Isolation and Structure of Pedilstatin from a Republic of Maldives Pedilanthus sp
Autor: | George R. Pettit, Sylvie Ducki, Rui Tan, Roberta S. Gardella, James B. McMahon, Michael R. Boyd, Peter M. Blumberg, Nancy E. Lewin, Dennis L. Doubek, Larry P. Tackett, Michael D. Williams |
---|---|
Rok vydání: | 2002 |
Předmět: |
Cell Survival
Stereochemistry Pharmaceutical Science Biology Pharmacognosy Antiviral Agents Analytical Chemistry Mice Structure-Activity Relationship Indian Ocean Islands Drug Discovery Tumor Cells Cultured Animals Humans Lymphocytes Enzyme Inhibitors Protein Kinase C Protein kinase C Pharmacology chemistry.chemical_classification Plants Medicinal Molecular Structure Leukemia P388 Lymphoblast Organic Chemistry Euphorbiaceae Biological activity Antineoplastic Agents Phytogenic Phorbols Terpenoid Enzyme Complementary and alternative medicine chemistry Cell culture Cancer cell HIV-1 Molecular Medicine |
Zdroj: | Journal of Natural Products. 65:1262-1265 |
ISSN: | 1520-6025 0163-3864 |
DOI: | 10.1021/np020115b |
Popis: | 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. |
Databáze: | OpenAIRE |
Externí odkaz: |