SIÇANLARDA TİYOFEN MANNİCH BAZLARININ ANALJEZİK VE ANTİ-İNFLAMATUAR ETKİLERİNİN ARAŞTIRILMASI

Öz

Amaç: Bu çalışma, doğrulanmış deneysel modeller kullanılarak bir dizi tiyofen mannich bazı türevinin analjezik ve anti-inflamatuar potansiyellerinin sentezlenmesi ve sistematik olarak değerlendirilmesi amacıyla gerçekleştirilmiştir. Çalışma, analjezinin hem merkezi hem de periferik mekanizmalarının yanı sıra akut ve kronik inflamatuvar yanıtlarının da değerlendirilmesini hedeflemiştir.

Gereç ve Yöntem: Sırasıyla merkezi ve periferik analjezik etkileri değerlendirmek amacıyla, termal ve kimyasal yöntemler kullanılarak aljezi oluşturuldu. İnflamasyon; karragenan ile indüklenen referans ilaç olarak pentazosin (10 mg/kg, s.c.) kullanılırken, periferik analjezik ve anti-inflamatuar modellerde standart ilaç olarak diklofenak (10 mg/kg) kullanıldı. Analjezik ve anti-inflamatuar aktivite değerlendirmeleri; test bileşiği 1'in sıcak plaka yönteminde yanıt süresini anlamlı düzeyde uzattığını, %1'lik asetik asit ile indüklenen abdominal kıvranma sayısını azalttığını, karragenan ve formalin ile indüklenen pençe ödemini hafiflettiğini ve hava kesesi modelinde eksüda hacmini düşürdüğünü gösterdi. Miyeloperoksidaz enzimi, IL-6 ve lökosit (WBC) sayısı gibi enflamatuar belirteçler incelendi.

Sonuç ve Tartışma: Test bileşiği 1, belirgin analjezik ve anti-inflamatuar aktivite göstermiştir.

Anahtar Kelimeler

• Analjezik
• inflamasyon
• karragenan
• mannich bazları
• tiyofen

ANALGESIC AND ANTI-INFLAMMATORY INVESTIGATION OF THIOPHENE MANNICH BASES IN RATS

Öz

Objective: The present investigation was undertaken to synthesize and systematically evaluate a series of thiophene mannich base derivatives for their analgesic and anti‑inflammatory potential using validated experimental models. The study aimed to assess both central and peripheral mechanisms of analgesia, as well as acute and chronic inflammatory responses.

Material and Method: Algesia was induced using both thermal and chemical methods to evaluate central and peripheral analgesic effects, respectively. Inflammation was induced through peripheral models, namely carrageenan-induced paw edema, granuloma pouch, and formalin-induced paw edema. The test compounds were administered at a dosage of 55 mg/kg. Pentazocine (10 mg/kg, s.c.) served as the reference drug for the central analgesic model, whereas diclofenac (10 mg/kg) was used as the standard drug for peripheral analgesic and inflammatory models. Evaluation of analgesic and anti-inflammatory activity demonstrated that test compound 1, significantly prolonged response latency in the hot plate method, reduced the number of abdominal writhes induced by 1% acetic acid, decreased carrageenan- and formalin-induced paw edema, and reduced the volume of exudates in the air pouch model. Inflammatory markers such as Myloperoxidase enzyme, IL-6 and WBC counts were assessed.

Result and Discussion: The test compound 1, has shown significant analgesic and anti-inflammatory activity.

Anahtar Kelimeler

• Analgesic
• carrageenan
• inflammation
• mannich bases
• thiophene

Destekleyen Kurum

KLE College of Pharmacy, Vidyanagar, Hubballi

Etik Beyan

All experimental procedures involving animals in this study were conducted in accordance with the guidelines and regulations for the care and use of laboratory animals and were approved by the Institutional Animal Ethics Committee (IAEC) of KLE College of Pharmacy, Vidyanagar, Hubballi, with the approval number KLESCOPH/IAEC.Clear/2011-2012/ph.chemistry/03 dated 13-08-2011.

Teşekkür

The authors are thankful to the principal and management of KLE College of Pharmacy, Vidyanagar, Hubballi for providing all facilities to carry out this research.

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