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Insight into NSAID-induced membrane alterations, pathogenesis and therapeutics: characterization of interaction of NSAIDs with phosphatidylcholine.
Author: BoggaraMohan Babu, DialElizabeth J, DoyenJanice R, GorensteinDavid G, JayaramanVasanthi, KrishnamoortiRamanan, LichtenbergerLenard M, O'NeilRoger G, VolkDavid E, ZhouYong
Original Abstract of the Article :
Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most widely consumed pharmaceuticals, yet both the mechanisms involved in their therapeutic actions and side-effects, notably gastrointestinal (GI) ulceration/bleeding, have not been clearly defined. In this study, we have used a number of...See full text at original site
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引用元:
https://pubmed.ncbi.nlm.nih.gov/22521764
データ提供:米国国立医学図書館(NLM)
Exploring the Mechanisms of NSAID-Induced Membrane Alterations and Developing Novel Therapeutics
This research dives deep into the complex world of pharmacology, specifically focusing on the mechanisms underlying the therapeutic actions and side effects of nonsteroidal anti-inflammatory drugs (NSAIDs). This research utilizes a combination of biochemical, structural, computational, and biological approaches to investigate the interactions of NSAIDs with cell membranes.
The study explores the affinity of NSAIDs to form ionic and hydrophobic associations with phosphatidylcholine (PC), a major component of cell membranes. It investigates the pH-dependent partitioning of NSAIDs into the phospholipid bilayer, potentially leading to significant changes in membrane properties, including hydrophobicity, fluidity, permeability, and stability. The authors propose that these membrane alterations could underlie the gastrointestinal (GI) toxicity associated with NSAIDs, including ulceration and bleeding.
The research further investigates the potential of modifying NSAIDs by associating them with PC to reduce their GI toxicity while maintaining their therapeutic efficacy. This approach aims to develop a novel class of PC-associated NSAIDs that offer a safer and more tolerable therapeutic option for patients.
The Importance of Understanding Drug-Membrane Interactions for Therapeutic Development
This study highlights the critical role of understanding drug-membrane interactions in developing new and safer therapeutic agents. The research demonstrates the potential of modifying NSAIDs to reduce their GI toxicity by understanding their interactions with cell membranes. It underscores the importance of considering the broader biological effects of drugs beyond their primary target.
The Importance of Balancing Therapeutic Efficacy and Safety in Drug Development
This research emphasizes the importance of balancing therapeutic efficacy and safety in drug development. The study demonstrates the potential of designing novel drugs with improved safety profiles by understanding the mechanisms of drug-membrane interactions. It highlights the need for a comprehensive approach that considers both the therapeutic potential and the potential adverse effects of new drug candidates.
Dr. Camel's Conclusion
This research is like a desert expedition, navigating the challenging terrain of NSAID-induced membrane alterations. The authors, like skilled explorers, utilize a multidisciplinary approach to understand the intricate interactions between NSAIDs and cell membranes. They reveal the potential to mitigate GI toxicity by modifying these interactions, offering a beacon of hope for developing safer and more effective NSAIDs. It reminds us that the journey towards optimal drug therapy requires a thorough understanding of the interplay between drugs and the human body to achieve a balance between efficacy and safety.
Date :
- Date Completed 2012-11-02
- Date Revised 2021-10-21
Further Info :
Related Literature
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