Background: Xanthohumol is known to exert anti-inflammatory properties but has poor oral bioavailability. Using advanced micellization technology, it has been possible to markedly enhance its bioavailability.
Purpose: In the present study, we compared the chronic anti-inflammatory activities of native and micellar xanthohumol in the rat adjuvant arthritis model, using diclofenac as a reference drug.
Methods: Adjuvant arthritis was induced by injecting Freund's complete adjuvant into the right hind paw of rats and monitoring paw volume over 3 weeks. The drugs were given daily for 3 weeks, starting from the day of adjuvant inoculation. Serum was collected at the end of the experiment to measure inflammatory and oxidative stress parameters. Statistical comparisons between different groups were carried out by one-way analysis of variance followed by Tukey-Kramer multiple comparison test.
Results: Micellar solubilized xanthohumol showed a better anti-inflammatory activity than its native form. The reduction in paw volume was reflected in corresponding changes in relevant mediators of inflammation like tumor necrosis factor-α, interleukin-6 and C-reactive protein, myloperoxidase and lipid peroxidation markers.
Conclusion: The findings confirm that micellar solubilization of xanthohumol enhances its anti-inflammatory activity, probably as a result of improving its bioavailabilty. The solubilized xanthohumol may prove to be a promising adjuvant tool for anti-inflammatory treatment and a potential anti-inflammatory alternative to synthetic drugs.
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http://dx.doi.org/10.1016/j.phymed.2020.153233 | DOI Listing |
J Phys Chem B
January 2025
Institute of Pharmaceutical Sciences, University of Freiburg, Freiburg 79104, Germany.
The selective insertion of membrane-impermeant amphiphiles such as detergents, (lipo)peptides, drugs, etc. into the leaflet of a membrane causes an imbalance between the intrinsic areas of the and leaflet, referred to as asymmetry stress or differential stress. The literature provides individual mechanisms of how membranes respond to such stress, which are relevant to membrane remodeling processes and leakage phenomena.
View Article and Find Full Text PDFChempluschem
January 2025
Kaiserslautern University of Technology: Rheinland-Pfalzische Technische Universitat Kaiserslautern-Landau, Chemistry, 67663, Kaiserslautern, GERMANY.
We report the synthesis of a series of detergents with a lactobionamide polar head group and a tail containing four to seven perfluorinated carbon atoms. Critical micellar concentrations (CMCs) were determined using isothermal titration calorimetry (ITC) and surface tension (SFT) measurements, showing a progressive decrease from 27 mM to about 0.2 mM across the series.
View Article and Find Full Text PDFSoft Matter
January 2025
Biophysical Chemistry Laboratory, Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi, India.
The adsorption and aggregation of amphiphiles at different solvent interfaces are of great scientific and technological importance. In this study, interfacial tension measurements of surface-active compounds-ionic liquid 2-dodecyl-2,2dimethylethanolammonium bromide (12Cho.Br) and cationic surfactant cetyltrimethylammonium bromide (CTAB)-were conducted both in the absence and presence of ciprofloxacin (CIP).
View Article and Find Full Text PDFJ Pharm Sci
December 2024
Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, 5230 Odense, Denmark. Electronic address:
Physiological and artificial solubilizing agents usually enhance apparent solubility of poorly soluble drugs, and in many cases also oral drug exposure. However, exposure may decrease in cases where micellization reduces the molecularly dissolved drug fraction, overriding the solubility advantage. While this information is critical to accurately anticipate the effect of drug micellization on oral absorption, the experimental determination of molecularly dissolved drug concentrations is complex and time consuming.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
December 2024
Department of Chemistry, Presidency University, Kolkata 700073, India. Electronic address:
Pyrene fluorescence in aqueous solutions of two surface active ionic liquids, namely, 1-decyl-3-methylimidazolium chloride, and 1-hexadecyl-3-methylimidazolium chloride was investigated in presence of a biopolymer sodium alginate. The principal objective of this study was to explore the influence of the length of the hydrocarbon tails of these surface active ionic liquids on the possible location of the probe (pyrene) molecules in presence of the additive. While an abrupt decrease in the values of the ratio of the intensity of the first vibronic band to that of the third band of pyrene emission spectrum with concentration was observed for 1-hexadecyl-3-methylimidazolium chloride in presence of sodium alginate like the polymer-free case reported earlier, there was a peculiar reversal for 1-decyl-3-methylimidazolium chloride + sodium alginate.
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