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Flavonoids from eight tropical plant species that inhibit the multidrug resistance transporter ABCG2.

ABSTRACT: Overexpression of ABCG2, a membrane-bound multi-drug transporter, can make tumor cells resistant to treatment with conventional chemotherapeutic agents. A high-throughput screening effort with the NCI repository of natural product extracts revealed that eight tropical plant extracts significantly inhibited the function of ABCG2. This activity was tracked throughout the extract fractionation process to a series of ABCG2 inhibitory flavonoids (1-13). Their structures were identified by a combination of NMR, mass spectrometry, and circular dichroism studies, and this resulted in the elucidation of (2S)-5,7,3'-trihydroxy-4'-methoxy-8-(3''-methylbut-2''-enyl)-flavonone (1), (2S)-5,7,3',5'-tetrahydroxy-8-[3'',8''-dimethylocta-2''(E),7''-dienyl]flavonone (3), and 5,7,3'-trihydroxy-3,5'-dimethoxy-2'-(3'-methylbut-2-enyl)flavone (12) as new compounds.

SUBMITTER: Versiani MA

PROVIDER: S-EPMC3805045 | biostudies-literature | 2011 Feb

REPOSITORIES: biostudies-literature

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Flavonoids from eight tropical plant species that inhibit the multidrug resistance transporter ABCG2.

Versiani Muhammad Ali MA Diyabalanage Thushara T Ratnayake Ranjala R Henrich Curtis J CJ Bates Susan E SE McMahon James B JB Gustafson Kirk R KR

Journal of natural products 20110128 2

Overexpression of ABCG2, a membrane-bound multi-drug transporter, can make tumor cells resistant to treatment with conventional chemotherapeutic agents. A high-throughput screening effort with the NCI repository of natural product extracts revealed that eight tropical plant extracts significantly inhibited the function of ABCG2. This activity was tracked throughout the extract fractionation process to a series of ABCG2 inhibitory flavonoids (1-13). Their structures were identified by a combinati ...[more]

PMID: 21275386

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