Crystal Structure Analysis of 1-Hydroxy-3,5-dimethoxy-9H-xanthen-9-one Isolated from Ajuga bracteosa Root Extract and Its Biological Studies

The structure of 1-hydroxy-3,5-dimethoxy-9 H-xanthen-9-one isolated from chloroform extract of Ajuga bracteosa root was analyzed by single-crystal X-ray diffraction. DPPH(1,1-diphenyl-2-picryl hydrazyl), ABTS(2,2?-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging activities(RSA) and Fe2+ chelating activities were carried out to determine the antioxidant potential of the compound. RSA values for the compound were 96%, 96% and 96% for all the three activities respectively at maximum concentration of the compound(100 μ gmL-1) with the IC50 values of 3.40, 4.86 and 0.10(μ gmL-1). Antidiabetic activities including antiglycation and α-glucosidase inhibition were also performed where the antiglycation activity was performed using two techniques including spectrofluorometric as well as spectrophotometric technique. Spectrofluorometric technique provided 97% antiglycation potential while 92% antiglycation potential was observed by spectrophotometric technique for the isolated compound. The compound at a concentration of 10 μ gmL-1 exhibited 31% α-glucosidase inhibitory potential with IC50 of 15.56 μ gmL-1. Antimicrobial activity data showed that the compound was active against all the studied pathogenic bacteria.     

NUMERICAL METHOD FOR SOLVING LINEAR BOUNDARY VALUE PROBLEMS BY THE CHEBYSHEVτ_METHOD

A new τ_method is presented for the two dimensional linear boundary value problems. Theoretical and numerical analyses are presented. These results indicate that our method works nicely and efficiently.     

Discovery of Novel Epoxyketone Peptides as Lipase Inhibitors

Obesity is the most common nutritional disorder in the developed world and is associated with important comorbidities. Pancreatic lipase (PL) inhibitors play a key role in the metabolism of human fat. A series of novel epoxyketones peptide derivatives were investigated for their pancreatic lipase inhibitory activity. The epoxyketone moiety is a well-known reactive electrophile group that has been used as part of proteasome inhibitors in cancer therapy, and it is widely believed that these are very selective for targeting the proteasome active site. Here we investigated various peptide derivatives with an epoxide warhead for their anti-lipase activity. The assessment of these novel epoxyketones was performed by an in-house method that we developed for rapid screening and identification of lipase inhibitors using GC-FID. Herein, we present a novel anti-lipase pharmacophore based on epoxyketone peptide derivatives that showed potent anti-lipase activity. Many of these derivatives had comparable or more potent activity than the clinically used lipase inhibitors such as orlistat. In addition, the lipase appears to be inhibited by a wide range of epoxyketone analogues regardless of the configuration of the epoxide in the epoxyketone moiety. The presented data in this study shows the first example of the use of epoxyketone peptides as novel lipase inhibitors.     

More Zariski pairs and finite fundamental groups of curve complements

We give a recipe for finding new examples of plane curves with a finite non-abelian fundamental group of the complement and new examples of Zariski pairs of plane curves. Received: 18 December 2000 / Revised version: 27 April 2001     

Design,Synthesis, and Biological Evaluation of Pyridazinones Containing the (2-Fluorophenyl) Piperazine Moiety as Selective MAO-B Inhibitors

Twelve pyridazinones (T1–T12) containing the (2-fluorophenyl) piperazine moiety were designed, synthesized, and evaluated for monoamine oxidase (MAO) -A and -B inhibitory activities. T6 was found to be the most potent MAO-B inhibitor with an IC₅₀ value of 0.013 µM, followed by T3 (IC₅₀ = 0.039 µM). Inhibitory potency for MAO-B was more enhanced by meta bromo substitution (T6) than by para bromo substitution (T7). For para substitution, inhibitory potencies for MAO-B were as follows: -Cl (T3) > -N(CH₃)₂ (T12) > -OCH₃ (T9) > Br (T7) > F (T5) > -CH₃ (T11) > -H (T1). T6 and T3 efficiently inhibited MAO-A with IC₅₀ values of 1.57 and 4.19 µM and had the highest selectivity indices (SIs) for MAO-B (120.8 and 107.4, respectively). T3 and T6 were found to be reversible and competitive inhibitors of MAO-B with K_i values of 0.014 and 0.0071, respectively. Moreover, T6 was less toxic to healthy fibroblast cells (L929) than T3. Molecular docking simulations with MAO binding sites returned higher docking scores for T6 and T3 with MAO-B than with MAO-A. These results suggest that T3 and T6 are selective, reversible, and competitive inhibitors of MAO-B and should be considered lead candidates for the treatment of neurodegenerative disorders like Alzheimer’s disease.     

Performance of Ni/10Sc1CeSZ anode synthesized by glycine nitrate process assisted by microwave heating in a solid oxide fuel cell fueled with hydrogen or methane

Journal of Solid State Electrochemistry - Nickel/scandia-ceria-stabilized-zirconia (Ni/10Sc1CeSZ) cermet is a potential anode for solid oxide fuel cells. The anode powder is prepared through a...