Patrick Still - Alkaloids from Microcos paniculata L. With Cytotoxic and Nicotinic Receptor Antagonistic Activities.

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      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)

      Abstract:

      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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