Pettit, G.R.; Ducki, S.; Tan, R.; Gardella, R.S.; McMahon, J.B.; Boyd, M.R.; Pettit, G.R.III; Blumberg, P.M.; Lewin, N.E.; Doubek, D.L.; Tackett, L.P.; Williams, M.D. J. Nat.Prod. 65: 1262-1265, 2002.
Abstract:
A new cancer cell growth inhibitor designated pedilstatin (1) was isolated from a Republic of Maldives Pedilanthus sp. The structure was determined to be 3-O-acetyl-12-O- [2'Z,4'E-octadienoyl]-4alpha- deoxyphorbol on the basis of high-resolution mass spectral and 2D NMR assignments. Pedilstatin was found to significantly inhibit growth of the P388 lymphocytic leukemia cell line with an ED50 of 0.28 µg/mL, to afford, at concentrations of 2-5 µM, protection (to 80%) of human-derived lymphoblastoid CEM-SS cells from infection and cell-killing by HIV-1, and to show inhibition of protein kinase C with a Ki of 620 ± 20 nM.
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