Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo

2019 ◽  
Vol 27 (4) ◽  
pp. 579-588 ◽  
Author(s):  
Jeffrey Boehm ◽  
Roderick Davis ◽  
Claudia E. Murar ◽  
Tindy Li ◽  
Brent McCleland ◽  
...  
Keyword(s):  
Solid State ◽  
Nrf2 Pathway ◽  
Solid State Stability

Absolute radiotracer concentration measurement using whole-body solid-state SPECT/CT technology: in vivo/in vitro validation

2019 ◽  
Vol 57 (7) ◽  
pp. 1581-1590
Author(s):  
John A. Kennedy ◽  
Ilya Reizberg ◽  
Rachel Lugassi ◽  
Shoham Himmelman ◽  
Zohar Keidar
Keyword(s):  
Solid State ◽  
Concentration Measurement ◽  
Whole Body ◽  
Ct Technology

scholarly journals Synthesis and Evaluation of Chirally Defined Side Chain Variants of 7-Chloro-4-Aminoquinoline To Overcome Drug Resistance in Malaria Chemotherapy

2016 ◽  
Vol 61 (3) ◽  
Author(s):  
Vasantha Rao Dola ◽  
Awakash Soni ◽  
Pooja Agarwal ◽  
Hafsa Ahmad ◽  
Kanumuri Siva Rama Raju ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Solid State ◽  
Side Chain ◽  
Detailed Structure ◽  
Preclinical Development ◽  
Malaria Parasites ◽  
Sar Studies ◽  
Structure Activity

ABSTRACT A novel 4-aminoquinoline derivative [(S)-7-chloro-N-(4-methyl-1-(4-methylpiperazin-1-yl)pentan-2-yl)-quinolin-4-amine triphosphate] exhibiting curative activity against chloroquine-resistant malaria parasites has been identified for preclinical development as a blood schizonticidal agent. The lead molecule selected after detailed structure-activity relationship (SAR) studies has good solid-state properties and promising activity against in vitro and in vivo experimental malaria models. The in vitro absorption, distribution, metabolism, and excretion (ADME) parameters indicate a favorable drug-like profile.

Degradation of major allergens and allergenicity reduction of soybean meal through solid-state fermentation with microorganisms

2018 ◽  
Vol 9 (3) ◽  
pp. 1899-1909 ◽  
Author(s):  
Anshu Yang ◽  
LingLing Zuo ◽  
Youfei Cheng ◽  
Zhihua Wu ◽  
Xin Li ◽  
...  
Keyword(s):  
Solid State ◽  
Solid State Fermentation ◽  
Soybean Meal ◽  
Major Allergens

The effect of fermentation on allergenicity of soybean meal was assessed both in vitro and in vivo.

scholarly journals Digital Solid-State SPECT/CT Quantitation of Absolute 177Lu Radiotracer Concentration: In Vivo and In Vitro Validation

2020 ◽  
Vol 61 (9) ◽  
pp. 1381-1387
Author(s):  
John A. Kennedy ◽  
Rachel Lugassi ◽  
Ronit Gill ◽  
Zohar Keidar
Keyword(s):  
Solid State

scholarly journals A novel co-processed directly compressible release-retarding polymer: In vitro, solid state and in vivo evaluation

2018 ◽  
Vol 4 (1) ◽  
pp. 29-40 ◽  
Author(s):  
Prashant Kumar Choudhari ◽  
H.K. Jain ◽  
P. Sharma ◽  
B. Srivastava
Keyword(s):  
Solid State ◽  
In Vivo Evaluation

scholarly journals In Vivo Airway Surface Liquid Cl− Analysis with Solid-State Electrodes

2001 ◽  
Vol 119 (1) ◽  
pp. 3-14 ◽  
Author(s):  
Ray A. Caldwell ◽  
Barbara R. Grubb ◽  
Robert Tarran ◽  
Richard C. Boucher ◽  
Michael R. Knowles ◽  
...  
Keyword(s):  
Solid State ◽  
Airway Surface Liquid ◽  
Culture Models ◽  
Normal Human ◽  
Surface Liquid ◽  
Multiple Species ◽  
Cell Culture Models ◽  
Made In

The pathogenesis of cystic fibrosis (CF) airways disease remains controversial. Hypotheses that link mutations in CFTR and defects in ion transport to CF lung disease predict that alterations in airway surface liquid (ASL) isotonic volume, or ion composition, are critically important. ASL [Cl−] is pivotal in discriminating between these hypotheses, but there is no consensus on this value given the difficulty in measuring [Cl−] in the “thin” ASL (∼30 μm) in vivo. Consequently, a miniaturized solid-state electrode with a shallow depth of immersion was constructed to measure ASL [Cl−] in vivo. In initial experiments, the electrode measured [Cl−] in physiologic salt solutions, small volume (7.6 μl) test solutions, and in in vitro cell culture models, with ≥93% accuracy. Based on discrepancies in reported values and/or absence of data, ASL Cl− measurements were made in the following airway regions and species. First, ASL [Cl−] was measured in normal human nasal cavity and averaged 117.3 ± 11.2 mM (n = 6). Second, ASL [Cl−] measured in large airway (tracheobronchial) regions were as follows: rabbit trachea and bronchus = 114.3 ± 1.8 mM; (n = 6) and 126.9 ± 1.7 mM; (n = 3), respectively; mouse trachea = 112.8 ± 4.2 mM (n = 13); and monkey bronchus = 112.3 ± 10.9 mM (n = 3). Third, Cl− measurements were made in small (1–2 mm) diameter airways of the rabbit (108.3 ± 7.1 mM, n = 5) and monkey (128.5 ± 6.8 mM, n = 3). The measured [Cl−], in excess of 100 mM throughout all airway regions tested in multiple species, is consistent with the isotonic volume hypothesis to describe ASL physiology.

scholarly journals Solid-state fermented brewer's spent grain enzymatic extract increases in vitro and in vivo feed digestibility in European seabass

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Helena Fernandes ◽  
Francisco Moyano ◽  
Carolina Castro ◽  
José Salgado ◽  
Francisca Martínez ◽  
...  
Keyword(s):  
Solid State ◽  
Solid State Fermentation ◽  
High Potential ◽  
In Vitro Digestibility ◽  
Brewer’S Spent Grain ◽  
Dietary Phosphorus ◽  
European Seabass ◽  
Spent Grain

AbstractBrewer’s spent grain (BSG) is the largest by-product originated from the brewery industry with a high potential for producing carbohydrases by solid-state fermentation. This work aimed to test the efficacy of a carbohydrases-rich extract produced from solid-state fermentation of BSG, to enhance the digestibility of a plant-based diet for European seabass (Dicentrarchus labrax). First, BSG was fermented with A. ibericus to obtain an aqueous lyophilized extract (SSF-BSG extract) and incorporated in a plant-based diet at increasing levels (0—control; 0.1%, 0.2%, and 0.4%). Another diet incorporating a commercial carbohydrases-complex (0.04%; Natugrain; BASF) was formulated. Then, all diets were tested in in vitro and in vivo digestibility assays. In vitro assays, simulating stomach and intestine digestion in European seabass, assessed dietary phosphorus, phytate phosphorus, carbohydrates, and protein hydrolysis, as well as interactive effects between fish enzymes and dietary SSF-BSG extract. After, an in vivo assay was carried out with European seabass juveniles fed selected diets (0—control; 0.1%, and 0.4%). In vitro digestibility assays showed that pentoses release increased 45% with 0.4% SSF-BSG extract and 25% with Natugrain supplemented diets, while amino acids release was not affected. A negative interaction between endogenous fish enzymes and SSF-BSG extract was observed in both diets. The in vivo digestibility assay corroborated in vitro data. Accordingly, the dietary supplementation with 0.4% SSF-BSG increased the digestibility of dry matter, starch, cellulose, glucans, and energy and did not affect protein digestibility. The present work showed the high potential of BSG to produce an added-value functional supplement with high carbohydrases activity and its potential contribution to the circular economy by improving the nutritional value of low-cost and sustainable ingredients that can be included in aquafeeds.

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