在Callicarpa macrophylla中,有五种未被描述的阿比类型的二烯
Gao-Xiang Du1, Tong Chen1, Ge Wang2
1School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, People's Republic of China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, People's Republic of China.
Fitoterapia
|July 31, 2023
概括
对Callicarpa macrophylla的植物化学分析产生了新型的四虫. 两种化合物,即B基亚德芬酸和F基全粒素,显著降低了细胞外PCSK9蛋白水平,表明了治疗潜力.
科学领域:
- 植物化学 植物化学
- 自然产品 化学 化学
- 药用植物研究 药用植物研究
背景情况:
- Callicarpa macrophylla是一种药用植物,具有丰富的传统使用历史.
- 迪特尔类是一种多样化的自然产品类别,具有广泛的生物活动.
- 细胞外PCSK9蛋白在胆固醇代谢中起着至关重要的作用,是心血管疾病治疗的目标.
研究的目的:
- 从Callicarpa macrophylla中分离和表征新型的四面体.
- 为了评估隔离的迪特尔类物质对细胞外PCSK9蛋白水平的抑制作用.
主要方法:
- 使用HRESIMS,1D和2DNMR光谱的植物化学研究.
- 通过CD比较,化学方法和X射线晶体衍射来确定绝对配置.
- PCSK9 AlphaLISA选试验,以评估在HepG2细胞介质中对PCSK9蛋白水平的抑制作用.
主要成果:
- 两种罕见的重新排列的阿比类型的二基 (巨基F-G) 和三种阿比基二基 (巨基H-J) 得到了新的特征.
- 此外,还确定了五种已知的双类动物.
- 贾德芬酸B和全息素F显著抑制了细胞外PCSK9蛋白水平 (分别在20μM时为56.80%和43.18%).
结论:
- 卡利卡拉帕巨 (Callicarpa macrophylla) 是结构上多样化的四类动物的来源,包括新型化合物.
- 贾德芬酸B和全息素F表现出强大的PCSK9抑制活性.
- 这些发现凸显了Callicarpa macrophylla衍生的二类药物的潜力,作为管理胆固醇水平的治疗剂.
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