Dienogest, a synthetic steroid, suppresses both embryonic and tumor-cell-induced angiogenesis

Nakamura, Masaki; Katsuki, Yukio; Shibutani, Yasunori; Oikawa, Tsutomu

doi:10.1016/s0014-2999(99)00765-7

Cited by 54 publications

(22 citation statements)

References 27 publications

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“…Mouse dorsal air sac assay was performed as previously described, with slight modifications. 4,5) Female ICR mice were purchased at 5-8 weeks old from Japan SLC (Shizuoka, Japan). A chamber covered with Millipore filters (Millipore, Billerica, MA) of 0.45 mm pore size on both sides was filled with either saline or S180 tumor cells (3:0 Â 10 6 cells) and implanted into a subcutaneous dorsal air sac, which was created by injecting air into the back of each mouse.…”

mentioning

confidence: 99%

Propolis Suppresses Tumor Angiogenesis by Inducing Apoptosis in Tube-Forming Endothelial Cells

Ohta

Kunimasa

Kobayashi

et al. 2008

Bioscience, Biotechnology, and Biochemistry

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mentioning

confidence: 99%

Propolis Suppresses Tumor Angiogenesis by Inducing Apoptosis in Tube-Forming Endothelial Cells

Ohta

Kunimasa

Kobayashi

et al. 2008

Bioscience, Biotechnology, and Biochemistry

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“…Ishikawa cell line expresses ER and PR, while HEC-88nu corresponds only to ER. When the Ishikawa cell line was treated with 5 and 18, it showed that a reticence of its growth 47 ; on the other hand, HEC-88nu did not respond to the treatment with compound 5. Nevertheless, compound 18 inhibited proliferation of this cell line; and this fact supports its action via non-PR mediated pathways.…”

Section: Current Use Of Progestins For Cancer Treatment Contraceptiomentioning

confidence: 94%

Recent advances in structure of progestins and their binding to progesterone receptors

Cabeza

Heuze

Sánchez

et al. 2014

Journal of Enzyme Inhibition and Medicinal Chemistry

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The role of progesterone in women's cancers as well as the knowledge of the progesterone receptor (PR) structure has prompted the design of different therapies. The aim of this review is to describe the basic structure of PR agonists and antagonists as well as the recent treatments for illness associated with the progesterone receptor. The rational design for potent and effective drugs for the treatment of female cancer must consider the structural changes of the androgen and progestogen skeleton which are an indicator of their activity as progestins or antiprogestins. The presence of a hydroxyl group at C-17 in the progesterone skeleton brings about a loss of progestational activity whereas acetylation induces a progestational effect. The incorporation of an ethynyl functional group to the testosterone framework results in a loss of androgenic activity with a concomitant enhancement of the progestational effect. On the other hand, an ester function at C-3 of dehydroepiandrosterone skeleton induces partial antagonism to the PR.

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“…Nakamura et al proposed inhibition of neovascularization as a mechanism for cell proliferation suppression by dienogest, reporting that vascularization in the mouse tissue implanted with S-180 tumor cells was markedly suppressed by 5-day consecutive oral treatment with dienogest (1 mg/kg/day) (47). Neovascularization is an important step for tumor cell growth, invasion and metastasis in lesions of cancer in general (including endometrial cancer), and its inhibition can lead to suppression of cancer cell proliferation.…”

Section: Applicability Of Dienogest To Treatment Of Endometrial Cancermentioning

confidence: 99%

Progestin therapy for endometrial cancer: The potential of fourth-generation progestin (Review)

et al. 2012

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Abstract. Progestin preparations are made of synthetic progesterone and have often been used for hormone therapy in gynecological patients with endometriosis or endometrial cancer. Hormone therapy using progestin is considered to be one of the effective means of treatment particularly when dealing with endometrial cancer (an estrogen-dependent tumor). Numerous reports have been published concerning its efficacy in advanced or recurrent cases of atypical endometrial hyperplasia or endometrial cancer. Dienogest has been developed as a fourth-generation progestin for hormone therapy for endometriosis that can be used with high safety for long periods of time. In Japan, dienogest has been recommended as a first-line drug for endometriosis-associated pain. However, its antitumor activity has also been attracting close attention following a report that this drug suppressed the proliferation in vitro of endometrial cancer-derived cell lines which failed to respond to other progestins such as medroxyprogesterine acetate (MPA). The mechanism for antitumor activity of dienogest is considered to differ from the mechanism for antitumor activity of conventional progestin preparations used for treatment of endometrial cancer. This drug is expected to be clinically applicable as a new drug for the treatment of endometrial cancer. Contents

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Dienogest, a synthetic steroid, suppresses both embryonic and tumor-cell-induced angiogenesis

Cited by 54 publications

References 27 publications

Propolis Suppresses Tumor Angiogenesis by Inducing Apoptosis in Tube-Forming Endothelial Cells

Propolis Suppresses Tumor Angiogenesis by Inducing Apoptosis in Tube-Forming Endothelial Cells

Recent advances in structure of progestins and their binding to progesterone receptors

Progestin therapy for endometrial cancer: The potential of fourth-generation progestin (Review)

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