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Cholinesterase and BACE1 Inhibitory Diterpenoids from Aralia cordata
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  • Cholinesterase and BACE1 Inhibitory Diterpenoids from Aralia cordata
  • Cholinesterase and BACE1 Inhibitory Diterpenoids from Aralia cordata
저자명
Jung. Hyun-Ah,Lee. Eun-Ju,Kim. Ju-Sun,Kang. Sam-Sik,Lee. Je-Hyun,Min. Byung-Sun,Choi. Jae-Sue
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2009년|32권 10호|pp.1399-1408 (10 pages)
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대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

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-$4{eta}$-ol (3); 18-nor-ent-kaur-16-ene-$4{eta}$-ol (4); ent-pimara-8(14),15-diene-19-ol (5); $7{alpha}$-hydroxy-ent-pimara-8(14),15-diene-19-oic acid (6); $7{eta}$-hydroxy-ent-pimara-8(14),15-diene-19-oic acid (7); ent-pimar-15-en-$8{alpha}$,19-diol (8); 7-oxo-ent-pimara-8(14),15-diene-19-oic acid (9); $16{alpha}$-hydroxy-17-isovaleroyloxy-ent-kauran-19-oic acid (10); 17-hydroxy-ent-kaur-15-en-19-oic acid (11); $15{alpha}$,$16{alpha}$-epoxy-17-hydroxy-ent-kauran-19-oic acid (12); $16{alpha}$,17-dihydroxy-ent-kauran-19-oic acid (13); and $16{alpha}$-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 $eta$-site amyloid precursor protein cleaving enzyme 1 (BACE1), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), peroxynitrite ($ONOO^-$), and nitric oxide ($NO{cdot}$) assays. Of the compounds tested, 8 exerted the most effective BChE inhibition with an $IC_{50}$ value of $7.58;{mu}M$, followed by 3, 13, 11, 2, and 10. Compounds 9~11 exhibited good BACE1 inhibitory activities with $IC_{50}$ values of $18.58{sim}24.10;{mu}M$. However, 11 showed marginal AChE inhibitory effect, and all compounds tested showed no scavenging activities on $ONOO^-$ and $NO{cdot}$ at a concentration of $100;{mu}M$.