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Bioactive indole alkaloids isolated from Alstonia angustifolia.


ABSTRACT: Bioassay-guided fractionation was conducted on a CHCl3-soluble extract of the stem bark of Alstonia angustifolia (Apocynaceae) collected in Vietnam using the HT-29 human colon cancer cell line, and led to the isolation of a new sarpagine-type indole alkaloid (1), together with nine known alkaloids, including four macroline-derived alkaloids (2-5), a sarpagine-type alkaloid (6), and four macroline-pleiocarpamine bisindole alkaloids (7-10). The structure of the new compound (1) was determined on the basis of spectroscopic data interpretation. Compounds 1-10 were evaluated in vitro for their NF-?B (p65) inhibitory activity against the Hela cells in an ELISA assay. The new sarpagine alkaloid, N(4)-methyltalpinine (1), was found to show significant NF-?B inhibitory activity (ED50 = 1.2 µM). Furthermore, all the isolates (1-10) were evaluated in vitro for their antileishmanial activity, and compounds (1-4, 6 and 8-10) exhibited leishmaniacidal activity against promastigotes of Leishmania mexicana.

SUBMITTER: Pan L 

PROVIDER: S-EPMC4287998 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature

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Bioassay-guided fractionation was conducted on a CHCl<sub>3</sub>-soluble extract of the stem bark of <i>Alstonia angustifolia</i> (Apocynaceae) collected in Vietnam using the HT-29 human colon cancer cell line, and led to the isolation of a new sarpagine-type indole alkaloid (<b>1</b>), together with nine known alkaloids, including four macroline-derived alkaloids (<b>2-5</b>), a sarpagine-type alkaloid (<b>6</b>), and four macroline-pleiocarpamine bisindole alkaloids (<b>7-10</b>). The structu  ...[more]

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