来自Strophioblachia fimbricalyx的结构多样化的变形类,通过诱导细胞亡,具有细胞毒性活动
Changshui Yang1, Houli Jiang2, Haoyu Mao2
1Department of Pharmacy, Institute of Translational Medicine, Medical College, Yangzhou University, Yangzhou, 225009, China; Jiangsu Key Laboratory of Integrated Traditional Chinese and Western Medicine for Prevention and Treatment of Senile Diseases, Yangzhou University, Yangzhou, 225009, China; The Key Laboratory of Syndrome Differentiation and Treatment of Gastric Cancer of the State Administration of Traditional Chinese Medicine, Yangzhou, 225009, China.
Phytochemistry
|February 24, 2024
概括
研究人员从Strophioblachia fimbricalyx中分离出了新的变形的氨酸衍生物. 化合物8和10显示出显著的细胞毒性和抗性活性,而化合物10在A549细胞中诱导了亡.
科学领域:
- 自然产品化学 自然产品化学
- 药用化学 医学化学
- 化学生物学 化学生物学
背景情况:
- 斯特罗菲奥布拉基亚 (Strophioblachia fimbricalyx) 是一种具有独特化学化合物的植物来源.
- 南衍生物经常表现出多样化的生物活动.
- 了解天然产品的化学多样性和生物活性对于药物发现至关重要.
研究的目的:
- 从Strophioblachia fimbricalyx.中分离和描述新型变形的氨酸衍生物.
- 评估这些化合物的细胞毒性和抗性活性.
- 阐明活性化合物的作用机制.
主要方法:
- 使用UPLC-MS/MS引导的分子网络来隔离化合物.
- 通过1D/2D NMR,HRESIMS,量子化学计算和X射线衍射来阐明结构.
- 对瘤细胞系的细胞毒性测定和机械学研究 (细胞周期,细胞亡).
主要成果:
- 隔离了十种氨酸衍生物,包括四种新产物 (1-4) 和一种新天然产物 (5).
- 芬布里卡利克松 (1) 和铁亚克西芬M (6) 代表了该属的新结构类型.
- 化合物8和10表现出显著的细胞毒性活性;化合物10通过诱导S相停止和亡而表现出抗瘤作用.
结论:
- 这项研究扩大了已知的来自Strophioblachia的氨酸衍生物的化学多样性.
- 化合物8和10是作为抗癌剂进一步研究的有希望的候选物.
- 特里戈霍维罗尔G (10) 通过细胞循环停止和亡诱导来发挥其抗瘤作用.
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