Effects of raloxifene hydrochloride on endometrial cancer cells in vitro

Hibner, M.; Magrina, Javier F.; Lefler, Scott R.; Cornella, Jeffrey L.; Pizarro, Antonio R; Loftus, Joseph C.

doi:10.1016/j.ygyno.2004.03.007

Cited by 15 publications

(11 citation statements)

References 25 publications

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“…Hibner et al (2004), in fact, showed that endometrial cell growth was increased by RAL compared with the control, similar to E2 with respect to the control. RAL and E2 together did not affect cell growth at any concentration.…”

Section: Discussionmentioning

confidence: 58%

“…In several in-vitro studies, endometrial cell lines showed a higher proliferation than hormone-free control cells when treated with RAL at any dosage (with the exception of supra-physiologic doses), whereas incubation with RAL induced less cellular growth than E2 or TAM (Boostanfar et al, 2003;Hibner et al, 2004;Leblanc et al, 2007).…”

Section: Discussionmentioning

confidence: 99%

“…E2 10 or 100 pg/ml did not stimulate cell growth, whereas cells treated with 1000 pg/ml grew significantly faster than the control cells. RAL did not inhibit the in-vitro growth of endometrial cancer cells and high concentrations even promoted cell growth (Hibner et al, 2004). Glaeser et al (2006) reported that the cell lines KLE, Ishikawa, and RL-95-2 were insensitive to RAL treatment: RAL did not alter cell proliferation of the three cell lines tested.…”

Section: Williams-brown Et Al (2011) Used the Nonmalignant Immortalimentioning

confidence: 97%

“…However, this growth was significantly less than E2-induced growth (Boostanfar et al, 2003). Hibner et al (2004) described the effects of RAL on an endometrial cancer cell line in vitro. Three different concentrations of E2 (10, 100, and 1000 pg/ml) and RAL (1, 10, and 100 ng/ml) were used.…”

Section: Williams-brown Et Al (2011) Used the Nonmalignant Immortalimentioning

confidence: 99%

See 3 more Smart Citations

Could in-vitro studies on Ishikawa cell lines explain the endometrial safety of raloxifene? Systematic literature review and starting points for future oncological research

Gizzo

Noventa²,

Gangi³

et al. 2015

European Journal of Cancer Prevention

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To evaluate all the in-vitro raloxifene (RAL) mechanisms of action on normal, Ishikawa, and different endometrium-derived cell lines to explain the in-vivo RAL endometrial effects, a systematic literature search was performed in the electronic databases MEDLINE, EMBASE ScienceDirect, and the Cochrane Library for the time period between 2002 and 2012. Outcomes were considered in relation to in-vitro stimulatory, inhibitory, or neutral actions of RAL in Ishikawa cell lines compared with different endometrial-derived cell lines (both cancerous and normal endometrium). We also considered all the RAL molecular mechanisms responsible for the in-vitro effects observed. More than 150 articles were available in the scientific database literature, but only 21 fulfilled our selection criteria. Although in-vitro studies appear to yield conflicting results, most evidence has shown that RAL seems to induce endometrial cell mitochondria-mediated apoptosis, and to inhibit estrogen-related cell proliferation and endometrial carcinogenesis by inducing antiangiogenic factors, and reducing cytoskeletal reorganization. If the endometrial safety profile of RAL is confirmed, in the near future, selective estrogen receptor modulators could represent an efficient alternative adjuvant treatment to tamoxifen (TAM) in women with breast cancer considered to be at an increased risk of endometrial disease. The confirmation of the endometrial safety profile could enable the proposal of RAL by clinicians as the most appropriate treatment for BRCA1-2 patients after prophylactic salpingo-oophorectomy.

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Section: Discussionmentioning

confidence: 58%

Section: Discussionmentioning

confidence: 99%

Section: Williams-brown Et Al (2011) Used the Nonmalignant Immortalimentioning

confidence: 97%

Section: Williams-brown Et Al (2011) Used the Nonmalignant Immortalimentioning

confidence: 99%

See 2 more Smart Citations

Could in-vitro studies on Ishikawa cell lines explain the endometrial safety of raloxifene? Systematic literature review and starting points for future oncological research

Gizzo

Noventa²,

Gangi³

et al. 2015

European Journal of Cancer Prevention

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show abstract

“…The basic mechanism of action of the SERM group is known to prevent binding of estrogen to the receptor by competition (5). Raloxifene is one of the members of the SERM group and approved by FDA for the treatment of osteoporosis (6,7). It is reported in the literature that raloxifene has a binding effect to estrogen receptors on breast tissue and endometrial cells but unlike tamoxifen it has no proliferation effect on the endometrial cells (7)(8)(9).…”

Section: Introductionmentioning

confidence: 99%

The Effectiveness of Raloxifene-Loaded Liposomes and Cochleates in Breast Cancer Therapy

Ağardan

Değim

Yılmaz³

et al. 2015

AAPS PharmSciTech

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Abstract. Liposome (spherical vesicles) and cochleate (multilayer crystalline, spiral structure) formulations containing raloxifene have been developed having dimethyl-β-cyclodextrin (DM-β-CD) or sodium taurocholate (NaTC). Raloxifene was approved initially for the treatment of osteoporosis but it is also effective on breast tissue and endometrial cells. Raloxifene inhibits matrix metalloproteinase-2 (MMP-2) enzyme, which is known to be responsible for tumor invasion and the initiation of angiogenesis during the tumor growth. Therefore, raloxifene was selected as a model drug. A series of raloxifene-loaded liposome and cochleate formulations were prepared. In vitro release studies and in vivo tests were performed. Breast cancer cell lines (MCF-7) were also used to find the most effective formulation. Highest antitumor activity was observed, and MMP-2 enzyme was also found to be inhibited with raloxifene-loaded cochleates containing DM-β-CD. These developed formulations can be helpful for further treatment alternatives and new strategies for cancer therapy.

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Lysosome-related biomarkers in preeclampsia and cancers: Machine learning and bioinformatics analysis

Tang,

Luo,

Shen

et al. 2024

Computers in Biology and Medicine

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Effects of raloxifene hydrochloride on endometrial cancer cells in vitro

Cited by 15 publications

References 25 publications

Could in-vitro studies on Ishikawa cell lines explain the endometrial safety of raloxifene? Systematic literature review and starting points for future oncological research

Could in-vitro studies on Ishikawa cell lines explain the endometrial safety of raloxifene? Systematic literature review and starting points for future oncological research

The Effectiveness of Raloxifene-Loaded Liposomes and Cochleates in Breast Cancer Therapy

Lysosome-related biomarkers in preeclampsia and cancers: Machine learning and bioinformatics analysis

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