Isolation and structure of pedilstatin from a republic of maldives Pedilanthus sp.
A new cancer cell growth inhibitor designated pedilstatin (1) was isolated from a Republic of Maldives Pedilanthus sp. The structure was determined to be 13-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 ED(50) of 0.28 microg/mL, to afford, at concentrations of 2-5 microM, 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 K(i) of 620 +/- 20 nM.
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D000998:Antiviral Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D019665:Euphorbiaceae / Q000737:chemistry*; D015497:HIV-1 / Q000378:metabolism; D006801:Humans; D007195:Indian Ocean Islands; D007941:Leukemia P388; D008214:Lymphocytes / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D010704:Phorbols / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D010704:Phorbols; C470237:pedilstatin; D011493:Protein Kinase C