Publication Details (including relevant citation information):
Patrick C. Still, Bitna Yi, Ryan Pavlovicz, Tatiana F. González-Cestari, Li Pan, Hee-Byung Chai, Tran Hgoc Ninh, Djaja D. Soejarto, Chenglong Li, James R. Fuchs, Dennis McKay, and A. Douglas Kinghorn (2012). Alkaloids from Microcos paniculata L. With Cytotoxic and Nicotinic Receptor Antagonistic Activities. Journal of Natural Products (submitted for publication and assigned to reviewers)
Microcos paniculata is a large shrub or small tree that grows in several countries in South and Southeast Asia. In the present study, three new piperidine alkaloids, microgrewiapines A-C (1-3), as well as three known compounds, inclusive of microcosamine A (4), 7′-(3′,4′-dihydroxyphenyl)-N-[4-methoxyphenyl)ethyl]propenamide (5), and liriodenine (6), were isolated from cytotoxic fractions of the separate chloroform-soluble extracts of the stem bark, roots, and leaves of M. paniculata. Compounds 1-6 and 1a showed a range of cytotoxicity values against the HT-29 human colon cancer cell line. When evaluated for their effects on human α3β4 or α4β2 nicotinic acetylcholine receptors (nAChRs), several of these compounds were shown to be active as nAChR antagonists. As a result of this study, microgrewiapine A (1) was found to be a selective cytotoxic agent for colon cancer cells over normal colon cells, and to exhibit nicotinic receptor antagonistic activity for both the hα3β4 and hα4β2 receptor subtypes.
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