腺,从Eupatorium adenophorum中获得的前所未有的甲:结构解,生物启发的总合成和神经保护性活动评估
Bo Yin1, Xiaohuan Li1, Zi-Xiang Li1
1Sichuan Engineering Research Center for Biomimetic Synthesis of Natural Drugs, School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, P. R. China.
研究人员从Eupatorium adenopharum中分离了 (-) -Adenophorone,这是一个新的子式基,从Eupatorium adenopharum. 它的结构通过合成和晶体学得到证实,并显示出显著的神经保护作用.
科学领域:
- 自然产品化学 自然产品化学
- 有机合成 有机合成
- 神经药理学神经药理学
背景情况:
- (-) -阿诺 (1) 是一种独特的中的多环聚烯,从Eupatorium adenopharum中分离出来.
- 三环[4.3.1.05,9 ]甲骨架代表了自然产品中前所未有的结构图案.
研究的目的:
- 为了阐明 (-) - 氨的结构.
- 开发一种生物启发的 (-) - 腺和相关化合物的总合成.
- 为了研究 (-) - 阿登诺的神经保护潜力.
主要方法:
- 使用光谱分析 (NMR,MS) 和X射线晶体学进行结构阐明.
- 总合成使用Reformatsky反应,氧化,化和MBH-Tsuji-Trost循环.
- 在体外测试中使用H2O2处理的SH-SY5Y和PC12细胞来评估神经保护.
主要成果:
- 确定了 (-) -阿诺的结构是明确的.
- 从 (-) - 卡中获得 (+) - 欧普托克斯A (2) 的简洁的8步合成,使用高立体控制.
- 从 (+) -euptox A 通过跨环状迈克尔添加的 (-) -Adenophorone 的生物灵感合成验证了拟议的生物合成途径.
- (-) -阿诺显示出强大的神经保护活性.
结论:
- 该研究成功确定了结构并合成了 (-) - 腺,为其生物合成提供了洞察力.
- 合成策略有效地构建了复杂的多环形基骨架.
- (-) -阿诺是神经保护疗法开发的有希望的候选药物.
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