Complexes of lanthanides(iii ) with mixed 2,2′-bipyridyl and 5,7-dibromo-8-quinolinoline chelating ligands as a new class of promising anti-cancer agents
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Abstract Five novel lanthanides(iii) complexes, [Lu(Me)(MBrQ)2NO3] (MeMBrQ-Lu), [Ho(MeO)(MBrQ)2NO3] (MeOMBrQ-Ho), [Ho(Me)(MBrQ)2NO3] (MeMBrQ-Ho), [La(Me)2(BrQ)2NO3] (MeBrQ-La) and [Sm(Me)(BrQ)2(CH3OH)NO3] (MeBrQ-Sm), have been synthesized, in which 2,2′-bipyridyl (4,4′-dimethyl-2,2′-bipyridyl (Me) and 4,4′-dimethoxy-2,2′-bipyridine (MeO)) and 5,7-dibromo-8-quinolinoline derivatives (5,7-dibromo-2-methyl-8-quinolinol (MBrQ-H) and 5,7-dibromo-8-quinolinol (BrQ-H)) act as the chelating ligands. The in vitro cytotoxic activities of the five Ln(iii) complexes have been studied with the SK-OV-3/DDP, NCI-H460 and HeLa cancer cells. MeMBrQ-Lu, MeOMBrQ-Ho, MeMBrQ-Ho, MeBrQ-La and MeBrQ-Sm show higher cytotoxicity against the HeLa cells (IC50 values of 1.00 nM–3.45 μM) than cisplatin (13.11 ± 0.53 μM). In particular, the MeOMBrQ-Ho and MeMBrQ-Ho complexes exhibit superior cytotoxic activity, with IC50 values at 1.00 ± 0.34 nM and 125.00 ± 1.08 nM. We further demonstrate that MeOMBrQ-Ho and MeMBrQ-Ho inhibit the proliferation of HeLa cells by inhibiting telomerase and targeting mitochondria to induce DNA damage-mediated apoptosis. In addition, MeOMBrQ-Ho significantly inhibits tumor growth with a tumor growth inhibition rate (IR) of 50.8% in a HeLa mouse xenograft model. Taken together, MeOMBrQ-Ho is a novel lanthanide(iii) complex with promising antitumor activity.Keywords:
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Objective To evaluate the synergistic effect of rapamycin and cisplatin in cervical cancer cell line HeLa.Methods By using HeLa cells,cell proliferation was assessed by MTT assay after exposure to rapamycin,cisplatin,or both in combination.Apoptosis was analyzed by flow cytometry.Immunoblot analysis was performed to detect the expression of phosphorylated 4E-BP1 and S6 kinase 1.Results Rapamycin and cisplatin inhibited growth of HeLa cells in a time-dependent manner.Simultaneous exposure of cisplatin in combination with rapamycin resulted in a significantly synergistic antiproliferative effect.Rapamycin increased cisplatin-induced apoptosis in HeLa cells.Rapamycin inhibited the expression of phosphorylated 4E-BP1 and S6 kinase 1 in HeLa cells,and combined treatment with cisplatin inhibited the expression over that of rapamycin alone.Conclusion The results of the current study provide evidence of a synergistic relation between rapamycin and cisplatin in both inhibition of HeLa cells growth and induction of apoptosis.This suggests that rapamycin and cisplatin may be a rational combination of a targeted therapy for cervical cancer.
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Objective To investigate the apoptosis inducing effect of N-4-hydroxyphenyl retinode(4-HPR)and Cisplatin on human HeLa cell lines.Methods MTT assay was employed to examine the growth suppression of the cells.TEM was used to observe the ultrastructural change of HeLa cells treated with 4-HPR and Cisplatin.The apoptosis rate and change in cell cycle of HeLa cells treated with 4-HPR or/and Cisplatin were examined by flow cytometer.Results 4-HPR and Cisplatin both could induce apoptosis of HeLa cells;combined use of 4-HPR and Cisplatin could enhance HeLa cells apoptosis.Conclusion 4-HPR and Cisplatin could induce apoptosis of HeLa cells,and their effect is synergetic.
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Objective To estimate the anti-tumor activity of the extracts of four traditional Chinese medicines. Methods MTT assay was applied to screen the anti-tumor effect of the extracts of four traditional Chinese medicines on two tumor cell lines in vitro. Results Different extracts had variable inhibitory effect on different tumor cell lines. The extracts of Livistona chinensis R.Br. and Pyrola calliantha H.Andres had remarkable anti-tumor activity on Hela cell line, with IC50 95.51 and 95.40 mg·L-1, respectively. The extract of Duchenea indica(Andr.)Foche had some inhibitory effect on Hela cell line, with IC50 138.23 mg ·L-1. The extract of Livistona chinensis R.Br. had some inhibitory effect on Bel-7402 cell line, with IC50 122.84 mg·L-1 . Conclusions The extracts of Livistona chinensis R.Br. and Pyrola calliantha H.Andres had remarkable inhibitory effect on Hela cell line.
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Medicinal plants are potential sources of anticancer agents screening. A large number of phytochemicals, including triterpenoids, have been reported to have significant cytotoxic effects on cancer cells. From the fruits of Ligustrum japonicum Thunb., thirteen triterpenoids (1 – 13) were isolated and evaluated for their cytotoxic activity against Hela and HL-60 cells. As results, 8 (oleanolic acid) showed significant effects on Hela with IC50 values of 5.5 µM, and moderate effects on HL-60 cells with IC50 values of 55.9 µM. Meanwhile, 10 (oleanderic acid) and 11 (3β-acetoxy-urs-12-en-28-oic acid) exhibited moderate inhibitory effects on Hela with IC50 value of 55.0 and 68.8 µM, respectively. Moreover, 10 showed cytotoxic effect on HL-60 cell line with IC50 value of 63.9 µM. To our knowledge, this is the first report that oleanderic acid was isolated from L. japonicum and investigated in cytotoxic effects on Hela and HL-60 cells.
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The combined effect of electrical stimulation and cisplatin administration on HeLa cells was investigated. The combination of electric potentials (-0.5 V to 0.5 V) with 10-Hz frequency and 1000 ng/mL cisplatin decreased cancer cell viability by 32% and was more effective than either treatment given alone. Combined treatment with cisplatin and electrical stimulation also increased the number of apoptotic cells. It is shown that the efficacy of cisplatin was enhanced in electrically stimulated HeLa cells, and the addition of electrical stimulation amplified the chemotherapeutic effect of cisplatin in cervical cancer cells.
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Objective To observe the effects of different dose of TRAIL and cisplatin on Hela cells.Methods Different concentration of TRAIL,TRAIL 100 ng/mL and cisplatin 10 μmol/L,combined TRAIL 100 ng/mL and cisplatin 10 μmol/L was treated on Hela cells for 24 hours respectively,the death rate of Hela cells was measured by ELISA.Results After being treated with different concentration TRAIL,Hela cells had death rates 10.91%,16.84%,22.79%,28.62%,34.85%;but after being treated with TRAIL,cisplatin,combined TRAIL and cisplatin,the Hela cells had death rates 28.07%,46.13%,75.51%.Conclusion TRAIL had obvious dose-effect on Hela cells and could increase the sensitivity of cells to drugs when combined with cisplatin.
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