Hyaluronic Acid Degradation Studies
Robert A. Greenwald in CRC Handbook of Methods for Oxygen Radical Research, 2018
Should it be desired to check the concentration of the HA, the best method is to use the carbazole assay to detect glucuronic acid. The original method of Bitter and Muir8 as modified is routinely done in the following manner. To 190 mℓ water in a 2-ℓ flask, add 9.5g sodium tetraborate decahydrate. Open a fresh 9-lb bottle of sulfuric acid, remove 500 cm3, and add this to the flask, which should be sitting in an ice bath since the dilution of the acid will be highly exothermic. Cool to room temperature and slowly (very carefully) add the solution back into the acid jug. Cap and mix by inversion. Dissolve 250 mg carbazole in 250 mℓ absolute ethanol. Both reagents are stable at room temperature for some time. As a standard, dissolve d-glucuronic acid lactone in water at 0.4 mg/mℓ. To perform the assay, add sample, standard, or water to a final volume of 0.2 μℓ in a pyrex test tube, add 0.1 μℓ carbazole, mix, and then add 2.5 μℓ of the sulfuric acid. Vortex this very well and incubate all the tubes at 100°C for 15 min. Cool and read the absorbance at 520 nm. Glucuronate accounts for 46.3% of the molecular weight of HA. (To convert uronate to HA, multiply by 2.16.)
Essential Oils in Cancer Therapy
K. Hüsnü Can Başer, Gerhard Buchbauer in Handbook of Essential Oils, 2020
Nagappan et al. (2011) evaluated the antiproliferative effects of three carbazole alkaloids (mahanine, mahanimbicine, and mahanimbine) and the EO from the leaves of Murraya koenigii L. (Rutaceae) against human breast (MCF-7), human cervical (HeLa), and murine leukemia cell lines (P388). From the EO of M. koenigii, 34 aromatic volatile constituents were identified. The two sesquiterpene hydrocarbons, β-caryophyllene (19.5%) and α-humulene (15.2%), represented the main volatile metabolites. To evaluate the anticancer activity, cells were treated with all compounds and the EOs dissolved in DMSO to a concentration of 30 μg/mL. The carbazole alkaloids and the EOs exhibit antiproliferative effects against all three tested cell lines in a dose-dependent manner: the higher the concentration of the tested compound, the lower the cell viability. Mahanimbine showed the most significant cytotoxic effects with IC50 values of 2.12, 5.00, and 1.98 μg/mL in the MCF-7, P388, and HeLa cell lines, respectively. These results could be important for the development of a new antitumor lead metabolite.
Presentation Format
Kitsakorn Locharoenrat in Research Methodologies for Beginners, 2017
Many metal-free organic dyes showed promising results in photovoltaic application. Those are derivatives of coumarin, triphenylamine, carbazole, and indoline [2,4,6]. Coumarin-153 is a derivative of coumarin, with additional electron-donor and electron-acceptor groups. Electron-donor group greatly lowers the energy of and . In addition electron-acceptor group is as well shifting fluorescence and absorption maximum peak to longer wavelengths, resulting in absorption peak of coumarin-153 at 430 nm, compared to 365 nm for coumarin [7]. For that reason, goal of this work is to efficiently combine ZnO, which is very commonly used material for solar cells because of its optical properties, with coumarin-153, which reported promising results in photovoltaic application with TiO2, in order to enhance efficiency of ZnO sunlight absorption [7–9].
Design, synthesis, and biological evaluation of novel carbazole derivatives as potent DNMT1 inhibitors with reasonable PK properties
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Ennian Li, Kai Wang, Bei Zhang, Siqi Guo, Senhao Xiao, Qi Pan, Xiaowan Wang, Weiying Chen, Yunshan Wu, Hesong Xu, Xiangqian Kong, Cheng Luo, Shijie Chen, Bo Liu
In summary, a series of novel carbazole-based derivatives were designed, synthesised, and evaluated for their biological activity. The structure-activity relationship of their anti-proliferative activity was explored. Among these compounds, WK-22 and WK-23 displayed appreciable human DNMT1 inhibitory activity in the micromolar range (IC50 = 4.9 µM and 5.0 µM). Simultaneously, both WK-22 and WK-23 has promising anti-proliferative effect on A549 and HCT116 cell lines. In further in vivo pharmacokinetic study, WK-23 displayed a better plasma exposure and prolonged elimination half-life (T1/2 = 7.9 h), especially the more acceptable oral bioavailability of (F% = 37.1) than WK-22 (F% = 27.0). Concomitantly, the molecule docking showed the binding pattern of WK-23 with DNMT1 is similar to that of DC_517, forming stable binding to DNMT1.
Synthetic cannabinoid receptor agonists: classification and nomenclature
Published in Clinical Toxicology, 2020
A. J. Potts, C. Cano, S. H. L. Thomas, S. L. Hill
To our knowledge the expanded possible analogues of MDMB-CHMCZCA have not yet emerged on the recreational market (e.g. AB-CHMCZCA, etc), however the development of MDMB-CHMCZCA is a logical response to the progressive legislative changes throughout the UK and wider EU that have restricted bicyclic indole and indazole core compounds [3, 25]. Additionally, the recent emergence of several tricyclic γ-carbolinone (i.e. dihydro-1H-pyrido[4,3-b]indol-1-one)-derived compounds also highlight the shifting clandestine synthesis of bicyclic to tricyclic cores. The systematic core letters “PEGACLONE” are derived from the chemical fragment “pentyl‐gamma‐carbolin‐1‐one” [57]. Compounds (or their metabolites) including CUMYL-PeGaClone (also known as SGT-151) and 5 F-CUMYL-PeGaClone (5 F-SGT-151) have been detected in urine samples of recreational users [57–59] and reported to the EMCDDA [60]. Future work should establish basic pharmacological and toxicological data for potential analogue compounds of carbazole and γ-carbolinone, preferably before they are identified on the recreational market.
Cell adhesion and twitching motility influence strong biofilm formation in Pseudomonas aeruginosa
Published in Biofouling, 2022
Alginate extraction was carried out following the protocol by Jones et al., 2013 (Jones et al. 2013). Briefly, a 24 h bacterial colony was scraped off theplate, resuspended in 0.85% NaCl, and collected by centrifugation (12,000 × g for 30 min). The supernatant was treated with 2% Cetyl Pyridium chloride and alginate was collected by centrifugation. The pellet was resuspended in 1 ml of 1 M NaCl, precipitated with cold isopropanol, and resuspended in normal saline. Alginate quantification was determined by carbazole assay (Cesaretti et al. 2003) with 96 well format modifications (Knutson and Jeanes 1968). 50 µl of resuspended alginate was treated with a 200 µl borate-sulfuric acid reagent (10 mM H3BO3 in concentrated H2SO4) at 100 °C for 15 min. Further, 50 µl of carbazole reagent (0.1%) was added and heated to 100 °C for 10 min. Absorbance was measured at 550 nm (Multiskan Go, Thermo Fisher Scientific, Waltham, MA, USA). Seaweed alginate was used as a standard to determine the concentration of alginate.
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