| Title : New AChE inhibitors from microbial transformation of trachyloban-19-oic acid by Syncephalastrum racemosum - Dos_2018_Bioorg.Chem_79_60 |
| Author(s) : Dos Santos GF , da Silva Lima G , Pereira de Oliveira G , de Souza Filho JD , da Silva Amaral L , Rodrigues-Filho E , Takahashi JA |
| Ref : Bioorg Chem , 79 :60 , 2018 |
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Abstract :
Trachyloban-19-oic acid (1) is a diterpene very abundant in nature and its structural modification can furnish new bioactive compounds. Biotransformation of 1 by fungus Syncephalastrum racemosum provided three derivatives, two hydroxylated products (2-3) and one product of rearrangement (4). Products 3 and 4 have never been reported so far, to the best of our knowledge. Structure of 3 was formed after oxidation and rearrangement of compound 2. Compounds 1-4 were evaluated for inhibition of acetylcholinesterase, enzyme linked to the symptomatic control of Alzheimer's disease. All the compounds presented inhibitory activity higher than starting material 1, and product 3 presented IC50=0.06muM, which is about six times higher than activity found for galanthamine (IC50=0.38muM), the positive control used in this assay. |
| PubMedSearch : Dos_2018_Bioorg.Chem_79_60 |
| PubMedID: 29723742 |
Dos Santos GF, da Silva Lima G, Pereira de Oliveira G, de Souza Filho JD, da Silva Amaral L, Rodrigues-Filho E, Takahashi JA (2018)
New AChE inhibitors from microbial transformation of trachyloban-19-oic acid by Syncephalastrum racemosum
Bioorg Chem
79 :60
Dos Santos GF, da Silva Lima G, Pereira de Oliveira G, de Souza Filho JD, da Silva Amaral L, Rodrigues-Filho E, Takahashi JA (2018)
Bioorg Chem
79 :60