This study aimed to search the α-glucosidase inhibitors from the barks part of Artocarpus elasticus. The responsible compounds for α-glucosidase inhibition were found out as dihydrobenzoxanthones (1–4) and alkylated flavones (5–6). All compounds showed a significant enzyme inhibition toward α-glucosidase with IC50s of 7.6–25.4 μM. Dihydrobenzoxanthones (1–4) exhibited a competitive inhibition to α-glucosidase. This competitive behaviour was fully characterised by double reciprocal plots, Yang’s method, and time-dependent experiments. The compound 1 manifested as the competitive and reversible simple slow-binding, with kinetic parameters k3 = 0.0437 µM−1 min−1, k4 = 0.0166 min−1, and = 0.3795 µM. Alkylated flavones (5–6) were mixed type I (KI < KIS) inhibitors. The binding affinities (KSV) represented by all inhibitors were correlated to their concentrations and inhibitory potencies (IC50). Moreover, compounds 1 and 5 were identified as new ones named as artoindonesianin W and artoflavone B, respectively. Molecular modelling study proposed the putative binding conformation of competitive inhibitors (1–4) to α-glucosidase at the atomic level.
We investigated the sintering and consolidation phenomena of silver nanoparticles under various thermal treatment conditions when they were patterned by a contact printing technique on polyimide substrate films. The sintering of metastable silver nanoparticles commenced at 180 o C, where the point necks were formed at the contact points of the nanoparticles to reduce the overall surface area and the overall surface energy. As the temperature was increased up to 250 o C, silver atoms diffused from the grain boundaries at the intersections and continued to deposit on the interior surface of the pores, thereby filling up the remaining space. When the consolidation temperature exceeded 270 o C, the capillary force between the spherical silver particles and polyimide flat surface induced the permanent deformation of the polyimide films, leaving crater-shaped indentation marks. The bonding force between the patterned silver metal and polyimide substrate was greatly increased by the heat treatment temperature and the mechanical interlocking by the metal particle indentation.
Chagas disease is one of the primary causes of heart diseases accounting to 50,000 lives annually and is listed as the neglected tropical disease. Because the currently available therapies have greater toxic effects with higher resistance, there is a dire need to develop new drugs to combat the disease. In this pursuit, the 3D QSAR ligand-pharmacophore (pharm 1) and receptor-based pharmacophore (pharm 2) search was initiated to retrieve the candidate compounds from universal natural compounds database. The validated models were allowed to map the universal natural compounds database. The obtained lead candidates were subjected to molecular docking against cysteine protease (PDB code: 1ME3) employing -Cdocker available on the discovery studio. Subsequently, two Hits have satisfied the selection criteria and were escalated to molecular dynamics simulation and binding free energy calculations. These Hits have demonstrated higher dock scores, displayed interactions with the key residues portraying an ideal binding mode complemented by mapping to all the features of pharm 1 and pharm 2. Additionally, they have rendered stable root mean square deviation (RMSD) and potential energy profiles illuminating their potentiality as the prospective antichagastic agents. The study further demonstrates the mechanism of inhibition by tetrad residues compromising of Gly23 and Asn70 holding the ligand at each ends and the residues Gly65 and Gly160 clamping the Hits at the center. The notable feature is that the Hits lie in close proximity with the residues Glu66 and Leu67, accommodating within the S1, S2 and S3 subsites. Considering these findings, the study suggests that the Hits may be regarded as effective therapeutics against Chagas disease.
The purpose of this study was to verify importance and satisfaction of destination attraction for water-based tourism in Jeju Island using Importance-Performance Analysis (IPA). The participants of this study consisted of 429 water-based tourism participants who visited Jeju Island in Korea. The collected data were analyzed and interpreted using SPSS program, frequency analysis, exploratory factor analysis, reliability analysis, and Importance-Performance Analysis. The results of this study were as follows. First, quadrant 1 included in season and climate comfort, local souvenirs, and hospitality of tourism program guide. Second, quadrant 2 included six items with sports activities rental facilities, scenic viewing activity, hospitality of local residents, accessibility of the island, convenience of local island transportation, and tourism safety. Third, quadrant 3 included four items with congestion of sightseeing spot, the reputation of a tourist destination, amusement facilities, affordable price, and traditional foods Fourth, quadrant 4 included eight items with marine related experience training activity, coastal landscape and terrain, marine sports activity, accommodation and shopping facilities, marine festivals and events activity, rest and recreational activity, history and cultural heritage, and service facilities.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
customersupport@researchsolutions.com
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.