Antiproliferative activity of the diterpenes jatrophone and jatropholone and their derivatives.
The antiproliferative activity of the diterpenes jatropholone A and B, 16 semi-synthetic derivatives thereof, and that of jatrophone and its three derivatives was assessed on human cell cultures. The cells used comprised normal lung fibroblasts (MRC-5), gastric adenocarcinoma (AGS), leukemia (HL-60), lung cancer (SK-MES-1), and bladder carcinoma (J82). Jatropholone A ( 1) was inactive against all the tumor cell lines; however, its acetylation rendered a compound with antiproliferative activity. The epimeric jatropholone B ( 8) was active against all the cancer cell lines, and its derivatives presented different effects on the selected cell lines. While jatrophone ( 19) showed strong anticancer activity, its derivatives 9beta,13alpha-dihydroxyisabellione and 13alpha-hydroxy-9 beta-acetoxyisabellione were less active.
Theoduloz
Cristina
C
Departamento de Ciencias Básicas Biomédicas, Facultad de Ciencias de la Salud, Universidad de Talca, Casilla 747, Talca, Chile.
Rodríguez
Jaime A
JA
Pertino
Mariano
M
Schmeda-Hirschmann
Guillermo
G
D000107:Acetylation; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004224:Diterpenes / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology / Q000627:therapeutic use*
D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes; D010936:Plant Extracts