College of Pharmacy, Kangwon National University, Chunchon, Republic of Korea.
J Ethnopharmacol. 2010 Feb 17;127(3):589-95. doi: 10.1016/j.jep.2009.12.020. Epub 2009 Dec 23.
The roots of Sophora flavescens have long been used in Chinese medicine for the treatment of fever, inflammatory disorders, ulcers and skin burns. Sophora flavescens contains flavonoids and alkaloids.
This study was conducted to develop a plant-based anti-inflammatory agent focused on chronic inflammatory disorders. To accomplish this, the alkaloid-free prenylated flavonoid-enriched fraction (PFS) of rhizomes of Sophora flavescens was prepared and its in vitro and in vivo anti-inflammatory activities were then evaluated for the first time.
The inhibitory activity of PFS on PGE(2), NO, IL-6 and TNF-alpha production of lipopolysaccharide (LPS)-treated RAW 264.7 cells was measured. Additionally, adjuvant-induced arthritis in rats was used as an animal model of chronic inflammation to establish the in vivo anti-inflammatory effects of PFS.
PFS inhibited cyclooxygenase-2 (COX-2)-catalyzed PGE(2) and inducible nitric oxide synthase (iNOS)-catalyzed NO production by lipopolysaccharide (LPS)-treated RAW 264.7 cells at 10-50 microg/ml, and these effects primarily occurred via COX-2 inhibition and iNOS down-regulation, respectively. PFS also inhibited IL-6 and TNF-alpha production. When tested against adjuvant-induced arthritis in rats (chronic inflammation), PFS strongly inhibited arthritic inflammation when administered orally at doses of 10-100mg/kg/day. In addition, PFS administered orally potently inhibited acetic acid-induced writhing in mice.
Our results suggest that PFS inhibits chronic inflammatory response and the inhibition of proinflammatory molecules such as COX-2, iNOS and IL-6 may contribute, at least in part, to the anti-inflammatory activity in vivo. Overall, these results indicate that PFS from Sophora flavescens may have the potential for treatment of chronic inflammatory disorders such as rheumatoid arthritis.
苦参的根在中国医学中一直被用于治疗发热、炎症性疾病、溃疡和皮肤烧伤。苦参含有黄酮类和生物碱。
本研究旨在开发一种以植物为基础的抗炎药物，专注于慢性炎症性疾病。为此，首次制备了苦参根茎的无生物碱的类异戊烯基化黄酮类化合物富集部分（PFS），并评估了其体外和体内抗炎活性。
测量 PFS 对脂多糖（LPS）处理的 RAW 264.7 细胞中 PGE（2）、NO、IL-6 和 TNF-α产生的抑制活性。此外，使用佐剂诱导的大鼠关节炎作为慢性炎症的动物模型，建立 PFS 的体内抗炎作用。
PFS 在 10-50 μg/ml 时抑制环加氧酶-2（COX-2）催化的 PGE（2）和诱导型一氧化氮合酶（iNOS）催化的 LPS 处理的 RAW 264.7 细胞中的 NO 产生，并且这些作用主要分别通过 COX-2 抑制和 iNOS 下调发生。PFS 还抑制 IL-6 和 TNF-α的产生。在大鼠佐剂诱导的关节炎（慢性炎症）中进行测试时，PFS 在 10-100mg/kg/天时口服给药强烈抑制关节炎炎症。此外，PFS 口服给药可有效抑制醋酸引起的小鼠扭体反应。
我们的结果表明，PFS 抑制慢性炎症反应，并且抑制促炎分子如 COX-2、iNOS 和 IL-6 可能至少部分有助于体内抗炎活性。总的来说，这些结果表明苦参的 PFS 可能具有治疗类风湿性关节炎等慢性炎症性疾病的潜力。
