来自Sinularia levi的细胞毒性代谢物得到了网络药理学的支持
Mingna Sun1, Miada F Abdelwahab2, Jianye Zhang1
1Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target & Clinical Pharmacology, The NMPA and State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences and the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou, China.
PloS one
|February 6, 2024
概括
西努拉利亚莱维珊瑚提取物对癌细胞,特别是Caco-2具有强大的抗增殖作用. 孤立的化合物,包括新型化合物,表现出不同的细胞毒性潜力,其中化合物25是最有效的.
科学领域:
- 海洋天然产品 化学 化学
- 癌症生物学 癌症生物学
- 药理学 药理学是指药理学的学科.
背景情况:
- 海洋环境是新型生物活性化合物的丰富来源.
- 珊瑚提取物,例如来自Sinularia levi的珊瑚提取物,已经显示出潜在的药用特性.
- 了解海洋天然产品的细胞毒性机制对于药物发现至关重要.
研究的目的:
- 评估Sinularia levi总提取物及其分离化合物的体外抗增殖活性,以对抗人类癌细胞系.
- 识别和描述S. levi提取物的主要植物成分.
- 阐明细胞毒性化合物的潜在作用机制.
主要方法:
- 使用Caco-2,MCF-7和HepG-2细胞系进行了体外抗增殖试验.
- 使用液体染色学结合高分辨率电喷射电离化质谱学 (LC-HR-ESI-MS) 的代谢分析.
- 用染色体和光谱技术进行的植物化学研究,用于隔离和识别代谢物.
- 分子对接分析以预测作用机制.
主要成果:
- 这种S. levi总提取物表现出强大的抗增殖作用,对Caco-2细胞具有最高的强度 (IC50 3.3μg/mL).
- 代谢分析和植物化学研究导致了类固醇和特类物质的鉴定,包括Sinularia属的两个新型化合物.
- 化合物25 (12-hydroperoxylsarcoph-10-ene) 对HepG-2,MCF-7和Caco-2细胞表现出显著的细胞毒性作用 (IC50为2.13-5.67μg/mL).
- 网络和分子对接分析表明,循环素依赖激酶1 (CDK1) 抑制是潜在的作用机制.
结论:
- 西努拉利亚莱维提取物及其分离化合物具有针对各种癌症细胞系的显著细胞毒性潜力.
- 化合物25是作为抗癌剂进一步研究的有希望的候选物.
- CDK1抑制可能是观察到的细胞毒性作用的关键机制,需要进一步的机制研究.
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