阿斯珀金和阿斯佩里米德C的总合成和抗炎活性
Kittisak Thongpat1, Natthawat Milehman1, Worarat Rojanaverawong2,3
1Division of Physical Science and Center of Excellence for Innovation in Chemistry, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90110, Thailand.
Journal of natural products
|August 7, 2024
概括
研究人员合成了asperjinone和asperimide C,证实了它们的结构. 阿斯珀金在细胞中表现出显著的抗炎作用,显示出治疗急性损伤的潜力.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
背景情况:
- γ-丁化物天然产品具有多样化的生物活性.
- 需要合成验证阿斯珀金 (1) 和阿斯珀米德C (2) 的结构.
- 了解这些化合物的生物活性对于药物发现至关重要.
研究的目的:
- 为了实现阿斯珀金 (1) 和阿斯佩里米德C (2) 的总合成,在racemic和chiral形式.
- 确认阿斯珀金的拟议结构 (1) 和阿斯佩里米德C (2) 的结构/绝对配置.
- 为了研究阿斯珀金的抗炎作用 (1).
主要方法:
- 使用Basavaiah的一Friedel-Crafts/maleic无水化物形成协议进行合成.
- 进行了两种化合物的全合成,分别是racemic和chiral形式.
- 在LPS诱导的炎症下,评估了近位管状上皮细胞 (RPTEC) 的抗炎活性.
主要成果:
- 成功合成了阿斯珀金 (1) 和阿斯佩里米德C (2),验证了拟议的结构.
- 合成阿斯珀金 (1) 显示出显著的抗炎活性,优于其他测试化合物和印梅他辛.
- 化合物1抑制了促炎性细胞因子基因表达 (TNF-α,IL-1β,IL-6),降低了iNOS和COX-2的表达,并抑制了NO的产生.
结论:
- 这项研究提供了有效的合成途径,以阿斯珀金和阿斯佩里米德C.
- 阿斯珀金 (1) 显示强大的抗炎性质,特别是在炎的背景下.
- 阿斯珀金 (1) 是开发用于急性损伤的新型治疗药物的有希望的候选药物.
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