Kimariyo Patrick Francis, Kurati Sony Priya, Babu Perupogu Suvarna, Moyo Alfredi Alfred, Muthyala Murali Krishna Kumar
AU College of Pharmaceutical Sciences, Pharmaceutical Chemistry Department, Andhra University, Visakhapatnam, Andhra Pradesh 530003, India.
Dar es Salaam Institute of Technology (DIT), Science and Laboratory Technology Department, Bibititi and Morogoro Rd Junction P. O. Box 2958. Dar es Salaam, Tanzania.
Iran J Basic Med Sci. 2024;27(9):1197-1208. doi: 10.22038/IJBMS.2024.75023.16295.
In this study, the SP-38 (Diterpene Lactone derivative) was designed, synthesized from clerodane diterpene (lactone) isolated from var. pendula, and tested for anti-arthritic activity using the FCA-induced arthritic rat model.
This study examined the 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.
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.
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.
在本研究中,设计并合成了SP - 38(二萜内酯衍生物),其由从垂枝变种中分离得到的克罗烷二萜(内酯)合成,并使用弗氏完全佐剂(FCA)诱导的关节炎大鼠模型测试其抗关节炎活性。
本研究通过口服给予三种不同剂量(20、10和5 mg/kg)的SP - 38,从0.1 ml FCA足底注射后第8天开始给药,持续21天直至第28天。检测关节炎指数、 paw肿胀、踝关节直径、体重以及生化、血液学、组织病理学和放射学参数。
与关节炎对照组相比,给予SP - 38可降低关节炎指数、 paw体积和关节肿胀。相应地,用SP - 38治疗的大鼠体重显著增加,生化、血液学、组织病理学和放射学参数得到改善。此外,在所有接受SP - 38治疗的大鼠中,它降低了CRP和RF的升高产生,同时降低了ESR。然而,SP - 38通过降低血清中肝功能标志物SGOT、SGPT和ALP的升高水平显示出有前景的肝脏保护作用。此外,在某些剂量下,与关节炎对照大鼠相比,脾脏指数、TNF -α和IL - 6水平显著降低。
本研究结果得出结论,SP - 38在Wistar大鼠FCA诱导的关节炎中具有显著的抗关节炎潜力。因此,SP - 38显示出有前景的抗关节炎活性,炎症、炎症标志物和促炎细胞因子水平的降低证明了这一点。