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81.
82.
Obesity is the worst health risk worldwide, which is linked to a number of diseases. Pancreatic lipase is considered as an affective cause of obesity and can be a major target for controlling the obesity. The present study was designed to find out best phytochemicals against pancreatic lipase through molecular docking combined with molecular dynamics (MD) simulation. For this purpose, a total of 3770 phytochemicals were docked against pancreatic lipase and ranked them on the basis of binding affinity. Finally, 10 molecules (Kushenol K, Rosmarinic acid, Reserpic acid, Munjistin, Leachianone G, Cephamycin C, Arctigenin, 3-O-acetylpadmatin, Geniposide and Obtusin) were selected that showed strong bonding with the pancreatic lipase. MD simulations were performed on top five compounds using AMBER16. The simulated complexes revealed stability and ligands remained inside the binding pocket. This study concluded that these finalised molecules can be used as drug candidate to control obesity. 相似文献
83.
Bilal Abuasal Shawn Thomas Paul W. Sylvester Amal Kaddoumi 《Biomedical chromatography : BMC》2011,25(5):621-627
γ‐Tocotrienol (γ‐T3) is a member of the vitamin E family. Recently, γ‐T3 has attracted the attention of the scientific community due to its potent anticancer activity and other therapeutic benefits. The objective of this study was to develop and validate a simple and practical reversed‐phase HPLC method with satisfactory sensitivity for the routine quantification of γ‐T3 in rat and human plasma. The separation of γ‐T3 from the plasma components was achieved with a C18 reversed‐phase column with an isocratic elution using a mixture of methanol, ethanol and acetonitrile (85:7.5:7.5, v/v/v) with a UV detection at 295 nm. γ‐T3 was extracted from rat and human plasma by liquid–liquid extraction with an average recovery of 60%. The method proved linear in the range 100–5000 ng/mL. The inter‐day precision ranged from 5.8 to 12.8% and the accuracy ranged from 92.4 to 108.5%, while the intra‐day precision ranged from 0.7 to 7.9% in both rat and human plasma. This data confirm that the developed method has a satisfactory sensitivity, accuracy and precision for the quantification of γ‐T3 in plasma. To assess its applicability the method was successfully applied to the quantitative analysis for pharmacokinetic studies of γ‐T3 in rats administered a 10 mg/kg single oral dose. Copyright © 2010 John Wiley & Sons, Ltd. 相似文献
84.
Muhammad Ajaz Hussain Anqa Zarish Khawar Abbas Muhammad Sher Muhammad Nawaz Tahir Wolfgang Tremel Muhammad Amin Abdul Ghafoor Bilal Ahmad Lodhi 《Cellulose (London, England)》2013,20(2):717-725
This article presents synthesis of novel macromolecular prodrugs of aceclofenac (an anti-inflammatory drug) onto hydroxypropylcellulose (HPC). The HPC-aceclofenac conjugates were prepared using an acylating agent 1,1′-carbonyldiimidazole (CDI) under homogenous reaction conditions. Aceclofenac was first activated by using CDI to form its N-acylimidazole. The N-acylimidazole of aceclofenac was then reacted with HPC polymer at 80 °C for 24 h. Highly pure prodrugs of aceclofenac were synthesized with a wide range of moderate to high degree of substitution (DS 0.41–2.12) as calculated by 1H NMR spectroscopy. The UV spectroscopic analysis has also revealed that the active drug aceclofenac was found in different conjugates from 28 to 67 mg/100 mg of HPC-aceclofenac conjugates which are in good agreement with DS calculated by 1H NMR spectroscopy. The gel permeation chromatography showed unimodal absorption that indicates no significant degradation in polymer chains during the reaction. The macromolecular prodrugs of aceclofenac were characterized using different spectroscopic and chromatographic techniques. The thermal analysis has revealed that HPC-aceclofenac conjugates (prodrugs) are 92 and 96 °C more stable than pure aceclofenac regarding their initial (Tdi) and maximum degradation temperatures (Tdm), respectively. The activation energy (Ea) and frequency factor (Z) of the degradation reactions were evaluated using Friedman, Broido and Chang methods. Degradation followed first order (n) kinetics. Transmission electron microscopy has revealed the formation of sponge like nano aggregates with population size distribution of around 80–150 nm. 相似文献
85.
Structural Chemistry - Noncovalent interactions involving halogen bonding interactions, one of the emerging interactions due to its directionality, have been a subject of interest for various... 相似文献
86.
We use the variational method to establish criteria for the existence of conjugate points and for the oscillation property of the linear differential Sturm–Liouville equation. 相似文献
87.
This article explores the use of antimony(III) chloride adsorbed on neutral alumina as an efficient catalyst for the one‐pot synthesis of benzo[b]1,4‐diazepines (83–94%) under solvent‐free conditions. The process is easy, efficient, ecofriendly, and economical. 相似文献
88.
Samer Aouad Amal Aoun Mira Skaf Madonna Labaki John El Nakat Bilal El Khoury Pierre Obeid Edmond Abi-Aad Antoine Aboukaïs 《Comptes Rendus Chimie》2013,16(10):868-871
The effects of CoxMgyAl2Oz mixed oxides composition and ruthenium addition on the oxidation of propylene and carbon black (CB) were investigated. Different reactive cobalt and ruthenium oxide species were formed following calcination at 600 °C. The addition of ruthenium was beneficial for the CB oxidation under “loose contact” conditions and for propylene oxidation when the cobalt content was intermediate to low. The calculated activation energy for CB oxidation was decreased from 151 kJ mol−1 for the uncatalyzed reaction to 111 kJ mol−1 over the best catalyst. 相似文献
89.
A short synthesis of Hagen’s gland lactones 1 and 2 from commercially available pentanal and heptanal, respectively, is outlined. The approach relies on sequential ring closing metathesis and intramolecular oxy-Michael addition as the key transformations. 相似文献
90.
Structures modification of fibers has been attracting significant attention in various fields and applications. Among different techniques of fabricating ultrathin fibers, electrospinning is the most commonly adopted method because of the ease of forming fibers with a wide range of properties and its exceptional advantages, such as the ability to spin into different shapes and sizes, as well as the adaptable porosity of electrospun fiber webs. The crimped structure has been attracting the attention of scientific researchers owing to its unique properties (eg, spring‐like behavior, supreme strain, remarkable specific surface area, good piezoelectric properties, excellent biological properties, and so on). Therefore, this study summarizes a review of the strategies and methods, reported so far, of generating electrospun crimped ultrathin fibers of various polymers. The review focuses on the polymer types, formation methods, characterizations, and applications of the electrospun crimped ultrathin fibers. We believe this work can serve as an important reference for the materials, strategies, and applications of crimped fibers. 相似文献