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Metabolomic approach for a rapid identification of natural products with cytotoxic activity against human colorectal cancer cells.

ABSTRACT: The discovery of bioactive compounds from natural sources entails an extremely lengthy process due to the timescale and complexity of traditional methodologies. In our study, we used a rapid NMR based metabolomic approach as tool to identify secondary metabolites with anti-proliferative activity against a panel of human colorectal cancer cell lines with different mutation profiles. For this purpose, fourteen Fabaceae species of Mediterranean vegetation were investigated using a double screening method: 1H NMR profiling enabled the identification of the main compounds present in the mixtures, whilst parallel biological assays allowed the selection of two plant extracts based on their strong anti-proliferative properties. Using high-resolution 2D NMR spectroscopy, putative active constituents were identified in the mixture and isolated by performing a bio-guided fractionation of the selected plant extracts. As a result, we found two active principles: a cycloartane glycoside and protodioscin derivative. Interestingly, these metabolites displayed a preferential anti-proliferative effect on colon cancer cell lines with an intrinsic resistance to anti-EGFR therapies. Our work provides an NMR-based metabolomic approach as a powerful and efficient tool to discover natural products with anticancer activities circumventing time-consuming procedures.

SUBMITTER: Graziani V

PROVIDER: S-EPMC5871890 | biostudies-other | 2018 Mar

REPOSITORIES: biostudies-other

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Metabolomic approach for a rapid identification of natural products with cytotoxic activity against human colorectal cancer cells.

Graziani Vittoria V Scognamiglio Monica M Belli Valentina V Esposito Assunta A D'Abrosca Brigida B Chambery Angela A Russo Rosita R Panella Marta M Russo Aniello A Ciardiello Fortunato F Troiani Teresa T Potenza Nicoletta N Fiorentino Antonio A

Scientific reports 20180328 1

The discovery of bioactive compounds from natural sources entails an extremely lengthy process due to the timescale and complexity of traditional methodologies. In our study, we used a rapid NMR based metabolomic approach as tool to identify secondary metabolites with anti-proliferative activity against a panel of human colorectal cancer cell lines with different mutation profiles. For this purpose, fourteen Fabaceae species of Mediterranean vegetation were investigated using a double screening ...[more]

PMID: 29593231

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Metabolomic approach for a rapid identification of natural products with cytotoxic activity against human colorectal cancer cells.

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Metabolomic approach for a rapid identification of natural products with cytotoxic activity against human colorectal cancer cells.

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