Tobias Blank, Charlie Puth, Annikka Kurz, Moritz Benka, Malik Rakhmanov, Iwanette Du Preez-Bruwer, Davis Mumbengegwi, Dietmar A. Plattner, Bernd Kammerer, Roman Huber, Robin Teufel, Olivier Potterat, Volker M. Lüth
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引用次数: 0
Abstract
Root extracts of Cryptolepis decidua are used in the traditional medicine of South-West Africa to treat various conditions. Here, we report the potent cytotoxic activity of a methanol root extract against a human adenocarcinomic cell line, which prompted us to establish a comprehensive metabolite profile. Overall, six previously undescribed compounds were isolated from this extract by a combination of open-column chromatography, centrifugal partition chromatography and preparative HPLC. They include two sarmentogenin-type cardenolides (2 and 3), an androstane lactone (5), two dinormonoterpenoid diglucosides, dinosides A and B (9 and 10), and a quinic acid derivative (12). In addition, six previously reported constituents were identified (1, 4, 6−8, 11). The structures of the isolates were elucidated using HPLC-MS2/3, HRESIMS and NMR spectroscopy. Feature-based molecular networking was used to map a comprehensive metabolite profile. The cytotoxic activity of the methanol extract was evaluated by WST-1 cell-viability assays, apoptosis/necrosis tests, and cell-cycle analyses. Cardenolides 1−3 were identified as the primary cytotoxic agents, exhibiting IC50 values of 0.25 μM (1), 2.20 μM (2), and 0.28 μM (3) in A549 human lung epithelial cancer cells, and 0.41 μM (1), 2.31 μM (2), and 0.39 μM (3) against peripheral blood mononuclear cells.
期刊介绍:
The Journal of Natural Products invites and publishes papers that make substantial and scholarly contributions to the area of natural products research. Contributions may relate to the chemistry and/or biochemistry of naturally occurring compounds or the biology of living systems from which they are obtained.
Specifically, there may be articles that describe secondary metabolites of microorganisms, including antibiotics and mycotoxins; physiologically active compounds from terrestrial and marine plants and animals; biochemical studies, including biosynthesis and microbiological transformations; fermentation and plant tissue culture; the isolation, structure elucidation, and chemical synthesis of novel compounds from nature; and the pharmacology of compounds of natural origin.
When new compounds are reported, manuscripts describing their biological activity are much preferred.
Specifically, there may be articles that describe secondary metabolites of microorganisms, including antibiotics and mycotoxins; physiologically active compounds from terrestrial and marine plants and animals; biochemical studies, including biosynthesis and microbiological transformations; fermentation and plant tissue culture; the isolation, structure elucidation, and chemical synthesis of novel compounds from nature; and the pharmacology of compounds of natural origin.