雌莫司汀磷酸钠

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生物活性 Estramustine phosphate sodium (EMP, Emcyt, Estracyt)是一种具有独特双重作用模式的抗肿瘤药。Estramustine phosphate sodium的代谢产物estrone和estradiol具有抗促性腺激素的活性，导致睾丸激素水平降低。Estramustine(estramustine phosphate sodium去磷酸化作用产生的细胞毒性代谢产物)是一种具有抗微管作用的抗前列腺肿瘤药物。
体外研究

Estramustine phosphate sodium (1 µg/mL) treatment suppressed PC3 cell growth.
Estramustine phosphate sodium (2 µg/mL) treatment significantly elevates phosphatidylserine eversion amount on PC3 cells. Estramustine phosphate sodium induces PC3 cell apoptosis.
Estramustine phosphate sodium (2 µg/mL) treatment decreases MiR-31 level. Estramustine phosphate odium induces s prostate cancer cell line PC3 apoptosis through reducing miR-31.
Estramustine phosphate sodium, a unique antitumour agent, is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.
Estrone and estradiol, products of the metabolism of Estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels similar to those achieved after surgical castration.

体内研究

Estramustine phosphate sodium (4-12 mg/kg; intraperitoneal injection; daily; for 2 weeks) inhibits PAC120 tumor growth 53% by day 35.

Animal Model:	Swiss nu/nu (nude) male mice (5-week-old) bearing PAC120 tumors
Dosage:	4 mg/kg, 12 mg/kg
Administration:	Intraperitoneal injection; daily; for 2 weeks
Result:	Suppressed the development of skin lesions and resulted in a dissociation between DTH response and antibody production.

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