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KMID : 0043320090320091245
Archives of Pharmacal Research
2009 Volume.32 No. 9 p.1245 ~ p.1251
Acetylcholinesterase Inhibitive Activity-Guided Isolation of Two New Alkaloids from Seeds of Peganum Nigellastrum Bunge by an In Vitro TLC- Bioautographic Assay
Wang Chang-Hong

Zheng Xi-yuan
Zhang Zi-jia
Chou Gui-xin
Wu Tao
Cheng Xue-mei
Wang Zheng-tao
Abstract
Acetylcholinesterase inhibitors (AChEIs) currently form the basis of the newest drugs available for the treatment of Alzheimer¡¯s disease. For the aim of screening effective AChEIs, the methanol extracts of the seeds of genus Peganum were found to show significant inhibitory activity of acetylcholinesterase enzyme (AChE) using an in vitro TLC-bioautographic assay. In further studies to seed of P. nigellastrum Bunge, activity-guided fractionation led to the isolation of two new alkaloids nigellastrine I (9) and nigellastrine II (10), and along with eight known alkaloids, vasicinone (1), vasicine (2), harmine (3), deoxyvasicinone (4), deoxyvasicine (5), harmaline (6), harmol (7), harman (8), in which harmol and harman were first isolated from species P. nigellastrum Bunge. As active constituents, all compounds showed good inhibitory activities against AChE. The results of in vitro semi-quality TLC-bioautographic assay showed that harmine, harmaline and harmol displayed a similar AChE inhibitive activities comparing to galanthamine. These results indicated that these alkaloids in P. nigellastrum Bunge could be a potent class of AChEIs.
KEYWORD
Peganum nigellastrum Bunge, Acetylcholinesterase, TLC-bioautographic assay, Alzheimer¡¯s disease, Alkaloid, Nigellastrine I, Nigellastrine II
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