鼠尾草新的羽扇烯三萜三醇及其抗胆碱酯酶活性。

A new lupene triterpenetriol and anticholinesterase activity of Salvia sclareoides.

作者信息

Rauter Amélia P, Branco Isabel, Lopes Rui G, Justino Jorge, Silva Filipa V M, Noronha João P, Cabrita Eurico J, Brouard Ignacio, Bermejo Jaime

机构信息

Centro de Química e Bioquímica, Departamento de Química e Bioquímica, Faculdade de Ciências da Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.

出版信息

Fitoterapia. 2007 Dec;78(7-8):474-81. doi: 10.1016/j.fitote.2007.02.013. Epub 2007 May 10.

DOI:10.1016/j.fitote.2007.02.013

PMID:17570616

Abstract

A new lupene triterpenetriol was isolated from the acetone extract of the aerial parts of Salvia sclareoides and characterised as (1beta,3beta)-lup-20(29)-ene-1,3,30-triol (1). In addition, nepetidin (2), nepeticin (3), lupendiol (4), (1beta,11alpha)-dihydroxy-lup-20(29)-en-3-one (5), ursolic acid (6), sumaresinolic acid (7) and hederagenin (8), were identified in this Salvia sp. To the best of our knowledge, the compounds 2 and 7 are new constituents in Salvia spp. The acetone, ethanol, butanol and water extracts of the plant were screened for the in vitro inhibitory activity of acetylcholinesterase (AChE) and butyrilcholinesterase (BChE), enzymes which play a role in the Alzheimer disease. All extracts inhibited acetylcholinesterase activity at 10 microg/ml, a remarkable activity since the standard drug rivastigmine does not inhibit acetylcholinesterase at the same concentration. Regarding the butyrilcholinesterase, the acetone extract at 1000 microg/ml was able to inhibit completely the enzyme activity and the butanol and ethanol extracts, at this concentration, produced a potent inhibition of BchE.

摘要

从南欧丹参地上部分的丙酮提取物中分离出一种新的羽扇烯三萜三醇，并将其鉴定为(1β,3β)-羽扇-20(29)-烯-1,3,30-三醇(1)。此外，在该丹参属植物中还鉴定出了尼泊尔啶(2)、尼泊尔宁(3)、羽扇豆醇(4)、(1β,11α)-二羟基-羽扇-20(29)-烯-3-酮(5)、熊果酸(6)、苏门树脂酸(7)和常春藤皂苷元(8)。据我们所知，化合物2和7是丹参属植物中的新成分。对该植物的丙酮、乙醇、丁醇和水提取物进行了乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)体外抑制活性的筛选，这两种酶在阿尔茨海默病中起作用。所有提取物在10μg/ml时均能抑制乙酰胆碱酯酶活性，这是一种显著的活性，因为标准药物卡巴拉汀在相同浓度下并不抑制乙酰胆碱酯酶。对于丁酰胆碱酯酶，1000μg/ml的丙酮提取物能够完全抑制酶活性，而在此浓度下，丁醇和乙醇提取物对丁酰胆碱酯酶产生了强效抑制作用。