4.4 Article

Screening of acetylcholinesterase inhibitors in marine organisms from the Caribbean Sea

期刊

NATURAL PRODUCT RESEARCH
卷 33, 期 24, 页码 3533-3540

出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2018.1481837

关键词

Acetylcholinesterase inhibitors; marine bioprospecting; cembranes; marine natural products; Eunicea knigthi; Pseudoplexaura porosa

资金

  1. Departamento Administrativo de Ciencia, Tecnologia e Innovacion [321-2011]
  2. Direccion de Investigacion, Universidad Nacional de Colombia [12529]

向作者/读者索取更多资源

The acetylcholinesterase inhibitory activity of 89 organic extracts from marine organisms was evaluated through a TLC bioautography methodology. Extracts from soft corals (Eunicea and Plexaura) were the most active compared with extracts from sponges. The bioguided chemical study of the most active extract, obtained from Pseudoplexaura porosa, 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 (1), correcting the structure reported to the Styelolide. Additionally, the acetylcholinesterase inhibitory activity of fourteen cembranoids (2?15) isolated from soft corals Eunicea knighti and Pseudoplexaura flagellosa was evaluated. Cembranoids 2, 3 and 4 were the most active compounds in the TLC bioassay. Then, the most promising cembranoids, 14-acetoxycrassine (1) and asperdiol (2), were tested quantitatively and they exhibited IC50 values of 1.40???0.113 and 0.358???0.130??M, respectively.

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