2. Academic Validation
  3. Proaporphine and aporphine alkaloids with acetylcholinesterase inhibitory activity from Stephania epigaea

Proaporphine and aporphine alkaloids with acetylcholinesterase inhibitory activity from Stephania epigaea

  • Fitoterapia. 2015 Jul;104:102-7. doi: 10.1016/j.fitote.2015.05.019.
Jian-Wei Dong 1,  Le Cai 1,  Yun-Shan Fang 1,  Huai Xiao 2,  Zhen-Jie Li 1,  Zhong-Tao Ding 3
Affiliations

Affiliations

  • 1 Key Laboratory of Medicinal Chemistry for Nature Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China.
  • 2 Key Laboratory of Medicinal Chemistry for Nature Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China; School of Pharmaceutical Sciences and Chemistry, Dali University, Dali 671000, PR China.
  • 3 Key Laboratory of Medicinal Chemistry for Nature Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China. Electronic address: ztding@ynu.edu.cn.
PMID: 26028544 DOI: 10.1016/j.fitote.2015.05.019
Abstract

An unusual proaporphine alkaloid bearing an isopropanenitrile group at isoquinoline nitrogen, named epiganine A (1) and a new aporphine alkaloid, epiganine B (2), together with eight known Alkaloids, pronuciferine (3), dehydrodicentrine (4), romerine (5), romeline (6), N-methylcalycinine (7), phanostenine (8), dicentrine (9), and N-methyllaurotetanine (10), were isolated from the roots of Stephania epigaea. The absolute configuration of 1 was determined by calculating electronic circular dichroism (ECD) and comparing with experimental data. Compounds 2 and 4 showed strong acetylcholinesterase (AChE) inhibitory effects with the IC50 values of 4.36 and 2.98μM, respectively. Compounds 5-9 also exhibited potent AChE inhibitory activities.

Keywords

Acetylcholinesterase inhibitory activity; Aporphine alkaloid; Dehydrodicentrine (PubChem CID: 3084326); Dicentrine (PubChem CID: 101300); Epiganine A; Epiganine B; N-methylcalycinine; N-methyllaurotetanine (PubChem CID: 16573); Phanostenine (PubChem CID: 12305138); Proaporphine alkaloid; Pronuciferine (PubChem CID: 200480); Romeline; Romerine (PubChem CID: 119204); Stephania epigaea.

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