Cholinesterase inhibitory activity and structure elucidation of a new phytol derivative and a new cinnamic acid ester from Pycnanthus angolensis

Revista Brasileira de Farmacognosia

Obafemi Awolowo University, Ile Ife, Nigeria¹  Obuotor, Efere M.¹  Agbedahunsi, Joseph M.¹  University of Ibadan, Nigeria¹  Adesanya, Saburi A.¹  Elufioye, Taiwo O.¹ 

关键词:  Pycnanthus angolensis;    Alzheimer's disease;    Cholinesterase inhibitors;    Bioactive compounds;   

DOI  :  10.1016/j.bjp.2016.01.010

来源: Sociedade Brasileira de Farmacognosia

【 摘 要 】

The leaves of Pycnanthus angolensis (Welw.) Warb., Myristicaceae, are used as memory enhancer and anti-ageing in Nigerian ethnomedicine. This study aimed at evaluating the cholinesterase inhibitory property as well as isolates the bioactive compounds from the plant. The acetylcholinesterase and butyrylcholinesterase inhibitory potentials of extracts, fractions, and isolated compounds were evaluated by colorimetric and TLC bioautographic assay techniques. The extract inhibited both enzymes with activity increasing with purification, ethyl acetate fraction being most active fraction at 65.66 ± 1.06% and 49.38 ± 1.66% against acetylcholinesterase and butyrylcholinesterase, respectively while the supernatant had 77.44 ± 1.18 inhibition against acetylcholinesterase. Two new bioactive compounds, (2E, 18E)-3,7,11,15,18-pentamethylhenicosa-2,18-dien-1-ol (named eluptol) and [12-(4-hydroxy-3-methyl-oxo-cyclopenta-1,3-dien-1yl)-11-methyl-dodecyl](E)-3-(3,4-dimethylphenyl)prop-2-enoate (named omifoate A) were isolated from the plant with IC50 of 22.26 µg/ml (AChE), 34.61 µg/ml (BuChE) and 6.51 µg/ml (AChE), 9.07 µg/ml (BuChE) respectively. The results showed that the plant has cholinesterase inhibitory activity which might be responsible for its memory enhancing action, thus justifying its inclusion in traditional memory enhancing preparations

【 授权许可】

Unknown