The authors investigated the effects of 2,4,6-trihydroxy-alpha-p-methoxyphenylacetophenone (compound D-58), a potent inhibitor of protein tyrosine kinases SYK and Bruton's tyrosine kinase (BTK), on IgE receptor/FcepsilonRI-triggered mast cell-mediated acute allergic responses in vitro and in vivo. Compound D-58 abrogated IgE receptor/FcepsilonRI-mediated SYK and BTK activation as well as calcium mobilization in mast cells. Mast-cell degranulation and leukotriene (LT) C(4) release was inhibited by compound D-58 in a concentration-dependent fashion. Notably, compound D-58 prevented the mast cell mediator-induced vascular hyperpermeability in an in vivo murine model of passive cutaneous anaphylaxis as measured by the prevention of extravasation of systemically administered Evans blue dye. The results uniquely indicate that compound D-58 has potent antiallergic properties. Therefore, further development of compound D-58 may provide the basis for new and effective treatment programs for severe allergic disorders.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1097/00045391-200111000-00006 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Binding of green tea epigallocatechin gallate to the arginine kinase active site from the brown recluse spider (): A potential synergist to chemical pesticides.
Heliyon
July 2024
Laboratorio de Estructura Biomolecular, Centro de Investigación en Alimentación y Desarrollo, A. C., Hermosillo, Sonora, Mexico.
spp. spiders can cause serious public health issues. Chemical control is commonly used, leading to health and environmental problems.
View Article and Find Full Text PDFIntegrative Analysis of Metabolome and Transcriptome Reveals the Mechanism of Color Formation in Yellow-Fleshed Kiwifruit.
Int J Mol Sci
January 2023
Key Laboratory of Breeding and Utilization of Kiwifruit in Sichuan Province, Sichuan Provincial Academy of Natural Resource Sciences, Chengdu 610065, China.
During the development of yellow-fleshed kiwifruit (), the flesh appeared light pink at the initial stage, the pink faded at the fastest growth stage, and gradually changed into green. At the maturity stage, it showed bright yellow. In order to analyze the mechanism of flesh color change at the metabolic and gene transcription level, the relationship between color and changes of metabolites and key enzyme genes was studied.
View Article and Find Full Text PDFSynthesis and evaluation of inhibitors of Mycobacterium tuberculosis UGM using bioisosteric replacement.
Bioorg Med Chem
September 2022
Department of Chemistry, University of Namur, Rue de Bruxelles 61, 5000 Namur, Belgium. Electronic address:
Article Synopsis
- There is a lack of effective treatments for drug-resistant tuberculosis (TB), prompting the need for new drug development focused on targeting the enzyme UGM, crucial for bacterial cell wall integrity.
- The study explores amides derived from rosmarinic acid as potential inhibitors of UGM, revealing that these amides have a significantly higher binding affinity compared to rosmarinic esters.
- One compound, 5h, shows promising binding strength to UGM, indicating that this approach could pave the way for designing new anti-TB drugs.
Identification and in vitro characterization of C05-01, a PBB3 derivative with improved affinity for alpha-synuclein.
Brain Res
December 2020
Centre for Psychiatry Research, Department of Clinical Neuroscience, Karolinska Institutet, & Stockholm Health Care Services, Region Stockholm, Stockholm, Sweden.
The neuropathological hallmark of Parkinsońs disease, multiple system atrophy and dementia with Lewy bodies is the accumulation of α-synuclein. The development of an imaging biomarker for α-synuclein is an unmet need. To date, no selective α-synuclein imaging agent has been identified, though initial studies suggest that the tau tracer [C]PBB3 displays some degree of binding to α-synuclein.
View Article and Find Full Text PDFEffects of a combination of plant bioactive lipid compounds and biotin compared with monensin on body condition, energy metabolism and milk performance in transition dairy cows.
PLoS One
June 2018
Institute of Veterinary Physiology, Freie Universität Berlin, Berlin, Oertzenweg, Germany.
The aim of this study was to test whether a combination of plant bioactive lipid compounds (also termed 'essential oils') and biotin (PBLC+B) could decrease the mobilization of body reserves and ketosis incidence in postpartum dairy cows. We compared non-supplemented control (CON) cows with cows receiving monensin (MON) as a controlled-release capsule at d -21, and with cows receiving PBLC+B from day (d) -21 before calving until calving (Phase 1) and further until d 37 after calving (Phase 2), followed by PBLC+B discontinuation from d 38 to d 58 (Phase 3). The PBLC+B cows had higher body weight and higher back fat thickness than CON cows and lesser body weight change than MON and CON cows in Phase 3.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!