Antitrypanosomal isoflavan quinones from Abrus precatorius
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- 作者：Yoshie Hata ; Samad Nejad Ebrahimi ; Maria De Mieri ; Stefanie Zimmermann ; Tsholofelo Mokoka ; Dashnie Naidoo ; Gerda Fouche ; Vinesh Maharaj ; Marcel Kaiser ; Reto Brun ; Olivier Potterat ; Matthias Hamburger
- 关键词：Trypanosoma brucei rhodesiense ; Isoflavan quinone ; Abrus precatorius ; Fabaceae ; ECD
- 刊名：Fitoterapia
- 出版年：March, 2014
- 年：2014
- 卷：93
- 期：Complete
- 页码：81-87
- 全文大小：543 K
文摘
Human African trypanosomiasis is a neglected tropical disease in sub Saharan Africa that is fatal if left untreated. In a search for new natural products with antitrypanosomal activity, we recently identified abruquinones B and I from Abrus precatorius as potent in vitro trypanocidal compounds with high selectivity indices. To obtain sufficient compound for in vivo efficacy tests in mice, a second batch of plant material was re-collected and extracted. However, the chemical profiles of the two batches differed, and additional abruquinones were isolated and identified by HR-ESI-MS, and 1D and 2D NMR (1H, 13C, COSY, HMBC, HSQC, and NOESY) spectroscopy. Abruquinones J (1), K (2), and L (3) were new, while abruquinones A (4) and D (5) were known from the first batch of plant material. The absolute configuration of compounds 1 to 3 was determined by comparison of electronic circular dichroism (ECD) spectra with calculated ECD data. Compounds 2 to 5 showed high in vitro activity against T. b. rhodesiense (IC50 of 0.01, 0.02, 0.02 and 0.01 渭M, respectively), and remarkable SIs of 508, 374, 1379, and 668, respectively.