Faculty of Pharmacy, University of Sargodha, Sargodha, Pakistan.
Nawaz Sharif Medical College, University of Gujrat, Gujrat, Pakistan.
Inflammopharmacology. 2021 Aug;29(4):1119-1129. doi: 10.1007/s10787-021-00840-9. Epub 2021 Jul 5.
Rheumatoid arthritis (RA) is a slowly progressing inflammatory autoimmune disease. Several features are involved in the RA pathogenesis in addition to environmental and genetic factors. Previously it has been reported that acetyl cholinesterase (AChE) activity is enhanced in old age and may contribute in the progression of RA. The current experimental work was projected to assess the activity of physostigmine (a cholinesterase inhibitor) for treatment of RA. In vitro and in vivo approaches were used for such evaluation. However, enzyme linked immunosorbent assays (ELISA) was performed to determine the concentrations of Prostaglandins E2 (PGE2) and tumor necrosis factor-α in arthritic rats after treatment with physostigmine. Moreover, anti-oxidant assays were employed to calculate the level of super oxide dismutase (SOD) and catalase peroxidase (CAT) in tissue of treated animals. The results claimed the dose dependent protective and stabilizing effect of physostigmine on denaturation of albumin (egg and bovine serum) protein and human red blood cell membrane, respectively, through in vitro studies. Furthermore, the physostigmine (10 and 20 mg/kg) significantly (p < 0.001) reduced the swelling of paw after induction of arthritis with formaldehyde or complete Freund's adjuvant (CFA) as compared to arthritic control animals. Moreover, significant (p < 0.001) reduction in the levels of inflammatory markers (PGE2 and TNF-α) at doses of 10 and 20 mg/kg of physostigmine has been observed in ELISA test. Likewise, there was a prominent rise in levels of SOD and CAT in animals treated with physostigmine. These findings pharmacologically conclude the anti-arthritic effect of physostigmine.
类风湿关节炎（RA）是一种进展缓慢的炎症性自身免疫性疾病。除了环境和遗传因素外，RA 的发病机制还涉及到几个特征。以前有报道称，乙酰胆碱酯酶（AChE）的活性在老年时增强，可能有助于 RA 的进展。目前的实验工作旨在评估毒扁豆碱（一种胆碱酯酶抑制剂）治疗 RA 的活性。采用体外和体内方法进行了这种评估。然而，酶联免疫吸附测定（ELISA）用于确定用毒扁豆碱治疗关节炎大鼠后前列腺素 E2（PGE2）和肿瘤坏死因子-α的浓度。此外，还采用抗氧化测定法来计算治疗动物组织中超氧化物歧化酶（SOD）和过氧化氢酶过氧化物酶（CAT）的水平。结果表明，毒扁豆碱在体外研究中对卵白蛋白和牛血清白蛋白以及人红细胞膜的变性具有剂量依赖性的保护和稳定作用。此外，与关节炎对照动物相比，毒扁豆碱（10 和 20 mg/kg）显著（p < 0.001）降低了甲醛或完全弗氏佐剂（CFA）诱导关节炎后爪子的肿胀。此外，在 ELISA 试验中，在 10 和 20 mg/kg 的毒扁豆碱剂量下，炎症标志物（PGE2 和 TNF-α）的水平也显著（p < 0.001）降低。同样，用毒扁豆碱治疗的动物的 SOD 和 CAT 水平明显升高。这些发现从药理学上得出了毒扁豆碱的抗关节炎作用。
