Screening of acetylcholinesterase inhibitors in marine organisms from the Caribbean Sea

被引:10
|
作者
Castellanos, Fabio [1 ]
Amaya-Garcia, Fabian [1 ]
Tello, Edisson [1 ,4 ]
Alejandro Ramos, Freddy [1 ]
Umana, Adriana [1 ]
Puyana, Monica [2 ]
Resende, Jackson A. L. C. [3 ]
Castellanos, Leonardo [1 ]
机构
[1] Univ Nacl Colombia, Dept Quim, Bogota, Colombia
[2] Univ Bogota Jorge Tadeo Lozano, Dept Ciencias Biol & Ambientales, Programa Biol Marina, Bogota, Colombia
[3] Univ Fed Fluminense, Inst Quim, Lab Difracao Raios X, Niteroi, RJ, Brazil
[4] Univ Sabana, Fac Ingn, Campus Puente Comun, Chia, Colombia
关键词
Acetylcholinesterase inhibitors; marine bioprospecting; cembranes; marine natural products; Eunicea knigthi; Pseudoplexaura porosa; DITERPENES; DISEASE;
D O I
10.1080/14786419.2018.1481837
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
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.
引用
收藏
页码:3533 / 3540
页数:8
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