来自紫背金盘的抗分枝杆菌麦角甾醇-5,8-内过氧化物。

Antimycobacterial ergosterol-5,8-endoperoxide from Ajuga remota.

作者信息

Cantrell C L, Rajab M S, Franzblau S G, Fronczek F R, Fischer N H

机构信息

Department of Chemistry, Louisiana State University, Baton Rouge, USA.

出版信息

Planta Med. 1999 Dec;65(8):732-4. doi: 10.1055/s-1999-14053.

DOI:10.1055/s-1999-14053

PMID:10630115

Abstract

In a bioassay-guided search for antimycobacterial natural products from higher plants, we have chemically investigated the methanol extract of aerial parts of Ajuga remota Benth. (Labiatae) for its active constituent(s). Bioactive chromatographic fractions of the crude extract provided the known triterpene ergosterol-5,8-endoperoxide plus the diterpenes clerodin, ajugarin-I, and ajugarin-II, which had been previously isolated from A. remota. This is the first report on the isolation of ergosterol-5,8-endoperoxide from this plant. The above compounds were tested in a radiorespirometric bioassay for activity against Mycobacterium tuberculosis. Ergosterol-5,8-endoperoxide showed a minimum inhibitory concentration (MIC) of 1 microgram/ml, while ergosterol-5,8-endoperoxide acetate, ergosterol, and ergosta-5,7,9(11),22-tetraen-3 beta-ol gave MICs of 8 micrograms/ml, > 128 micrograms/ml, and 128 micrograms/ml, respectively. Clerodin, ajugarin-I, and ajugarin-II were inactive with MICs of > 128 micrograms/ml.

摘要

在一项以生物测定法指导从高等植物中寻找抗分枝杆菌天然产物的研究中，我们对紫背金盘（唇形科）地上部分的甲醇提取物进行了化学研究，以确定其活性成分。粗提取物的生物活性色谱馏分得到了已知的三萜类化合物麦角甾醇-5,8-内过氧化物以及二萜类化合物克罗狄醇、紫背金盘素-I和紫背金盘素-II，这些化合物先前已从紫背金盘中分离得到。这是首次关于从该植物中分离出麦角甾醇-5,8-内过氧化物的报道。上述化合物在放射性呼吸测定生物测定法中测试了对结核分枝杆菌的活性。麦角甾醇-5,8-内过氧化物的最低抑菌浓度（MIC）为1微克/毫升，而麦角甾醇-5,8-内过氧化物乙酸酯、麦角甾醇和麦角甾-5,7,9(11),22-四烯-3β-醇的MIC分别为8微克/毫升、>128微克/毫升和128微克/毫升。克罗狄醇、紫背金盘素-I和紫背金盘素-II无活性，MIC>128微克/毫升。