AI Article Synopsis
- - Trachyloban-19-oic acid (1) is a natural diterpene that can be modified to create new bioactive compounds through biotransformation by the fungus Syncephalastrum racemosum, resulting in three novel derivatives (2-4).
- - The newly formed compound 3 was synthesized from compound 2 through oxidation and rearrangement, while compounds 3 and 4 have not been previously documented.
- - All derivatives (1-4) showed greater inhibitory activity against acetylcholinesterase, a key enzyme related to Alzheimer's treatment, with product 3 exhibiting an impressive IC value of 0.06 μM, outperforming the standard galanthamine (IC = 0.
Article 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 IC = 0.06 μM, which is about six times higher than activity found for galanthamine (IC = 0.38 μM), the positive control used in this assay.
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| http://dx.doi.org/10.1016/j.bioorg.2018.04.011 | DOI Listing |
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Article Synopsis
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