Xie Tian-Zhen, Zhao Yun-Li, Wang Huan, Chen Yi-Chi, Wei Xin, Wang Zhao-Jie, He Ying-Jie, Zhao Li-Xing, Luo Xiao-Dong
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, PR China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, PR China.
J Ethnopharmacol. 2022 Jul 15;293:115290. doi: 10.1016/j.jep.2022.115290. Epub 2022 Apr 19.
"Li-Lu", the roots and rhizomes of Veratrum grandiflorum (Melianthiaceae), has been historically used as a traditional folk medicine for the treatment of wrist pain, fractures, sores, and inflammation in Yunnan Province, China. However, the anti-inflammatory and analgesic studies of this plant have seldom reported.
To evaluate the anti-inflammatory and analgesic properties related to the traditional usage of V. grandiflorum both in vitro and in vivo, and further explore the accurate bioactive compounds from the medicinal plant.
Phytochemical investigation was carried out by chromatographic methods and their structures were established based on extensive spectra and comparison with corresponding data in the reported literatures. Anti-inflammatory activities were assessed by the suppression of lipopolysaccharide-activated inflammatory mediators in RAW 264.7 macrophage cells in vitro. Furthermore, anti-inflammatory and analgesic effects were evaluated based on carrageenan-induced paw edema and acetic acid-stimulated writhing in mice.
The methanol extract (ME) of V. grandiflorum significantly alleviated the paw edema caused by carrageenan and the writhing numbers induced by acetic acid. Subsequent phytochemical investigation led to isolated of 21 steroidal alkaloids, including seven new compounds, veragranines C-I (1-7). Anti-inflammatory test indicated that steroidal alkaloids could decrease the expression of cyclooxygenase-2 (COX-2), interleukin-1β (IL-1β), and tumor necrosis factor α (TNF-α) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage cells at a concentration of 5.0 μg/ml in vitro, comparable to DXM. Moreover, five new steroidal alkaloids (2, 4, 5, 6, and 7) and two major steroidal alkaloids (9 and 13) significantly decreased the numbers of writhing in mice at the doses of 0.5 and/or 1.0 mg/kg (p < 0.01/0.05), roughly comparable to Dolantin™ at 10.0 mg/kg.
The investigation supported the traditional use of V. grandiflorum and provided new steroidal alkaloids as potent analgesic agents.
“藜芦”，即大理藜芦（刺茉莉科）的根和根茎，在中国云南省历史上一直被用作传统民间药物，用于治疗手腕疼痛、骨折、疮疡和炎症。然而，对这种植物的抗炎和镇痛研究鲜有报道。
在体外和体内评估与大理藜芦传统用途相关的抗炎和镇痛特性，并进一步探索这种药用植物中的精确生物活性化合物。
采用色谱方法进行植物化学研究，并根据广泛的光谱数据以及与已报道文献中的相应数据进行比较来确定其结构。通过抑制体外RAW 264.7巨噬细胞中脂多糖激活的炎症介质来评估抗炎活性。此外，基于角叉菜胶诱导的小鼠爪肿胀和醋酸刺激的小鼠扭体反应来评估抗炎和镇痛效果。
大理藜芦的甲醇提取物（ME）显著减轻了角叉菜胶引起的爪肿胀以及醋酸诱导的扭体次数。随后的植物化学研究导致分离出21种甾体生物碱，包括7种新化合物，藜芦大碱C - I（1 - 7）。抗炎试验表明，甾体生物碱在体外浓度为5.0μg/ml时可降低脂多糖（LPS）刺激的RAW 264.7巨噬细胞中环氧合酶 - 2（COX - 2）、白细胞介素 - 1β（IL - 1β）和肿瘤坏死因子α（TNF - α）的表达，与地塞米松相当。此外，5种新的甾体生物碱（2、4、5、6和7）和2种主要的甾体生物碱（9和13）在剂量为0.5和/或1.0mg/kg时显著减少小鼠的扭体次数（p < 0.01/0.05），大致与10.0mg/kg的度冷丁相当。
该研究支持了大理藜芦的传统用途，并提供了新的甾体生物碱作为有效的镇痛剂。
