Inhibitory potency of Withania somnifera extracts against DPP-4: an in vitro evaluation

Background: Pharmacologic treatments for type 2 diabetes are based upon  increasing insulin availability and improving sensitivity to insulin. Nowadays,  glucagon like peptide-1 (GLP-1) based therapies aims at glucose control through DPP-4 inhibitors. DPP-4 is a transmembrane glycoprotein belongs to prolyl  oligopeptidase family, with the specificity of removing X-Pro or X-Ala dipeptides from the N-terminus of polypeptides. GLP-1 effect by stimulating glucose-dependent insulin release from the pancreatic islets, inhibit inappropriate post-meal glucagon release and slow gastric emptying promoting leaky gut. The current study investigated DPP-4 inhibitory activity of catechin, isolated from Withania somnifera (WS), for ethnopharmacological treatment of type 2 diabetes and aimed to increase availability of GLP-1and sensitivity to insulin.Materials and Methods: Young and matured fresh roots, leaves, and fruits of WS plant extract were considered and were systematically evaluated for DPP-4 inhibitory activity using in vitro method, enzyme kinetics, phytochemical analysis, RP-HPLC, LCMS and 1H and 13C NMR method and structure-activity relationship (SAR) studies.Results: In this study, methanol (100% and 80%) extracts of WS matured root exhibited maximum DPP-4 inhibitory activity when compared to other extracts. The maximum DPP-4 inhibitory activity was found in 100% methanol extract of matured root. Phytobioactive was purified by RP-HPLC. The compound purified was found to be flavonoid and was characterized (LCMS, 1H and 13C NMR studies), identified as catechin. Auxiliary, molecular docking was performed using Ligand Fit method using PatchDock package. The study revealed the binding affinity of catechin with DPP-4 to be -6.601 kcal/mol with 13 hydrogen interactions with the receptor and was very similar to the standard potent blockers withaferin A and others (cuscohygrine, scopoletin, sitoindoside IV, tropine), further confirming its hyperglycemic potency.Conclusion: The study reveals that, 100% methanol extract of WS matured roots contains the compound- catechin, which exhibits DPP-4 inhibitory activity resulting in increased level of bioactive GLP-1 and GIP. In this background, we concluded that the WS will be a better source for further development as new antidiabetic drugs.Keywords: Gly-pro-p-nitroanilide (GPPN), Diprotin-A (Ile-Pro-Ile), Catechin, Withaferin-A, Diabetes and Molecular docking

Efficient Neural Architecture Search for Emotion Recognition

Automated human emotion recognition from facial expressions is a well-studied problem and still remains a very challenging task. Some efficient or accurate deep learning models have been presented in the literature. However, it is quite difficult to design a model that is both efficient and accurate at the same time. Moreover, identifying the minute feature variations in facial regions for both macro and micro-expressions requires expertise in network design. In this paper, we proposed to search for a highly efficient and robust neural architecture for both macro and micro-level facial expression recognition. To the best of our knowledge, this is the first attempt to design a NAS-based solution for both macro and micro-expression recognition. We produce lightweight models with a gradient-based architecture search algorithm. To maintain consistency between macro and micro-expressions, we utilize dynamic imaging and convert microexpression sequences into a single frame, preserving the spatiotemporal features in the facial regions. The EmoNAS has evaluated over 13 datasets (7 macro expression datasets: CK+, DISFA, MUG, ISED, OULU-VIS CASIA, FER2013, RAF-DB, and 6 micro-expression datasets: CASME-I, CASME-II, CAS(ME)2, SAMM, SMIC, MEGC2019 challenge). The proposed models outperform the existing state-of-the-art methods and perform very well in terms of speed and space complexity

INHIBITORY POTENCY OF WITHANIA SOMNIFERA EXTRACTS AGAINST DPP-4: AN IN VITRO EVALUATION

Background: Pharmacologic treatments for type 2 diabetes are based upon increasing insulin availability and improving sensitivity to insulin. Nowadays, glucagon like peptide-1 (GLP-1) based therapies aims at glucose control through DPP-4 inhibitors. DPP-4 is a transmembrane glycoprotein belongs to prolyl oligopeptidase family, with the specificity of removing X-Pro or X-Ala dipeptides from the N-terminus of polypeptides. GLP-1 effect by stimulating glucose-dependent insulin release from the pancreatic islets, inhibit inappropriate post-meal glucagon release and slow gastric emptying promoting leaky gut. The current study investigated DPP-4 inhibitory activity of catechin, isolated from Withania somnifera (WS), for ethnopharmacological treatment of type 2 diabetes and aimed to increase availability of GLP-1and sensitivity to insulin. Materials and Methods: Young and matured fresh roots, leaves, and fruits of WS plant extract were considered and were systematically evaluated for DPP-4 inhibitory activity using in vitro method, enzyme kinetics, phytochemical analysis, RP-HPLC, LCMS and 1H and 13C NMR method and structure-activity relationship (SAR) studies. Results: In this study, methanol (100% and 80%) extracts of WS matured root exhibited maximum DPP-4 inhibitory activity when compared to other extracts. The maximum DPP-4 inhibitory activity was found in 100% methanol extract of matured root. Phytobioactive was purified by RP-HPLC. The compound purified was found to be flavonoid and was characterized (LCMS, 1H and 13C NMR studies), identified as catechin. Auxiliary, molecular docking was performed using Ligand Fit method using PatchDock package. The study revealed the binding affinity of catechin with DPP-4 to be -6.601 kcal/mol with 13 hydrogen interactions with the receptor and was very similar to the standard potent blockers withaferin A and others (cuscohygrine, scopoletin, sitoindoside IV, tropine), further confirming its hyperglycemic potency. Conclusion: The study reveals that, 100% methanol extract of WS matured roots contains the compound- catechin, which exhibits DPP-4 inhibitory activity resulting in increased level of bioactive GLP-1 and GIP. In this background, we concluded that the WS will be a better source for further development as new antidiabetic drugs

Impact of climate variability on recent and future status of lepidopterous insects of pigeonpea at Banaskantha region of Gujarat (India)

Pigeonpea (cajanus cajan) is grown across varied agro climatic zones and Gujarat contributes 9.6% of 3.75 million hectares (mha) in India. Information and communication technology (UT) based pest surveillance of lepidopterous insect dynamics in relation to climate change during kharif (2011 -16) revealed non significance on Grapholita critics (Meyr.) and Maruca vitrata (Fab.) and significant impact on H. armigera in piget›npea at Banaskantha region of Gujarat. Besides positive effect of significantly increasing Rainfall (RF) and Maximam temperature (MaxT) and decreasing Minimum Temperature (MinT) had shown significant positive and negative impacts on Helicoverpa armigera. Seasonal dynamics across preceding and successive years followed the order of 201 > 2015 > 2012 > 2013 > 2014 > 2016, 2012, 201 I & 2013 > 2014 > 2015 & 2016 and 2011 > 2012, 2013 & 2015 > 2014 2016 for Helicoverpa armigera and M. vitrata, respectively. future scenario› of lepidopterous insects for 2020, 2050 and 2050 with changing climate using representative concentration pathway 4.5 for MaxT, MinT and RF had shown significant negative associations but for non-significance of MaxT in 2050, projecting reduced population of Helicoverpa during the whole of current century. Use of crop. climate and pest/disease dynamics and their management data provide ample and immediate scope of understanding effects of climate change and implement adaptive IPM strategies.‹irtnigeru. Seasonal dynamics across preceding and successive years followed the order of 20.11 > 2015 > 20.12 > 20.13 > 2014 > 20.1.6, 201.2 20.1 I & 201.3 > 20.14 > 2015 & 20.16 and 201.1 > 201.2, 201.3 & 20.15 > 201.4 20.16 for H. ormigci ‹i, N c i/ico and .If. vi/rniri, rcspcctivcly. future scenario› of lepidopterous insects for 2020, 2050 and 2050 with changing climate using representative concentration pathu'ay 4.5 for MaxT, MinT and kF had show sign ificant negative associations but for non-signi ficance ot” Ma xT in 2050, projecting reduced population of Ne//cr›rcryo during the whole of current century. Use of’crop. climate and pest/disease dynamics and their management data provide ample and immediate scope of understanding effects of climate change and implement ad.ip i¥’K Pi strategies

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Investigation of polyacrylonitrile solution inhomogeneity by dynamic light scattering

Dynamic light scattering (DLS) has been used to quantify nanoscale heterogeneity in the industrially significant polyacrylonitrile (PAN) polymer solution. The heterogeneity in polymer solution, traced by the ratio of amplitudes of the slow to fast mode, is observed to be related to various parameters, such as molecular weight of the polymer, the type of co-monomer, processing time, concentration of the solution, and the choice of the solvents. It has been identified that low molecular weight PAN homopolymer have the least heterogeneity issues. Amongst the chosen co-polymers for this study, similar degree of heterogeneity was observed at concentration slightly above the critical concentration at which the polymer chains begin to overlap. Whereas, at higher concentration, PAN-methacrylic acid (4 wt%) copolymer showed the least heterogeneity issue. The aggregate diffusion coefficient of PAN-methacrylic acid (4 wt%) copolymer solution in dimethylformamide (DMF) and N,N-dimethylacetamide (DMAc) are respectively determined to be approximate to 1.6 x 10(-12) cm(2)/s and approximate to 1.6 x 10(-13) cm(2)/s, which results in an estimated aggregate size of 9 nm and 90 nm. POLYM. ENG. SCI., 55:1403-1407, 2015. (c) 2015 Society of Plastics Engineersclose0

Probe diffusion of single-walled carbon nanotubes in semidilute solutions of polyacrylonitrile homo- and copolymers: Effects of topological constraints and polymer/Nanorod interactions

With varying the molecular weight, copolymer chemical structure and concentration, the probe diffusion behavior of single-walled carbon nanotubes (SWCNTs) in N, N-dimethylacetamide (DMAc) solutions of polyacrylonitrile (PAN) was studied by dynamic light scattering (DLS) technique. In combination with the systematic viscosity property investigation for PAN/DMAc system, the probe diffusion results provided insight to understand the interactions between PAN and SWCNTs. It was found that, due to depletion interaction, the SWCNT diffusion positively deviates from the Stokes–Einstein (SE) relation in PAN homopolymer solutions. However, in PAN copolymer solution, the SWCNT diffusion mostly obeys the SE relation, which was speculated as a result of hydrogen-bonding formation between the carboxylic acid functional groups in PAN copolymers and on purified SWCNTs. Moreover, due to the unique features of SWCNT probes – very long, extremely rigid, and adjustable bundle diameter, the SWCNT probe diffusion unambiguously revealed the topological constraints of polymer network responsible for the retardation of thin rod diffusion. Quantitative analysis indicated that the correlation length rather than the ???tube??? diameter of polymer liquid is the critical length scale to dictate the diffusion retardation of SWCNTs in polymer solutions.close3