Cholinesterase-inhibiting withanolides from Ajuga bracteosa

Cholinesterase-inhibiting withanolides from Ajuga bracteosa
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DOI:
10.1002/cbdv.200490091
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发表时间:
2004-01-01
影响因子:
2.9
通讯作者:
Choudhary, MI
Choudhary, MI
中科院分区:
化学3区
文献类型:
--
作者:
Riaz, N;Malik, A;Choudhary, MI

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三个新的睡茄内酯,bracteosin A(=(22 R)-5 β,6 β:22,26-二环氧基-4 β,28-二羟基-3 β-甲氧基麦角甾-24-烯-1,26-二酮; 1),bracteosin B(=(22 R)-5 β,6 β:22,26-二环氧基-4 β,28-二羟基-3 β-甲氧基-1,26-二氧麦角甾-24-烯-19-酸; 2),和bracteosin C(=(22 R)-22,26-环氧-4 β,6 β,27-三羟基-3 β-甲氧基麦角甾-24-烯-1,26-二酮; 3)。从大苞筋骨草的全株中分离得到一系列化合物。通过1D-和2D-NMR技术等波谱分析推测了它们的结构。此外,二氢clerodin-1,clerodinA,lupulinA,和二氢ajugapitin也首次从该物种中分离。化合物1-3对胆碱酯酶具有明显的抑制作用,且呈浓度依赖性。
Three new withanolides, bracteosin A (= (22R)-5beta,6beta: 22,26-diepoxy-4beta,28-dihydroxy-3beta-methoxyergost-24-ene-1,26-dione; 1), bracteosin B (= (22R)-5beta,6beta: 22,26-diepoxy-4beta,28-dihydroxy-3beta-methoxy-1,26-dioxoergost-24-en-19-oic acid; 2), and bracteosin C (= (22R)-22,26-epoxy-4beta,6beta,27-trihydroxy-3beta-methoxyergost- 24-ene-1,26-dione; 3). have been isolated from the whole plants of Ajuga bracteosa. Their structures were deduced by spectral analysis, including 1D- and 2D-NMR techniques. In addition, dihydroclerodin-1, clerodinin A, lupulin A, and dihydroajugapitin have also been isolated for the first time from this species. Compounds 1-3 exhibited evident inhibitory potential against cholinesterase enzymes in a concentration-dependent fashion.