马钱子叶中三萜类化合物和甾醇及其相关化合物的抗锥虫活性

Antitrypanosomal activity of triterpenoids and sterols from the leaves of Strychnos spinosa and related compounds.

作者信息

Hoet Sara, Pieters Luc, Muccioli Giulio G, Habib-Jiwan Jean-Louis, Opperdoes Fred R, Quetin-Leclercq Joëlle

机构信息

Laboratoire de Pharmacognosie, Unité d'Analyse Chimique et Physico-Chimique des Médicaments et Pharmacognosie, Université Catholique de Louvain, UCL 72.30-CHAM, Avenue E. Mounier 72, B-1200 Bruxelles, Belgium.

出版信息

J Nat Prod. 2007 Aug;70(8):1360-3. doi: 10.1021/np070038q. Epub 2007 Jul 19.

DOI:10.1021/np070038q

PMID:17637068

Abstract

Fractionation of an antitrypanosomal lipophilic leaf extract from Strychnos spinosa led to the isolation of eight triterpenoids and sterols in this plant part for the first time. Two of these were found to possess in vitro antitrypanosomal activity, namely, saringosterol (14) and 24-hydroperoxy-24-vinylcholesterol (15), with IC(50) values of 7.8 +/- 1.2 and 3.2 +/- 1.2 microM, respectively. The latter compound was isolated from a plant source for the first time. A comparative study on the antitrypanosomal activity of the isolated triterpenoids and sterols and some related compounds has indicated that the presence of an oxygenated function at C-28 or an oxygenated side chain at C-17 seems to be important for the antitrypanosomal activity of triterpenoids and sterols, respectively.

摘要

对马钱子（Strychnos spinosa）的抗锥虫亲脂性叶提取物进行分馏，首次从该植物部位分离出8种三萜类化合物和甾醇。其中两种被发现具有体外抗锥虫活性，即鲨甾醇（14）和24-氢过氧-24-乙烯基胆固醇（15），其IC50值分别为7.8±1.2和3.2±1.2微摩尔。后一种化合物是首次从植物来源中分离得到。对分离出的三萜类化合物、甾醇及一些相关化合物的抗锥虫活性进行的比较研究表明，C-28位的氧化官能团或C-17位的氧化侧链分别对三萜类化合物和甾醇的抗锥虫活性似乎很重要。