|
KMID : 0043320090320101399
|
|
Archives of Pharmacal Research
2009 Volume.32 No. 10 p.1399 ~ p.1408
|
|
|
Cholinesterase and BACE1 Inhibitory Diterpenoids from Aralia cordata
|
|
Choi Jae-Sue
Jung Hyun-Ah
Lee Eun-Ju
Kim Ju-Sun
Kang Sam-Sik
Lee Je-Hyun
Min Byung-Sun
|
|
|
Abstract
|
|
|
|
Fourteen diterpenes were isolated from the n-hexane fraction of the roots of Aralia cordata(syn. = A. continentalis). Through spectroscopy, the chemical structures were determined as:ent-pimara-8(14),15-diene-19-oic acid (1); ent-kaur-16-en-19-oic-acid (2); 18-nor-ent-pimara-8(14),15-diene-4β-ol (3); 18-nor-ent-kaur-16-ene-4β-ol (4); ent-pimara-8(14),15-diene-19-ol (5); 7α-hydroxy-ent-pimara-8(14),15-diene-19-oic acid (6); 7β-hydroxy-ent-pimara-8(14),15-diene-19-oic acid (7); ent-pimar-15-en-8α,19-diol (8); 7-oxo-ent-pimara-8(14),15-diene-19-oic acid (9);16α-hydroxy-17-isovaleroyloxy-ent-kauran-19-oic acid (10); 17-hydroxy-ent-kaur-15-en-19-oic acid (11); 15α,16α-epoxy-17-hydroxy-ent-kauran-19-oic acid (12); 16α,17-dihydroxy-ent-kauran-19-oic acid (13); and 16α-methoxy-17-hydroxy-ent-kauran-19-oic acid (14). Compounds 4, 5, 8, 12, and 14 were first isolated from this plant. The anti-Alzheimer and antioxidant effects of ent-pimarane-type diterpenes 1, 3, 5, 8, and 9, as well as ent-kaurane-type diterpenes 2, 4, and 10~13, were evaluated via β-site amyloid precursor protein cleaving enzyme 1 (BACE1), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), peroxynitrite (ONOO?), and nitric oxide (NO· ) assays. Of the compounds tested, 8 exerted the most effective BChE inhibition with an IC50 value of 7.58 μM, followed by 3, 13, 11, 2, and 10. Compounds 9~11 exhibited good BACE1 inhibitory activities with IC50 values of 18.58~24.10 μM. However, 11 showed marginal AChE inhibitory effect, and all compounds tested showed no scavenging activities on ONOO? and NO· at a concentration of 100 μM.
|
|
|
KEYWORD
|
|
|
Aralia cordata, Diterpenes, BACE1, AChE, BChE, Araliaceae
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|
|