The Effect of 17 Sesquiterpenes on Cell Viability and Telomerase Activity in the Human Ovarian Cancer Cell Line HO-8910

Abstract

Using the MTT assay and the telomeric repeat amplification protocol (TRAP)-based PCR-ELISA assay, the cytotoxicity and telomerase inhibiting ability of 17 sesquiterpenes (extracted from Chinese herbs) were tested in the human ovarian cancer cell line HO-8910. The results indicated that seven sesquiterpenes inhibited cell proliferation without having an effect on telomerase activity; two sesquiterpenes inhibited neither cell proliferation nor telomerase activity; and the other eight sesquiterpenes inhibited both cell proliferation and telomerase activity to a certain extent. Without exception, none of these 17 sesquiterpenes could only inhibit telomerase activity without inhibiting cell proliferation. This indicated that the telomerase inhibiting activity is not a universal mechanism for all anticancer drugs but is only one of several possible mechanisms. The structure-activity relationships of 5 groups of sesquiterpenes are also discussed. This study may help to develop anticancer drugs.

DNA Topoisomerase Inhibitory Activity of Constituents from the Flowers of <i>Inula japonica</i>

“…Two new (1, 2) and twelve known compounds (3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) were isolated by various chromatographic separations from the EtOAc extract of the flowers of I. japonica (Fig. 1) (Fig.…”

“…Therefore, S configuration on C-2 of 2 was suggested and all relevant chiral centers in 2 were assigned as 1S, 2S, 4S, 5S, 8S and 10R configurations. Structures of 3-14 were identified by comparison of 1 H-and C 13 -NMR, FAB-MS spectral data and optical rotation values with those previously reported to be budlein B (3), 23) 6β-hydroxytomentosin (4), 24) 6-deacetoxybritanin (5), 25) 4-epipulchellin (6), 26) britanin (7), 27) tomentosin (8), 28) (+)-dihydroquercetin (9), 29) (−)-syringaresinol (10), 30) quercetagetin 3,4′-dimethy ether (11), 31) luteolin (12), 32) britanin G (13) 33) and inuchinenolide C (14) 34) (see the Supplementary materials). These compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) were tested for inhibitory activities of DNA topoisomerases I and II (Fig.…”

“…1) Some terpenes [2][3][4][5][6][7] and flavonoids 8,9) have previously been isolated from this medicinal plant and have been reported to possess diverse biological activities, such as anti-diabetes, 10) antihypolipidemia, 11) hepatoprotective, 12) anti-inflammatory 7) and anti-tumor 1,2,13) effects. We have been isolating compounds that inhibited topoisomerases I and II from the source of medicinal plants.…”

Monoclonal antibodies against ROR1 induce apoptosis of chronic lymphocytic leukemia (CLL) cells

“…26 Briefly, 1 Â 10 5 CLL cells were incubated in 0.5 ml of RPMI-1640 (without phenol red) (Invitrogen) containing 10% fetal bovine serum in triplicates. Anti-ROR1 MAbs as well as isotype controls were added from 1 --20 mg/ml.…”

Sesquiterpenoids from the Aerial Parts of Inula japonica

“…Fourteen sesquiterpenoids with an eudesmane C-atom skeleton, including four new ones, (1b,5a,7b,8b,11b)-5-hydroperoxy-1-hydroxyeudesm-4(15)-eno-12,8-lactone (1), (1b,5a,7b,8b)-8-(acetyloxy)-5-hydroperoxy-1-hydroxycostic acid methyl ester (12), and a mixture of (1b,3b,4b,7b,8b)-1,3-dihydroxyeudesma-5,11(13)-dieno-12,8-lactone (7) and (1b,3b,4b,7b,8b,11b)-1,3-dihydroxyeudesm-5-eno-12,8-lactone (8), were isolated from the aerial parts of Inula japonica (Asteraceae). Their structures were determined by extensive spectroscopic methods, and those of 7 and 12 confirmed by means of single-crystal X-ray diffraction analysis.…”