Synthesis,Biochemistry, and Computational Studies of Brominated Thienyl Chalcones: A New Class of Reversible MAO‐B Inhibitors

A series of (2E)‐1‐(5‐bromothiophen‐2‐yl)‐3‐(para‐substituted phenyl)prop‐2‐en‐1‐ones ( TB1 – TB11 ) was synthesized and tested for inhibitory activity toward human monoamine oxidase (hMAO). All compounds were found to be competitive, selective, and reversible toward hMAO‐B except (2E)‐1‐(5‐bromothiophen‐2‐yl)‐3‐(4‐nitrophenyl)prop‐2‐en‐1‐one ( TB7 ) and (2E)‐1‐(5‐bromothiophen‐2‐yl)‐3‐(4‐chlorophenyl)prop‐2‐en‐1‐one ( TB8 ), which were selective inhibitors of hMAO‐A. The most potent compound, (2E)‐1‐(5‐bromothiophen‐2‐yl)‐3‐[4‐(dimethylamino)phenyl]prop‐2‐en‐1‐one ( TB5 ), showed the best inhibitory activity and higher selectivity toward hMAO‐B, with K_i and SI values of 0.11±0.01 μm and 13.18, respectively. PAMPA assays for all compounds were carried out in order to evaluate the capacity of the compounds to cross the blood–brain barrier. Moreover, the most potent MAO‐B inhibitor, TB5 , was found to be nontoxic at 5 and 25 μm , with 95.75 and 84.59 % viability among cells, respectively. Molecular docking simulations were carried out to understand the crucial interactions responsible for selectivity and potency.     

Composition and Recyclability Analysis of Poly(Vinyl Chloride) Recovered from Computer Power Cables and Commercial Wires

The product‐based recycling of the electrical and electronic devices and their by‐products are limited due to their complex characteristics and dissimilar material characteristics. However, such recycling procedures give clear ideas about the composition and possible recycling options of the materials present in them. Consequently, the present study deals with isolation and recycling of the major polymeric fraction present in the waste computer power supply cables (CPS) and electrical power supply (EPS) wires isolated from the household items. The composition analysis of CPS and EPS indicates that the poly(vinyl chloride) (PVC) is the major polymeric fraction along with minor content of polyethylene (PE) and polycarbonate (PC). Further, this research compares the mechanical recyclability of the PVC recovered from the CPS and EPS. Among the PVC's analyzed, PVC isolated from the EPS has been indicated superior mechanical properties. Similarly, thermal degradation analysis (TGA) indicated higher thermal stability for the PVC isolated from EPS. Besides, the flammability of the PVC specimens was studied and concluded with the possible mechanism occurring during combustion. Moreover, this study points out that PVC recovered from EPS and CPS can be mechanically recycled for the elimination of the waste. J. VINYL ADDIT. TECHNOL., 26:213–223, 2020. © 2019 Society of Plastics Engineers     

A Novel Approach to Improve the Speech Intelligibility Using Fractional Delta-amplitude Modulation Spectrogram

Abstract

Speech enhancement is an interesting research area that aims at improving the quality and intelligibility of the speech that is affected by the additive noises, such as airport noise, train noise, restaurant noise, and so on. The presence of these background noises degrades the comfort of listening of the end user. This article proposes a speech enhancement method that uses a novel feature extraction which removes the noise spectrum from the noisy speech signal using a novel fractional delta-AMS (amplitude modulation spectrogram) feature extraction and the D-matrix feature extraction method. The fractional delta-AMS feature extraction strategy is the modification of the delta-AMS with the fractional calculus that increases the sharpness of the feature extraction. The extracted features from the frames are used to determine the optimal mask of all the frames of the noisy speech signal and the mask is employed for training the deep belief neural networks (DBN). The two metrics root mean square error (RMSE) and perceptual evaluation of speech quality (PESQ) are used to evaluate the method. The proposed method yields a better value of PESQ at all level of noise and RMSE decreases with increased noise level.     

TR1, a new member of the tumor necrosis factor receptor superfamily, induces fibroblast proliferation and inhibits osteoclastogenesis and bone resorption

A newly identified member of the tumor necrosis factor receptor (TNFR) superfamily shows activities associated with osteoclastogenesis inhibition and fibroblast proliferation. This new member, called TR1, was identified from a search of an expressed sequence tag database, and encodes 401 amino acids with a 21-residue signal sequence. Unlike other members of TNFR, TR1 does not contain a transmembrane domain and is secreted as a 62 kDa glycoprotein. TR1 gene maps to chromosome 8q23-24.1 and its mRNA is abundantly expressed on primary osteoblasts, osteogenic sarcoma cell lines, and primary fibroblasts. The receptors for TR1 were detected on a monocytic cell line (THP-1) and in human fibroblasts. Scatchard analyses indicated two classes of high and medium-high affinity receptors with a kD of approximately 45 and 320 pM, respectively. Recombinant TR1 induced proliferation of human foreskin fibroblasts and potentiated TNF-induced proliferation in these cells. In a coculture system of osteoblasts and bone marrow cells, recombinant TR1 completely inhibited the differentiation of osteoclast-like multinucleated cell formation in the presence of several bone-resorbing factors. TR1 also strongly inhibited bone-resorbing function on dentine slices by mature osteoclasts and decreased 45Ca release in fetal long-bone organ cultures. Anti-TR1 monoclonal antibody promoted the formation of osteoclasts in mouse marrow culture assays. These results indicate that TR1 has broad biological activities in fibroblast growth and in osteoclast differentiation and its functions.     

Effects of water on the rheological characteristics of biscuit dough and quality of biscuits

 The influence of water on the rheological characteristics of biscuit dough and quality of biscuits was studied. A variation of even 1% in water content considerably changed the various rheological characteristics of biscuit dough. Increasing water content by 3% significantly increased the compliance from 32.6% to 45.6%, and decreased the extrusion time from 100 s to 34 s, the apparent biaxial extensional viscosity from 3.06×10⁵ Pas to 1.5×10⁵ Pas, and the consistency from 943 Ns to 620 Ns for dough based on weak wheat flour. The elastic recovery of biscuit dough increased significantly from 0.425 mm to 0.535 mm. Dough became more cohesive and adhesive with increasing water content, whilst biscuits became harder, as indicated by increases in density, breaking strength and compression strength. Received: 14 September 1998     

Studies on protein and its high‐molecular‐weight subunit composition in relation to chapati‐making quality of Indian wheat cultivars

In order to predict the suitability of wheat for chapati making, 15 Indian wheat cultivars were studied for various protein characteristics in relation to chapati‐making quality. The cultivars varied considerably in their protein characteristics and chapati‐making potential. Results clearly indicated that both quantitative and qualitative characteristics of proteins influenced the chapati‐making potential of cultivars. Puffed height, the important qualitative parameter of chapati, was positively correlated with protein content (r = 0.62, p < 0.05), gluten content (r = 0.79, p < 0.01), sodium dodecyl sulphate (SDS) sedimentation value (r = 0.57, p < 0.05) and Glu‐1 quality scores of high‐molecular‐weight (HMW) subunits (r = 0.66, p < 0.01). Overall quality score of chapati was positively correlated with gluten content (r = 0.64, p < 0.01), SDS sedimentation value (r = 0.60, p < 0.05) and Glu‐1 score (r = 0.58, p < 0.05). HMW subunit composition varied considerably among cultivars. Cultivars having 5 + 10 subunits at the Glu‐1D chromosome, a protein content of about 130 g kg^?1 and SDS sedimentation value around 75 ml yielded excellent chapatis, while those having 2 + 12 subunits, a protein content of about 115 g kg^?1 and SDS sedimentation value around 55 ml resulted in poor chapatis. Interestingly, the presence of the 1BL/1RS chromosome in cultivars had no adverse effect on chapati quality. © 2003 Society of Chemical Industry     

Influence of additives on the rheological characteristics and baking quality of wheat flours

 The response of Indian commercially milled flour to different additives was studied. The incorporation of reducing agents, such as l-cysteine hydrochloride (l-cysteine HCl), reduced the water absorption capacity (WAC) and stability of medium-strong wheat flour as well as weak wheat flour. This effect was also shown by other reducing agents or enzymes; however, the extent of change was found to be greater in medium-strong wheat flour. Surfactants/emulsifiers, such as glycerol monostearate, sodium stearoyl lactylate, and diacetyl tartaric esters of monoglycerides (DATEM), did not alter the WAC significantly, but marginally improved the stability of the dough. The change observed in the extensograph was greater with reducing agents and enzymes. In general, use of l-cysteine HCl or α-amylase or protease reduced the resistance to extension and increased the extensibility, depending on the level of addition. l-cysteine HCl, however, gave a greater reduction in the resistance to extension in medium-strong than in weak flour. On the other hand, use of surfactants/emulsifiers increased the resistance to extension and decreased the extensibility, and the effect was greater with DATEM. The bread volume improved considerably on incorporation of l-cysteine HCl, while DATEM also increased the loaf volume considerably at a 1% level in weak flour. Maximum improvement in loaf volume was found for DATEM in the case of weak flour, indicating that the responses of flour to different additives were different. Received: 10 February 1999 / Revised version: 27 April 1999     

Trust Based Detection and Elimination of Packet Drop Attack in the Mobile Ad-Hoc Networks

The mobile ad hoc network (MANET) is communication network of a mobile node without any prior infrastructure of communication. The network does not have any static support; it dynamically creates the network as per requirement by using available mobile nodes. This network has a challenging security problem. The security issue mainly contains a denial of service attacks like packet drop attack, black-hole attack, gray-hole attack, etc. The mobile ad-hoc network is an open environment so the working is based on mutual trust between mobile nodes. The MANETs are vulnerable to packet drop attack in which packets travel through the different node. The network while communicating, the node drops the packet, but it is not attracting the neighboring nodes to drop the packets. This proposed algorithm works with existing routing protocol. The concept of trusted list is used for secure communication path. The trusted list along with trust values show how many times node was participated in the communication. It differentiates between altruism and selfishness in MANET with the help of energy level of mobile components. The trust and energy models are used for security and for the differentiation between altruism and selfishness respectively.     

Three-dimensional structure of diferric bovine lactoferrin at 2.8 A resolution

The three-dimensional structure of diferric bovine lactoferrin (bLf) has been determined by X-ray crystallography in order to investigate the factors that influence iron binding and release by transferrins. The structure was solved by molecular replacement, using the coordinates of diferric human lactoferrin (hLf) as a search model, and was refined with data to 2.8 A resolution by simulated annealing (X-PLOR) and restrained least squares (TNT). The final model comprises 5310 protein atoms (residues 5 to 689), 124 carbohydrate atoms (from ten monosaccharide units, in three glycan chains), 2 Fe3+, 2 CO32- and 50 water molecules. This model gives an R-factor of 0.232 for 21440 reflections in the resolution range 30.0 to 2.8 A. The folding of the bLf molecule is essentially the same as that of hLf, but bLf differs in the extent of closure of the two domains of each lobe, and in the relative orientations of the two lobes. Differences in domain closure are attributed to amino acid changes in the interface, and differences in lobe orientations to slightly altered packing of two hydrophobic patches between the lobes. Changed interdomain interactions may explain the lesser iron affinity of bLf, compared with hLf, and two lysine residues behind the N-lobe iron site of bLf offer new insights into the "dilysine trigger" mechanism proposed for iron release by transferrins. The bLf structure is also notable for several well-defined oligosaccharide units which demonstrate the structural factors that stabilise carbohydrate structure. One glycan chain, attached to Asn545, appears to contribute to interdomain interactions and may modulate iron release from the C-lobe.