Synthesized pyrrole ester ameliorates adjuvant­induced arthritis in Wistar rats by alleviating inflammation and downregulating the pro­inflammatory cytokines.

Piperine is an amide alkaloid responsible for producing the pungent smell that comes from black pepper. Piperine has been explained to exhibit significant properties such as anti-rheumatic, anti-inflammatory, and antihypertensive effects. The aim of the study was to synthesize pyrrole ester from piperine and evaluate its anti-arthritis effects in adjuvant-induced arthritis female Wistar rats. In this study, pyrrole ester (AU-5) was designed, synthesized and evaluated for ant-arthritic activity in adjuvant-induced arthritis Wistar rats. The synthesized pyrrole ester (AU-5) was administered in three selected doses (20, 10 and 5 mg/kg) to the arthritic-induced model. The administered ester significantly inhibited the increase in arthritis index, paw and ankle joint swelling compared to the arthritic control group. Similarly, the treated rats exhibited a remarkable increase in body weight increase, improved haematological, biochemical, histopathological and radiological parameters. Moreover, the excess production of rheumatoid factor (RF), C-reactive protein (CRP) and erythrocyte sedimentation rate (ESR) was noticeably attenuated in all AU-5-treated rats. However, the spleen index, tumour necrosis factor (TNF-α) and interleukin-6 (IL-6) were distinctly lowered compared to arthritic control rats. Moreover, AU-5 showed promising liver protection by lowering the level of liver function markers Serum glutamic pyruvic transaminase (SGPT), Serum glutamic-oxaloacetic transaminase (SGOT) and alkaline phosphatase (ALP) in serum. Henceforth, it might be concluded that AU-5 has an anti-arthritic effect which can be credited to the down regulation of inflammatory markers and the pro-inflammatory cytokines.

Synthesized diterpene lactone derivative attenuated Freund's complete adjuvant-induced arthritis in Wistar rats.

Objectives: In this study, the SP-38 (Diterpene Lactone derivative) was designed, synthesized from clerodane diterpene (lactone) isolated from Polyanthia longifolia var. pendula, and tested for anti-arthritic activity using the FCA-induced arthritic rat model. Materials and Methods: This study examined the in vivo effects of SP-38 using three different doses (20, 10, and 5 mg/kg) by oral administration for 21 days from day 8 after 0.1 ml FCA sub-planter injection until day 28. Arthritis index, paw swelling, ankle diameter, body weight as well as biochemical, hematological, histopathological, and radiological parameters were examined. Results: Administered SP-38 reduced arthritis index, paw volume, and joint swelling compared to the arthritic control group. Accordingly, rats treated with SP-38 showed a remarkable increase in body weight and improved biochemical, hematological, histopathological, and radiological parameters. Furthermore, it reduced the increased production of CRP and RF while simultaneously decreasing ESR in all SP-38-treated rats. However, SP-38 showed promising liver protection by reducing elevated serum levels of liver and kidney function markers SGOT, SGPT, and ALP. Furthermore, splenic index, TNF-α, and IL-6 levels were significantly reduced compared to arthritic control rats at certain doses. Conclusion: The result of the present study concludes that SP-38 has significant anti-arthritic potential in FCA-induced arthritis in Wistar rats. SP-38 therefore showed promising anti-arthritic activity, as evidenced by attenuation of inflammation, inflammatory markers, and pro-inflammatory cytokine levels.