Syntheses and spectroscopic studies of potential antitumor copper(II) complexes with 5-phenylazo-3-methoxy salicylidene thiosemicarbazone and N4 substituted thiosemicarbazones

Five new copper(II) complexes of 5-phenylazo-3-methoxy salicylidene thiosemicarbazone and N4 substituted thiosemicarbazones have been synthesized. They have been characterized by chemical analyses, magnetic, conductance data, and by ultraviolet (UV)--visible, infrared, and electron spin resonance spectra. The complexes have the general formula CuL2, where HL is the ligand. One representative complex has been screened in vitro and in vivo against P388 lymphocytic leukemia cells sensitive and resistant to adriamycin (P388/S and P388/R). It has shown promising growth inhibition activity. We are reporting here for the first time the antineoplastic activity of this complex against experimental tumor systems.     

Characterisation of copolymer, poly (hydroxybutyrate-co-hydroxyvalerate) (PHB-co-PHV) produced by Halomonas campisalis (MCM B-1027), its biodegradability and potential application

Characterisation of polyhydroxyalkanoate (PHA) film produced by haloalkalitolerant Halomonascampisalis (MCM B-1027) in 14 L SS fermenter revealed it to have composition of monomer units, HB:HV as 96:4 as analysed by ¹H NMR indicating the PHA as a co-polymer of PHB-co-PHV, molecular weight by gel permeation chromatography as 2.08 × 10⁶, melting temperature 166.51 °C, tensile strength 18.8 MPa; two relaxations namely beta transition corresponding to the glass rubber transition and alpha transition corresponding to crystalline relaxation by Dynamic Mechanical Thermal analysis and only one relaxation corresponding to MWS interfacial polarisation with activation energy of 129 kJ/mol by broadband dielectric spectroscopy. Optical microscopic studies showed typical Maltese-cross pattern of spherulites. The PHA film was found to be biodegradable by standard ASTM method as well as by soil burial method. The leak proof polymer bags prepared from the film could be used as a packaging material.     

Synthesis and anti-inflammatory activity of some new 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazole derivatives

A series of 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazoles were designed and synthesized in order to obtain new compounds with potential anti-inflammatory activity. The title compounds were screened for in vivo anti-inflammatory activity by using Carrageenan induced rat paw edema method. Diclofenac sodium was used as a standard drug for comparison. Out of the 30 compounds tested, compound 19a, 19b, 25a, 25b exhibited significant anti-inflammatory activity. Selected compounds were also screened for in vitro COX-2 inhibition assay and analgesic activity in the acetic acid induced writhing model.     

Modulation in light utilization by a microalga Asteracys sp. under mixotrophic growth regimes

Photosynthesis Research - This study is the first to explore the influence of incident light intensity on the photosynthetic responses under mixotrophic growth of microalga Asteracys sp. When grown...     

High-Fat Diet Induces Hepatic Insulin Resistance and Impairment of Synaptic Plasticity

High-fat diet (HFD)-induced obesity is associated with insulin resistance, which may affect brain synaptic plasticity through impairment of insulin-sensitive processes underlying neuronal survival, learning, and memory. The experimental model consisted of 3 month-old C57BL/6J mice fed either a normal chow diet (control group) or a HFD (60% of calorie from fat; HFD group) for 12 weeks. This model was characterized as a function of time in terms of body weight, fasting blood glucose and insulin levels, HOMA-IR values, and plasma triglycerides. IRS-1/Akt pathway was assessed in primary hepatocytes and brain homogenates. The effect of HFD in brain was assessed by electrophysiology, input/output responses and long-term potentiation. HFD-fed mice exhibited a significant increase in body weight, higher fasting glucose- and insulin levels in plasma, lower glucose tolerance, and higher HOMA-IR values. In liver, HFD elicited (a) a significant decrease of insulin receptor substrate (IRS-1) phosphorylation on Tyr608 and increase of Ser307 phosphorylation, indicative of IRS-1 inactivation; (b) these changes were accompanied by inflammatory responses in terms of increases in the expression of NFκB and iNOS and activation of the MAP kinases p38 and JNK; (c) primary hepatocytes from mice fed a HFD showed decreased cellular oxygen consumption rates (indicative of mitochondrial functional impairment); this can be ascribed partly to a decreased expression of PGC1α and mitochondrial biogenesis. In brain, HFD feeding elicited (a) an inactivation of the IRS-1 and, consequentially, (b) a decreased expression and plasma membrane localization of the insulin-sensitive neuronal glucose transporters GLUT3/GLUT4; (c) a suppression of the ERK/CREB pathway, and (d) a substantial decrease in long-term potentiation in the CA1 region of hippocampus (indicative of impaired synaptic plasticity). It may be surmised that 12 weeks fed with HFD induce a systemic insulin resistance that impacts profoundly on brain activity, i.e., synaptic plasticity.     

Protein-Functionalized PLGA Nanoparticles of Lamotrigine for Neuropathic Pain Management

Lamotrigine (LTG), a sodium and calcium channel blocker, has demonstrated efficacy for the treatment of neuropathic pain in multiple, randomized, controlled trials. However, its potential clinical applications in neuropathic pain are limited due to the risk of dose-dependent severe rashes associated with high dose and prompt dose escalation. Further, the poor pharmacokinetic profile due to non-selective distribution to organs other than brain reduces the efficacy of dosage regimen. Therefore, the aim of present investigation is to develop surface-engineered LTG nanoparticles (NPs) using transferrin and lactoferrin as ligand to deliver higher amount of drug to brain and improve the biodistribution and pharmacokinetic profile of drug with prolonged duration of action and reduced accumulation in non-target organs. The LTG NPs were prepared by nanoprecipitation and optimized by factorial design for high entrapment and optimized particle size. The optimized NPs were surface functionalized by conjugating with the lactoferrin (Lf) and transferrin (Tf) as ligands. The developed NPs were characterized for different physicochemical parameters and stability. The in vivo biodistribution showed preferential targeting to brain and reduced accumulation in non-target organs over a prolonged duration of time. Finally, partial sciatic nerve injury model was used to demonstrate the increased pharmacodynamic response as antinociceptive effect. Both biodistribution and pharmacodynamic study in mice confirmed that the approach used for LTG can help to increase clinical applications of LTG due to brain targeting and reduced side effects.KEY WORDS: brain targeting, factorial design, lactoferrin, lamotrigine, transferrin     

Preparation and optical parameter characterization of two aldehyde derivative thin films for photonic applications by drop casting method

In this study, thin films of polymer poly(methyl methacrylate) were prepared using a drop casting method. Two newly synthesized aldehyde derivatives, 2‐bromomalonaldehyde and 5,6‐dihydroimidazo[2,1‐b]thiazole‐2‐carbaldehyde, were used at different concentrations to dope the films. The prepared films were transparent and therefore studied for application in photonics. Optical characterization of the samples was carried out using different spectroscopy techniques. Absorption spectra for both samples were obtained using a UV–vis light spectrophotometer. Other significant optical parameters, such as refractive index, extinction coefficient, and band gap energies, were calculated from the absorption spectra. The effect of doping concentration on these parameters was studied. Emission spectra were obtained using a fluorescence spectrophotometer and the effect of doping was observed. Fourier transform infrared spectra of the doped films were obtained and compared with the pure compound to note changes in peak values and peak intensity. This present work studied the effect of doping on optical properties and examined the application of the samples for photonics.     

Spiro Benzodiazepine Substituted Fluorocoumarins as Potent Anti-Anxiety Agents

Russian Journal of Bioorganic Chemistry - 1,5-Benzodiazepines are one of the important class of tranquilizers. The fusion of heterocyclic systems like coumarins and indolines with the...