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Mathew, Bijo,Baek, Seung Cheol,Grace Thomas Parambi, Della,Pil Lee, Jae,Joy, Monu,Annie Rilda, P. R.,Randev, Rugma V.,Nithyamol, P.,Vijayan, Vijitha,Inasu, Sini T.,Mathew, Githa Elizabeth,Lohidakshan, The Royal Society of Chemistry 2018 MedChemComm Vol.9 No.11
<P>A series of 13 phenyl substituted thiosemicarbazones (SB1-SB13) were synthesized and evaluated for their inhibitory potential towards human recombinant monoamine oxidase A and B (MAO-A and MAO-B, respectively) and acetylcholinesterase. The solid state structure of SB4 was ascertained by the single X-ray diffraction technique. Compounds SB5 and SB11 were potent for MAO-A (IC50 1.82 ± 0.14) and MAO-B (IC50 0.27 ± 0.015 μM), respectively. Furthermore, SB11 showed a high selectivity index (SI > 37.0) for MAO-B. The effects of fluorine orientation revealed that SB11 (<I>m</I>-fluorine) showed 28.2 times higher inhibitory activity than SB12 (<I>o</I>-fluorine) against MAO-B. Furthermore, inhibitions by SB5 and SB11 against MAO-A and MAO-B, respectively, were recovered to near reference levels in reversibility experiments. Both SB5 and SB11 showed competitive inhibition modes, with <I>K</I>i values of 0.97 ± 0.042 and 0.12 ± 0.006 μM, respectively. These results indicate that SB5 and SB11 are selective, reversible and competitive inhibitors of MAO-A and MAO-B, respectively. Compounds SB5, SB7 and SB11 showed moderate inhibition against acetylcholinesterase with IC50 values of 35.35 ± 0.47, 15.61 ± 0.057 and 26.61 ± 0.338 μM, respectively. Blood-brain barrier (BBB) permeation was studied using the parallel artificial membrane permeation assay (PAMPA) method. Molecular docking studies were carried out using AutoDock 4.2.</P>
Mathew, Aleyamma,George, Preethi Sara,Arjunan, Asha,Augustine, Paul,Kalavathy, MC,Padmakumari, G,Mathew, Beela Sarah Asian Pacific Journal of Cancer Prevention 2016 Asian Pacific journal of cancer prevention Vol.17 No.6
Background: Increasing breast cancer (BC) incidence rates have been reported from India; causal factors for this increased incidence are not understood and diagnosis is mostly in advanced stages. Trivandrum exhibits the highest BC incidence rates in India. This study aimed to estimate trends in incidence by age from 2005-2014, to predict rates through 2020 and to assess the stage at diagnosis of BC in Trivandrum. Materials and Methods: BC cases were obtained from the Population Based Cancer Registry, Trivandrum. Distribution of stage at diagnosis and incidence rates of BC [Age-specific (ASpR), crude (CR) and age-standardized (ASR)] are described and employed with a joinpoint regression model to estimate average annual percent changes (AAPC) and a Bayesian model to estimate predictive rates. Results: BC accounts for 31% (2681/8737) of all female cancers in Trivandrum. Thirty-five percent (944/2681) are <50 years of age and only 9% present with stage I disease. Average age increased from 53 to 56.4 years (p=0.0001), CR (per $10^5$ women) increased from 39 (ASR: 35.2) to 55.4 (ASR: 43.4), AAPC for CR was 5.0 (p=0.001) and ASR was 3.1 (p=0.001). Rates increased from 50 years. Predicted ASpR is 174 in 50-59 years, 231 in > 60 years and overall CR is 80 (ASR: 57) for 2019-20. Conclusions: BC, mostly diagnosed in advanced stages, is rising rapidly in South India with large increases likely in the future; particularly among post-menopausal women. This increase might be due to aging and/or changes in lifestyle factors. Reasons for the increased incidence and late stage diagnosis need to be studied.
Barrie, Michael Jonathan Mathew & Jun, Jaehyun. (2022). Numeral classifiers in Eastern Tamang. The Linguistic Association of Korea Journal, 30(1), 113-131. In this paper, we examine numeral classifiers and number marking in one dialect of Eastern Tamang. As Tamang is a relatively understudied dialect continuum, we give a basic description of the empirical facts. We then employ various diagnostics from the literature and one we created ourselves to determine whether classifiers compose with nouns or with numerals. We conclude that since the classifier composes with numerals, the numeral classifier is a constituent that composes with the NP. We also examine number marking and observe that the plural marker is obligatory in some environments for animate nouns, but not for inanimate nouns. We conclude by making some tentative remarks that this dialect of Eastern Tamang might be undergoing a transition from a classifier language to a number language.
Barrie, Michael Jonathan Mathew and Sung, Moonhyun. 2018. Dissecting Inchoatives and Causatives: English get Constructions. Language and Information, 22.3. 91-108. In this paper, we present data from English get-constructions and from Northern Iroquoian to challenge the recent consensus that in no languages are causatives built on inchoatives. Our data suggest the need for distinct functional projections for the causative and inchoative. We argue that while they are bundled in other situations, the functional heads for the causative and inchoative can be split as described in the present paper. This line of research follows recent trends in investigating the fine structure of the vP layer (Alexiadou et al. 2015, Harley 2013, Kim 2011, Marantz 2013, Pylkkänen 2008, Ramchand 2008, Legate 2014). We propose a syntactic mechanism for bundling and, in doing so, account for differences in the range of possible meanings with adverbs between canonical causatives and get-causatives. Briefly, get-causatives have unbundled causative and inchoative heads and have a wider ranger of adverbial meanings due to the projection of independent CausP and InchP. Canonical causatives have a bundled Caus-Inch head, projecting a single Caus/InchP, which leads to fewer sites for adverbs to adjoin and accordingly to a narrower range of adverbial meanings. (Sogang University)
Two derivatives of star shaped compounds based on naphthylamine benzene고리에 methoxy기와 ethoxy기가 치환기로 연결되어있는 naphthylamine 관련 화합물을 합성하였다. 합성한 화합물의 전자 및 열적특성을 cyclic voltametry (CV) 및 differential scanning calorimetry (DSC)를 이용하여 조사하였다. Two derivatives of star shaped compounds based on naphthylamine with symmetric trisubstituted benzene as core, methoxy and ethoxy as end substitutions are synthesized. The synthesized compounds are characterized by UV-visible, FT-IR and NMR spectrometric techniques. The electronic and thermal properties of the compounds are studied using cyclic voltametry (CV) and differential scanning calorimetry (DSC) respectively. The data's obtained have similarity with the arylamines that have been already used in optoelectronic devices. So these compounds are interesting materials for applications in such devices.
The logistic distribution is generalized using the Marshall-Olkin scheme and its generalization. Some properties are studied. First order autoregressive time series model with Marshall-Olkin semi-logistic distribution as marginal is developed and studied.
<P>Optically pure beta-amino acids are of high pharmacological significance since they are used as key ingredients in many physiologically active compounds. Despite a number of enzymatic routes to these compounds, an efficient synthesis of beta-amino acids continues to pose a major challenge for researchers. omega-Transaminase has emerged as an important class of enzymes for generating amine compounds. However, only a few omega-transaminases have been reported so far which show activity towards aromatic beta-amino acids. In this study, (S)-omega-transaminase from Burkholderia graminis C4D1M has been functionally characterized and used for the production of chiral aromatic beta-amino acids via kinetic resolution. The enzyme showed a specific activity of 3.1 U/mg towards rac-beta-phenylalanine at 37 degrees C. The K-m and K-cat values of this enzyme towards rac-beta-phenylalanine with pyruvate as the amino acceptor were 2.88 mM and 91.57 min(-1) respectively. Using this enzyme, racemic beta-amino acids were kinetically resolved to produce (R)-beta-amino acids with an excellent enantiomeric excess (> 99%) and similar to 50% conversion. Additionally, kinetic resolution of aromatic beta-amino acids was performed using benzaldehyde as a cheapamino acceptor. (C)2015 Elsevier B.V. All rights reserved.</P>
<P><B>Abstract</B></P> <P>To date, numerous delivery systems based on either organic or inorganic material have been developed to achieve efficient and sustained delivery of therapeutics. Hydrogels, which are three dimensional networks of crosslinked hydrophilic polymers, have a significant role in solving the clinical and pharmacological limitations of present systems because of their biocompatibility, ease of preparation and unique physical properties such as a tunable porous nature and affinity for biological fluids. Development of an <I>in situ</I> forming injectable hydrogel system has allowed excellent spatial and temporal control, unlike systemically administered therapeutics. Injectable hydrogel systems can offset difficulties with conventional hydrogel-based drug delivery systems in the clinic by forming a drug/gene delivery or cell-growing depot in the body with a single injection, thereby enabling patient compliance and comfort. Carbohydrate polymers are widely used for the synthesis of injectable <I>in situ</I>-forming hydrogels because of ready availability, presence of modifiable functional groups, biocompatibility and other physiochemical properties. In this review, we discuss different aspects of injectable hydrogels, such as bulk hydrogels/macrogels, microgels, and nanogels derived from natural polymers, and their importance in the delivery of therapeutics such as genes, drugs, cells or other biomolecules and how these revolutionary systems can complement existing therapeutic delivery systems.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>