Cytotoxic Activity of Labdane Type Diterpenes Against Human Leukemic Cell Linesin vitro

Abstract

Nine labdane type diterpenes isolated from the plant Cistus creticus subsp. creticus and from the resin "Ladano" which is excreted on the surface of the leaves and stems of this plant, were examined for their in vitro cytotoxic activity against 14 human leukemic cell lines. Compound 1, (13E)-labd-13-ene-8 alpha,15-diol, exhibited cytotoxic activity against 13 of the cell lines tested, while compound 2, (13E)-labd-7,13-dienol, was active only against HL60 cells. Further compound 1 was examined for its effect on the uptake of [3H]-thymidine as a marker of DNA synthesis.

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

“…Labd-13(E)-ene-8α,15-diol (62) was cytotoxic to human T and pre-B cell lines . This compound had growth inhibitory and cytotoxic effects against numerous human and one mouse cancer cell lines, though this activity was weak in many cases (Chinou et al, 1994;Demetzos et al, 1994Demetzos et al, , 2001Dimas et al, 1998). It was found to reduce DNA synthesis (Dimas et al, 1998).…”

“…This compound had growth inhibitory and cytotoxic effects against numerous human and one mouse cancer cell lines, though this activity was weak in many cases (Chinou et al, 1994;Demetzos et al, 1994Demetzos et al, , 2001Dimas et al, 1998). It was found to reduce DNA synthesis (Dimas et al, 1998). 13-Epi-manoyl oxide-18-oic acid (63) inhibited larval growth of Pectinophora gossypiella (Elliger et al, 1976), whereas 62 stimulated oviposition by Heliothis virescens (tobacco budworm moth) (Jackson et al, 1991).…”

Derivatives of grindelic acid: From a non-active natural diterpene to synthetic antitumor derivatives

“…Organic layers were dried with MgSO 4 and resulting crude was purified by silica gel chromatography. 4 …”

“…138.5 µl of Ti(OPr-i) 4 (133.46 mg, 0.47 mmol) and 93.8 µl of (R,R)-(+)-DET (112.98 mg, 0.55 mmol) were added sequentially. The mixture was stirred at the same temperature for 20 min, and TBHP (0.14 ml, 5.5 M in isooctane, 0.78 mmol) was added slowly.…”

“…It is noteworthy that some semi synthetic compounds derived from a natural framework sometimes show higher bioactivity than the original natural product. Taking into account their broad range of biological activities, such as enzyme inducing, modulation of immune cell function, and cytotoxic against human tumor cell lines, [3][4][5][6] labdane diterpenes have attracted scientific interest.…”