Antiparasitic Compounds from Cupania cinerea with Activities against Plasmodium falciparum and Trypanosoma bruceirhodesiense

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• 作者：M. Salome虂 Gachet ; Olaf Kunert ; Marcel Kaiser ; Reto Brun ; Martin Zehl ; Walter Keller ; Ricardo A. Mun虄oz ; Rudolf Bauer ; Wolfgang Schuehly
• 刊名：Journal of Natural Products
• 出版年：2011
• 出版时间：April 25, 2011
• 年：2011
• 卷：74
• 期：4
• 页码：559-566
• 全文大小：847K
• 年卷期：v.74,no.4(April 25, 2011)
• ISSN：1520-6025

文摘

In a survey of plants from Ecuador with antiprotozoal activity, Cupania cinerea was found to show significant in vitro activity against the Plasmodium falciparum K1 strain and Trypanosoma brucei rhodesiense. Subsequently, activity-guided isolation of the n-hexane and dichloromethane extracts from the bark of C. cinerea afforded two diterpene glycosides (1 and 2), named cupacinoside and 6鈥?de-O-acetylcupacinoside, and a lactonized triterpene bearing an oxepin moiety named cupacinoxepin (3), together with the known compounds scopoletin (4), caryophyllene oxide (5), two bisabolane sesquiterpenes (6 and 7), lichexanthone (8), gustastatin (9), lupenone (10), betulone (11), 17尾,21尾-epoxyhopan-3-one (12), taraxerol (13), and taraxerone (14). For compound 3, X-ray crystallography was employed to elucidate the relative configuration. For cupacinosides (1) and (2) and cupacinoxepin (3), in vitro activities against the P. falciparum K1 strain (IC₅₀1, 1.3; 2, 1.8; and 3, 8.7 渭M) and T. b. rhodesiense (IC₅₀1, 4.5; 2, 15.8; and 3, 71.6 渭M) were found. Cytotoxicity toward L-6 cells is discussed for all the compounds isolated.