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源自尼泊尔的革叶野扇花叶片中的新型胆碱酯酶抑制甾体生物碱。

New cholinesterase inhibiting steroidal alkaloids from the leaves of Sarcococca coriacea of Nepalese origin.

作者信息

Kalauni Surya K, Choudhary Muhammad Iqbal, Khalid Asaad, Manandhar Mangala Devi, Shaheen Farzana, Gewali Mohan Bikram

机构信息

Central Department of Chemistry, Tribhuvan University, Nepal.

出版信息

Chem Pharm Bull (Tokyo). 2002 Nov;50(11):1423-6. doi: 10.1248/cpb.50.1423.

DOI:10.1248/cpb.50.1423
PMID:12419902
Abstract

From the leaves of Sarcococca coriacea two new steroidal alkaloids, epoxynepapakistamine-A [(20S)-20-(N-methylamino)-3beta-(tigloylamino)-5alpha-pregna-16alpha,17alpha-epoxy-2beta,4beta-di-O-acetate] (1), and epoxysarcovagenine-D [(20S)-20-(N-methylamino)-3beta-(tigloylamino)-5alpha-pregna-2-en-16alpha,17alpha-epoxy-4-one] (2), and two known compounds funtumafrine C [(20S)-20-(N,N-dimethylamino)-5alpha-pregna-3-one] (3) and N-methylfuntumine (4) were isolated. Their structures were elucidated on the basis of their spectral properties. The compounds 1, 3 and 4 were found to have cholinesterase inhibitory activity when tested for the inhibition of electric eel acetylcholinesterase and horse serum butyrylcholinesterase. They inhibited both enzymes in a concentration dependent fashion.

摘要

从厚叶清香桂的叶子中分离出两种新的甾体生物碱,环氧新帕基胺 -A [(20S)-20-(N-甲基氨基)-3β-(惕各酰氨基)-5α-娠烷 -16α,17α-环氧 -2β,4β-二 -O-乙酸酯](1)和环氧肉珊瑚宁-D [(20S)-20-(N-甲基氨基)-3β-(惕各酰氨基)-5α-娠烷 -2-烯 -16α,17α-环氧 -4-酮](2),以及两种已知化合物丰土马弗林C [(20S)-20-(N,N-二甲基氨基)-5α-娠烷 -3-酮](3)和N-甲基丰土明(4)。根据它们的光谱性质阐明了它们的结构。当测试对电鳗乙酰胆碱酯酶和马血清丁酰胆碱酯酶的抑制作用时,发现化合物1、3和4具有胆碱酯酶抑制活性。它们以浓度依赖性方式抑制这两种酶。

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