NOPR Collection:

Exploring selectivity requirements for peripheral versus central benzodiazepine receptor bindingaffinity: QSAR modeling of 2-phenylimidazo[1,2-a]pyridine acetamides using topological and physicochemical descriptors

2016-07-20T06:37:33Z

Title: Exploring selectivity requirements for peripheral versus central benzodiazepine receptor bindingaffinity: QSAR modeling of 2-phenylimidazo[1,2-a]pyridine acetamides using topological and physicochemical descriptors Authors: Dalai, Manoj Kumar; Leonard, J Thomas; Roy, Kunal Abstract: Considering the potential of peripheral benzodiazepine receptor (PBR) Jigands in therapeutic applications and clinical benefit in the management of a large spectrum of different indications, quantitative structure-activity relationship (QSAR) study has been attempted to explore the structural and physicochemical requirements for selectivity of 2-phenylimidazo[1,2- a]pyridineacetamides for binding with peripheral over central benzodiazepine receptors (CBRs). For PBR binding affinity, molar refractivity (MR) shows a parabolic relation with binding affinity suggesting that binding affinity increases with increase in volume of the compounds, until it reaches the critical value, after which the affinity decreases. … Page(s): 105-118

Isoproterenol ameliorates workstress-induced rat skeletal muscle degeneration

2016-07-20T06:37:19Z

Title: Isoproterenol ameliorates workstress-induced rat skeletal muscle degeneration Authors: Garg, Asha; Sharma, Sushma Abstract: β-Agonists though have been widely studied for their protein anabolic effects in skeletal muscles, but the lipid status under work stress and agonist treatment have not been understood well in the skeletal muscles and heart of rat. In the present study, adult male Wistar rats were subjected to work overload stress and β agonist isoproterenol treatment (2 mg kg^-1 day^-1intraperitoneally) to examine, whether it attenuates work stress-induced changes or not. Simultaneously, β₂ antagonist butoxamine (2 mg kg^-1 day^-1 intraperitoneally) was administered to another isoproterenol-treated group. Work stress led to myofibrillar degeneration as well as rapid utilization of lipid to meet increased energy demands and for muscle repair, which was reflected through histochemical localization of lipids and biochemical estimation of cholesterol and triglycerides. Significantly decreased cholesterol levels in skeletal muscles and heart muscles were noticed. As expected, isoproterenol reversed the conditions by raising cholesterol and triglyceride levels significantly in the skeletal muscles and also by ameliorating the degenerative changes in muscle fibres as induced by work overload. However, severe accumulation of lipids in heart infers towards deleterious effects of isoproterenol on heart and thus remains a limiting factor for its immediate clinical application. Further research is needed to separate desirable effects of β agonists on skeletal muscles from any undesirable effects on the heart, so as to optimize their therapeutic potential. Page(s): 82-87

Effect of endosulfan on growth, ⍺ amylase activity and plasmids amplification in Bacillus subtilis

2009-02-27T05:25:57Z

Title: Effect of endosulfan on growth, ⍺ amylase activity and plasmids amplification in Bacillus subtilis Authors: Tolan, Veysel; Ensari, Yavuz Abstract: Endosulfan, a chlorinated hydrocarbon insecticide of cyclodiene subgroup acts as a contact poison in a wide variety of organisms. In the present study, the effect of endosulfan on the growth, α amylase activity and plasmid amplification was investigated in Bacillus subtilis system. The bacteria were grown in medium, incubated with different concentrations (32, 48, 64 and 80 μg/mL) of endosulfan. The bacterial growth was gradually seen after 1st day at up to 48 μg/L endosulfan. The 48 μg/L endosulfan inhibited approximately 50% of the bacterial growth. No growth was observed at and after 64 μg/L endosulfan, for all days (1-5). Also, no ⍺ amylase activity was found in the supernatant of the culture medium containing 64 and 80 μg/L endosulfan, whereas slight activity was observed with 32 and 48 μg/L endosulfan concentration. The amount of plasmid increased up to 50% in the presence of 32 μg/L endosulfan. Endosulfan had no effect on the ⍺ amylase activity in vitro. Page(s): 123-126

Rapid regulatory effect of tri-iodothyronine (T₃) on antioxidant enzyme activities in a fish Anabas testudineus (Bloch): Short-term in vivo and in vitro study

2009-02-27T05:25:50Z

Title: Rapid regulatory effect of tri-iodothyronine (T₃) on antioxidant enzyme activities in a fish Anabas testudineus (Bloch): Short-term in vivo and in vitro study Authors: Sreejith, P; Oommen, O V Abstract: The short-term action of thyroid hormone tri-iodothyronine (T₃) was studied in vivo and in vitro on antioxidant enzyme activities in a teleost Anabas testudineus (Bloch). T₃ injection in vivo (200 ng) in normal fish decreased the lipid peroxidation products and increased superoxide dismutase (SOD), catalase and glutathione peroxidase (GPx) activities after 30 min. T₃ in vitro (10⁻⁶ M) increased the antioxidant activities of catalase, glutathione reductase (GR), GPx and glutathione level after 15/30 min, except SOD, substantiating in vivo effects in normal fish. The results suggest a rapid regulatory effect of thyroid hormone in vivo and in vitro, in the removal of reactive oxygen species in A. testudineus. Page(s): 119-122