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Citation: TANG Huang, ZHONG Shuming, ZHAO Lizhen, ZHAO Haitao. Synthesis, Inhibition of β-Amyloid Aggregation and Antioxidation of Oxoisoaporphine-Melatonin Hybrids[J]. Chinese Journal of Applied Chemistry, ;2012, 29(5): 510-514. doi: 10.3724/SP.J.1095.2012.00281 shu

Synthesis, Inhibition of β-Amyloid Aggregation and Antioxidation of Oxoisoaporphine-Melatonin Hybrids

1.
Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources(Ministry of Education of China), School of Chemistry & Chemical Engineering of Guangxi Normal University, Guilin 541004, China

Corresponding author: TANG Huang,
Received Date: 28 June 2011
Available Online: 9 September 2011
Fund Project: 广西自然科学基金资助项目(083095) (083095)广西研究生教育创新计划项目(2010106020703M68) (2010106020703M68)

Two oxoisoaporphine-melatonin hybrids(compound 2a and 2b) have been designed,synthesized and tested for their ability to inhibit acetylcholinesterase,butyrylcholinesterase,acetylcholinesterase-induced β-amyloid(Aβ) aggregation.Their inhibitory mechanism and antioxidant properties were also studied.The synthetic compounds(2a and 2b) exhibited moderate AChE inhibitory activity with IC₅₀ values in the micromolar range in most cases.Non-competitive binding mode was found for these derivatives.Moreover,the compounds(2a and 2b) exhibit high acetylcholinesterase-induced Aβ antiaggregating activity with inhibitory potencies ranging from 79.3% to 84.7%,and significant antioxidant properties with peroxyl radical absorbance capacities ranging from 1.1-to 1.5-fold the value of trolox.
- oxoisoaporphine derivatives,
- melatonin,
- cholinesterase,
- antioxidant,
- Aβ antiaggregating
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