来自Datura stramonium的维他诺化物:两种前所未有的B环-seco衍生物和抗炎活性类似物
Juan Pan1, Gang-Tao Bu1, Si-Yi Wang2
1"Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education"+Traditional Chinese Medicine (TCM) Biological Genetics (Heilongjiang Province Double First-Class Construction Interdiscipline), Harbin, China.
研究人员从Datura stramonium L.叶中发现了13种新的维他诺化物,其中两种化合物在细胞模型中显示出强烈的抗炎活性,比德甲更强.
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:
- 达图拉 (Datura stramonium L.) 是一种具有传统使用历史的植物.
- 维他诺化物是类固醇乳的一类,具有多样化的生物活性.
- 炎症是一种复杂的生物反应,与各种疾病有关.
研究的目的:
- 从Datura stramonium L.中分离和描述新型维他诺化物.
- 评估隔离化合物的抗炎潜力.
- 识别潜在的化合物用于治疗与炎症有关的疾病.
主要方法:
- 采用紫外线引导的分离技术进行了提取物分离.
- 高分辨率电喷射电离质谱 (HRESIMS) 和核磁共振 (NMR) 光谱学用于结构阐明.
- 进行了体外试验,以评估对BV2微质细胞中脂聚糖 (LPS) 诱导的氧化 (NO) 生产的抑制作用.
主要成果:
- 他们分离了13种以前未报告的维他诺化物 (1-13) 和9种已知的类似物 (14-22).
- 化合物1和2是新型维他诺化物,其特点是B环裂变和两个形式基.
- 化合物16和22表现出强大的抗炎活性,IC50值分别为6.72±0.08μM和7.48±0.28μM,表现优于德克萨米他 (IC50=8.04±0.60μM).
结论:
- 达图拉·斯特拉莫尼奥姆 (Datura stramonium L.) 叶片是结构独特的维他诺化物 (withanolides) 的丰富来源.
- 隔离的化合物,特别是16和22,具有显著的抗炎性质.
- 这些发现凸显了D.斯特拉作为开发新抗炎疗法的来源的潜力.
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