. As a new finding, we here report that in 34% of the orbits we observed OM-fibers, which proceeded from IOF caudally to the facies infratemporalis of the maxilla. OM had a mean width of 4±1mm, a mean length of 22±5mm and its mean mass was 0.22±0.19g. The subsequent histological analysis of all specimens showed features of smooth muscle tissue: long, spindle-like cells with a centrally located cell nucleus (hematoxylin-eosin staining) which were innervated by tyrosine-hydroxylase immunopositive adrenergic fibers. We conclude that precise knowledge on OM might be very helpful not only to students in medicine and dentistry during anatomical dissection courses, but also to head and neck surgeons, ear-nose-throat specialists and neurosurgeons working in this field.

The Contribution of Beverages to Intakes of Energy and MyPlate Components by Current, Former, and Never Smokers in the United States.

BACKGROUND: Although beverage intake patterns have been shown to differ by smoking status, it is unknown whether the contributions of beverages to intakes of energy and MyPlate components also differ. OBJECTIVE: The purpose of this study was to compare beverage intakes and contributions of energy and MyPlate components by source (food alone, beverages alone, and food and beverages together) in diets of adult current, former, and never smokers. DESIGN AND PARTICIPANTS: Dietary data from 4,823 men and 4,672 women aged ≥20 years who participated in What We Eat in America, National Health and Nutrition Examination Survey 2005-2008, were analyzed. MAIN OUTCOME MEASURES: Beverage intake and the contributions to energy and MyPlate components by beverages. STATISTICAL ANALYSIS: Regression analyses identified differences in intake among groups. RESULTS: Current smokers consumed more total beverages, coffee, and sugar-sweetened beverages than never and former smokers (P<0.001). Male current smokers drank more alcoholic beverages than never and former smokers, whereas female current and former smokers both consumed more alcoholic beverages than never smokers. Current smokers obtained more energy from beverages than their nonsmoking counterparts, although total energy intake did not differ. Intakes of added sugars, alcohol, and empty calories were higher for current than never smokers, and differences were accounted for by current smokers' beverage choices. CONCLUSIONS: This study adds to the body of research on smoking and dietary behavior by showing that not only do smokers consume a higher volume of beverages, but they also have a higher intake of energy provided by beverages, mainly empty calories from added sugars and alcohol. Our findings highlight the importance of assessing beverages' contribution to the total diet. Recognizing the common co-occurrence of smoking and specific beverage choices can help target health promotion and disease prevention efforts for this subpopulation.