New AChE inhibitors from microbial transformation of trachyloban-19-oic acid by Syncephalastrum racemosum

作者：dos Santos Gabriel Franco; Lima Gesiane da Silva; de Oliveira Geane Pereira; de Souza Filho Jose Dias; Amaral Luciana da Silva; Rodrigues Filho Edson; Takahashi Jacqueline Aparecida^*

来源：Bioorganic Chemistry, 2018, 79: 60-63.

DOI：10.1016/j.bioorg.2018.04.011

• Syncephalastrum racemosum
• Biotransformation
• Trachyloban-19-oic acid
• Acetylcholinesterase
• Alzheimer's disease

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= 0.06 mu M, which is about six times higher than activity found for galanthamine (IC50= 0.38 mu M), the positive control used in this assay.

• 出版日期2018-9