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El-Sawy E.,National Research Center of Egypt | Bassyouni F.,National Research Center of Egypt | Abu-Bakr S.,National Research Center of Egypt | Rady H.,National Research Center of Egypt | Abdlla M.,Pharmaceutical Company
Acta Pharmaceutica | Year: 2010

Starting from 1-benzyl- (2a) and 1-benzoyl-3-bromoacetyl indoles (2b) new heterocyclic, 2-thioxoimidazolidine (4a, b), imidazolidine-2,4-dione (5a, b), pyrano(2,3-d)imida-zole (8a, b and 9a, b), 2-substituted quinoxaline (11a, b-17a, b) and triazolo(4,3-a)quinoxaline derivatives (18a, b and 19a, b) were synthesized and evaluated for their antimicrobial and anticancer activities. Antimicrobial activity screening performed with concentrations of 0.88, 0.44 and 0.22 μg mm-2 showed that 3-(1-substituted indol-3-yl)quinoxalin- 2(1H)ones (11a, b) and 2-(4-methyl piperazin-1-yl)-3-(1-substituted indol-3-yl) quinoxalines (15a, b) were the most active of all the tested compounds towards P. aeruginosa, B. cereus and S. aureus compared to the reference drugs cefotaxime and piperacillin, while 2-chloro-3-(1-substituted indol-3-yl)quinoxalines (12a, b) were the most active against C. albicans compared to the reference drug nystatin. On the other hand, 2-chloro-3-(1-benzyl indol-3-yl) quinoxaline 12a display potent efficacy against ovarian cancer xenografts in nude mice with tumor growth suppression of 100.0 ± 0.3 %.

Yu S.A.,Seoul National University | Choe E.K.,Seoul National University | Oh T.Y.,Pharmaceutical Company | Park K.J.,Seoul National University
Korean Journal of Physiology and Pharmacology | Year: 2014

Gastrointestinal motility consists of phasic slow-wave contractions and the migrating motor complex (MMC). Eupatilin (Stillen®) has been widely used to treat gastritis and peptic ulcers, and various cytokines and neuropeptides are thought to be involved, which can affect gastrointestinal motility. We performed a study to identify the effects of eupatilin on lower gastrointestinal motility with electromechanical recordings of smooth muscles in the human ileum and colon. Ileum and colon samples were obtained from patients undergoing bowel resection. The tissues were immediately stored in oxygenated Krebs-Ringer's bicarbonate solution, and conventional microelectrode recordings from muscle cells and tension recordings from muscle strips and ileal or colonic segments were performed. Eupatilin was perfused into the tissue chamber, and changes in membrane potentials and contractions were measured. Hyperpolarization of resting membrane potential (RMP) was observed after administration of eupatilin. The amplitude, AUC, and frequency of tension recordings from circular and longitudinal smooth muscle strips and bowel segments of the ileum and colon were significantly decreased after admission of eupatilin. Eupatilin elicited dose-dependent decreases during segmental tension recordings. In conclusion, eupatilin (Stillen®) showed inhibitory effects on the human ileum and colon. We propose that this drug may be useful for treating diseases that increase bowel motility, but further studies are necessary.

Shpakov A.O.,RAS Sechenov Institute of Evolutionary Physiology and Biochemistry | Derkach K.V.,RAS Sechenov Institute of Evolutionary Physiology and Biochemistry | Zharova O.A.,Pharmaceutical Company | Shpakova E.A.,RAS Institute of Macromolecular Compounds | Bondareva V.M.,RAS Sechenov Institute of Evolutionary Physiology and Biochemistry
Biologicheskie Membrany | Year: 2015

Binding of the type 3 melanocortin receptor (M3R) functionally coupled to Gs-proteins with omelanocytestimulating hormone (a-MSH) or M3R agonist γ-MSH results in activation of adenylyl cyclase (AC) in the brain, which is responsible for the M3R-mediated regulation of physiological and biochemical processes in the CNS and in the periphery. Decrease in the activity of M3R leads to changes in the energy metabolism, metabolic syndrome, and abnormalities in the nervous and cardiovascular systems. However, the molecular mechanisms of these alterations and the role of the adenylyl cyclase signaling system (ACSS) in them are still poorly understood. The aim of this work was to study the effect of long-term (13 months, 8 injections) immunization of male rats with BSA-conjugated peptide A-[PTNPYCICTTAH269-280]-A (A-[269-280]-A) corresponding to the third extracellular loop of rat M3R on the functional activity of ACSS in the brain, testis and myocardium of rats and on its regulation by neurotransmitters and hormones. At the end of the experiment the body weight of animals was lowered, fat mass was increased and dyslipidemia was observed; besides sensitivity to insulin was reduced, despite an increase in the insulin secretion in response to glucose loading. In the brain of immunized rats the AC stimulating effects of y-MSH, norepinephrine, serotonin, and PACAP-38 were reduced, the stimulating effect of dopamine was increased and the AC inhibitory effects of serotonin and 5-nonyloxytryptamine, an agonist of subtype IB/ID 5-hydroxytryptamine receptor, were amplified, while the AC effects of M3R/M4R-agonist a-MSH and M4R-agonist THIQ did not change. In the myocardial membranes the increase of AC stimulation by agonists of β3-adrenergic receptor (β3-AR) and the decrease of the AC stimulating effects of β1 and β2-agonists, as well as the weakening of the AC effect of relaxin were found. In the testicular membranes the AC stimulating effects of chorionic gonadotropin and PACAP-38, and GppNHp, non-hydrolysable GTP analog were decreased. These data indicate that the weakening of M3R signaling leads to significant changes in the sensitivity of ACSS in the brain, myocardium and testis to hormones that play a key role in the functioning of the nervous, cardiovascular and reproductive systems, and these changes were characterized by hormone and receptor specificity. Identification of the disturbances in ACSS is one of the approaches to study the etiology and pathogenesis of the diseases associated with inhibition of M3R-melanocortin signaling system in the brain.

Gu Q.,Pharmaceutical Company
Zhongguo xiu fu chong jian wai ke za zhi = Zhongguo xiufu chongjian waike zazhi = Chinese journal of reparative and reconstructive surgery | Year: 2011

To carry out a comprehensive and objective evaluation of viscosupplementation, so as to provide the actual judgments of effectiveness, development trends, and direction. The related literature was reviewed, and the keys were the assessments from the international relevant advisory bodies and insurance companies and the evidence-based medicine on clinic. Viscosupplementation has been gradually accepted. Although there are many different clinical views of the viscosupplementation in the molecular weight of hyaluronan, injection dose, and the indications, intra-articular injection of hyaluronan for the treatment of osteoarthritis is well accepted. Viscosupplementation is one of the methods of treating osteoarthritis. As it has been already verified that hyaluronan is effective in treating osteoarthritis of the knee and the periarthritis of shoulder, the hip joint injection is gradually recognized, and other small joints are going gradually.

Liu S.,Shanghai University | Huang J.,Shanghai University | Chen Z.,Shanghai University | Chen N.,Shanghai University | And 3 more authors.
Journal of Raman Spectroscopy | Year: 2015

Liquid chromatography andmass spectrometry were time-consuming and expensive as the main methods for the drug analysis at present, and the samplesmust be pretreated. The Raman spectroscopy measurementmethodswere fast and simple, so the Raman spectroscopy methods for the drug analysis were explored in this paper. An optical fiber nano-probe coated with gold nanoparticles was fabricated and used with surface-enhanced Raman spectroscopy (SERS) to measure levofloxacin lactate. The resulting SERS spectra of levofloxacin lactate in mouse blood that was detected by the optical fiber nano-probe clearly showed the characteristic wave numbers of levofloxacin lactate, indicating that optical fiber nano-probes can be used with spectral techniques to analyze drugs in vitro or potentially even in vivo. Copyright © 2015 John Wiley & Sons, Ltd.

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