New diterpenoid alkaloids from Aconitum heterophyllum Wall: Selective butyrylcholinestrase inhibitors

Authors: Nisar, Muhammad1; Ahmad, Manzoor2; Wadood, Noreen3; Lodhi, Muhammad Arif2; Shaheen, Farzana2; Choudhary, M. Iqbal2

Source: Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 24, Number 1, February 2009 , pp. 47-51(5)

Publisher: Informa Healthcare

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Abstract:

Two new diterpenoid alkaloids, heterophyllinine-A (1) and heterophyllinine-B (2), along with two known alkaloids dihydroatisine (3) and lycoctonine (4) were isolated from the roots of Aconitum heterophyllum Wall. The structure of (1) and (2), were deduced on the basis of spectral data. Compounds 1-2 inhibited acetylcholinesterase (AChE, EC 3.1.1.7) and butyrylcholinesterase (BChE, EC 3.1.1.8) enzymes in a concentration-dependent manner with percent inhibition ranging between 4.24% and 6.94 % and 79.1 % and 82.75 % for AChE and BChE, respectively indicating that compounds 1 and 2 are about thirteen times more specific to BChE than AChE.

Keywords: Aconitum heterophyllum wall; norditerpenoid alkaloids; heterophyllinine-A; heterophyllinine-B; acetylcholinesterase; butyrylcholinesterase

Document Type: Research article

DOI: 10.1080/14756360801906202

Affiliations: 1: Institute of Chemical Sciences and Department of Pharmacy, University of Peshawar, Peshawar, Pakistan 2: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan 3: Department of Biochemistry, Kabir Medical College, Peshawar, Pakistan

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