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Anti--amyloid aggregation activity of enantiomeric furolactone-type lignans from (Jack) I.C.N. | LitMetric

Anti--amyloid aggregation activity of enantiomeric furolactone-type lignans from (Jack) I.C.N.

Nat Prod Res

School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, People's Republic of China.

Published: February 2020

AI Article Synopsis

  • A study of Jack I.C.N. twigs and leaves identified three pairs of enantiomeric furolactone-type lignans, including two new compounds.
  • Chiral HPLC was successfully used for the first time to separate these enantiomers, and their structures were confirmed through spectroscopic analysis and ECD comparisons.
  • The isolated compounds were tested for their ability to inhibit -amyloid aggregation, with one compound showing a superior inhibitory effect compared to the positive control, and molecular dynamics were used to analyze ligand-receptor interactions.

Article Abstract

The phytochemical investigation on the twigs and leaves of (Jack) I.C.N. led to the isolation of three pairs of furolactone-type lignans enantiomers, including a pair of new compounds (1,5,6)-Kachiranol () and (1,5,6)-Kachiranol () and four known compounds (/ and /). Separation of the furolactone-type lignans enantiomeric mixtures was achieved using chiral HPLC for the first time. Their structures were determined by spectroscopic analysis and comparison between the experimental and calculated electronic circular dichroism (ECD) spectra. All optical pure compounds were evaluated for their inhibitory effects on -amyloid aggregation by ThT assay. Among them, the inhibitory activity of the compound (71.1%) was higher than the positive control (61.0%) and other compounds. In addition, molecular dynamics and molecular docking were employed to explore the binding relationship between the ligand and the receptor.

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Source
http://dx.doi.org/10.1080/14786419.2018.1488705DOI Listing

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