Earticle

Glucagon-like peptide 2 receptor, a GPCR, binds with the glucagon-like peptide, GLP-2 and regulates various metabolic functions in the gastrointestinal tract. It plays an important role in the nutrient homeostasis related to nutrient assimilation by regulating mucosal epithelium. GLP-2 receptor affects the cellular response to external injury, by controlling the intestinal crypt cell proliferation. As they are therapeutically attractive towards diseases related with the gastrointestinal tract, it becomes essential to analyse their structural features to study the pathophysiology of the diseases. As the three dimensional structure of the protein is not available, in this study, we have performed the homology modelling of the receptor based on single- and multiple template modeling. The models were subjected to model validation and a reliable model based on the validation statistics was identified. The predicted model could be useful in studying the structural features of GLP-2 receptor and their role in various diseases related to them.

Glucagon like pepide-2, one of the GLPs, is involved in various metabolic functions in the gastrointestinal tract. It plays a major role in the regulation of mucosal epithelium and the intestinal crypt cell proliferation. Because of their therapeutic importance towards the diseases in the gastrointestinal tract, it becomes necessary to study their interaction with its receptor, GLP-2R. In this study, we have developed protein-protein docking complexes of GLP-2 – GLP-2 receptor. Homology models of GLP-2 are developed, and a reliable model out of the predicted models was selected after model validation. The model was bound with the receptor, to study the important interactions of the complex. This study could be useful in developing novel and potent drugs for the diseases related with GLP-2.

The chemical shifts in the 13C NMR spectra of 2,3,4,5-tetraphenyl-1-silacyclopentdienide dianion [SiC4Ph4]2−•2[K+] (3) and 2,3,4,5-tetraphenyl-1-germacyclopentdienide dianion [GeC4Ph4]2−•2[K+] (4) were compared to those of [SiC4Ph4]2−•2[Li+] (5), [SiC4Ph4]2−•2[Na+] (6), and [GeC4Ph4]2−•2[Li+] (7). The average polarizations in two phenyl groups of two potassium salts are decreased over 15% to 20% comparing to those of the lithium salts and sodium salt {[EC4Ph4]2−•2[M+] (E=Si, Ge, M=Li, Na) due to the effect of the counter potassium cation.

Diabetes mellitus has become a major growing public health problem worldwide. More than 90% of all diabetes cases are classified as type 2 diabetes (T2D), which is also known as non-insulin dependent diabetes. Protein tyrosine phosphatase 1B (PTP1B) plays an important role in the negative regulation of insulin signal transduction pathway and has emerged as novel therapeutic strategy for the treatment of type 2 diabetes. PTP1B inhibitors enhance the sensibility of insulin receptor (IR) and have favorable curing effect for insulin resistance-related diseases. Recently twelve antidiabetic xanthones were isolated from the bark of Garcinia xanthochymus. Hence, in the present study, molecular docking was carried out for these twelve xanthones. The objective of this work is to study the interaction of the newly isolated xanthones with PTP1B. The docking results showed that xanthones have good interactions and has better docking score with PTP1B and suggest LYS120 and ASP181 are the important residues involved in interaction between PTP1B enzyme and the xanthones.

Vascular endothelial growth factor (VEGF) is an important signaling protein involved in angiogenesis, which is the formation of new blood vessels from pre-existing vessels. Consequently, blocking of the vascular endothelial growth factor receptor (VEGFR-2) by small molecule inhibitors leads to the inhibition of cancer induced angiogenesis. In this study, we performed a two dimensional quantitative structure activity relationship (2D-QSAR) study of 38 N-Phenyl-N’-{4-(4- quinolyloxy) phenyl} urea derivatives as VEGFR-2 inhibitors based on hologram quantitative structure−activity (HQSAR). The model developed showed reasonable q 2=0.521 and r 2=0.932 values indicating good predictive ability and reliability. The atomic contribution map analysis of most active compound (compound 7) indicates that hydrogen and oxygen atoms in the side chain of ring A and oxygen atom in side chain of ring C contributes positively to the activity of the compounds. The HQSAR model developed and the atomic contribution map can serve as a guideline in designing new compounds for VEGFR-2 inhibition.

In this study, HEMA, MMA, AA, and EGDMA were used as basic combinations for manufacturing hydrophilic lenses for ophthalmic applications. In addition, AIBN (thermal polymerization initiator), 2H2M (photo polymerization initiator), and 3-hydroxypyridine (additive) were used to manufacture hydrophilic ophthalmic lenses through thermal polymerization and photo polymerization before their physical properties were measured. The results showed that when ophthalmic lenses were prepared via thermal polymerization and photo polymerization using 3-hydroxypyridine as an additive, their optical and physical properties and surface structures were different in each case, but they all satisfied the physical properties required for ophthalmic lenses.

An antimicrobial peptides-producing Bacillus strain CBS73 was isolated from fermented food (kimchi) that produces low-molecular-weight proteins with broad-spectrum antimicrobial activity. Our goal was to explore the therapeutic potential of antimicrobial substances produced by Bacillus species. Peptide CBS73 was purified from Bacillus subtilis subsp. subtilis with identity of 99.79%. It was found to be stable at pH 4.0-10.0 and temp 20- 60oC. A protein band around 5.2 kDa was detected in tricine-SDS-PAGE and band was confirmed by MALDI-TOF test. Peptide CBS73 showed antimicrobial activity against MDR bacteria. The minimal inhibitory concentration (MIC) of peptide CBS73 for vancomycin-resistant S. aureus (VRSA), vancomycin resistant Enterococci (VRE) and Salmonella typhimurium ranged from 10-40 μg/mL. The antioxidant activity of peptide CBS73 was measured by DPPH scavenging, reducing power activity and total phenolic content. Cell viability and NO production result showed less cytotoxic effect upto 12 μg/mL. Peptide CBS73 could be a promising antimicrobial agent for clinical application.

In this paper, it is aim to implement a wheelchair monitoring system that provides users with customized medical services easily in everyday life, together with mobility guarantee, which is the most basic requirement of the elderly and disabled persons with physical disabilities. The case-based intelligent wheelchair monitoring system proposed in this study is based on a case-based k-NN algorithm, which implements a system for constructing and inferring examples of various biometric and environmental information of wheelchair users as a knowledge database and a monitoring interface for wheelchair users. In order to confirm the usefulness of the case-based k-NN algorithm, the SVM algorithm showed an average accuracy of 84.2% and the average accuracy of the proposed case-based k-NN algorithm was 86.2% And showed higher performance in terms of accuracy. The system implemented in this paper has the advantage of measuring biometric information and data communication regardless of time and place and it can provide customized service of wheelchair user through user friendly interface.

Non-hydrolyzable fluorinated organosilicon compounds as an eletrolyte for the application of lithium-ion batteries (LIB) are synthesized. New synthetic method for the perfluorinated organosilicon compound containing spacer such as ethyl and propyl group with cyano moiety instead of ethylene glycol to prevent hydrolysis and to promote conductivity are developed in one pot reaction with moderately high yield. Air-sensitive boron trifluoride etherate is no longer required in this reaction. The products are characterized by spectroscopic analysis.