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Delta(9)-tetrahydrocannabinol inhibits 17beta-estradiol-induced proliferation and fails to activate androgen and estrogen receptors in MCF7 human breast cancer cells.
Anticancer Res. 2008 Jan-Feb; 28(1A):85-9.AR

Abstract

BACKGROUND

Delta(9)-tetrahydrocannabinol (THC) exerts palliative effects in cancer patients, but produces adverse effects on the endocrine and reproductive systems. Experimental evidence concerning such effects is controversial. Whether THC exhibits estrogenic or androgenic activity in vitro was investigated.

MATERIALS AND METHODS

Estrogenic effects of THC were analyzed in vitro by measuring the proliferation of estrogen-sensitive MCF7 cells. Androgenic activity was investigated by the A-Screen assay that measures androgen-dependent inhibition of proliferation of the androgen receptor (AR)-positive human mammary carcinoma cell line, MCF7-AR1.

RESULTS

In contrast to 17beta-estradiol, included as positive control with an EC50 value (concentration required for 50% of maximal 17beta-estradiol-induced proliferation) of 1.00 x 10(-12) M, THC failed to induce cell proliferation in the MCF7 cell line at concentrations between 10(-13) and 10(-4) M. THC inhibited 17beta-estradiol-induced proliferation in wild-type MCF7 and MCF7-AR1 cells, with an IC50 value of 2.6 x 10(-5) M and 9 x 10(-6) M, respectively.

CONCLUSION

THC failed to act as an estrogen, but antagonized 17beta-estradiol-induced proliferation. This effect was independent of the AR expression level.

Authors+Show Affiliations

Institute of Pharmacology and Toxicology, University of Zurich, Switzerland. Andre.vonBueren@kispi.uzh.chNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

18383828

Citation

von Bueren, A O., et al. "Delta(9)-tetrahydrocannabinol Inhibits 17beta-estradiol-induced Proliferation and Fails to Activate Androgen and Estrogen Receptors in MCF7 Human Breast Cancer Cells." Anticancer Research, vol. 28, no. 1A, 2008, pp. 85-9.
von Bueren AO, Schlumpf M, Lichtensteiger W. Delta(9)-tetrahydrocannabinol inhibits 17beta-estradiol-induced proliferation and fails to activate androgen and estrogen receptors in MCF7 human breast cancer cells. Anticancer Res. 2008;28(1A):85-9.
von Bueren, A. O., Schlumpf, M., & Lichtensteiger, W. (2008). Delta(9)-tetrahydrocannabinol inhibits 17beta-estradiol-induced proliferation and fails to activate androgen and estrogen receptors in MCF7 human breast cancer cells. Anticancer Research, 28(1A), 85-9.
von Bueren AO, Schlumpf M, Lichtensteiger W. Delta(9)-tetrahydrocannabinol Inhibits 17beta-estradiol-induced Proliferation and Fails to Activate Androgen and Estrogen Receptors in MCF7 Human Breast Cancer Cells. Anticancer Res. 2008 Jan-Feb;28(1A):85-9. PubMed PMID: 18383828.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Delta(9)-tetrahydrocannabinol inhibits 17beta-estradiol-induced proliferation and fails to activate androgen and estrogen receptors in MCF7 human breast cancer cells. AU - von Bueren,A O, AU - Schlumpf,M, AU - Lichtensteiger,W, PY - 2008/4/4/pubmed PY - 2008/4/11/medline PY - 2008/4/4/entrez SP - 85 EP - 9 JF - Anticancer research JO - Anticancer Res VL - 28 IS - 1A N2 - BACKGROUND: Delta(9)-tetrahydrocannabinol (THC) exerts palliative effects in cancer patients, but produces adverse effects on the endocrine and reproductive systems. Experimental evidence concerning such effects is controversial. Whether THC exhibits estrogenic or androgenic activity in vitro was investigated. MATERIALS AND METHODS: Estrogenic effects of THC were analyzed in vitro by measuring the proliferation of estrogen-sensitive MCF7 cells. Androgenic activity was investigated by the A-Screen assay that measures androgen-dependent inhibition of proliferation of the androgen receptor (AR)-positive human mammary carcinoma cell line, MCF7-AR1. RESULTS: In contrast to 17beta-estradiol, included as positive control with an EC50 value (concentration required for 50% of maximal 17beta-estradiol-induced proliferation) of 1.00 x 10(-12) M, THC failed to induce cell proliferation in the MCF7 cell line at concentrations between 10(-13) and 10(-4) M. THC inhibited 17beta-estradiol-induced proliferation in wild-type MCF7 and MCF7-AR1 cells, with an IC50 value of 2.6 x 10(-5) M and 9 x 10(-6) M, respectively. CONCLUSION: THC failed to act as an estrogen, but antagonized 17beta-estradiol-induced proliferation. This effect was independent of the AR expression level. SN - 0250-7005 UR - https://www.unboundmedicine.com/medline/citation/18383828/Delta_9__tetrahydrocannabinol_inhibits_17beta_estradiol_induced_proliferation_and_fails_to_activate_androgen_and_estrogen_receptors_in_MCF7_human_breast_cancer_cells_ L2 - http://ar.iiarjournals.org/cgi/pmidlookup?view=long&pmid=18383828 DB - PRIME DP - Unbound Medicine ER -