Synthesis of Fibrauretin Derivatives and Their Inhibition on Acetylcholinesterase Activity
10.11895/j.issn.0253-3820.171239
- VernacularTitle:黄藤素衍生物的合成及其抑制乙酰胆碱酯酶活性研究
- Author:
Zhi-Heng XING
1
;
Na LYU
;
Zhong-Mei HE
;
Yu-Gang GAO
;
Yan ZHAO
;
Hong-Yan ZHU
;
He YANG
;
Lian-Xue ZHANG
Author Information
1. 吉林农业大学 人参工程技术创新中心
- Keywords:
Fibrauretin;
Esterification reaction;
Acetylcholinesterase;
Inhibitory activity
- From:
Chinese Journal of Analytical Chemistry
2018;46(5):684-689
- CountryChina
- Language:Chinese
-
Abstract:
The structure of fibrauretin made by our lab was modified. Fibrauretin was demethylated at 9-site under high temperature pyrolysis at 160℃-180℃ and was reacted with a series of acid chlorides. Twele derivatives of fibrauretin were obtained. The structure of each derivative was determined by1H-NMR and13C-NMR. The derivatives were 9-O-benzoyl-fibrauretin, 9-O-( 2-methylbenzoyl)-fibrauretin, 9-O-( 4-methylbenzoyl)-fibrauretin, 9-O-(3, 5-dimethylbenzoyl)-fibrauretin, 9-O-(4-(chloromethyl) benzoyl)-fibrauretin and other derivatives. The 12 derivatives are all new chemical compounds. Taking ATCI as substrate,the inhibitory activity on acetylcholinesterase (AChE) from the head of flies of the fibrauretin and its derivatives were screened. The results showed that most of the derivatives had improved their inhibitory activity on AChE through esterification reaction. Compounds 9-O-(4-methylbenzoyl)-fibrauretin, 9-O-(3,5-dimethylbenzoyl)-fibrauretinand 9-O-(4-(chloromethyl)benzoyl)-fibrauretin had significant inhibitory effect on AChE,and the inhibitory activity was stronger than the that of donepezil.
