Department of Pharmacology, School of Medical Sciences, University of Cape Coast, P.M.B. University Post Office, Cape Coast, Ghana.
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, 800 E Leigh Street, Richmond, VA 23298, United States.
Bioorg Chem. 2020 May;98:103744. doi: 10.1016/j.bioorg.2020.103744. Epub 2020 Mar 9.
Two natural products, compounds 1 and 2 were isolated from the root bark of Ziziphus abyssinica for the first time and were structurally elucidated as β-amyrin and polpunonic acid, respectively. Both compounds were further subjected to an in vivo study in rats to evaluate their anti-arthritic potency. Compared to the arthritic control group, rats treated with different doses of 1 or 2 (3, 10, and 30 mg/kg) exhibited significantly higher total change in body weight as well as lower arthritic scores and total change in paw edema and erythema. Histopathological examinations of the hind paws of the rats further demonstrated the beneficial effects of both compounds as they significantly reversed cartilage erosion, subchondral cyst, and Weichselbaum's lacunae formation. Evidence of bone remodeling was also observed in all groups of rats treated with 1 or 2. Hematological and serum biochemical parameters were not significantly affected by treatment of 1 or 2. Taken together, the results from the present study suggest potential therapeutic benefit of β-amyrin and polpunonic acid in rheumatoid arthritis and related inflammatory disorders.
首次从安石榴(Ziziphus abyssinica)根皮中分离得到两种天然产物，化合物 1 和 2，并分别将其结构鉴定为β-香树脂醇和波普诺酸。将这两种化合物进一步在大鼠体内进行抗关节炎活性评价。与关节炎对照组相比，不同剂量的 1 或 2（3、10 和 30mg/kg）治疗的大鼠的体重总变化、关节炎评分以及爪肿胀和红斑的总变化明显更高。对大鼠后爪的组织病理学检查进一步证明了这两种化合物的有益作用，因为它们可显著逆转软骨侵蚀、软骨下囊泡和 Weichselbaum 陷窝的形成。在所有用 1 或 2 治疗的大鼠组中也观察到了骨重塑的证据。1 或 2 的治疗对血液学和血清生化参数没有显著影响。综上所述，本研究结果表明β-香树脂醇和波普诺酸在类风湿关节炎和相关炎症性疾病中有潜在的治疗益处。
