The antioxidant action of tamoxifen and its metabolites Inhibition of lipid peroxidation

Wiseman, Helen; Laughton, Miranda J.; Arnstein, H. R. V.; Cannon, Michael; Halliwell, Barry

doi:10.1016/0014-5793(90)81371-t

Cited by 81 publications

(52 citation statements)

References 21 publications

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“…1) and thus may exert their reported antioxidant action [7] by a similar membrane stabilizing effect, which we observe as an inhibition of lipid peroxidation.…”

Section: Introductionsupporting

confidence: 53%

“…Tamoxifen, 4-hydroxytamoxifen and 17/3-oestradiol also show an inhibitory effect on lipid peroxidation when added in ethanol externally to preformed liposomes [7], whereas cholesterol and ergosterol under similar conditions have no activity (H.W., unpublished data). This difference may reflect the ease with which the drugs and hormones used are able to enter liposomes and also natural membranes [7].…”

Section: Discussionmentioning

confidence: 97%

“…This difference may reflect the ease with which the drugs and hormones used are able to enter liposomes and also natural membranes [7].…”

Section: Discussionmentioning

confidence: 99%

“…4-Hydroxytamoxifen is produced by the metabolism of tamoxifen via cytochrome P-450 action in humans [2][3][4][5][6]. We have recently reported that tamoxifen and 4-hydroxytamoxifen are antioxidants in that they are potent inhibitors of lipid peroxidation in microsomal and preformed liposomal membrane systems when added in the carrier solvent ethanol [7]. However, the chemical structure of tamoxifen ( Fig.…”

Section: Introductionmentioning

confidence: 99%

“…1) indicates that it is unlikely to act as a chain-breaking antioxidant because the compound contains no easily donatable hydrogen atom. Furthermore, chain-breaking antioxidants usually introduce a lag period into the peroxidation timecourse and this was not observed for tamoxifen or 4-hydroxytamoxifen, even though the latter compound possesses a potentially donatable hydrogen atom [7].…”

Section: Introductionmentioning

confidence: 99%

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Mechanism of inhibition of lipid peroxidation by tamoxifen and 4‐hydroxytamoxifen introduced into liposomes

et al. 1990

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The anticancer drug tamoxifen when introduced into phospholipid liposomes during their preparation inhibited Fe(III)-ascorbate induced lipid peroxidation to a greater extent than similarly introduced cholesterol. Ergosterol was equipotent with tamoxifen, but much less effective than 4-hydroxytamoxifen. Possible mechanisms underlying these effects are discussed in relation to structural mimicry of the sterols by these triphenylethylene drugs as membrane stabilizers against lipid peroxidation.

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“…1) and thus may exert their reported antioxidant action [7] by a similar membrane stabilizing effect, which we observe as an inhibition of lipid peroxidation.…”

Section: Introductionsupporting

confidence: 53%

Section: Discussionmentioning

confidence: 97%

“…This difference may reflect the ease with which the drugs and hormones used are able to enter liposomes and also natural membranes [7].…”

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Mechanism of inhibition of lipid peroxidation by tamoxifen and 4‐hydroxytamoxifen introduced into liposomes

et al. 1990

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Effect of tamoxifen on lipid peroxide and antioxidative system in postmenopausal women with breast cancer

Thangaraju

Vijayalakshimi

Sachdanandam

1994

Cancer

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Background. Current evidence clearly indicates that free radicals play a prominent role in the incidence and development of breast cancer. Available literature suggests that tamoxifen is a potent suppressor of lipid peroxide formation in both animal and human systems. The purpose of this study was to understand the rate of lipid peroxidation and the status of antioxidants in tamoxifen‐treated postmenopausal women with breast cancer. Methods. A short term evaluation of 6 months' tamoxifen therapy (10 mg twice a day) in 64 postmeno‐pausal women was conducted. The rate of serum lipid peroxidation and the status of enzymic and nonenzymic antioxidants were evaluated before and after 3 and 6 months' tamoxifen treatment. Results. At 3 and 6 months' evaluation, tamoxifen‐treated patients showed a significantly decreased concentration of malondialdehyde (P < 0.001), an end product of lipid peroxidation, and remarkably increased levels of enzymic and nonenzymic antioxidants. In addition to that, the concentrations of serum selenium and vitamins A, C, and E were increased significantly (P < 0.01 for each) in these patients. Conclusion. The results suggest that tamoxifen therapy exerts significant positive effects on the rate of lipid peroxidation and protective systems in postmenopausal women with breast cancer.

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Mechanisms of Estrogenic Protection against gp120-Induced Neurotoxicity

Howard

Brooke

Sapolsky

2001

Experimental Neurology

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The antioxidant action of tamoxifen and its metabolites Inhibition of lipid peroxidation

Cited by 81 publications

References 21 publications

Mechanism of inhibition of lipid peroxidation by tamoxifen and 4‐hydroxytamoxifen introduced into liposomes

Mechanism of inhibition of lipid peroxidation by tamoxifen and 4‐hydroxytamoxifen introduced into liposomes

Effect of tamoxifen on lipid peroxide and antioxidative system in postmenopausal women with breast cancer

Mechanisms of Estrogenic Protection against gp120-Induced Neurotoxicity

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