Department of Natural Products, National Institute of Pharmaceutical Education and Research, SAS Nagar, India.
Planta Med. 2010 Oct;76(14):1564-9. doi: 10.1055/s-0030-1249779. Epub 2010 Apr 8.
Evaluation of the topical anti-inflammatory activity of chloroform and ethyl acetate extracts of RUMEX NEPALENSIS roots in a TPA-induced acute inflammation mouse model demonstrated a significant reduction in ear edema. The extracts were further tested on purified enzymes for COX-1 and COX-2 inhibition to elucidate their mechanism of action, and a strong inhibition was observed. Six anthraquinones and two naphthalene derivatives were isolated from the ethyl acetate extract. Among the isolated compounds, emodin was found to be a potent inhibitor with slight selectivity towards COX-2, and nepodin exhibited selectivity towards COX-1. Emodin, endocrocin, and nepodin also exhibited significant topical anti-inflammatory activity in mice. Interestingly, nepodin showed better radical scavenging activity than trolox and ascorbic acid against DPPH and ABTS radicals. The strong radical scavenging activity of chloroform and ethyl acetate extracts could be explained by the presence of nepodin as well as by the high phenolic content of the ethyl acetate extract. Thus, the anti-inflammatory effect of R. NEPALENSIS roots was assumed to be mediated through COX inhibition by anthraquinones and naphthalene derivatives and through the radical scavenging activities of naphthalene derivatives.
评价 RUMEX NEPALENSIS 根的氯仿和乙酸乙酯提取物在 TPA 诱导的急性炎症小鼠模型中的局部抗炎活性表明,耳肿胀明显减轻。进一步在纯化的 COX-1 和 COX-2 抑制剂上测试提取物,以阐明其作用机制,观察到强烈的抑制作用。从乙酸乙酯提取物中分离出六种蒽醌和两种萘衍生物。在所分离的化合物中,大黄素被发现是一种对 COX-2 具有轻微选择性的有效抑制剂,而尼泊尔定对 COX-1 具有选择性。大黄素、内克罗辛和尼泊尔定也表现出显著的小鼠局部抗炎活性。有趣的是,尼泊尔定对 DPPH 和 ABTS 自由基的清除活性优于 Trolox 和抗坏血酸。氯仿和乙酸乙酯提取物的强自由基清除活性可以用尼泊尔定的存在以及乙酸乙酯提取物的高酚含量来解释。因此,R. NEPALENSIS 根的抗炎作用被认为是通过蒽醌和萘衍生物对 COX 的抑制以及萘衍生物的自由基清除活性来介导的。