Abstract:
En
|
Text:
En
|
PDF:
En
Stemodin (1) is a diterpene produced by Stemodia maritima L. (Scrophulariaceae) and shows antiviral and tumor cell proliferation inhibitory activities. Chemical modifications of 1 were performed to produce the known stemodinone (2), two new stemodinone oximes, Z (3) and E (4), and seven new oxime esters derivatives (5, 6, 7, 8, 9, 10, and 11). All derivatives were evaluated for their cytotoxic activity in HL60 (promyelocytic leukemia), SNB-19 (astrocytoma), HCT-116 (colon carcinoma), and PC3 (prostate) human cancer cell lines, and L929 (healthy murine cells). Oximes 3 and 4 showed lower cytotoxic values than 1 against all cancer cell lines tested. However, esters 9 and 10 exhibited cell growth inhibition percentages higher than 1 against PC3, SNB-19, and HCT-116 cancer cell lines, ranging from 62.96 to 94.27%. Many of these values exceed that presented by doxorubicin (66.05-86.87%). All compounds showed no cytotoxic effect on healthy cells at the tested concentration of 25 µg mL-1. (1 L Scrophulariaceae (Scrophulariaceae activities 2, 2 , (2) oximes (3 4, (4) 5, 5 (5 6 7 8 11. 11 . 11) HL HL6 promyelocytic leukemia, leukemia leukemia) SNB19 SNB 19 SNB-1 astrocytoma, astrocytoma (astrocytoma) HCT116 HCT 116 HCT-11 colon carcinoma, carcinoma carcinoma) PC prostate (prostate L92 cells. cells) However SNB19, 19, 6296 62 96 62.9 9427 94 27 94.27% 66.0586.87%. 66058687 66.05 86.87% 66 05 86 87 (66.05-86.87%) mL1. mL1 mL 1. mL-1 ( (2 (4 SNB1 SNB- (astrocytoma HCT11 HCT-1 L9 629 62. 942 94.27 0586 66.0586.87% 6605868 6605 66.0 8687 86.87 0 (66.05-86.87% mL- HCT1 HCT- 94.2 058 66.0586.87 660586 660 66. 868 86.8 (66.05-86.87 94. 66.0586.8 66058 86. (66.05-86.8 66.0586. (66.05-86. 66.0586 (66.05-86 66.058 (66.05-8 (66.05- (66.05 (66.0 (66. (66 (6