基于基因组和光谱特征的自然巨乳的发现
Yern-Hyerk Shin1, Ji Hyeon Im1, Ilnam Kang2
1Natural Products Research Institute, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
Journal of the American Chemical Society
|January 12, 2023
概括
一种新的方法结合了基因组和光谱分析,以有效地发现天然巨乳. 这种方法确定了具有重要的生物活性,包括抗癌和抗菌性质的新型巨乳剂.
科学领域:
- 自然产品化学
- 基因组学
- 微生物学
背景情况:
- 由于缺乏有针对性的搜索方法,因此难以发现具有多种生物活性的自然产品.
- 在结构上是独一无二的,具有显著的治疗潜力.
研究的目的:
- 通过整合基因组和光谱签名,开发自然宏观素的有针对性的发现方法.
- 识别和描述来自细菌来源的新型巨乳素.
主要方法:
- 基于基因组特征的PCR查细菌DNA库以识别潜在的巨乳菌株.
- 基于光谱签名的早期识别使用1H-15N HSQC-TOCSY NMR检测和结构类型分配.
- 净化和详细的光谱分析以阐明新化合物的结构.
主要成果:
- 确定了43种潜在的巨乳菌株,效率为3. 6%.
- 发现了三种新型麦克罗拉克坦:一种α-麦克罗拉克坦 (2),一种β-甲基麦克罗拉克坦 (3),以及一种经过修改的麦克罗拉克坦结构 (1).
- 穆兰 (2) 对癌细胞系具有显著的细胞毒性 (IC50=1. 58μM对HCT116).
- 康科拉克坦 (3) 对黄金葡萄球菌A类酶有抑制作用.
结论:
- 开发的基于基因组和光谱签名的方法为发现新的自然巨乳素提供了有效的策略.
- 这种方法广泛适用于发现其他含的天然产品.
- 鉴定出的新型麦克罗拉克坦具有有前途的药理特性,需要进一步研究.
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