来自Euphorbia peplus的高氧化恩特-阿比坦双酸乳及其抗炎活性
Ying Yan1, Ming-You Peng1, Ying Yang2
1State Key Laboratory of Functions and Applications of Medicinal Plants & College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang 550014, China.
来自Euphorbia peplus的11种新化合物显示出抗炎作用. 化合物6显著降低了炎症媒介,可能是潜在的治疗炎症相关疾病.
科学领域:
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 欧比亚是一种多种生物活性化合物的来源.
- 恩特-阿比坦二烯酸乳具有各种生物活性.
- 炎症是许多疾病的关键因素.
研究的目的:
- 从Euphorbia peplus中分离和表征新的ent-abietane diterpenoid乳.
- 评估这些化合物的抗炎潜力.
- 为了确定潜在的治疗剂的炎症相关疾病.
主要方法:
- 使用NMR,HRESIMS和单晶X射线衍射进行隔离和结构阐明.
- 通过ECD和DP4+计算来确定绝对配置.
- 在LPS诱导的RAW 264.7巨细胞的体外抗炎测定,测量氧化和细胞因子mRNA表达.
主要成果:
- 鉴定出了11种新的ent-abietane双酸乳 (euphjatrophanes H-R) 的发现.
- 化合物6-9,12-16和19抑制了氧化的产生.
- 化合物6,9,11,和16抑制了关键的炎症性细胞因子mRNA表达 (IL-6,IL-1β,TNFα).
- 化合物6显示了剂量依赖的抑制和调节的FOXO1表达和NF-κB p65酸化.
结论:
- 从Euphorbia peplus中发现了新的ent-abietane二类乳.
- 一些化合物表现出显著的抗炎性质.
- 化合物6是开发新型抗炎疗法的有希望的候选者.
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