Journals / Turkish Journal of Pharmaceutical Sciences / 2015 / Cilt: 12 - Sayı: 3

Parasetamol'ün Orto Pozisyonel İzomeri Ortosetamol'ün (2-Asetamidofenol) Anti-Platelet ve Anti-Artritik Aktivitesi

Anti-Platelet and Anti-Arthritic Activity of Orthocetamol (2- Acetamidophenol): An Ortho (O) Positional Isomer of Paracetamol

Pages
315–325
DOI
—
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

Our results demonstrate that 2-acetamidophenol may be a strong drug candidate for the prevention of cardiovascular diseases and rheumatoid arthritis.

📌 3 Key Takeaways

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Objective & Hypothesis:Platelet aggregation plays a pivotal role in the pathogenesis of cardiovascular diseases and rheumatoid arthritis.
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Key Findings & Data:It is a nonacetylated monophenolic drug with mild anti-platelet and anti-inflammatory activity at high dose range which is clinically insignificant.
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Conclusion & Impact:Our results demonstrate that 2-acetamidophenol may be a strong drug candidate for the prevention of cardiovascular diseases and rheumatoid arthritis.
🔬Design:Modeling & Simulation
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

Platelet aggregation plays a pivotal role in the pathogenesis of cardiovascular diseases and rheumatoid arthritis. Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used for the prevention of such diseases. NSAIDs are associated with the severe risk of ulcer and bleeding disorders due to their acetylated chemical structure. Paracetamol is often regarded as NSAIDs. It is a nonacetylated monophenolic drug with mild anti-platelet and anti-inflammatory activity at high dose range which is clinically insignificant. In the current research work we evaluated the effects of 2-acetamidophenol, a positional isomer of paracetamol against in vitro human platelet aggregation and collagen induced rheumatoid arthritis model. We used two aggregating agents namely arachidonic acid and adenosine 5'- diphosphate against 2-acetamidophenol. Aggregation was monitored through a dual channel aggregometer. We found that 2-acetamidophenol has several times more potent anti-platelet and antiarthritic potential than aspirin. Our results demonstrate that 2-acetamidophenol may be a strong drug candidate for the prevention of cardiovascular diseases and rheumatoid arthritis.

Özet

Platelet agregasyonu kardiyovasküler hastalıklar ve romatoit artritin patojenezinde önemli bir rol oynamaktadır. Bu tarz hastalıkların önlenmesi için non-steroidal anti-inflamatuar ilaçlar (NSAİİ) kullanılmaktadır. NSAİ ilaçların, ülser ve kanama bozuklukları gibi ciddi riskleri asetilli kimyasal yapıları ile ilişkilidir. Parasetamol genellikle NSAİİ olarak kabul edilen, klinik olarak anlamsız sayılan yüksek dozda hafif bir anti-platelet ve anti-inflamatuvar aktivite gösteren non-asetilli monofenolik bir bileşiktir. Bu çalışmada, parasetamolün pozisyonel izomeri olan 2-asetamidofenolün, in vitro insan platelet ve kolajen kaynaklı romatoid artrit modellerine karşı etkileri değerlendirilmiştir. Agregasyon ajanı olarak araşidonik asit ve adenosin-5'-difosfat kullanılmıştır. Agregasyon çift kanal agrometre ile izlenmiştir. 2- Asetamidofenolün aspirin ile kıyaslandığında daha güçlü anti-platelet ve anti-artritik aktivite gösterdiği bulunmuştur. Elde edilen sonuçlar, 2-asetamidofenolün kardiyovasküler hastalıklar ve romatizmal artritin önlenmesi için güçlü bir ilaç adayı olabileceğini göstermektedir.

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Cite This Article

QURESHI, Z., ASLAM, M., SAEED, T. Z., SIAL, A. (2015). Parasetamol'ün Orto Pozisyonel İzomeri Ortosetamol'ün (2-Asetamidofenol) Anti-Platelet ve Anti-Artritik Aktivitesi. Turkish Journal of Pharmaceutical Sciences, Cilt: 12 - Sayı: 3, 315–325. https://ajindex.com/articles/403739

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