加勒比海海洋生物中乙酰胆碱酯酶抑制剂的筛选

Screening of acetylcholinesterase inhibitors in marine organisms from the Caribbean Sea.

机构信息

Departamento de Química, Universidad Nacional de Colombia , Bogota , Colombia.

Programa de Biología Marina, Departamento de Ciencias Biológicas y Ambientales, Universidad de Bogotá Jorge Tadeo Lozano , Bogotá , Colombia.

出版信息

Nat Prod Res. 2019 Dec;33(24):3533-3540. doi: 10.1080/14786419.2018.1481837. Epub 2018 Jun 4.

DOI:10.1080/14786419.2018.1481837

PMID:29863905

Abstract

The acetylcholinesterase inhibitory activity of 89 organic extracts from marine organisms was evaluated through a TLC bioautography methodology. Extracts from soft corals ( and ) were the most active compared with extracts from sponges. The bioguided chemical study of the most active extract, obtained from , led to the isolation of a diterpene with spectroscopic properties consistent to those published to the cembrane Steylolide. However, further analysis by X-ray diffraction indicated that the compound was the 14-acetoxycrassine (), correcting the structure reported to the Styelolide. Additionally, the acetylcholinesterase inhibitory activity of fourteen cembranoids (-) isolated from soft corals and was evaluated. Cembranoids , and were the most active compounds in the TLC bioassay. Then, the most promising cembranoids, 14-acetoxycrassine () and asperdiol (), were tested quantitatively and they exhibited IC values of 1.40 ± 0.113 and 0.358 ± 0.130 μM, respectively.

摘要

通过 TLC 生物自显影方法评估了 89 种海洋生物有机提取物对乙酰胆碱酯酶的抑制活性。与海绵提取物相比，软珊瑚（和）的提取物活性最高。从最活跃的提取物（来自）进行的生物导向化学研究导致分离出一种二萜，其光谱性质与已发表的cembrane Steylolide 一致。然而，通过 X 射线衍射的进一步分析表明，该化合物是 14-乙酰氧基克瑞辛（），纠正了 Styelolide 报道的结构。此外，还评估了从软珊瑚和中分离得到的 14 种cembranoids（-）的乙酰胆碱酯酶抑制活性。cembranoids 、和是 TLC 生物测定中最活跃的化合物。然后，对最有前途的cembranoids，14-乙酰氧基克瑞辛（）和asperdiol（）进行了定量测试，它们的 IC 值分别为 1.40±0.113 和 0.358±0.130 μM。